Penicillin

Z Kinderchir, 1982 Apr, 35(4), 140 - 4
{Post-splenectomy infections and Pneumococcus vaccination in paediatric surgery (author's transl)}; Belohradsky BH et al.; Morbidity and lethality rates in pneumococal infections are higher among children with underlying diseases associated with restricted or absent splenic function . Vaccination with polyvalent vaccine is indicated in all children who are more than 2 years old and who have been splenectomized or have a congenital asplenia . Since protection by vaccination is 80% only, we combine the vaccination with penicillin prophylaxis for at present at least three to five years after splenectomy and draw the express attention of parents and family physicians to the limited nature of protection afforded by vaccination . An increase in the immunogenicity of polysaccharid antigen vaccine might lead to successful vaccination of children below 2 years of age who are notable for a particularly high risk of infection . First reports have been published in literature on the possibility of re-implantation of splenic tissue after post-traumatic rupture (17, 27, 28) so that it may become possible to employ this method additionally to pneumococcus vaccination . In case of haematological indication for splenectomy this should be postponed as far as possible until the child has completed his fifth year of life.

Tohoku J Exp Med, 1982 Apr, 136(4), 439 - 46
Studies on recovery of liver function of operated biliary atresia; Chiba T et al.; Serial liver function studies were analyzed in 42 biliary atresia patients who had undergone portoenterostomy . Values for serum bilirubin, ZTT, TTT, and gamma globulin returned to normal levels three months after operation in patients with good bile excretion . These tests remained abnormal in those with poor bile output . Alkaline phosphatase and serum transaminase values remained high during the early postoperative period, requiring a much longer duration to return to normal . The biological activity of sulfobenzyl penicillin (SBPC) in the serum and bile was determined by serial broth dilution in 15 children with biliary atresia . Eleven patients were studied 10 days to 2 weeks after an apparent successful portoenterosotomy while four others were clinically well and anicteric three to four years postoperatively . The biliary concentration of SBPC was very low despite good bile output during the early postoperative period . The SBPC levels increased three time during the remote postoperative period . The bile concentration of SBPC is lower than normal, however, and it seems that the ability of the liver to excrete this material may never reach normal levels despite apparent good clinical hepatic function.

Ann Intern Med, 1982 Apr, 96(4), 502 - 4
Penicillin-binding proteins in bacteria; Tomasz A; The last 5 to 6 years have witnessed an outburst of renewed interest in the beta-lactam antibiotics . One of the main factors contributing to this was the introduction of the simple and powerful technique of sodium dodecyl sulphate electrophoresis for the identification of bacterial membrane components--penicillin binding proteins--that bind radioactive penicillin and most likely represent the primary biochemical targets of penicillin action in the bacterial cell . Application of this technique has led to a remarkable number of novel observations that have substantially modified our view of the mode of action of beta-lactam antibiotics.

Hosp Pharm, 1982 Apr, 17(4), 202 - 4, 209-11
A multihospital medication allergy audit: a means to quality assurance; Hoffmann RP et al.; Seventeen community hospitals within the 16 division of the Sisters of Mercy Health Corporation cooperatively participated in a medication allergy audit program . Initial and follow-up audits were conducted at each hospital to determine whether allergy information for penicillin- or aspirin-sensitive patients was appropriately communicated to the pharmacist . A total of 483 patient records were reviewed during each audit which corresponded to 12% of each hospital's average patient census . In the initial audit, the overall acceptance rate for the combined hospitals was 62.3% . Following the first audit, each hospital undertook corrective follow-up measures in an attempt to improve its results . In the second audit, the overall acceptance rate improved significantly to 78.9% . It is concluded that this auditing process followed by corrective follow-up measures was an effective mechanism for improving the communication of patient allergy information and is a means to quality assurance . Future audits will be necessary to determine whether the beneficial effects produced will be sustained or improved.

Nouv Presse Med, 1982 Mar 6, 11(11), 843 - 6
{Leukocyte aggregation test for assessing cell-mediated immunity: its use in drug allergy (author's transl)}; Rouveix B; The author has designed a new quantitative leucocyte aggregation test a measure cell-mediated immunity in man . The test involves continuous recording of light absorbance by stirred leucocyte suspensions . Potentially, measurement of direct leucocyte aggregation offers considerable advantages in terms of sensitivity, reproducibility and simplicity of execution . The technique was initially developed in animals and made it possible to assay very small amounts of lymphokines . The results obtained in man with antigenic drugs, such as penicillin, confirm that the aggregation test is much more sensitive than the migration inhibition test . Its precise significance remains uncertain, but it already promises to constitute a simple and highly reliable means of diagnosing and preventing drug hypersensitivity.

Arch Fr Pediatr, 1982 Mar, 39(3), 141 - 4
{Sickle cell anemia and functional asplenia (author's transl)}; Beauvais P; On the occasion of 34 spleen scintigrams performed in children with sickle cell anemia, the frequency and precocity of the "functional asplenia" is emphasized and its relationship with the infectious history of such children is discussed . The anti-bacterial role of the spleen and the responsibility, at least partial, or asplenia in the susceptibility of patients with sickle cell anemia to infections, especially pneumococcal ones, are reviewed . The pathophysiologic mechanism of functional asplenia is then discussed . The author concludes that asplenia has no predictive value in selecting children "at risk" for infection and stresses the necessity of a systematic prevention by penicillin therapy and antipneumococcal vaccination in such patients before 4 years of age.

Aust Fam Physician, 1982 Mar, 11(3), 182 - 3, 186-7
Gonorrhoea and non gonococcal urethritis in the male . The specialist view; Young PS; Although exact figures of the incidence of gonococcal and non gonococcal urethritis is Australia are not available the majority of cases seen in sexually transmitted disease clinics are male patients with these conditions . Evidence of increasing resistance of the gonococcus to penicillin--particularly that due to plasmid mediated penicillinase production--and current interest in Chlamydia trachomatis associated diseases in males, females and neonates, necessitate constant review of the diagnosis and treatment of these conditions.

J Bacteriol, 1982 Mar, 149(3), 1150 - 3
Penicillin is an active-site inhibitor for four genera of bacteria; Yocum RR et al.; The hypothesis that penicillin acts as an active-site inhibitor cell wall biosynthesis was tested by a method of partial proteolytic mapping of penicillin-binding sites versus substrate-binding sites in cell wall D-alanine carboxypeptidases . This enzyme was obtained from four genera of bacteria, purified, and tested.

Int J Radiat Oncol Biol Phys, 1982 Mar-Apr, 8(3-4), 453 - 6
The lethal interaction of X ray and penicillin induced lesions following X-irradiation of Escherichia coli B/R in the presence of hypoxic cell sensitizers; Gillies NE et al.; When Escherichia coli B/r were x-irradiated under anoxia in the presence of different electron-affinic sensitizers and then incubated in broth containing penicillin (at a concentration that did not kill unirradiated cells) additional killing of the bacteria occurred provided the sensitizers were of relatively high lipophilicity . The overall effect was to increase the efficiency of these sensitizers . It is concluded that sensitizer-dependent latent radiation lesions(s) are produced in membrane components of the cell envelope that interact with damage caused by penicillin in the peptidoglycan layer and this causes the additional lethality.

J Trauma, 1982 Mar, 22(3), 186 - 9
Effectiveness of penicillin irrigation in control of infection in sutured lacerations; Lindsey D et al.; We studied the incidence of infection in lacerations in a controlled, double-blind, Armitage sequential clinical trial . After standard prescribed preparation of the wound area, and immediately before suture, each laceration was flooded with the 10 ml content of a numbered, amber glass vial . Half of the vials contained a solution of 0.9% NaCl; half contained a 5% solution of sodium benzyl penicillin . No other factors were controlled . A single observer made the determinations of presence or absence of infection, purulent or nonpurulent, early and late after suture . After study of 260 lacerations the study indicated a clear superiority of penicillin over saline in lowering the incidence of infection with a statistical significance of p less than 0.00005 . In a sample of this size the 95% confidence limits of the magnitude of the superiority of penicillin cover a wide range, but it appears that two out of three or three out of four infections can be averted merely by flooding the wound with penicillin immediately before suture.

Drug Intell Clin Pharm, 1982 Mar, 16(3), 205 - 10
Benzathine penicillin G in the treatment of neurosyphilis; Cuddy PG; The definition, pathogenesis, incidence, diagnosis, and treatment of neurosyphilis are discussed . Controlled trials of benzathine penicillin in the treatment of neurosyphilis are reviewed, as are recent case reports of benzathine penicillin failures . Although few well-controlled studies exist to document conclusively the efficacy of benzathine penicillin in the treatment of neurosyphilis, its use is recommended in selected situations.

Otolaryngol Head Neck Surg, 1982 Mar-Apr, 90(2), 266 - 9
Malignant external otitis: a dangerous misnomer?
Lucente FE, Parisier SC, Som PM, Arnold LM.
Review of our experience in treating 16 patients with malignant external otitis, along with survey of the compromised defense mechanisms of diabetic patients, confirms the need for immediate, intense, and vigilant therapy . Radioisotope scans, high-resolution computed tomography scans, and multidirectional tomograms are used to delineate the extent of the disease . Therapy includes intravenous aminoglycoside and penicillin derivatives, limited surgery, and hyperbaric oxygenation . In view of the tendency for this infection to extend beyond the external auditory canal and to produce an invasive lethal osteomyelitis, we feel that the tendency to classify this disease as a variant of diffuse external otitis may foster undertreatment.

Am J Vet Res, 1982 Mar, 43(3), 545 - 7
In vitro susceptibility of selected isolates of Brucella abortus to penicillin; Stinebring WR et al.; Brucella abortus isolates (n = 134) from 38 dairy herds in Vermont, Florida, and Canada exhibited 2 growth patterns on medium containing 5 U of penicillin/ml . The B abortus isolates from 7 herds in Vermont were always susceptible to the antibiotic at that concentration . Eleven of 12 isolates from 1 herd in Florida and 25 isolates (biotypes 1 and 4) from 30 Canadian herds grew at greater than or equal to 5 U of penicillin/ml, as determined using a gradient plate method . Penicillin susceptibility may be of value in identifying the source of infections in cattle.

Br J Anaesth, 1982 Mar, 54(3), 343 - 7
Anticonvulsant activity of Althesin on experimental epilepsy; De Riu PL et al.; Anaesthetic doses of Althesin were tested in rabbits using two experimental models of epilepsy: generalized (OHP; oxygen at high pressure-induced seizure) and partial (penicillin cortical-induced seizure) . Althesin in both models always produced anticonvulsant activity which was more powerful in generalized convulsions . This agent was successful in preventing and treating OHP seizures . The authors conclude that a clinical history of convulsions must not be considered a contraindication to the use of this anaesthetic which has particularly useful properties for neurosurgery.

J Pharm Sci, 1982 Mar, 71(3), 351 - 3
Separation of penicillin and its major degradation products by ion-pair reversed-phase high-pressure liquid chromatography; Ghebre-Sellassie I et al.; An ion-pair reversed-phase high-pressure liquid chromatographic technique capable of separating penicillin and its major degradation products within 8 min was developed . The influence of pH, counterion concentration, buffer concentration, and organic modifier content was studied and the observed behavior of the compounds during the chromatographic process was discussed.

J Pharmacol Exp Ther, 1982 Mar, 220(3), 660 - 71
gamma-Aminobutyric acid (GABA) receptor stimulation . I . Neuropharmacological profiles of progabide (SL 76002) and SL 75102, with emphasis on their anticonvulsant spectra; Worms P et al.; Progabide (4-({(4-chlorophenyl) (5-fluoro-2-hydroxyphenyl)-methylene}amino) butanamide) is a gamma-aminobutyric acid (GABA) receptor agonist which readily enters the brain . In the body, progabide is metabolized to three active metabolites: SL 75102, gabamide and GABA . Progabide and SL 75102 readily enter the brain and GABA and gabamide are also formed within this organ . Both progabide and SL 75102 exhibit a broad spectrum of anticonvulsant activities against seizures which involve GABA-mediated events (bicuculline, picrotoxinin and pentylenetetrazol) or which are apparently independent of GABAergic mechanisms (penicillin, strychnine, electroshock and audiogenic seizures) . These data support the hypothesis that direct GABA receptor stimulation is an effective means of controlling convulsions of various origins . Progabide and SL 75102 have relatively minor secondary effects in comparison to commonly used antiepileptics . Myorelaxation occurs, but only at doses higher than the ED50 values in convulsant tests . Furthermore, these compounds are not sedative . Finally, these GABA agonists have a complex action in the extrapyramidal system . Anticonvulsant doses are antagonistic to dopamine receptor-mediated behaviors, whereas much lower doses seem to facilitate the effects of dopaminergic transmission.

Immunology, 1982 Mar, 45(3), 537 - 43
Mice do not respond with delayed hypersensitivity to penicillin-derived determinants; Kristofferson A et al.; Penicillin structures of varying lipophilicity were used to induce delayed hypersensitivity (DH) in different strains of mice . Epicutaneous application on inflamed skin or intracutaneous or subcutaneous injection with Freund's complete adjuvant did not induce DH, despite the fact that picrylchloride readily produced such responses . Sheep, rabbit and mouse red cells as well as mouse lymph node and epidermal cells conjugated with various amounts of penicillin injected subcutaneously in the base of the tail did not induce a DH reaction to penicillin either, whereas such responses to other cellular components and also to the TNP determinant after using picryl sulphonic acid conjugated spleen cells were recorded . Since the mice in other studies have been shown to respond with antibodies to soluble penicilloyl protein conjugates, but never to penicillin itself, we concluded that this species of animal is incapable of responding to penicillin with DH.

Mycopathologia, 1982 Feb 19, 77(2), 103 - 9
Contribution to the fungal flora of cereal grains in Egypt; El-Kady IA et al.; 30 genera and 77 species, in addition to 4 varieties were isolated from 25 samples of each of barley, wheat, maize and sorghum grains collected from different places in Egypt . The broadest spectrum of genera and species was recorded in wheat (25 genera and 59 species + 4 varieties) followed by barley (21 genera and 52 species + 2 varieties), sorghum (14 genera and 33 species + 2 varieties) and maize grains (11 genera and 29 species + 2 varieties) . Aspergillus, Fusarium, Penicillium, and Rhizopus were the most common genera in the four grains, except maize where Penicillin emerged in low frequency . Aspergillus was the main component of the fungal flora of the four grains and contributed 79-94.4% of the gross total count of fungi . From the preceding genera A . niger, A . flavus, A . fumigatus, F . oxysporum, P . chyrsogenum, P . corylophilum, P . notatum and R . stolonifer were the most frequent.

Can J Ophthalmol, 1982 Feb, 17(1), 21 - 3
Distribution of penicillin in the cornea, tears and aqueous humour at various times following a single intravenous injection; Avaria M et al.; Bioassays performed by the disc diffusion technique on samples of blood, tears, aqueous humour and cornea from 30 rabbits killed 4 to 24 hours following a single intravenous injection of benzylpenicillin (40 mg/kg) showed that the penicillin content of these fluids and tissues progressively decreased with time . However, even after 24 hours the agent could be detected in the samples . The peripheral and central cornea contained similar amounts of penicillin up to 16 hours; thereafter, the peripheral cornea contained more of the agent.

Am J Clin Pathol, 1982 Feb, 77(2), 210 - 3
Prevalence of penicillin-resistant pneumococci in Houston, Texas; Krause KL et al.; Pneumococci resistant to penicillin have been reported in increasing numbers world-wide . A survey for resistance to penicillin G in 222 clinical isolates taken from patients in Houston is reported here . Thirteen (5.9%) of the isolates screened exhibited moderate levels of resistance with MIC's ranging from 0.125-0.5 microgram/ml . The authors recommend routine screening for pneumococcal resistance in isolates from blood, cerebrospinal fluid and tissue exudates.

Invest Ophthalmol Vis Sci, 1982 Feb, 22(2), 220 - 7
Liposomes in topical drug delivery; Schaeffer HE et al.; The possible use of liposomes as topical drug delivery vehicles for both water- and lipid-soluble drugs has been investigated . Data for two characteristic drugs, penicillin G and indoxole, are presented . Liposome uptake by the cornea is greatest for positively charged liposomes, less for negatively charged liposomes, and least for neutral liposomes, suggesting that the initial interaction between the corneal surface and liposomes is electrostatic adsorption . Positively charged unilamellar liposomes enhanced transcorneal flux of penicillin G across isolated rabbit cornea more than fourfold . Liposomal entrapment of drug is prerequisite to enhanced transport; corneal penetration was not enhanced when liposomes that were preformed in the absence of drug were mixed with penicillin G immediately before application to the cornea . Although penicillin G is water-soluble, the findings indicate that it secondarily associates with liposome membranes, possibly by insertion of its hydrophobic end into the lipid bilayer . Indoxole, however, was incorporated directly into the membranes of pure phosphatidyl choline liposomes . Liposome-mediated drug flux efficiency after topical instillation in rats was significantly greater than that obtained with equivalent concentration of drug delivered in polysorbate 80 . Ten times more drug in polysorbate 80 was required to equal liposome-mediated flux efficiency . The findings suggest that liposomes enhance corneal penetration of drug by adsorbing to the corneal surface, with direct transfer of drug from liposomal to epithelial cell membranes.

Epilepsia, 1982 Feb, 23(1), 35 - 45
Feline generalized epilepsy induced by tranexamic acid (AMCA); Pellegrini A et al.; Epileptic activities induced by topical application of tranexamic acid (AMCA) and penicillin to the cortex of 12 cats in acute experiments were compared . Both substances when diffusely applied on a wide cortical area of both hemispheres at very low concentration produced an EEG pattern consisting of spike-wave bursts similar to the electrographic manifestations seen in feline generalized epilepsy induced by large parenteral doses of sodium penicillin . These epileptic bursts could be triggered by repetitive stimulation of nucleus centralis medialis . Increased concentrations of both AMCA and penicillin led to the appearance of bilaterally synchronous spikes and poly-spikes which were not further excited by NCM stimulation . Two factors seem to play an important role in eliciting spike-wave bursts in both models: (1) the area of the cortex exposed to the epileptogenic agent and (2) the concentration of the epileptogenic agent used . The similar effects observed in 5 chronic animals either by intravenous injection of high doses of AMCA or by intramuscular injection of sodium penicillin confirm the results obtained in acute experiments and suggest a new way of inducing feline generalized epilepsy.

Biochem J, 1982 Feb 1, 201(2), 425 - 7
Interaction of the pBR 322-coded RTEM beta-lactamase with substrates . Evidence for specific conformational transitions; Citri N et al.; The rate of inactivation of RTEM-1 beta-lactamase by Pronase is accelerated by class A ('resistant') penicillins . Other substrates (class S penicillin and cephalosporins) protect against the inactivation . Cefoxitin, a semi-synthetic cephamycin, induces a more extensive, hysteretic response . In its presence the enzyme is inactivated by trypsin as well as by Pronase.

Antimicrob Agents Chemother, 1982 Feb, 21(2), 195 - 200
Induction of cell lysis in Escherichia coli: cooperative effect of nocardicin A and mecillinam; Berenguer J et al.; Nocardicin A and mecillinam are two beta-lactam antibiotics with poor bacteriolytic activity against Escherichia coli . However, the combined use of these drugs resulted in the induction of a fast lytic response in E . coli cells . For this cooperative effect to take place, the formation of a complex between penicillin-binding protein 2 and mecillinam is apparently necessary . This suggests that penicillin-binding protein 2 might be actively involved in the response of E . coli to bacteriolytic beta-lactam antibiotics.

Br J Dermatol, 1982 Feb, 106(2), 183 - 90
The role of penicillin in the pathogenesis of chronic urticaria; Boonk WJ et al.; Intracutaneous tests with penicilloyl-polylysine (PPL) and benzyl-penicillin G (PG) were performed in 245 patients suffering form chronic recurrent urticaria, including physical urticaria . Positive results were observed in fifty-nine patients (24%) . Sera from fifty-seven of these fifty-nine patients were investigated for circulating anti-penicilloyl antibodies by an enzyme-linked immunosorbent assay (ELISA) and a passive haemagglutination test (HA) . The results were compared to those form the ELISA and HA in a control group of thirty-five patients who had shown clinical allergic reactions to penicillin and had positive skin tests to PPL and/or PG . The in vitro tests revealed positive results in 12.3% and 37.1% respectively . In forty-three patients the course of the positive intracutaneous tests to penicillin, together with the duration of chronic urticaria, was followed over a period of time up to 3.5 years . In twenty-two out of forty-two patients with positive intracutaneous tests to penicillin, a diet free of dairy products proved to have a curative effect, compared to two out of forty control subjects with chronic urticaria and negative skin tests to penicillin . These studies indicate that penicillin has an important role in the aetiology and maintenance of chronic urticaria.

Fortschr Med, 1982 Jan 28, 100(4), 146 - 9
{Therapy of acute diseases of the upper airway . Comparison of 2 antiseptic pharyngeal sprays in otorhinolaryngologic practice}; Klingbeil W; 100 out-patients with subacute or acute stages of pharyngitis, tonsillitis, pharyngotonsillitis or angina participated in a randomized 3 day trial on antiseptic mouth-sprays comparing one containing a combination of chlorhexidine, tramazoline and aluminiumtrilactate with one containing only hexetidine . At the beginning of therapy and 3 days afterwards the local symptoms rubor and tumefaction of the throat, dysphagia, fur, swelling and tenderness of the cervical superficial lymph nodes were classified according to a graded scale . Using the combination these symptoms were markedly improved in 34 patients, improved in 7; 8 showed no alteration and one patient showed a deterioration (n = 50) . With the monosubstance 18 patients showed good improvement, 11 an improvement, 17 no change and 3 patients a deterioration (n = 49), one patient needed penicillin-treatment during the trial . Under treatment with the combination the symptoms rubor and tumefaction of the throat showed a significant better improvement . The possible role played by a vasodilator are discussed.

Brain Res, 1982 Jan 28, 232(1), 41 - 56
Membrane depolarization and prolongation of calcium-dependent action potentials of mouse neurons in cell culture by two convulsants: bicuculline and penicillin; Heyer EJ et al.; The convulsant compounds bicuculline (BICUC) and penicillin (PCN) are antagonists of GABA-mediated synaptic inhibition . In addition, we have shown that BICUC and PCN produced membrane depolarization of mouse spinal cord neurons in primary dissociated cell culture by blocking a potassium conductance, a non-synaptic direct effect . Both compounds also prolonged calcium-dependent action potentials of mouse dorsal root ganglion and spinal cord neurons in cell culture . Thus, BICUC and PCN had both synaptic and non-synaptic actions . The possibility that both synaptic and non-synaptic actions of BICUC and PCN are involved in their convulsant mechanism of action is discussed.

Brain Res, 1982 Jan 7, 231(1), 131 - 41
Penicillin epileptogenesis in the rat: diffusion and the differential laminar sensitivity of the cortex cerebri; Holmes O et al.; When penicillin is applied electrophoretically from a fluid-filled microelectrode into the substance of the somatosensory cortex of the rat under urethane anaesthesia, the latent period for production of interictal epileptic spikes is least when the electrode lies 0.7 mm below the cortical surface . With low electrophoretic currents of --50 to 100 nA the increase in latent period as the tip of the electrode is placed further and further away from this level can be quantitatively accounted for by the time taken for penicillin to diffuse and to reach a threshold concentration throughout a critical mass of tissue at the 0.7 mm level . With these low currents, the generators of the interictal spikes are confined to a band of cortex centred at the 0.7 mm level . This is true even when the penicillin is applied away from the sensitive layer; in this circumstance the duration of electrophoresis needed to evoke interictal spikes is greater but when they do eventually appear the spikes are generated at the 0.7 mm layer . Histologically, the sensitive layer has been identified as the deep part of layer III . So far as the generation of interictal spikes is concerned, there is no evidence that, with low electrophoretic currents, penicillin has effects other than at the deep part of layer III; all the available evidence indicates that the penicillin has to diffuse to this layer and produces its effects there.

J Gynecol Obstet Biol Reprod (Paris), 1982, 11(5), 589 - 91
{A case of post partum gonococcal arthritis}; Pigne A et al.; The authors report a case of gonorrhoea occurring immediately after delivery, characterized by acute inflammatory polyarthritis . The diagnosis was made from swabs taken from the lochia that were cultured on enriched media . The outcome of the disease treated with penicillin was good after 48 hours . The new-born's state of health after swabs take from the nostrils were positive was satisfactory all the time . A review of the literature shows how rare these conditions are, how serious they can sometimes be, and the management that should be undertaken in order to prevent complications occurring.

Ann Med Interne (Paris), 1982, 133(8), 564 - 8
{Early syphilitic hepatitis . Two cases}; Echard M et al.; Two patients are presented as cases of secondary syphilitic hepatitis . Clinical and biological signs coincided with usual description of this affection . Syphilitic serological tests were all very positive . These two patients were homosexual men . In one case, we have found treponema in hepatic biopsy, underelectron microscope only, which confirmed the diagnosis . Evolution of both patients was improved by anti-syphilitic penicillin the rapy . Thus, this is an important diagnosis, which should not missed, because of the good prognosis of this affection with specific treatment, and because of the increasing frequency of syphilis for 20 years.

J Gynecol Obstet Biol Reprod (Paris), 1982, 11(7), 829 - 32
{Pneumococcal peritonitis . An unusual diagnosis in gynecology}; Muray JM et al.; The authors, having had a case of primary pneumococcal peritonitis, review the features of this pathological condition which has become rare, and of gynaecological pneumococcal infections . Pneumococcal peritonitis presents as a very serious peritonitis and the usual diagnosis that is first made is peritonitis due to appendicitis . Pneumococcal peritonitis can be primary but it is possible that it is often secondary to genital pneumococcal infections . Treatment should always be by laparotomy to confirm the diagnosis, with a peritoneal toilet which is needed in order to stop a pelvic abscess developing . Antibiotics, which are usually of the penicillin group, should be given for at least 15 days . The treatment can be varied in those rare cases where cirrhotic ascites or serious nephrotic syndromes develop in children . Putting in drains and removing the appendix when it is normal are both useless.

Aust J Biol Sci, 1982, 35(4), 363 - 72
Mechanisms of organic acid and monosaccharide transport in the kidney of the brush-tailed possum, Trichosurus vulpecula; Miller JH et al.; The mechanisms of organic acid and monosaccharide transport in the kidney of T . vulpecula were investigated using the renal cortical slice preparation . The kinetics, the sensitivity to inhibitors of metabolism and sodium transport, and the specificity of the concentrative uptake of p-amino-hippurate and alpha-methyl-D-glucoside were examined and compared with published results from studies in eutherian mammals . Some minor differences between metatherians and eutherians were noted with regard to the specificities of the renal slice uptake systems . Penicillin G, a competitor of organic acid transport in eutherian kidneys, did not interact with the marsupial uptake system, and sodium acetate, which stimulates transport in other mammals, inhibited p-aminohippurate uptake in the slice of the possum kidney . 2-Deoxy-D-glucose, which interacts with the phlorizin-sensitive monosaccharide transport system in the dog, rat and rabbit kidney, had no effect on alpha-methyl-D-glucoside uptake in the possum, and the magnitude of the interaction of D-fructose resembled that reported in the dog and rat but was greater than the inhibition reported in the rabbit . D-Glucuronic acid and D-glucuronic acid lactone inhibited alpha-methyl-D-glucoside uptake in the possum but had no effect on uptake in rat renal slices . In consideration of the reported variability of these parameters between different classes of eutherians, it was concluded that the primary mechanisms involved in organic solute transport by the proximal nephron of metatherians and eutherians were not significantly different.

Soc Sci Med, 1982, 16(23), 2055 - 64
Penicillin, battery acid and sacrifice . Cures and causes in Nyole medicine; Whyte SR; The existence of therapeutic alternatives, a very widespread feature of medical systems, is to be distinguished from medical pluralism, which characterizes situations where orthodoxy and power accrue to one group of medical professionals . Local African medical systems are dynamic and inclusive and this is the basis for the ready incorporation of Western biomedical elements . Analysis of the medical perceptions, treatments and practitioners of the Nyole of Eastern Uganda reveals that new divination techniques and exotic sorcery medicines have been absorbed as well . Some of the recent changes in Nyole medicine may be indicative of a growing medical individualism . Explanations and treatments directed toward the social and ritual situation of the sufferer still bear the greatest ideological weight.

Prog Clin Biol Res, 1982, 98, 73 - 81
Treatment of patients with sickle cell anemia--another view; Charache S et al.; Sickle cell anemia is a bad disease, and it occurs in black patients who still face obstacles that whites don't appreciate . Even if a new cure burst forth, it would not be available to many patients, and others would be afraid of it . It probably would not be as safe or effective as chloroquine for malaria or penicillin for pneumonia--and as a result, we should try to improve our present means for delivering care . Treatable complications must be recognized, and painful episodes must be managed with knowledge that no type of pain is exclusively physical or mental . If patients are to function in society, they must have marketable skills--and the current educational system in the United States is not prepared to provide such skills to such difficult students . Finally, there will be some lost souls, hopeless patients who live a shadowy life from which rescue seems nearly impossible . They need specialized care which is not currently available . Such care in special protected environments could be cost-effective, but would require such prolonged enthusiasm and commitment that it may be impossible to achieve.

Pediatr Radiol, 1982, 12(2), 99 - 101
Coincidental occurrence of actinomycosis and Ewing's sarcoma in a child; Bjork O et al.; Pulmonary consolidation, rarefaction of adjacent ribs and pleural effusion, a triad frequently considered characteristic of actinomycosis, seemed in the present case to support this serologically entertained diagnosis . However, the subsequent course of disease disclosed the most uncommon association of actinomycosis an metastatic Ewing's sarcoma of the lung . The possibility of combined occurrence of an opportunistic infection by actinomyces and malignancy, calls for open biopsy in cases not responding to penicillin treatment or with an unexpected evolution of the clinical manifestations.

Arthritis Rheum, 1982 Jan, 25(1), 42 - 7
Schönlein-Henoch syndrome in patients with familial Mediterranean fever; Flatau E et al.; Ten episodes of Schonlein-Henoch purpura (SHP) in 8 patients with familial Mediterranean fever (FMF) were observed . Five episodes developed 3-14 days after penicillin injections, suggesting an etiologic association . FMF and SHP have clear clinical similarities, and if the frequency of association of the 2 diseases is indeed high, perhaps a common etiologic factor should be sought . An immune complex mechanism might be the link between these 2 disease entities.

Am Surg, 1982 Jan, 48(1), 25 - 7
Pelvic actinomycosis associated with use of intrauterine device: a new challenge for the surgeon; Doberneck RC; PIP: Recent reports suggest that pelvic inflammatory disease (PID) is more common among users of the IUD than among those using other forms of contraception and that there is an association between IUD use and pelvic actinomycosis . In 1979 a woman at the University of New Mexico Hospital died from pelvic actinomycosis, the 2nd reported death from this disease associated with the use of an IUD, although her death from pulmonary embolus and Candida endocartidis should more appropriately be considered a complication of intravenous hyperalimentation . At least 25 patients are reported to have had serious pelvic actinomycosis associated with the use of an IUD . No particular type of IUD seems less likely to be associated with actinomycosis . Actinomyces are normally present in the gut and oropharynx, so that inoculation of the vagina with stool or saliva in combination with trauma induced by the foreign body such as an IUD may allow the actinomyces to enter tissues . Actinomyces are easily detected by Papanicolaou-stained cervicovaginal smears and are present in as many as 25% of symptomatic women using IUDs . Culture techniques usually fail in detecting actinomyces, the need for an anaerobic environment or overgrowth by bacteria which invariably accompany actinomyces are the usual causes of failure . Usual signs of IUD-associated actinomycosis are pelvic and lower abdominal or back pain, vaginal discharge, fever, and elevation of leukocyte count which are similar to symptoms of mild PID . Therefore these symptoms demand a Papanicolaou-stained cervicovaginal smear and search for actinomyces . Treatment includes removal of the IUD and administration of penicillin . However at least 1 patient after receiving treatment returned later with actinomycotic tubo-ovarian and subphrenic abscesses . A period of at least 4-6 weeks of therapy is usually recommended . Most patients with pelvic masses underwent hysterectomy and bilateral salpingo-oophorectomy in addition to penicillin and IUD removal; a few were successfully treated with drainage of an intra-abdominal abscess .

Acta Neurol Scand, 1982 Jan, 65(1), 51 - 8
EEG monitoring of focal lesions of the blood-brain barrier; Remler MP et al.; This paper presents a modified method for the EEG detection and monitoring of small focal blood-brain barrier (BBB) lesions . The method uses high dose IV penicillin (1.2 X 10(6) mu/kg) to produce a spike focus at BBB lesions, penicillin encephalopathy . The EEG is recorded and the epileptic spikes are counted by an automatic computer program . The computer produces an objective quantitative results . The method is verified empirically on traumatic and radiation BBB lesions.

Klin Padiatr, 1982 Jan, 194(1), 31 - 4
{Hearing defects after purulent meningitis (author's transl)}; Overkamp H et al.; 80 children in the age of 4 to 20 years who got over a purulent meningitis in infancy or childhood were examined by means of several audiological methods . Two children (2,5 percent) were found to be deaf . In 4 cases (5 percent) deafness was detected only unilateral not preferring the right or left ear . Hearing impairment after the eights cranial nerve damage was found in four children . 4 children suffered from severe to profound hearing defects on one side or bilateral . No correlation could be found between incidence and severity of the hearing defects to the total dose of the antibiotics that were penicillin, ampicillin and gentamycin . Before the background of the literature reported on this subject and the presented results hearing impairment after purulent meningitis seems to be more likely a sequela of inflammation than a toxic side-effect of the antibiotics.

Int Arch Allergy Appl Immunol, 1982, 67(3), 262 - 6
Antibody responses to impurities of penicillin in infants and rabbits; Ahlstedt S et al.; Antibody responses to penicilloyl were recorded in infants and children treated for about 1 week with intravenous ampicillin . In this single-blind, randomized study two commercially available preparations were compared, one of high-grade purity (less than 0.1 microgram antigen per gram) and the other slightly contaminated with high molecular weight proteinaceous material (1.5 microgram antigen per gram) according to a radioimmunoassay . The results showed no significant increase in the antibody titers in any of the patient groups . The immunogenic properties of high molecular weight proteinaceous impurities isolated from phenoxymethyl penicillin during manufacture were tested in rabbits given daily subcutaneous injections with 0.1-10 micrograms of the antigen over 10 day periods . When the 10-day period was repeated, the rabbits injected with more than 2 micrograms of antigen responded with both IgM/IgG and IgE antibodies . The clinical as well as the animal study indicates that antigen impurities in the preparations of the order of 2 micrograms per gram or less do not elicit a significant antibody response . However, the study in rabbits demonstrates that high molecular weight impurities can induce penicillin allergy if present in about 10-fold higher quantities than those usually found in the commercial penicillin preparations of today.

Br Heart J, 1982 Jan, 47(1), 101 - 2
Penicillin-sensitive Moraxella prosthetic endocarditis . Near disaster caused by failure to treat with penicillin; Chen W et al.; A patient with late prosthetic endocarditis resulting from Moraxella non-liquefaciens is reported . Correct laboratory indentification is of therapeutic importance as Moraxella is often highly sensitive to penicillin . Because of suspected penicillin sensitivity, antibiotics other than penicillin were used, but failed to control the endocarditis . Prompt response occurred when penicillin was given . Penicillin remains by far the most effective antibiotic for the treatment of endocarditis, particularly when affecting prosthetic valves, and caused by organisms sensitive to penicillin.

Infect Immun, 1982 Jan, 35(1), 187 - 92
Transfer of resistance with syphilitic immune cells: lack of correlation with mitogenic activity; Schell RF et al.; Hamsters infected intradermally with Treponema pallidum Bosnia A develop extensive chronic skin lesions, usually accompanied by metastatic lesions involving the paws, lips, and anal region and by lymph nodes teeming with treponemes . Throughout the course of syphilitic infection, cells from the inguinal lymph nodes responded poorly to stimulation with suboptimal, optimal, or supraoptimal concentrations of concanavalin A, phytohemagglutinin P, or lipopolysaccharide . The response of syphilitic spleen cells was variable . Depression of lymphocyte reactivity to mitogens preceded clinical signs of infection and correlated well with the chronicity of syphilitic infection . When syphilitic hamsters were treated with a curative dose of penicillin, their mitogenic responses returned to normal or were slightly elevated . No correlation existed between mitogenic activity and the ability of lymphoid cells to induce an effective immune response when transferred to normal recipients . No significant differences in protection were detected among recipients of immune cells with or without activity to mitogens . These results demonstrate that lymphocyte transformation by mitogens in vitro is not a measure of effective treponemicidal activity and so may not be a valid indicator of the protective immune status of syphilitic animals.

Arch Intern Med, 1982 Jan, 142(1), 139 - 40
Meningovascular syphilis after 'appropriate' treatment of primary syphilis; Moskovitz BL et al.; Meningovascular syphilis developed in a patient two years after the treatment of primary syphilis with a single intramuscular injection of 2.4 million units of penicillin G benzathine as recommended by the Centers for Disease Control . Although it could not be established with certainty whether this infection represented a reinfection or a treatment failure, the case emphasizes the necessity for serologic follow-up examination in all patients treated for primary syphilis.

Gastroenterology, 1982 Jan, 82(1), 135 - 9
Rectal mass caused by Treponema pallidum: confirmation by immunofluorescent staining; Quinn TC et al.; A 37-yr-old homosexual man presented with mild anorectal symptoms, a diffuse maculopapular rash, constitutional symptoms, and a reactive serologic test for syphilis . Sigmoidoscopy revealed a 2 x 2-cm indurated rectal mass 5 cm above the anal verge . Darkfield examination of rectal exudate revealed motile treponemes and rectal biopsy of the mass showed diffuse infiltration of plasma cells and lymphocytes . Large numbers of spirochetes were present on silver stain of the rectal biopsy specimen and these were shown to be Treponema pallidum by indirect immunofluorescence . The rectal mass and symptoms resolved following penicillin therapy . This case and a review of previously reported cases of anorectal syphilis emphasize the significance of these often neglected and misdiagnosed lesions of syphilis.

Acta Odontol Scand, 1982, 40(5), 299 - 305
The effect of penicillin- and tetracycline-containing medicaments on the microhardness of human dental enamel . An in vitro study; Bjorvatn K et al.; While the sugar content of various medicaments has been accepted as a hazard to dental health, the possible detrimental effect of the medicaments per se has been largely overlooked . In the present study the microhardness of dental enamel was examined before and after the exposure to various salts of penicillin, to tetracycline chloride, and to human saliva . The Vickers hardness index was found to 1 . remain stable or increase slightly in enamel exposed to saliva, nonaqueous penicillin suspensions and certain watery solutions of phenoxymethylpenicillin calcium . 2 . decrease to a moderate degree in most aqueous penicillin solutions, and 3 . decrease drastically in tetracycline solutions and in phenoxymethylpenicillin calcium solutions containing citrate . The results indicate that a direct reaction may take place between the dental enamel and the medicament and/or its degradation products when antibiotic compounds are taken per os.

Eur J Clin Pharmacol, 1982, 23(3), 245 - 8
Absorption of penicillin and paracetamol after small intestinal bypass surgery; Terry SI et al.; Drug absorption was studied in morbidly obese patients before and after jejunoileal bypass . The absorption of phenoxymethyl penicillin was considerably increased whilst that of paracetamol was unchanged.

J Int Med Res, 1982, 10(5), 379 - 82
Bioavailability of paediatric mixtures containing phenoxymethylpenicillin calcium or potassium salt; Soininen K et al.; The bioavailability of the calcium and potassium salts of phenoxymethyl-penicillin (dose 38,000 I.U./kg) was investigated in eight healthy adult volunteers . Administration of the calcium salt as an aqueous oral mixture resulted in a mean peak plasma concentration of 8.52 mg/l (SD 1 X 96) and that of the potassium salt mixture in a concentration of 8.40 mg/ml (SD 2.61), p greater than 0.1 . The median time-to-peak levels were 0.75 h and 1.0 h, respectively (p greater than 0.1) . The mean AUC for the calcium salt mixture was 16.94 mg X h/l (SD 3.31) and for the potassium salt 15.84 mg X h/l (SD 4.76), p less than 0.09 . These findings confirm that an aqueous mixture of calcium phenoxymethylpenicillin is equivalent to a mixture of potassium phenoxymethylpenicillin.

J Int Med Res, 1982, 10(1), 42 - 5
Single oral dose rosoxacin in the treatment of gonorrhoea in males; Limson BM et al.; A study of the new anti-bacterial agent, rosoxacin, a quinoline derivative was made in male subjects with uncomplicated acute gonorrhoea using a single oral dose of 200 mg and a single dose of 300 mg . Of the eight patients who received a single dose of 200 mg, post-treatment urethral smears and cultures for N . gonorrhoeae were positive in all and these subjects were considered as treatment failures . In contrast, a single dose of 300 mg was highly effective as all twenty-four who received this dose were cured as judged by negative urethral smears and cultures on the 7th post-treatment day . Of the thirty-eight isolates of M . gonorrhoeae obtained in the study, fifteen (39.5%) were penicillinase-producing, indicating that rosoxacin is effective in treating penicillin-resistant gonorrhoea . Mild to moderate dizziness and/or drowsiness was experienced by four of twenty-nine patients evaluated for safety on the 300 mg single dose, giving an incidence of side-effects of 14% . The symptoms were of brief duration and were self-limiting . A single oral dose of this drug appears to be an ideal treatment for the rapid cure of acute gonorrhoea.

Vet Med Nauki, 1982, 19(5), 85 - 94
{Clinico-pharmacological trial of the preparation streptobicillin depot-syringae mammariae}; Tsolov S et al.; Streptobicillin depot-syringae mammariae contains: benzathin-penicillin--1,200,000 UI, streptomycin sulfa--1,000,000 UI, vitamin A oleosum--15,000 UI in a suitable base up to 10 ml . It is intended for the therapy and prophylaxis of inapparent mastitis of cows during the dry period . The preparation was tested in a total of 301 udder quarts of cows in terms of tolerance (general and local), depot effect, residual amounts, bactericidic effect, and therapeutic effect . The preparation was found to be well tolerated by the body and the parenchyma of the udder . The duration of its effect was 25 days . No residual amounts were found in the milk during the following lactation . The bactericidic effect in vitro reached 92.4 per cent, and in vivo--87.3 per cent of the cases . Positive therapeutic effect was found in 87.1 per cent of the cases, with subclinical mastitis it being 80.2 per cent, with latent infections--96.2 per cent, with secretion disturbances--94.3 per cent . Results revealed that the preparation was suitable to control inapparent mastitis in cows during the dry period.

Folia Microbiol (Praha), 1982, 27(6), 370 - 6
DNA synthesis in Escherichia coli B/r after UV-irradiation; Kucerova H et al.; When studying the kinetics of DNA synthesis, growth and cell division in Escherichia coli B/r after irradiation with different doses of UV-radiation (254 nm) we could demonstrate, by means of pulse incorporation of 3H-thymidine, a lag in DNA synthesis after the irradiation . The relative rate of the restored DNA synthesis (related to the number of viable cells) was higher than in the non-irradiated culture . After 3 h the rate of DNA synthesis settled at a constant value, which was identical with the control rate up to the "critical dose" of 20 J/m2 . The irradiated cell population is heterogenous and contains basically two categories of cells--surviving and non-surviving . Cells of both types contribute to DNA synthesis restored after the lag period to a different extent . During the first hour after the irradiation even the nonviable portion of the population, i.e . cells that do not form colonies but are still penicillin-sensitive, is involved in the DNA synthesis.

Exp Brain Res, 1982, 47(1), 154 - 7
Effect of sodium ions on penicillin-induced epileptiform activity in vitro; Hablitz JJ et al.; Intra- and extracellular recordings were obtained from the CA1 region of guinea pig hippocampal slices maintained in vitro . We studied the effect of reducing the extracellular sodium concentration on penicillin-induced epileptiform responses . In control experiments, Tris and choline were assayed as sodium substitutes . Choline was found unsuitable, since it induced repetitive firing in the absence of any convulsant agent . Replacement of 50% of the extracellular sodium ( {Na+}o) with Tris reduced the amplitude of the presynaptic fiber volley, the field EPSP, and the population spike . Intracellular studies showed that when {Na+}o was lowered, action-potential amplitudes were reversibly depressed by an amount close to that predicted by the Nernst relation . Orthodromically elicited epileptiform discharges, induced by penicillin, were reduced in a low-sodium medium when constant stimulus currents were employed . If orthodromic stimulus strengths in normal and low-sodium states were equated on the basis of the field-EPSP amplitude, no significant diminution of the depolarizing-wave component of the epileptiform response was observed . These results suggest that a synaptic component underlies penicillin-induced epileptiform discharges.

Intensive Care Med, 1982 Jan, 8(1), 33 - 8
Cefotaxime in treatment of meningitis and ventriculitis? Evaluation of drug concentrations in human cerebrospinal fluid; Bruckner O et al.; In three groups of patients levels of cefotaxime in serumand cerebrospinal fluid were determined . Therapeutic value and efficacy are discussed in meningitis patients . Nine concentrations of cefotaxime in lumbar and ventricular CSF out of 19 in a group of seven neurosurgical patients with mild to moderate impairment of the blood-CSF-barrier were higher than 0.5 micrograms/ml . In seven determinations in a second group of six patients with no or very little dysfunction of the blood-cerebrospinal-fluid barrier only twice cefotaxime was not detectable in lumbar CSF . Concentrations of cefotaxime in 25 determinations of lumbar or ventricular CSF in six patients with bacterial meningitis ranged from 1.1 micrograms/ml to 19.2 micrograms/ml . Treatment with cefotaxime alone was successful in a patient with E . coli meningitis and ventriculitis after infection of a ventriculo-atrial shunt and in another patient with pneumococcal meningitis and penicillin allergy . The other four patients with bacterial meningitis were treated successfully by antibiotics including cefotaxime.

Infection, 1982, 10 Suppl 3, S221 - 6
{Studies with azlocillin, mezlocillin, penicillin-g-potassium and sisomicin on tolerance in the cornea and the kinetics of inhibiting concentrations in the cornea and aqueous humor in rabbits}; Gauri KK et al.; We studied the effect of azlocillin, mezlocillin and sisomicin in concentrations of 1, 2.5 and 5% on the regeneration of stromal corneal wounds in rabbits following subconjunctival injections and treatment with eye drops . Concentrations of the antibiotics were also determined in corneal tissue and in aqueous humor and compared with that of penicillin G-potassium . Together with azlocillin, sisomicin proved to be the most effective and the safest . Mezlocillin only inhibited wound regeneration slightly and thus mezlocillin appears to be inferior to the other two antibiotics investigated in the local treatment of the eye.

Infection, 1982, 10 Suppl 3, S172 - 5
Mezlocillin in the treatment of gonorrhea; Kataniwa Y et al.; Mezlocillin (2 g) was administered by a single intravenous injection to 32 male patients with gonorrheal urethritis and to five female patients with gonorrheal cervicitis, none of whom had received any pre-treatment or had had any complications . The results of the treatment were "good" in 32 cases (86.5%), "fair" in three (8.1%) and "poor" in two patients (5.4%) . One of the two "poor" cases showed no sensitivity to any penicillin derivative . Nausea during injection was observed twice, but the patients recovered immediately after the injection.

Infection, 1982, 10 Suppl 3, S158 - 65
{Mezlocillin in neonatal medicine}; Sitka U et al.; The acylureido penicillin mezlocillin was tested clinically and pharmacologically in neonates and young infants who received the antibiotic for prophylactic and therapeutic reasons . On the basis of blood level determinations following the administration of various dosages, we consider a dose of 200 mg/kg per day necessary for premature babies and 300-400 mg/kg per day for full-term babies . Pharmacokinetic data showed age-dependent features . The clinical results were good in 40 children treated with mezlocillin . Twenty of these children received a combination of mezlocillin and gentamicin . No child died of an infection . Therapy was not successful in three babies suffering from productive bronchopulmonary infections . Important side-effects were not observed.

Curr Med Res Opin, 1982, 8(4), 247 - 52
A controlled study of mezlocillin in uncomplicated acute gonorrhoea; Khan MH et al.; In a randomized trial, 149 patients with uncomplicated gonorrhoea were treated with a single intramuscular dose of 1.0 g mezlocillin, 150 with 2.0 g ampicillin plus 1.0 g probenecid orally and 150 with a single dose of 1.8 mega units of procaine penicillin . Cure rates at 3, 10 and 17 days after treatment were 97%, 99% and 96% for mezlocillin, 95%, 99% and 95% for ampicillin, and 97%, 98% and 98% for procaine penicillin, respectively . The incidence of post-gonococcal urethritis was 11.3% for ampicillin plus probenecid, 10.9% for procaine penicillin and 10.5% for mezlocillin . Side-effects after all three regimens were minimal.

Physiol Bohemoslov, 1982, 31(3), 203 - 12
Penicillin activates spontaneous motility in chick embryos; Sedlacek J; The development of the motor reaction to i.v . injection of the sodium salt of penicillin G in a dose of 0.9 x 10(6) I.U./kg egg weight was studied in chick embryos (normal and spinal) from the 11th to the 19th day of incubation . Penicillin first caused standard activation of embryonal motility from the 15th day of incubation, in both normal and spinal embryos . Activation was at first continuous in character (a twofold increase in the frequency of spontaneous movements) . In 17- and particularly in 19-day embryos a typical paroxysmal reaction developed, with pronounced intervals of motor rest . The proportion of the spinal component in the penicillin reaction was abut 40% and of the supraspinal component about 60% of total motor activity . In older embryos (after the 15th day of incubation), the motor reaction to penicillin could be effectively modified by the systemic administration of glycine and GABA . It is concluded from the results that penicillin does not activate embryonal motor activity until a given stage of development of the CNS has been attained . It is a developmental phenomenon with a spinal and a supraspinal component, in which central inhibitory mechanisms participate.

Dtsch Z Verdau Stoffwechselkr, 1982, 42(2-3), 85 - 93
{Cholestatic jaundice induced by D-penicillamine and oral steroid contraceptive in progressive systemic sclerosis (author's transl)}; Wozel G et al.; PIP: A 25 year old woman with progressive systemic sclerosis was treated with D-penicillamine (DPA) . 30 days after the initiation of therapy, cholestatic jaundice was observed . Moreover, for 2 years, the patient has taken the pill . Both drugs were discontinued, the jaundice disappeared, and the laboratory findings of the liver were normal . A rechallenge of DPA after 9 months induced no reaction . An underlying chronic liver disease before cholestasis could be excluded by liver biopsy . Allergic cutantests and lymphocyte transformation test with DPA and penicillin gave normal results . The frequency of cholestatic jaundice caused by DPA therapy is discussed and the possible pathomechanism is analyzed . (author's modified)

Int Arch Allergy Appl Immunol, 1982, 68(4), 352 - 7
Development and use of three new radioallergosorbent tests in the diagnosis of penicillin allergy; Edwards RG et al.; The synthesis and characterisation of three novel reagents for use in the radioallergosorbent test (RAST) for the diagnosis of penicillin allergy are described . The antigenic determinants involved are the benzyl penicillanyl, thiol-linked benzyl penicillenate and thiol-linked penicillamine . These reagents, and also one specific for the benzyl penicilloyl group, have been used to evaluate the sea of subjects suspected of suffering from penicillin allergy and to explore the aetiology of the respiratory dyspnoea experienced by some workers exposed to penicillin-containing dusts . The use of these reagents, while confirming the importance of the penicilloyl or major determinant of penicillin allergy, has shown that there is heterogeneity in the IgE response of penicillin-allergic patients and some patients have IgE antibody specific for one or more of the new determinants only . These reagents will, therefore, increase diagnostic capabilities . Their use has also confirmed that the disorder induced by occupational exposure to penicillins is not primarily mediated by IgE antibody specific for allergenic determinants represented by any of the available reagents.

Electroencephalogr Clin Neurophysiol, 1982 Jan, 53(1), 1 - 13
Laminar analysis of spindles and of spikes of the spike and wave discharge of feline generalized penicillin epilepsy; Kostopoulos G et al.; Intracortical laminar profiles of spindles and spikes of spike and wave complexes in feline generalized penicillin epilepsy were studied using two methods: (i) sequential microelectrode recordings at various cortical depths, and simultaneous recordings at multiple cortical depths using a fine multi-contact electrode . Raw EEG data and EEG epochs averaged with respect to peaks of surface EEG waves were analyzed . Spindles and the spikes of the spike and wave complexes showed similar laminar profiles . This supports the hypothesis that the two are basically the same cortical electrophysiological phenomenon, the spike being a spindle wave enhanced and slightly altered because of the penicillin-induced increased cortical excitability . The latter causes the weight of the thalamic input to shift from superficial to more deep lying synapses . Both surface negative and surface positive phases of spindles and of spikes of spike and wave complexes show similar laminar profiles, those of the former suggesting activation of excitatory synapses in the superficial cortical layers, those of the latter suggesting activation of more deeply located excitatory synapses . The profiles generally conform to the dipole hypothesis of cortical electrogenesis and suggest that spindles and spikes of spike and wave complexes are generated by the same pyramidal neurons, probably through activation of the same sets of synapses . Some inconstant and relatively minor deviations of the laminar profiles from the pattern predicted by the dipole theory of cortical electrogenesis were encountered and are tentatively explained in the light of some of the complexities of the microanatomical organization of mammalian neocortex.

Neuroscience, 1982, 7(8), 1955 - 61
Neuronal responses to putative neurotransmitters during penicillin epileptogenesis; Avoli M et al.; An epileptogenic process was induced within the rat frontoparietal cortex by microiontophoretic applications of penicillin . The temporal development of the penicillin-induced activity was divided into (a) a first phase characterized by an increased rate of neuronal firing, (b) a pre-paroxysmal phase wherein neurons began to fire clusters of action potentials and (c) a paroxysmal phase characterized by a discharge of action potential clusters . The excitatory responses to glutamate and to acetylcholine appeared to be enhanced during the first and pre-paroxysmal phases, whereas a loss of the excitatory effectiveness of both glutamate and acetylcholine occurred during the final paroxysmal phase . Forty nine of 69 neurons studied (71%) showed a decreased sensitivity to gamma-aminobutyrate during the first phase of penicillin iontophoresis . However, during this same time, glycine-induced inhibition was not decreased . During the second phase, gamma-aminobutyrate-induced inhibition was even less effective, and glycine started to lose effectiveness . During the third phase, both these inhibitory neurotransmitters failed to affect the neuronal activity . The other 29% of the neurons studied showed a general diminution to the actions of both gamma-aminobutyrate and glycine when penicillin-induced action potential clusters appeared . Our results suggest that penicillin interferes with gamma-aminobutyrate-mediated inhibition in a large proportion of cortical neurons of the rat . Furthermore, these cortical neurons show changes in the responses to both excitatory and inhibitory neurotransmitters that closely parallel the development of penicillin-induced activity.

Biochim Biophys Acta, 1981 Dec 29, 671(2), 109 - 16
Studies on the primary structures of the exocellular D-alanyl-D-alanine peptidases of Streptomyces strain R61 and Actinomadura strain R39; Duez C et al.; The Mr 37 000 D-alanyl-D-alanine peptidase excreted by Streptomyces R61 and the Mr 53 000 D-alanyl-D-alanine peptidase excreted by Actinomadura R39 are both characterized by a very uneven distribution of the basic (Arg + Lys) amino acid residues . Trypsin degradation of the heat-denatured enzymes generates (1) thirteen soluble peptides which contain from 2 to 28 residues in the case of the R61 enzyme and nineteen soluble peptides which contain 2 to 39 residues in the case of the R39 enzyme; and (2) three large segments or core peptides which, irrespective of the enzymes from which they originate, consist of 50-60, 70-80 and 110-120 residues . About 90% of the basic (Arg + Lys) amino acid residues are recovered in the soluble tryptic peptides . The core peptides represent 62% (Mr approximately 23 000) and 45% (Mr approximately 24 000) of the untreated R61 and R39 enzymes, respectively . One 28-residue soluble peptide isolated from the R61 enzyme represents the N-terminal portion of the protein whose sequence has been established . The penicillin attachment site of the R61 enzyme has been located in one of the core peptides . For the R39 enzyme, indirect evidence shows that the penicillin binding site is probably within one of the soluble peptides.

JAMA, 1981 Dec 4, 246(22), 2583 - 4
Cerebrospinal fluid penicillin levels during therapy for latent syphilis; Ducas J et al.; Cerebrospinal fluid and serum penicillin levels were determined in patients with latent syphilis . Mean serum concentration one week after the third weekly dose of 2.4 million units penicillin G benzathine was 0.32 units/mL . Concurrent administration of probenecid orally produced a mean serum penicillin level of 0.41 units/mL . Doubled penicillin doses without and with daily orally administered probenecid resulted in mean serum concentrations of 0.75 and 1.00 units/mL, respectively . Two of six patients in the last group had CSF penicillin concentrations greater than 0.03 units/mL.

Rev Electroencephalogr Neurophysiol Clin, 1981 Dec, 11(3-4), 317 - 23
{Transcortical reflexes of proprioceptive origin and motor epilepsy (author's transl)}; Gioanni Y et al.; The long-loop reflex involved in the triggering of paroxysmal activities by proprioceptive afferents is examined in monkeys with a chronic alumina focus and in cats with an acute penicillin focus . Electrical stimulation of a tibial nerve in monkeys as well as muscle stretch in cats elicit a cortical 'evoked spike', i.e., an evoked potential followed by an epileptic spike, accompanied by one or two motor bursts in the muscles concerned . With a very small acute focus, this transcortical reflex is shown to be quite topical: muscles in the vicinity are not affected . Relationships between evoked spike and myoclonic jerk are examined and it is shown that motor efferents usually follow the pyramidal tract . The concept of a transcortical reflex of proprioceptive origin is discussed on the basis of data collected from these models.

Infect Immun, 1981 Dec, 34(3), 930 - 7
Effects of metabolic inhibitors on extracellular fructosyltransferase production in Actinomyces viscosus; Chak W et al.; Extracellular fructosyltransferase (levansucrase; EC 2.4.1.10) production in Actinomyces viscosus T14AV was demonstrated to occur concomitantly with cellular growth . The inhibition of both cellular ribonucleic acid and protein synthesis resulted in no further accumulation of enzyme activity . The antibiotic sodium clofibrate differentially inhibited the production of fructosyltransferase by strain T14AV . Furthermore, the antibiotic preferentially inhibited {14C}acetate incorporation into cellular lipid, but did not affect protein synthesis . In addition, no inhibition of fructosyltransferase production was observed upon the addition of the fatty acid acid synthesis inhibitor cerulenin . On the other hand, extracellular fructosyltransferase production was apparently stimulated in the presence of the cell wall synthesis inhibitors penicillin, amphomycin, and tunicamycin . These results are discussed in terms of the mechanism of extracellular protein production in A . viscosus.

Clin Obstet Gynecol, 1981 Dec, 24(4), 1187 - 97
Medical and surgical management of the pelvic abscess; Benigno BB; PIP: A pelvic abscess is the end stage in the progression of a genital tract infection and is frequently preventable . The abscess may fill the pelvis and occasionally the lower abdomen, and is usually posterior to the uterus and bound by the sigmoid colon, loops of small bowel, cul-de-sac, and sidewalls of the pelvis . A tubo-ovarian abscess may occur in the acute stage of pelvic inflammatory disease (PID) but is more common with chronic or subacute PID . An abscess occurs when pus from the fallopian tube spills onto the ovary and infects it at the site of follicular rupture or by direct penetration . Pelvic and abdominal pain which is bilateral and aggravated by motion and intercourse, and fever possibly exceeding 103 degrees fahrenheit with leucocytosis, tachycardia, and prostration are the most common symptoms of pelvic abscess . The pelvic examination may reveal all gradations of pathology, but because of the degree of guarding and tenderness it elicits, the abscess may elude the examiner . The rectal examination, computerized tomography, and ultrasonography are useful in diagnosis . Other disorders such as acute appendicitis and ecoptic pregnancy may be mistaken for abscess . Patients with pelvic abscesses should be immediately admitted to hospital regardless of the size of the abscess because the broad-spectrum anerobic antibiotic coverage needed is most effectively provided there . Preservation of normal tubal function is rarely possible in patients developing tubal abscesses . Bed rest, fluid and electrolyte replacement, nasogastric suction when indicated, and antibiotics are the basis of medical treatment . Controversy exists regarding appropriate antibiotic therapy, but the probable presence of anaerobic organisms should be kept in mind . Patients with pelvic abscesses are frequently given a triple antibiotic regimen including clindamycin, gentamicin, and aqueous penicillin . Guidelines for the failure of medical management in patients with a pelvic abscess include persistent fever, increase in size of abscess, persistent ileus, suspicion of rupture, septic shock, and uncertainty of the diagnosis . A posterior colpotomy is preferable to a laparotomy if surgical treatment is necessary, but it is only suitable for selected patients . Removal of a pelvic abscess frequently involves a total abdominal hysterectomy . Operating instructions and diagrams are included . Rupture of a pelvic abscess is life threatening and requires immediate surgery .

Zh Mikrobiol Epidemiol Immunobiol, 1981 Dec, (12), 36 - 9
{Comparative study of the behavior of capsular and noncapsular pneumococcus variants in the L929 cell culture}; Gotvianskaia TP et al.; The comparative study of the behavior of the capsular and noncapsular variants of pneumococci, serotype 27, in culture L929 revealed that under the conditions of the experiment both variants showed the same capacity for adhesion, but the capsular variant had a stronger cytopathic effect which was retained after subculturing the infective material in the cell culture . The possibility of isolating the noncapsular variant of pneumococci from culture L929 on a solid nutrient medium lasted only 9 hours, while the capsular variant could be isolated during the whole experiment . The noncapsular variant showed greater sensitivity to the action of penicillin and more pronounced capacity for L-transformation in vitro than the capsular one.

Pediatr Res, 1981 Dec, 15(12), 1533 - 7
Chronic granulomatous disease: mode of action of sulfamethoxazole/trimethoprim; Gmunder FK et al.; Four possible modes of action for the clinically observed effectiveness of sulfamethoxazole/trimethoprim in chronic granulomatous disease were evaluated: (1) inhibition of bacterial catalase, (2) improvement of granulocyte oxygen metabolism, (3) synergism of the antibiotic with nonoxygen-dependent granulocyte killing mechanisms, and (4) a purely antibiotic effect based on uptake and concentration of the antibiotic by and within granulocytes . While the first three mechanisms were excluded, the fourth mechanism is highly probable; sulfamethoxazole was found to reach granulocyte associated concentrations 1.7-fold and trimethoprim 4.1-fold of extracellular levels . Penicillin G, a known nonpenetrating antibiotic, reached 0.3-fold, and tetracycline, a known penetrating agent, 7.1-fold the extracellular level . These findings indicate that sulfamethoxazole/trimethoprim is an antibiotic combination uniquely suited for the long-term prophylaxis of infections in patients with defects of intracellular phagocyte killing.

Antibiotiki, 1981 Dec, 26(12), 920 - 32
{E . coli penicillin amidase . Methods for estimating the close ionization constants of ionogenic groups of the enzyme complex with substrates containing free amino groups}; Nys PS et al.; The possible use of various procedures for estimation of the ionization constants of the Michaelis complex by the pH dependence of the maximum enzymatic reaction rate is discussed . It is shown that the procedures described in the literature for estimation of the close ionization constants of the enzyme-substrate complexes have limitations and in some cases cannot be used . The paper presents the methods for estimation of the constants and means for quantitative description of the bell-shaped pH dependence of the kinetic and equilibrium parameters of the biocatalytic reaction . The equations recommended in the paper were used in analysis of the pH dependences of the maximum rate of the reactions during the enzymatic synthesis of cefalexin catalysed with immobilized penicillinamidase (IPA) (CE 3.5 . 1.11) . The ionization constants of the enzyme-substrate complexes of IPA were compared during hydrolysis and synthesis of the compounds acylated with phenylacetic and aminophenylacetic acids . The effect of the nature of the leaving substrate group and added nucleophilic gent on the electrochemical state of the Michaelis complex is discussed.

Br J Vener Dis, 1981 Dec, 57(6), 357 - 62
Sexually transmitted diseases in Ethiopia . Social factors contributing to their spread and implications for developing countries; Plorde DS; PIP: The high prevalence of all types of sexually transmitted diseases (STD) in Ethiopia, estimated in various field studies at 32-70%, led to analysis of the economic and psychosocial factors influencing the spread of these diseases . These factors were examined primarily in relation to the Amhara people, who comprise 30% of the Ethiopian population and live in the central highlands . Increases in migration and urbanization associated with the struggle toward economic development have weakened family and community relationships and encouraged sexual promiscuity, leading to an increase in STD incidence . The disruptive effects of sudden land nationalization caused many farmers to leave the land, forcing their wives to seek employment, which puts them at high risk of contracting the spreading STD . Moreover, there are far more women than men in the roadside and market villages, and STD are spread when men travel through or bring goods to market . Most marriages among the Amhara are temporary, with dissolution obtainable by mutual agreement . This custom provides women with opportunities for numerous transient sexual liaisons . Because of the limited employment opportunities available to women in Ethiopia, many select beer selling and prostitution as a way to earn an income . Thus, changes in the social structure, particularly in relation to the status of women, are contributing to the spread of STD . In general, neither health professionals nor the general population in Ethiopia understand the transmission process of STD, the serious nature of the problem, or how these diseases should be treated . Most treatment is provided by relatively untrained "dressers." Laboratory tests are often not performed, and penicillin is administered indiscriminately . Longterm solution of the STD problem requires Ethiopia to: 1) join other African countries in establishing data on census and disease prevalence to assess the extent of the problem, 2) increase the availability of good health services and the number of trained personnel, 3) adopt an appropriate health education strategy, and 4) change the status of women by increasing their educational and occupational opportunities . As a 1st step, a committee has been appointed to devise a plan to eliminate prostitution .

J Immunol, 1981 Dec, 127(6), 2410 - 4
The transition from specific to nonspecific desensitization in human basophils; MacGlashan DW Jr et al.; Human basophils can be desensitized to IgE-mediated stimuli either specifically (to the desensitizing antigen only) or nonspecifically (to all antigens) . It has been suggested that the specificity of desensitization depends on the number of membrane-bound, antigen-specific IgE antibody molecules per basophil . We have varied the number of IgE antibody molecules/basophil by passive sensitization of mixed leukocyte preparations with increasing concentrations of purified IgE anti-penicillin (BPO) antibody . The cells were then desensitized with penicillin-human serum albumin (BPO-HSA) . Desensitization was specific (lack of response to BPO-HSA only) with 1000 specific antibody molecules/basophil, and increasingly nonspecific (greater than 70% desensitization to rechallenge with anti-IgE and ragweed antigen E as well as lack of response to BPO-HSA) as the number of antibody molecules was increased to 14,000 . This formally established that the number of specific IgE antibody molecules/basophil determines the mode of desensitization.

Dtsch Med Wochenschr, 1981 Nov 13, 106(46), 1541 - 4
{Arterial vascular occlusion in penicillin allergy (author's transl)}; Martin M et al.; A nodular exanthema of the skin was observed in an 8-year-old girl . She had been treated with penicillin a few days ago because of a gastrointestinal infection . Continuation of penicillin treatment led to occlusion of larger arteries with gangrene of the forefoot . This was accompanied by septic temperatures and superinfected skin lesions . Angiologic and angiographic investigations showed a right-sided femoro-popliteal occlusion and occlusions of the arteries of the lower leg . On the left side there was spasm of the superficial femoral artery . After cessation of penicillin and high-dose steroid therapy rapid restitution occurred . Arterial spasms regressed, the occlusions remained persistent, but there was adequate collateral blood supply and ischaemic acral necroses healed . An allergic reaction of the intermediary type involving major arteries can be considered causative underlying pathology.

Med Klin, 1981 Nov 6, 76(23), 653 - 5
{Rat bite disease with meningoencephalitic involvement}; Kiefer H et al.; Reported is the case of a 32 years old man, who developed a severe condition with recurrent fever episodes, lymphadenopathy, liver and spleen enlargement, and severe headaches 6 weeks after having been bitten by a rat . The headaches even increased during the further course . Psychological tests indicated an increased instability and irritability . The brain scan revealed diffuse cerebral ischemias (on the basis of an increased cerebrovascular resistance) . Following the treatment with penicillin, the symptoms cleared almost completely . Although the pathogenic organism could not be identified, the findings and the clinical course of the disease indicate the presence of sodoku with meningoencephalopathic involvement.

J Am Vet Med Assoc, 1981 Nov 1, 179(9), 896 - 8
Malignant hyperthermia in a halothane-anesthetized horse; Waldron-Mease E et al.; Malignant hyperthermia developed in a 4-year-old Thoroughbred horse following 3 hours and 15 minutes of halothane anesthesia, with supplementary succinylcholine . Clinical signs included fever, sweating, hyperventilation, tachycardia, and decreased blood pressure followed by a rapid increase in blood pressure . Biochemical aberrations included hypocalcemia, hyperkalemia, hyperphosphatemia, myoglobinuria, and high creatine phosphokinase and ornithine carbamyl transferase activities . Treatment consisted initially of surface cooling with cold water, alcohol and ice, IV administration of cooled balanced electrolyte solutions and sodium bicarbonate, and removal from the anesthetic and rebreathing circuit . Oxygen was given by endotracheal insufflation . The rectum was then packed with ice, the horse was moved to a recovery raft and pool, and his body was packed in ice . Xylazine and dantrolene were given during recovery from anesthesia . Following recovery, treatment consisted of administration of balanced electrolyte solutions, calcium borogluconate, potassium penicillin, meperidine, and additional dantrolene . Muscle biopsy demonstrated exaggerated contracture responses to halothane and caffeine, confirming a diagnosis of malignant hyperthermia . The horse was returned to training following a routine postsurgical convalescent period.

Ann Emerg Med, 1981 Nov, 10(11), 593 - 5
Acute necrotizing ulcerative tonsillitis and gingivitis (Vincent's infections); Kaplan D; The cases of two patients with acute necrotizing ulcerative infections are reported . One had involvement of the tonsil and the other, of the gingivae . In both cases a Gram stain revealed abundant fusiform rods and spirochetes . Both patients responded to treatment with oral penicillin, showing improvement and/or healing in three to six days . These two cases demonstrate the usefulness of the Gram stain in supporting a diagnosis which would otherwise rest solely on clinical grounds.

Res Vet Sci, 1981 Nov, 31(3), 281 - 3
Effect of repeated biopsy sampling on endometrial concentrations of sodium benzylpenicillin following intramuscular injection in pony mares; Allen WE et al.; Endometrial concentrations of sodium benzylpenicillin were determined in biopsy samples from anoestrous pony mares after intramuscular administration of the penicillin at 22,000 iu/kg . Serum samples, collected at the same time as biopsies, were also assayed for their penicillin content . In experiment 1 a single pair of blood and tissue samples was taken from each mare between five and 360 minutes after injection . In experiment 2 each mare was sampled consecutively six times (between five and 300 minutes) after injection . Both serum and endometrial concentration reached a peak between 15 and 30 minutes after injection . Tissue concentrations were lower than serum, except after 180 minutes in experiment 2 . This suggests that at the time intervals used in the present study, serial biopsies eventually caused an increase in the endometrial content of penicillin.

Med J Zambia, 1981 Nov-1982 Jan, 16(1), 11 - 3
Abdominal actinomycosis; Elem B et al.; Four cases of abdominal actinomycosis managed during a two year period at Ndola Central Hospital are reported with a review of relevant literature . Difficulties associated in diagnosing this form of the disease are stressed . It is suggested that a limited form of surgery in combination with parenteral penicillin therapy is usually effective in the management of abdominal actinomycosis.

Med J Zambia, 1981 Nov-1982 Jan, 16(1), 11 - 3
Abdominal actinomycosis; Elem B et al.; Four cases of abdominal actinomycosis managed during a two year period at Ndola Central Hospital are reported with a review of relevant literature . Difficulties associated in diagnosing this form of the disease are stressed . It is suggested that a limited form of surgery in combination with parentral penicillin therapy is usually effective in the management of abdominal actinomycosis.

Rev Infect Dis, 1981 Nov-Dec, 3 suppl, S289 - 92
Vancomycin for treatment of bacterial meningitis; Gump DW; Clinical experience with vancomycin for the treatment of bacterial meningitis has not been extensive . Presently available data indicate that when meningeal inflammation is present intravenously administered vancomycin penetrates into cerebrospinal fluid and therapeutically effective levels of drug therein are frequently attained . Treatment of meningitis with vancomycin has been effective in clinical situations that precluded the use of the commonly administered agents, i.e., in infections due to resistant strains or to unusual organisms, in patients allergic to penicillin, and in patients for whom therapy with a first-choice antibiotic has failed . When response to intravenously administered vancomycin was unsatisfactory, the addition of intrathecal therapy resulted in a favorable outcome in some patients . Combination therapy with agents that act synergistically with vancomycin has been beneficial . Vancomycin warrants serious consideration as a useful alternate antibiotic for the treatment of bacterial meningitis.

Otolaryngol Head Neck Surg, 1981 Nov-Dec, 89(6), 910 - 11
Peritonsillar abscess: needle aspiration; Herzon FS et al.; Needle aspiration and antibiotics (usually penicillin) were used as the sole initial treatment of peritonsillar abscess in 29 patients over a 2 1/2-year period . Positive aspirations occurred in 23 patients, 19 (82%) of whom had complete resolution of their abscesses without further initial therapy . The implications of these findings are discussed.

Antimicrob Agents Chemother, 1981 Nov, 20(5), 693 - 5
Comparative efficacy of piperacillin and penicillin G in treatment of gonococcal urethritis; Landis SJ et al.; The comparative efficacy of 2 g of piperacillin and 4.8 X 10(6) U of penicillin G in the treatment of uncomplicated gonococcal urethritis was assessed in a randomized prospective study . Sixty-five evaluable patients received piperacillin, and 55 received penicillin G . All patients received either therapy were cured of gonorrhea . We conclude that piperacillin is as efficacious as aqueous procaine penicillin G in the therapy of uncomplicated gonococcal urethritis.

Antimicrob Agents Chemother, 1981 Nov, 20(5), 613 - 9
Penetration of moxalactam into its target proteins in Escherichia coli K-12: comparison of a highly moxalactam resistant mutant with its parent strain; Komatsu Y et al.; An eschericia coli K-12 mutant highly resistant to moxalactam but only slightly resistant to other beta-lactam antibiotics was obtained by mutagen treatment . The affinity of moxalactam for its target penicillin-binding proteins was unchanged, as was the level of beta-lactamase activity . The penetration of {14C} moxalactam, however, was markedly reduced in the mutant . Electrophoretic analysis revealed alterations of the outer membrane proteins . A reduction in the amount of one of the pore-forming proteins (porins) was especially noteworthy . These data suggest that moxalactam resistance is the result of an alteration in the outer membrane structure.

Clin Pharmacokinet, 1981 Nov-Dec, 6(6), 475 - 9
Mecillinam in cerebrospinal fluid in children; Garborg O; The penetration of mecillinam, a new beta-lactam penicillin-like antibiotic, into cerebrospinal fluid (CSF) was investigated in 11 children in whom all but 1 was presumed to have non-inflamed meninges . 30 minutes after a single intravenous dose of 30mg/kg, a concentration of approximately 0.30 micrograms/ml was achieved in the CSF (corresponding mean serum concentration 75 micrograms/ml), and this level was maintained during the next 4 hours in spite of rapidly declining serum concentrations, indicating a slow equilibration of mecillinam over the blood-liquor barrier . 1 child with suspected inflamed meninges showed a much higher CSF level of 12.1 micrograms/ml . It is concluded that mecillinam, as is the case for other penicillins, apparently crosses non-inflamed meninges poorly.

Clin Allergy, 1981 Nov, 11(6), 579 - 87
Radioallergosorbent test with conjugates specific for 'minor' haptenic determinants in the diagnosis of IgE-mediated penicillin allergy in man; Kraft D et al.; Penicillamine-polylysine, benzylpenicillanyl-human serum albumin and ampicillin-polymers were coupled to CNBr-activated paper discs and used in addition to penicilloyl G and penicilloyl V discs in RAST investigations . Sera from sixty patients with case histories of penicillin allergy and with positive or negative skin tests to different penicillin determinants and from seventeen subjects with atopic diseases caused by allergens other than penicillin were tested . The penicilloyl-('major' determinant) specific RAST (Phadebas RAST Penicilloyl G and V) was positive in twenty out of twenty-four patients with positive skin tests to penicilloyl-polylysine, in eight out of twelve patients with sole skin reactivity to 'minor' determinants, and in five out of twenty-four patients with negative skin tests to all antigens used . The penicillamine-specific RAST was the only positive in vitro test in four patients with negative skin tests (two) or sole positive skin reactivity to 'minor' determinants (two), whereas benzylpenicillanyl and ampicillin-polymer discs added no more information than the penicilloyl structures in all patients tested . Antibodies specific to 'minor' determinants apparently show strong in vitro cross-reactivity with the penicilloyl determinant . It is, therefore, concluded that 'minor' determinant specific conjugates are of marginal importance for in vitro diagnosis of penicillin-allergic patients.

Can J Ophthalmol, 1981 Oct, 16(4), 187 - 91
Enhancement and inhibition of phagocytic activity in the retinal pigment epithelium; Markowitz S et al.; The phagocytic activity of the pigmented epithelium of the bovine retina was studied with an organ culture model . Latex particles coated with immunoglobulin, or bovine rod outer segments, both labelled with radioactive iodine, were the objects to be phagocytosed . Various agents were tested with this model for their effects on phagocytosis by the retinal pigment epithelium . Iodoacetate significantly inhibited phagocytosis, as did penicillin, though to a lesser extent . Concanavalin A and gentamicin enhanced phagocytosis . Dimethyl sulfoxide had no effect . The results with lymphokines were not conclusive.

Sex Transm Dis, 1981 Oct-Dec, 8(4), 266 - 79
A survey of 251 patients with acute syphilis treated in the collaborative penicillin study of 1943-1950; Kampmeier RH et al.; The dramatic and apparently curative effect of penicillin for the treatment of acute syphilis led to follow-up studies for only comparatively brief periods, and the acceptance of the long-term benefit of penicillin has rested on uncontrolled clinical impressions . More certainty about the efficacy of penicillin was sought by a follow-up review of 251 patients treated between March 1944 and December 1950 under the Penicillin Study of the Office of Scientific Research and Development (OSRD) and continued under U . S . Public Health Service after World War II . Eighty-eight patients were interviewed and examined . Telephone conversation or correspondence was had with 43 subjects; an additional nine are known to be living but did not respond to letters . Thirty-two patients died greater than or equal to 20 years after treatment, and 21 patients died within less than 20 years of treatment . Fifty-eight patients could not be found . Treatment failures were documented . Syphilis was not shown to be the cause of disability or death, except for a patient with meningovascular syphilis who died soon after initial treatment . Disabilities recorded and deaths documented revealed only diseases common to any middle-aged population . The outcomes of 17 pregnancies of women treated for acute syphilis were documented . Blood samples obtained from the 88 subjects examined were tested at the Center for Disease Control (Atlanta, Ga.); the results are recorded and discussed . Methods for locating the patients are described, and the psychosocial findings for the 88 patients interviewed are presented . The study has confirmed the clinical impressions of the therapeutic effectiveness of penicillin, which have been accepted for greater than 30 years.

Acta Physiol Scand, 1981 Oct, 113(2), 245 - 52
Synaptic triggering of epileptiform discharges in Ca2 pyramidal cells in vitro; Gjerstad L et al.; Intra- and extracellular recordings were made in the transverse hippocampal slice in vitro to study the requirements for the triggering of epileptiform discharges of CA1 cells . Spontaneous and induced epileptiform discharges were produced by adding small amounts of sodium benzyl penicillin . Recorded intracellularly, the epileptiform activity consisted of a burst of action potentials superimposed on a depolarizing wave . Extracellular recordings demonstrated a marked synchronization . The epileptiform activity of the CA1 cells appeared without changes in the passive membrane properties or in the spike generating mechanism . Spontaneous epileptiform discharges of the CA2 cells depended upon a synaptic activation from the CA3 region . Stimulation of afferent fibres evoked an early and a late burst response in the CA2 cells . The long latency burst was caused by a re-excitation from the CA3 region . The early burst response seems to be an intrinsic property of the CA1 cells and may be induced by synaptic activation of either apical or basal dendrites . The findings suggest that synaptic depolarization is necessary for the generation of epileptiform discharges of the CA1 cells.

Jpn J Pharmacol, 1981 Oct, 31(5), 661 - 75
Effects of penicillin on electrical activities of neurons in guinea-pig hippocampal slices; Abe H et al.; Epileptogenic action of penicillin (PC) was investigated in thin slices prepared from the guinea-pig hippocampus . Bath-applied PC (1.7 mM) provoked an epileptiform activity . A series of cellular events before during and after application of PC were shown by stable intracellular recording from the same neuron . The effect of PC became progressively pronounced when the temperature of the medium was raised from 30 degrees C to 40 degrees C . PC-induced epileptiform activity showed odd time courses, i.e., recurrent reduction during perfusion of PC and abrupt reversion during washing . Increased potassium concentration in the medium increased the rate of occurrence of the spontaneous epileptiform activity induced by PC . Removal of chloride from the medium converted the PC-induced epileptiform activity to colonic relapsing discharges . In the laminar field potential analysis, 'sink' for the epileptiform activities induced by PC appeared at a broad region of the middle and distal portions of the apical dendrite, whereas 'sink' for potentials considered to reflect mainly synaptic events appeared at a relatively restricted region of the proximal and middle portions of the apical dendrite . Together with other observations, these results led to the conclusion that not only the synaptic but also the non-synaptic process is involved in initiation of the epileptiform activity.

Drug Intell Clin Pharm, 1981 Oct, 15(10), 802 - 6
Reversible neutropenia associated with ampicillin therapy in pediatric patients; Kumar K et al.; Hematologic abnormalities associated with penicillin compounds are uncommon, and neutropenia associated with ampicillin is reported even less frequently . Neutropenia developed in three pediatric patients after high-dose (150-400 mg/kg) ampicillin therapy over a period of 3 to 12 days . In all cases, the white blood cell and neutrophil counts returned towards normal within 4 to 11 days after discontinuation of the antibiotic . Bone marrow examination revealed a maturation arrest in one and slight shift to the left in the maturation of granulocytic cells in another . Other marrow components were normal . Red blood cells, reticulocytes, platelets, and hemoglobin did not show any abnormal alteration in any of the patients . Physicians administering ampicillin, particularly in high doses, should be alert to the possible development of neutropenia; however, all reported neutropenias have been reversible.

J Gen Microbiol, 1981 Oct, 126(Pt 2), 311 - 9
Selection for increased penicillin titre following hybridization of divergent lines of Aspergillus nidulans; Simpson IN et al.; Sexual hybridization of two divergent lines of Aspergillus nidulans, which had been selected for increased penicillin titre through successive cycles of mutagenesis, released considerable variation for this character . The recovery of segregants with titres equivalent to that of the unselected ancestor suggested that mutations in different genes had been selected in the two lines . However, complementary segregants with substantially improved titres were not found, indicating interactions, probably of a duplicate nature, among the induced mutations . All the genetic variation released by hybridization was fixed following two generations of selection for high titre, but only a small gain over the initial selection lines was achieved . Hybridization of divergent strains has been widely advocated as a means of strain development . The failure to achieve the anticipated gains in this programme is attributed primarily to the unfavourable interactions amongst the induced mutations . Whether similar interactions occur generally in crosses between strains selected by mutagenesis remains to be established and will be an important factor in determining the contribution of recombinational approaches to yield improvement.

Acta Pharmacol Toxicol (Copenh), 1981 Oct, 49(4), 301 - 4
The effect of food on the oral absorption of penicillin V preparations in children; Finkel Y et al.; The oral absorption of pc V in different preparations, given at various times before and after a meal, was investigated in children with upper respiratory infections . The best absorption with respect to peak concentration was observed when potassium pc V (Calciopen) was given after at least two hours of fasting with no food intake within the following hour . Shorter periods of fasting (1, 1/2, 0 hrs) before drug intake resulted in significantly lower plasma concentrations . When drug intake was followed by a meal, the absorption was also decreased to some extent . When pc V was given in an oil suspension (Fenoxypen), or in a small volume (Roscopenin) together with a meal, the peak concentration was significantly lower than when pc V was given in an aqueous solution with a larger volume (Calciopen).

Arch Microbiol, 1981 Oct, 130(2), 150 - 4
beta-Lactamase activity and resistance to penicillins in Myxococcus xanthus; von Kruger WM et al.; Several mutants and other variants of Myxococcus xanthus HP100 were obtained with differences in their sensitivity to carbenicillin and other penicillin derivatives . The specific activities of beta-lactamase in different resistant organisms varied from strain to strain but were consistently higher than in HP100 . The relative molecular mass (Mr) of the enzyme in M . xanthus HP100 was found to be 22,300 . In certain carbenicillin resistant strains a second fraction of beta-lactamase activity of molecular weight 186,000 presumed to be an octamer of the other form was present . The enzyme was found in cell free extracts and also in culture supernatants of all carbenicillin resistant mutants but not in culture supernatants of strain HP100 . In all the carbenicillin resistant mutants a part of the intracellular enzyme activity was released by osmotic shock and this activity may be periplasmic . The forms of the enzyme present in the culture supernatants and released by osmotic shock were monomeric . Carbenicillin resistance was not transferable between strains by conjugation . One resistance allele inhibited the transfer of the R factor Sa between myxococci.

Jpn J Antibiot, 1981 Oct, 34(10), 1401 - 9
{Chemotherapy of biliary tract infections . XIV . Biliary excretion and gallbladder tissue levels of piperacillin (author's transl)}; Tanimura H et al.; Piperacillin, a new injectable synthetic penicillin, was evaluated against biliary tract infections . 1 . Two grams of piperacillin was intravenously administered to patients received cholecystectomy . The mean level in gallbladder bile of PIPC was 795.6 microgram/ml except for 3 cases in obstruction of the cystic duct . The mean gallbladder tissue level was 31.2 microgram/g . The gallbladder tissue level in the cases with obstruction of the cystic duct was high levels as 71.3 microgram/g and 79.5 microgram/g . 2 . The excretion of PIPC into bile was compared with TIPC and APPC using crossover method . When administered 2 g of PIPC, the peak biliary levels were 950 microgram/ml to 2,120 microgram/ml at 2 hours and 20 minutes to 2 hours and 40 minutes after the administration, and biliary recoveries during 6 hours were 2.84% to 11.6% . The peak levels and biliary recoveries were lower after administration of TIPC 2 g . Mn and Zn were excreted enormously together with APPC into human bile . 3 . The influence on clinical laboratory findings was negligible . Therefore, PIPC may be expected to show excellent effects of biliary tract infections except rare occurrence of drug eruption.

Allergy, 1981 Oct, 36(7), 471 - 8
Challenge of penicillin-allergic volunteers with penicillin-contaminated meat; Lindemayr H et al.; In order to obtain information about the clinical course and immunological background of possible allergic reactions due to penicillin-containing food, nine volunteers with penicillin allergy proved by case history, positive skin tests and/or positive penicilloyl-specific RAST were exposed to penicillin-contaminated pork . For this purpose a farm pig from an inbred strain received "therapeutic" doses of benzyl procain penicillin before being slaughtered . Meat samples were taken from muscle tissues, kidney and liver and analyzed by diffusion and extraction methods . Very small amounts of penicillin were detectable in muscle tissue, whereas kidney material contained up to five times as much (0.12 mcg/g) . Except two cases which reacted with itchy sensations after ingestion of penicillin contaminated meat "a la tartare", all probands were clinically free of symptoms . Assaying penicilloyl-specific IgE antibodies by RAST during the trial, a tendency to increased levels in the serum after 2 and 24 h was noted, whereas the titers of BPO-specific IgG antibodies measured by the red cell-linked antigen-antiglobulin reaction (RCLAAR) remained unchanged . It is concluded from this study that small and hidden amounts of penicillin and its derivatives in food seldom induce anaphylactic reactions in penicillin allergic patients.

Physiologie, 1981 Oct-Dec, 18(4), 241 - 5
Penicilloyl-dextran conjugates as reagents for skin testing in penicillin allergy; Cirstea M et al.; A procedure for implanting amino groups in the dextran molecule is described . The aminated polymer prepared from a dextran sample with a molecular weight of 20,000 was found to contain approximately 16 amino groups per molecule . Similarly to polylysine, the aminated dextran may be penicilloylated by incubation with penicillin at high pH . The penicilloyl-dextran (P-Dex) conjugate prepared in this way was found to contain approximately 8 penicilloyl (PO) groups per molecule . P-Dex was found practically nonimmunogenic in rabbits and showed itself antigenically active in precipitin, passive hemagglutination and passive cutaneous anaphylaxis (PCA) tests performed with a PO specific antiserum . A good correlation was found between the skin tests performed parallelly with P-Dex and penicilloyl-polylysine (PPL) in four subjects with penicillin allergy.

Electroencephalogr Clin Neurophysiol, 1981 Oct, 52(4), 372 - 4
Effects of post-ictal depression on experimental spike and wave discharges; Avoli M et al.; The effects of post-ictal depression on spike and wave (SW) discharges of feline generalized penicillin epilepsy (FGPE) were studied . After tonic-clonic seizures which are not uncommon in FGPE spindle bursts appeared during the post-ictal period . Upon recovery spontaneous and thalamically evoked SW discharges reappeared . Spindles before penicillin and during post-ictal depression showed a similar intraburst frequency (twice that of SW discharges) in the same animal . These findings add further evidence to the notion that any depression of cortical excitability in FGPE leads to replacement of SW by spindles and thus supports the hypothesis that SW discharges occur in hyperexcitable cortex in response to normally spindle-inducing thalamocortical volleys.

Clin Chem, 1981 Oct, 27(10), 1642 - 50
A candidate reference method for determination of total protein in serum . I . Development and validation; Doumas BT et al.; We developed a candidate Reference Method for measuring total serum protein by use of the biuret reaction . The method involves a previously described biuret reagent (Clin . Chem . 21: 1159, 1975) and Standard Reference Material (SRM) 927 bovine albumin (National Bureau of Standards) as the standard . At 25 degrees C, color development for 30 or 60 min provides identical serum protein values . Glucose (up to 10 g/L) and bilirubin (up to 300 mg/L) do not interfere . Hemoglobin, at 3 g/L, increases apparent serum protein by 0.4 g/L . The presence of dextran in serum causes easily detected turbidity, but this interference can be eliminated by centrifuging the reaction mixture . Therapeutic concentrations of ampicillin, carbenicillin, penicillin, oxacillin, nafcillin, chloramphenicol, cephalothin, and methicillin in blood do not interfere, nor do triglycerides up to 10 g/L . Within-run and day-to-day standard deviations of the method are 0.1 and 0.4 g/L, respectively.

Stroke, 1981 Sep-Oct, 12(5), 581 - 8
Simultaneous measurement of blood flow and glucose metabolism by autoradiographic techniques; Mies G et al.; A double tracer autoradiographic technique using 131I-iodo-antipyrine and 14C-deoxyglucose is presented for the simultaneous measurement of blood flow and cerebral glucose utilization in the same animal . 131I is a gamma emitting isotope with a half life of 8.06 days and can be detected with adequate resolution on standard autoradiographic films . Autoradiograms are made before and after decay of 131I; the time interval between the 2 exposures and the concentration of the 2 tracers is adjusted to avoid significant cross-contamination . In this way, 2 film exposures are obtained which can be processed quantitatively like single tracer autoradiograms . The validity of the method for the investigation of local coupling of flow and metabolism was tested under various physiological and pathophysiological conditions . Coupling was tight in barbiturate-anesthetized healthy animals, but not under halothane anesthesia where uncoupling occurred in various subcortical structures . Focal seizures induced by topical application of penicillin on the cortical surface led to a coupled increase of metabolism and flow in thalamic relay nuclei but not at the site of penicillin administration where increased glucose utilization was not accompanied by similar increase in blood flow . Both coupled and uncoupled increases in local glucose utilization were observed in spreading depression and in circumscribed areas of experimental brain tumors . The results obtained demonstrate that double tracer autoradiography allows allows the very precise local assessment of cerebral blood flow and glucose utilization, and, therefore, is particularly suited to the study of regional coupling processes under various experimental conditions.

Antibiotiki, 1981 Sep, 26(9), 696 - 9
{Penicillin and streptomycin penetration into tissue by a modified electrophoretic method}; Ragelis SIu; A total of 377 experiments with healthy rabbits of the same species, age, weight and sex were performed with the use of the galvanization apparatus "Potok-1" . The penetration levels of penicillin and streptomycin into the tissues, i.e . the skin, muscles and bone after their administration with the modified method of electrophoresis were determined . It was found that the tissue levels of the antibiotics administered with the modified method of electrophoresis increased with an increase in the current density, the procedure time and the antibiotic concentrations . The levels of penicillin and streptomycin in the skin, muscles and bones on administration with the modified method of electrophoresis were higher than those on administration of the antibiotics with the routine method of electrophoresis . The higher the time of the material storage in a refrigerator, the lower the penicillin level in the tissues.

Ann R Coll Surg Engl, 1981 Sep, 63(5), 342 - 4
Amputation for peripheral vascular disease: experience of a district general hospital; Haynes IG et al.; Two hundred and ninety major lower-limb amputations were performed on 286 patients during the period 1969-79 . The early mortality rate was 6.9% . The mean age of the amputees was 70.2 (range 35-91) years . The commonest site for amputation was above the knee (77.2%) . Failure to obtain immediate satisfactory healing of the stump occurred in 18.4% and reamputation was required in 5.6% . The hospital mortality rate was 25.5% . Routine prophylactic penicillin was not given . One patient developed gas gangrene.

J Pharmacobiodyn, 1981 Sep, 4(9), 706 - 10
Detection of Residual penicillin in milk by sensitive enzyme immunoassay; Miura T et al.; A convenient and precise method by an application of a highly sensitive enzyme immunoassay of penicillin to detect the veterinary penicillin residue in milk was studied . The procedures of the assay to detect more than 0.01 microgram/ml of ampicillin in milk were developed . Five commercial milk samples were tested by the assay procedure, and no veterinary ampicillin residue was detected in any of them.

Proc Natl Acad Sci U S A, 1981 Sep, 78(9), 5856 - 60
Heterogeneity of newly inserted and preexisting murein in the sacculus of Escherichia coli; de Pedro MA et al.; In vivo studies of murein biosynthesis show that newly synthesized murein unexpectedly differs in its chemical composition from preexisting murein . New murein is loosely crosslinked with the preexisting sacculus; in a maturation process involving further transpeptidation, the final stage of crosslinkage in murein is achieved . Newly inserted murein initially carries pentapeptide subunits, which are the donor of the secondary transpeptidation reaction . In mutants with defective penicillin-binding protein 4 the secondary transpeptidation step is abolished . Uncoupling of the secondary transpeptidation reaction from crosslink formation during the initial insertion of new murein was also found in a mutant with a defect in lipoprotein biosynthesis . We conclude that the initial transpeptidation of murein and crosslink formation during the maturation of newly inserted murein are catalyzed by two different enzyme systems.

J Neurosci, 1981 Sep, 1(9), 1022 - 35
Possible mechanisms of enkephalin action on hippocampal CA1 pyramidal neurons; Dingledine R; (1) Intracellular and extracellular recordings were made from CA1 pyramidal neurons in an in vitro rat hippocampal slice preparation, while {D-Ala2, D-Leu5}enkephalin (DADL) was applied by perfusion at a known concentration (1 to 5 X 10-7 M), in a small droplet, or by iontophoresis into the cellular and dendritic layers of the slice . The effects of DADL on synaptic potentials and membrane properties were studied in an effort to determine the mechanisms underlying its epileptogenic action in the hippocampus . (2) DADL increased the size and often the duration of excitatory postsynaptic potentials (EPSPs) generated on either the apical or basal dendrites; this resulted in an increased discharge probability for a constant orthodromic stimulus . Extracellular field potential recordings showed a larger population spike for a given size field EPSP . These effects of DADL could be reversed substantially by perfusion with naloxone (1 to 5 X 10-7 M) and appeared qualitatively different from the epileptiform actions of penicillin . (3) DADL did not appear to increase the intrinsic excitability of the soma membrane, since membrane potential, input resistance, spike threshold, and antidromic field potentials all were unchanged . In addition, the shape of the membrane charging curve during hyperpolarizing current injection was not changed noticeably by DADL . (4) At the concentrations tested, DADL did not attenuate recurrent inhibition in the CA1 region, as evaluated by comparing in the absence and presence of DADL: (a) antidromically evoked recurrent inhibitory postsynaptic potentials (IPSPs) and their dependence of membrane potential, (b) the reduction of a synaptically driven population spike by a prior antidromic volley, (c) iontophoretic GABA (gamma-aminobutyric acid) responses . Similarly, IPSPs evoked by orthodromic stimulation appeared either unaffected or occasionally enhanced by DADL . (5) By iontophoretic mapping, it was shown that the DADL-sensitive sites are limited to stratum oriens and stratum pyramidale . Local application of DADL into stratum radiatum was relatively ineffective in enhancing the efficacy of synapses located in this region . (6) The dendritic input-output relationship between the presynaptic fiber volley and the field EPSP was not changed by DADL . This finding and the results of the iontophoretic mapping experiments suggest that increased excitatory transmitter release was not involved . (7) The data are consistent with the proposal that DADL selectively attenuates a dendritic IPSP which is virtually invisible to the soma, although the possibility cannot be ruled out that DADL may, in addition, act to enhance the responsiveness of pyramidal dendritic membrane to excitatory synaptic activation.

Tropenmed Parasitol, 1981 Sep, 32(3), 165 - 70
A diagnostic skin test for Onchocerca volvulus infection; Ngu JL et al.; Onchocerca supernatant (OS) was prepared by a technique permitting live microfilariae to migrate from nodule tissue through agar gel into sterile Hanks balanced salt/Penicillin-Streptomycin solution where they metabolized . The OS, after dialysis, was passed through Seitz viral filter and either concentrated or lyophilized . Using rabbit antiserum in immunodiffusion and immunoelectrophoresis tests, microfilariae proteins and also human protein were detected in out OS . No common antigens were found between this and somatic extracts of Loa loa, O . gutturosa, O . volvulus, L . carinii, D . immittis and A . lumbricoides . 125I labelled OS was purified by passage through protein A column and then through immunosorbent column of horse anti-human serum linked to CNB-activated sepharose 4B . Autoradiography, after sodium dodecyl sulphate polyacylamide slab gel eletrophoresis of purified OS, showed 10 protein bands in the molecular range 10,000 to 125,000 . Skin prick tests with OS, shown not to be contaminated with Hepatitis B antigens, elicited immediate hypersensitivity reaction . Using our criteria, positive reactions were seen in 81% of proven onchocerca cases and only occasionally in Loasis 4.5%, ascaridiasis 13.5% or healthy controls 2.4% . The poor skin reactivity to OS in loasis was not due to immunosuppression as these patients, when also infested with ascaris, reacted just as well as onchocerca patients with ascaris to skin prick test using somatic extracts of ascaris.

Antibiotiki, 1981 Sep, 26(9), 643 - 7
{Penicillin formation by biochemical mutants of Penicillium chrysogenum and their spontaneous revertants}; Lebed' ES et al.; The capacity for the antibiotic production in the auxotrophs of Penicillium chrysogenum with various deficiency and their revertants was studied . It was found that the capacity for penicillin synthesis was impaired to various degrees in the majority of the auxotrophs . Variants with the penicillin production levels by 13--20 per cent higher than those in the initial prototrophic strain were isolated for the first time in selection of the eukaryotes with the method of obtaining highly active revertants from auxotrophs according to the scheme "prototroph-auxotroph-prototroph".

Med Clin North Am, 1981 Sep, 65(5), 1073 - 81
Steroids in allergic disease; Webb DR; From the experience above, it may be concluded that corticosteroid therapy in allergic disease has become more effective than ever before . The expected variations in usage of new important pharmacologic agents is seen with special clarity in the use of corticosteroids . The wide acclaim for the "miracle drug of the 1950's", which followed penicillin of the 1940's, soon gave away to anguish about side-effects that threatened to abolish its use entirely in the late 1950's . The 1960's brought alternate day therapy for chronic usage and recognition that short term usage was relatively safe . The 1970's saw proliferation of topically active steroids similar to those so important to the practice of Dermatology in the previous decade . Results in treating asthma and nasal diseases have been excellent and extensive research for adverse effects has been largely unrevealing.

Neurology, 1981 Sep, 31(9), 1163 - 6
Quantitative evaluation of anticonvulsant effects on penicillin-induced spike foci in cats; Bustamante L et al.; We evaluated the effects of phenytoin, carbamazepine, phenobarbital, sodium valproate, and ethosuximide on penicillin-induced spike foci . Phenytoin, carbamazepine, and phenobarbital at blood levels within or slightly above the human therapeutic range in humans increased spike frequency, decreased spike duration, and abolished after discharges . Ethosuximide and sodium valproate had no statistically significant effect even at blood levels considered toxic in humans . The experimental spike focus and the method of analysis appear useful for: (1) detection of new potentially anticonvulsant drugs, (2) classifying new potentially anticonvulsant drugs according to the type of clinical seizure for which benefit is most likely, and (3) comparing different anticonvulsant drugs.

J Allergy Clin Immunol, 1981 Sep, 68(3), 171 - 80
Skin testing to detect penicillin allergy; Sullivan TJ et al.; Skin testing for penicillin allergy with penicillin G (Pen G), penicilloic acid (PA), and penicilloyl poly-L-lysine (PPL) was performed on 740 subjects, and the results were assessed from epidemiologic and immunologic perspectives . Approximately 95% of these patients had histories of apparent allergic reactions to beta-lactam antibiotics, and 63% were skin-test positive . The prevalence of positive skin tests was related to the time that had elapsed between clinical reactions and skin testing . Ninety-three percent were skin-test positive 7 to 12 mo after reactions, and 22% were positive 10 yr or more after reactions . Patients under 30 yr of age had a prevalence of positive skin tests 1.7-fold higher than older patients . Testing with PPL, PA, and Pen G detected 76.3%, 55.3%, and 57.1% of the positive patients, respectively . Omission of PPL, PA, or Pen G would have led to a failure to detect 25.6%, 7.2%, and 6.2% of the positive patients, respectively . Subjects with skin tests positive to penicillin often reacted to skin tests with other beta-lactam antibiotics; 73% (41 of 56) reacted to ampicillin and 51% (38 of 74) reacted to cephalothin . No serious allergic reactions were provoked by testing . None of the 83 skin test--negative patients treated with beta-lactam antibiotics immediately after testing experienced acute allergic reactions . Two patients developed mild urticaria beginning 3 and 5 days into therapy . One skin test--negative patient experienced urticaria 3 hr after receiving oral penicillin 6 mo after skin testing . This patient's skin-test status immediately before therapy was unknown . These results support the position that testing with PPL, PA, and Pen G is a rapid, safe, and effective method for identifying patients at risk, or not at risk, for allergic reactions to penicillin.

J Am Acad Dermatol . 1981 Aug;5(2):222.
Tetracycline and oral contraceptives; Coskey RJ; PIP: Several female patients with acne have asked me if they could take tetracycline along with oral contraceptives (OCs) . I checked this information in the Physicians Desk Reference and found that all of the manufacturers of OCs except for Parke, Davis, and Company, state that many drugs, including tetracycline, may make the OCs less effective . According to Syntex Laboratories, Inc., OCs may become less effective through drug interaction with rifampin, isoniazid, ampicillin, tetracycline, neomycin, penicillin 5, chloramphenicol, sulfonamides, nitrofurantoin, barbiturates, phenytoin, primidone, analgesics, tranquilizers, and antimigraine preparations . Furthermore, on their inserts which are given to the patient, it is stated that the use of OCs has been associated with reduced effectiveness and an increased incidence of breakthrough bleeding when used in conjunction with antibiotics such as rifampin, ampicillin, and tetracycline, or with certain other drugs such as barbiturates, phenylbutazone, or phenytoin sodium . An additional form of contraceptive protection should be used in any cycles during which these drugs are ingested . Ortho Pharmaceutical Corporation and Mead Johnson Pharmaceutical use the same wording on their package inserts for the physician and the patient . Wyeth Laboratories and Searle Laboratories also provide similar information . I believe dermatologists are most concerned about tetracycline's interaction with OCs . I could find only 1 paper which referred to a pregnancy which occurred while a patient was taking OCs and tetracycline . According to an article in the British Medical Journal, 38 reports of pregnancies occurring in women who had received antibiotics other than rifampicin along with OCs were received by the Committee on Safety of Medicines . However, they did not state which antibiotics were given . Although evidence of problems resulting from concurrent use of tetracycline and OCs is not overwhelming, it seems worthwhile for dermatologists to be aware of the preceding information . I myself have discontinued giving oral antibiotics to those patients taking OCs . author's modified

Epilepsia, 1981 Aug, 22(4), 443 - 52
The effects of transient functional depression of the thalamus on spindles and on bilateral synchronous epileptic discharges of feline generalized penicillin epilepsy; Avoli M et al.; A transient functional depression of thalamic activity (TFDTA) was induced in acute experiments in cats by the microinjection of 25% KCl into the thalamus . Spontaneous and evoked thalamic electrical activity was markedly depressed at the site of KCl microinjection . Spread of this depression to other thalamic areas often occurred, mainly when KCl was injected into the midline thalamus . In normal cats both spontaneous and evoked cortical spindle bursts as well as other evoked thalamocortical responses were reduced or abolished during the KCl-induced TFDTA . The generalized spike-and-wave discharges of feline generalized epilepsy were also suppressed for the duration of TFDTA, while incidental focal cortical interictal and ictal epileptic discharges, as well as generalized tonic-clonic seizure discharge, remained unaffected . The same effects were observed in animals with lesions of the mesencephalic reticular formation, indicating that the suppression of spindles and spike-and-wave discharges cannot be attributed to a release of the activity of the reticular formation by the TFDTA . An unexplained occurrence of generalized tonic-clonic EEG seizure was observed in most cases late after thalamic KCl microinjection, usually after the spike-and-wave discharges had recovered . These data are consistent with the hypothesis that the spontaneous bilaterally synchronous epileptic bursts of feline generalized penicillin epilepsy are not only closely related to spindles but are crucially dependent on thalamic inputs to the cerebral cortex.

Proc Natl Acad Sci U S A, 1981 Aug, 78(8), 5026 - 30
Cloning arg3, the gene for ornithine carbamoyltransferase from Saccharomyces cerevisiae: expression in Escherichia coli requires secondary mutations; production of plasmid beta-lactamase in yeast; Crabeel M et al.; The yeast arg3 gene, coding for ornithine carbamoyltransferase (carbamoylphosphate:L-ornithine carbamoyltransferase, EC 2.1.3.3), has been cloned on a hybrid pBR322-2-micrometers plasmid . The cloned gene gives a normal regulatory response in yeast . It is not expressed at 35 degrees C when a mutation preventing mRNA export from the nucleus at this temperature is included in the genetic make-up of the carrier strain . In Escherichia coli, no functional expression can be observed from the native yeast arg3 gene . The study of a mutant plasmid (M1) producing low levels of yeast carbamoyltransferase in E . coli has permitted the localization and orientation of arg3 on the plasmid . The mutation involved is a deletion that alters the regulatory response of arg3 in yeast . The plasmid bla gene produces detectable amounts of beta-lactamase (penicillin amido-beta-lactamhydrolase, EC 3.5.2.6) in yeast: the data provide an estimate of the beta-lactamase activity associated with one exemplar of the plasmid expressing arg3 (0.6 units).

Br J Vener Dis, 1981 Aug, 57(4), 226 - 31
Jarisch-Herxheimer reaction in complement-depleted rabbits . Histological and immunofluorescence studies of early cutaneous lesions; Aronson IK et al.; The possible role of complement in the pathogenesis of the Jarisch-Herxheimer reaction was assessed in cutaneous syphilitic lesions in two groups of rabbits treated with penicillin; in one group complement was depleted before penicillin therapy . Serial biopsy specimens were similar histologically in both groups . The activation of the complement pathways did not seem to play a role in the pathogenesis of early cutaneous syphilitic lesions in rabbits during the Jarisch-Herxheimer reaction.

Am J Ophthalmol, 1981 Aug, 92(2), 210 - 4
Secondary syphilitic uveitis; Belin MW et al.; A patient with secondary syphilis had positive serum and cerebrospinal fluid findings . Fluorescent-antibody darkfield testing demonstrated spirochetes (Treponema pallidum) in the aqueous . There were clinical signs of secondary syphilis, including palmar skin lesions and frontal balding, and bilateral nasal altitudinal visual field loss . The discrete, waxy, yellow-white retinal lesions became increasingly pigmented and later migrated anteriorly into the vitreous chamber . The patient was treated with large amounts of penicillin (total dosage, 440 million units) and probenecid . Visual acuity improved to R.E . : 6/9 (20/30) and L.E.: 6/12 (20/40) and the inflammatory reaction disappeared . A second aqueous tap eight weeks after therapy ended showed no spirochetes by fluorescent-antibody testing.

J Bacteriol, 1981 Aug, 147(2), 354 - 61
Penicillin-binding proteins of Rhodopseudomonas sphaeroides and their membrane localization; Shepherd WD et al.; Cytoplasmic membranes (CM) prepared from both chemotrophic and phototrophic cells of Rhodopseudomonas sphaeroides possess penicillin-binding proteins (PBPs), as demonstrated by binding of {125}furazlocillin to isolated membranes, the subsequent separation of the constituent PBPs by sodium dodecyl sulfate-polyacrylamide gel electrophoresis, and their detection by autoradiography . The major PBP present in CM from R . sphaeroides corresponds in molecular weight to PBP-5, the predominant PBP present in CM of Escherichia coli . In contrast, the outer membrane of R . sphaeroides shows only low-level furazlocillin-binding activity on a per milligram of protein basis compared with chemotrophic CM . The intracytoplasmic membrane (ICM) derived from phototrophic cells contains less than 5% of the furazlocillin-binding activity of the CM . Based on the specific localization of PBPs in the CM, it is possible to provide quantitative estimates of the extent of CM present in preparations of ICM . This method demonstrates that highly purified preparations of ICM contain less than 5% CM . Additionally, the assay for PBPs demonstrates that during ICM remodeling, which occurs upon a shift from phototrophic to chemotrophic growth, there is no significant insertion of PBPs into the ICM over the first two generations after a shift to chemotrophic growth.

Lab Anim Sci, 1981 Aug, 31(4), 379 - 81
Venereal spirochetosis of rabbits: eradication; Cunliffe-Beamer TL et al.; Venereal spirochetosis of rabbits, caused by Treponema cuniculi, have been observed since the 1940's in the rabbit colony maintained at The Jackson Laboratory . Treatment of individual rabbits with obvious clinical lesions using a product containing crystalline penicillin and dihydrostreptomycin caused lesions to heal but venereal spirochetosis persisted in the colony . Clinical and serological responses of rabbits receiving three subcutaneous injections of benzathine penicillin G-procaine penicillin G (either 42,000 or 84,000 IU/kg body weight/week) at 7 day intervals were monitored . Both doses were effective . Lesions healed within 2 weeks of the first treatment . Rapid plasma reagin titers declined markedly or disappeared by the sixth week after the first treatment . Based upon the above findings and results of previous epizootiological studies, a program to eradicate venereal spirochetosis from this enzootically infected colony was successfully undertaken.

Am J Hosp Pharm, 1981 Aug, 38(8), 1167 - 70
In vitro inactivation of gentamicin, tobramycin, and netilmicin by carbenicillin, azlocillin, or mezlocillin; Henderson JL et al.; The in vitro inactivation of gentamicin, tobramycin, and netilmicin, when combined with carbenicillin, azlocillin, and mezlocillin, was studied . Plasma samples containing the aminoglycosides at a concentration of 5-8 micrograms/ml in combination with the penicillins in concentrations of 500, 250, and 50 micrograms/ml were incubated at room temperature and 37 degrees C for 0.3, 1, 3, 6, and 9 days . The aminoglycoside concentration was determined by radioimmunoassay or enzyme immunoassay . The extent of inactivation was dependent on penicillin concentration, contact time, and temperature . Penicillin concentrations of 500 micrograms/ml caused the greatest loss of aminoglycoside, while little loss occurred at the 50-micrograms/ml penicillin level . Carbenicillin, in concentrations of 250 and 500 micrograms/ml, inactivated all three aminoglycosides to a greater extent than either azlocillin or mezlocillin . The initial rate of decline in aminoglycoside concentration was greater at 37 degrees C than at room temperature . The new acylureidopenicillins, azlocillin and mezlocillin, inactivate the aminoglycosides studied, in a similar manner to that previously described for carbenicillin.

Trop Anim Health Prod, 1981 Aug, 13(3), 177 - 82
Treatment of contagious caprine pleuropneumonia; Rurangirwa FR et al.; A combination of dihydrostreptomycin sulphate (250 mg/ml) and penicillin G procaine (200,000 iu/ml) was used to treat contagious caprine pleuropneumonia caused by F38 strain of mycoplasma . A single dose of either 20, 30, 40 or 50 mg/kg body weight of the dihydrostreptomycin sulphate led to the recovery of the treated goats . The recovered goats did not transmit CCPP to susceptible goats housed with them for 2 months . The goats which recovered were found to be solidly immune to an in-contact challenge in which all the control goats died of CCPP . The treated and recovered goats were found not to be carriers of the organism.

Electroencephalogr Clin Neurophysiol, 1981 Aug, 52(2), 127 - 39
Modulation of proprioceptive transcortical reflexes in the cat with a penicillin epileptic motor focus; Encabo H et al.; Mechanisms responsible for the triggering of paroxysmal events by proprioceptive afferents, previously described in the monkey with a chronic epileptic focus, were studied in more detail in the cat with a penicillin focus . To analyse the topical organization of this reflex triggering, the focus was restricted to very small areas of the motor cortex; in this study only pericruciate areas were considered in which stimulation elicited a motor response in one of the several forelimb muscles tested, and which received afferents from that muscle . When the focus was located in the post-sigmoid gyrus, stimulation (usually by stretch) of the given (target) muscle first elicited a cortical spike following the evoked response, and secondly a late phasic EMG response (about 40 msec latency) quite distinct from purely spinal reflexes . Cortical spikes and late EMG responses were closely correlated, especially considering their probability of occurrence or their parallel latency fluctuations . In most cases, this effect was limited to the muscle whose motor area had been treated with penicillin: stretching muscles in the vicinity was ineffective, nor were these muscles activated when the target muscle was stimulated . Evidence is given for the participation of a transcortical reflex in the generation of the late phasic response and for the involvement of the pyramidal tract in this reflex.

Science, 1981 Jul 24, 213(4506), 462 - 3
Epileptogenic agents enhance transmission at an identified weak electrical synapse in Aplysia; Rayport SG et al.; To examine the possibility that alterations in the effectiveness of electrical synapses might participate in epileptogenesis, the effects of several convulsants on an identified weak electrical synapse in Aplysia were examined . Application of pentylenetetrazole, strychnine, or tetraethylammonium led to a dramatic increase in the size of the electrical postsynaptic potential mediated by the synapse; penicillin was considerably less effective . In a number of animals, the increased electrical synaptic effectiveness led to the abnormal conduction of spikes across the synapse . If convulsants have a similar action in mammalian cortex, enhanced transmission at weak electrical synapses may provide abnormal pathways for the flow of seizure activity and contribute in part to the synchronous firing of neurons characteristic of epileptic activity.

Vet Rec, 1981 Jul 18, 109(3), 56 - 7
Prevention of post weaning mastitis in ewes; Hendy PG et al.; The efficacy of a dry cow cerate in protecting the dry ewe against mastitis was tested in three flocks . Of 931 ewes, 462 were infused, shortly after their lambs were weaned, with a dry cow cerate containing 1 g procaine penicillin and 0.5 g dihydrostreptomycin sulphate . The remaining 469 served as untreated controls . At tupping, when the sheep were examined for clinical evidence of mastitis, 21 cases (4.5 per cent) were recorded among the controls but only seven (1.5 per cent) among the treated ewes . There was variation in the distribution of cases between individual flocks but overall the incidence of mastitis in the treated sheep was lower and significantly different from that among the control ewes.

Experientia, 1981 Jul 15, 37(7), 687 - 9
Irreversible inactivation of yeast glucose-6-P dehydrogenase by penicillin G; Han PF et al.; Yeast glucose-6-P dehydrogenase is irreversibly inactivated by penicillin G . Kinetic data show that 1 molecule of penicillin G reacts with each active unit when the enzyme is inactivated . The rate of inactivation increases greatly with increasing pH . This irreversible inactivation by penicillin G is largely prevented by pyridoxal-P, a reversible inactivator or this enzyme . Prior treatment of penicillin G with penicillinase totally abolishes its ability to inactivate the enzyme.

Scand J Haematol, 1981 Jul, 27(1), 45 - 50
Prolonged bleeding time with adequate platelet count in hospital patients; Wisloff F et al.; 100 patients with a modified Ivy bleeding time longer than 10 min in the presence of more than 80 x 10(9)/l blood platelets were studied retrospectively . 72 patients had repeated bleeding times between 10 and 20 min or one or more measurements exceeding 20 min, and were considered to have an unquestionable platelet dysfunction . 39 (54%) of these 72 patients were receiving large doses of antibiotics . Nearly one half of the patients on antibiotics had a bleeding tendency, but most of these patients had additional features that may have interfered with platelet function, or a coagulation defect . In the remaining 33 patients, the prolonged bleeding time was associated with von Willebrand's disease, liver disease, leukaemia/myeloproliferative disease, paraproteinaemia or aspirin ingestion . High doses of penicillin seem to be the most common cause of qualitative platelet disorders in general hospital practice.

Isr J Med Sci, 1981 Jul, 17(7), 572 - 85
Mycoplasma infections of plants; Bove JM; Plants can be infected by two types of wall-less procaryotes, spiroplasmas and mycoplasma-like organisms (MLO), both located intracellularly in the phloem tissues of affected plants . Spiroplasmas have been cultured, characterized and shown to be true members of the class Mollicutes . MLO have not yet been cultured or characterized; they are thought to be mycoplasma-like on the basis of their ultrastructure as seen in situ, their sensitivity to tetracycline and resistance to penicillin . Mycoplasmas can also be found on the surface of plants . These extracellularly located organisms are members of the following genera: Spiroplasma . Mycoplasma and Acholeplasma . The presence of such surface mycoplasmas must not be overlooked when attempts to culture MLO from affected plants are undertaken . Sensitive serological techniques such as the enzyme-linked immunosorbent assay (ELISA) can successfully be used to compare the MLO located in the phloem of affected plants with those eventually cultured from the same plants . In California and Morocco periwinkles naturally infected with both Spiroplasma citri and MLO have been reported . With such doubly infected plants, the symptom expression has been that characteristic of the MLO disease (phyllody or stolbur), not that given by S . citri . Only S . citri can be cultured from such plants, but this does not indicate that S . citri is the causal agent of the disease expressed by the plant . In California many nonrutaceous plants have been found to be infected with S . citri . Stubborn affected citrus trees represent an important reservoir of S . citri, and Circulifer tenellus is an active leafhopper vector of S . citri . Hence, it is not surprising that in California MLO-infected fruit trees could also become infected with S . citri but it would not mean that S . citri is the causal agent of the disease . Criteria are discussed that are helpful in distinguishing between MLO infections and S . citri infections.

Antibiotiki, 1981 Jul, 26(7), 549 - 51
{Experimental allergy to penicillin}; Urazalin MM; The inhalation method for penicillin sensitization with a long-term excitation of the respiratory tract mucosa with formalin was studied in experiments with rabbits . It was shown that inhalation of formalin significantly increased the frequency of the animal sensitization to penicillin . It is suggested that inflammation due to the formalin effect promoted penicillin binding by tissue proteins with formation of full value antigens from penicillin which resulted in the high frequency of the animal sensitization . The data may be used in studies on the allergenic properties of drugs.

Ann Neurol, 1981 Jul, 10(1), 11 - 7
Penicillin- and barium-induced epileptiform bursting in hippocampal neurons: actions on Ca++ and K+ potentials; Hotson JR et al.; Both barium (Ba++) and penicillin produce spontaneous epileptiform burst generation in hippocampal neurons in vitro . Recent investigations suggest that Ba++ acts by both adding to a calcium (Ca++)-mediated depolarization and reducing potassium (K+) conductance . In contrast, it has been proposed that penicillin produces burst generation by attenuating inhibitory postsynaptic potentials . However, some evidence suggests that penicillin may also directly alter intrinsic membrane properties . We therefore compared the actions of penicillin and Ba++ on three intrinsic Ca++- or K+-mediated membrane events, namely, CA++ spikes, Ca++-dependent anomalous rectification, and K+-dependent afterhyperpolarization . Ba++ augmented the Ca++ potentials and attenuated the K+-dependent afterhyperpolarization; penicillin had no demonstrable effect on these events . Ba++ produced rhythmical burst firing and oscillations of the membrane potentials, while penicillin caused sporadic burst generation followed by a longlasting afterhyperpolarization . Synchronized, orthodromically evoked burst firing occurred after exposure to penicillin but not to Ba++ . Ba++ and penicillin are prototypes of agents which induce epileptogenesis in mammalian cortical neurons by two different but probably interrelated mechanisms . Ba++ causes burst generation by disrupting a delicate balance between depolarizing Ca++ potentials and repolarizing, hyperpolarizing K+ potentials . Penicillin does not affect Ca++- or K+-mediated membrane events; other data suggest that it produces burst generation in hippocampal pyramidal neurons by attenuating gamma-aminobutyric acid-mediated synaptic inhibition, which in turn ordinarily limits intrinsic bursting.

Neurology, 1981 Jul, 31(7), 846 - 51
The independence of closely spaced discrete experimental spike foci; Lueders H et al.; Stable spike foci generated by weak penicillin solutions had a minimal area of distribution of 12.5 mm2 . Two foci separated by 4 mm on the same gyrus were consistently dependent and simultaneous . An area of "positive surround" between the two spikes did not prevent dependency . This contradicts the hypothesis that "positive surround" prevents spreading of epileptiform discharges . Spike foci separated by 6 mm were almost always independent . Bursts of afterdischarges remained independent if the primary spikes were independent . Postafterdischarge suppression and spreading depression of Leao affected independent spike focus selectively . These experiments suggest that cross-talking between cortical columns is limited to column 1 to 2 mm apart.

Thromb Haemost, 1981 Jun 30, 45(3), 200 - 3
A survey of 215 non-hemophilic patients with inhibitors to Factor VIII; Green D et al.; Information was obtained by questionnaire about 215 non-hemophilic patients who developed inhibitors against factor VIII (antihemophilic factor) . The majority of the patients were over 50 years of age, and approximately equal numbers of males and females were reported . Rheumatoid arthritis was present in 8% of the cases, 7% occurred during pregnancy or the post-partum period, and in several there was an association with allergy to penicillin, asthma, "auto-immune" diseases, or malignancy . In 46% of cases, no underlying disorders were identified . Major bleeding was observed in 87% of patients, and in 22%, death was attributed either directly or indirectly to the presence of the inhibitor . In 11 of 31 patients receiving no therapy other than supportive transfusions of blood or factor VIII concentrate, the inhibitor disappeared after being present for an average duration of 14 months . Corticosteroids were thought to be effective in abolishing the inhibitor in 22 of 45 patients in whom these were the only drugs administered . Twenty-eight patients received azathioprine as well as corticosteroids; in 19, the inhibitor declined or disappeared during treatment . Finally, 80 patients were treated with cyclophosphamide; in 37 there was a favorable outcome . Inhibitors in children and post-partum patients were more likely to disappear spontaneously or with steroid therapy, whereas those in patients with rheumatoid arthritis or other "autoimmune" disorders required treatment with alkylating agents . However, before any specific therapy can be recommended for this disorder, prospective trials of potential therapeutic agents should be conducted in selected subgroups.

Biochim Biophys Acta, 1981 Jun 23, 664(3), 527 - 37
Phospholipid metabolism of dog liver under hypoxic conditions induced by ligation of the hepatic artery; Matsumoto J et al.; Ischemic hypoxic liver was induced in dogs by ligation of the hepatic artery . About 67% of the dogs died of liver necrosis within 1 or 2 days (severe cases), and the rest survived (mild cases) . In the severe cases, the decreases in the contents of total lipids, phospholipids and proteins of the liver after 24 h were 24, 46 and 12%, respectively, of the original values . The marked decrease in phospholipids was due to decreases in the microsomal and mitochondrial fractions . In the mild cases, similar but smaller decreases occurred and decrease of phospholipids occurred only in the microsomal fraction . The main phospholipids were choline and ethanolamine glycerophospholipids, and their molecular species were analyzed . In the severe cases, ligation resulted in relative increases in mono- and diene species and a decrease in polyene species . No increase in phospholipase activity was found at various times after ligation of the hepatic artery . Penicillin-treated dogs all survived and showed little decrease in liver phospholipids.

Epilepsia, 1981 Jun, 22(3), 347 - 63
Toward a unified theory of focal penicillin epileptogenesis: an intracortical evoked potential investigation; Ebersole JS et al.; Microinjection of picoliter quantities of isotonic sodium penicillin through one barrel of a double micropipet into cortical area 17 of cats induced discrete and temporary foci of epileptogenic alteration in evoked potentials . These were elicited by punctate visual stimuli, recorded through the second barrel and from a second micropipet located in surrounding cortex . Penicillin induced (1) an initial graded increase in the primary latency, "physiologic" response and subsequently (2) a new "late" response which evolved into (3) an "interictal" spike potential . The enhanced physiologic response appears to represent a direct effect of penicillin upon neuronal excitability . The epileptic "late response" possessed distinctive properties that suggest that additional involvement of local circuit interactions within the neuronal population affected by the penicillin . We conclude that penicillin epileptogenesis in striate neocortex is dependent upon both intrinsic neuronal and population interaction abnormalities . Relationships of this unified theory to those of the "epileptic neuron" and "epileptic aggregate" are discussed.

Arch Neurol, 1981 Jun, 38(6), 390 - 1
CSF perfusion to treat intraventricular penicillin toxicity; Callaghan JT et al.; A shunt infection and meningitis developed in a patient receiving methotrexate intravenously for CNS leukemia . Convulsions and respiratory failure followed the intraventricular administration of 300,000 units of penicillin G potassium . Perfusion with 900 mL of Ringer's lactate removed an amount of penicillin equal to that injected intraventricularly plus some from systemic treatment.

P N G Med J, 1981 Jun, 24(2), 74 - 9
Tropical infections contracted in Papua New Guinea and imported into Western Australia; Charters AD; Diseases contracted in Papua New Guinea (PNG) and observed in Western Australia (WA) have comprised malaria, amoebiasis, ancylostomiasis, filariasis and leprosy . This small series of cases demonstrates the prolongation of incubation periods of malaria following chemoprophylaxis, the spread of chloroquine-resistant strains of Plasmodium falciparum (both to Western and Eastern regions of PNG), the ineffectiveness of chloroquine against Entamoeba histolytica in the intestine and the value of oral penicillin as a prophylactic for filarial lymphangitis.

Int J Oral Surg, 1981 Jun, 10(3), 173 - 9
Alveolitis after operative removal of third molars in the mandible; Krekmanov L; The aim of the investigation was to assess the importance of various factors in the aetiology of alveolitis sicca dolorosa . Two hundren partially erupted or totally impacted mandibular third molars were surgically removed . The patients were divided into four groups . The patients in group 1 were premedicated with a single dose of penicillin-V (phenoxymethylpenicillin), those in group 2 with an antisialogogue (methylscopolamine nitrate), and those in group 3 with an antifibrinolytic agent (tranexamic acid) . Group 4 were non-premedicated controls . The frequency of alveolitis in the groups 1 and 2 was significantly less than in the groups 3 and 4 . This indicates the importance of salivary contamination of the surgical field and of infection as aetiologic factors in alveolitis.

EEG EMG Z Elektroenzephalogr Elektromyogr Verwandte Geb, 1981 Jun, 12(2), 69 - 75
{Influence of clonazepam on interictal penicillin-spikes (author's transl)}; Pockberger H et al.; This paper deals with the action of Clonazepam on Penicillin induced interictal discharges . In 7 rabbits Penicillin was applied epicortically in a concentration of 25,000 or 50,000 I.U . The intracortical recordings were made with an 8 fold electrode, made by thin-film technology . Clonazepam (0.5 or 1.0 mg/kg) was given intravenously 30 to 45 min after the Penicillin application . Under Clonazepam the occurrence of double-und multiple interictal discharge is abolished . Single spikes become shorter and are significantly reduced in amplitude . Current Source-Density analysis showed that the configuration of sources and sinks is not altered under the action of this drug . However the spatio-temporal distribution is reduced drastically . If the shape of interictal spikes is compared by means of averaging technique before and after the application of Clonazepam, one observes a significant decrease in the standard deviation . These results indicate that excitatory processes are reduced by an enhancement of inhibitory phenomena within the cerebral cortex.

J Bacteriol, 1981 Jun, 146(3), 1117 - 23
Sodium dodecyl sulfate-sensitive septation in a mitomycin C-sensitive, mtc, mutant of Escherichia coli; Higashi T et al.; A mitomycin C-sensitive, mtc, mutant of Escherichia coli has an altered cell surface and is sensitive to sodium dodecyl sulfate (SDS) . The mutant, M27, formed multinucleate nonseptated filaments in the presence of a low concentration of SDS (50 microgram/ml) . When the culture grown at that concentration of SDS was diluted with an SDS-free medium, the filaments began to divide at a very rapid rate after a lag of about 20 min . Chloramphenicol inhibited this recovery division when added within 10 min after SDS dilution but did not inhibit the division when added 20 min after dilution . Penicillin G at a low concentration, which is enough to cause filamentation, had virtually no effect on the recovery division of SDS-induced filaments . The division of penicillin G-induced filaments was inhibited by SDS.

Med J Aust, 1981 May 30, 1(11), 577 - 8
Treatment of bacterial meningitis in children without intravenous fluids; Shann F et al.; It would be easier and cheaper, and there would be less risk of cerebral oedema, if bacterial meningitis could be adequately treated without the intravenous administration of fluid . Fifty children with bacterial meningitis were treated with intramuscular injections of benzyl penicillin, probenecid given orally and chloramphenicol palmitate suspension given orally, and the outcome was evaluated prospectively . Seven (14%) of the 50 children died . In a control group of 50 children with bacterial meningitis treated with the intravenous administration of benzyl penicillin and chloramphenicol sodium succinate, the outcome was determined retrospectively . Twelve (24%) of the 50 children died . The difference in mortality rate was 10% +/- 15.7% (+/- 2 SE), which is not significant . Except in the rare case of a child with shock or persistent vomiting, bacterial meningitis can be effectively treated with six-hourly intramuscular injections of penicillin, and probenecid and chloramphenicol given orally.

Ann Microbiol (Paris), 1981 May-Jun, 132(3), 253 - 65
Isolation of L-forms from the spleens of Brucella suis-infected, penicillin-treated mice; Schmitt-Slomska J et al.; Previous attempts to obtain in vitro wall-deficient stable L-forms of various strains of Brucella have failed because the obtained spheroplasts revert quickly to bacterial form . Here, we report the isolation of L-forms from mice infected with a B . suis strain type 1 and treated with penicillin . In defined experimental conditions, L-type microcolonies associated with tissue debris were observed in primary spleen cultures, even on antibiotic free media . After several transfers on penicillin-containing medium . typical, tissue-free L colonies were obtained . At first, when cultivated on antibiotic-free medium, these colonies reverted to the bacterial form (identified as B suis, biotype 1) . Later, after approximately fifteen transfers on penicillin-supplemented medium, they no longer reverted even after several subcultures on antibiotic-free medium . The L-forms' ultrastructural features included many giant empty bodies, considerable variation in size, shape and density of the wall-deficient cells, and many multilayered membranes . The stabilized L-forms were propagated in vitro and inoculated into mice, and then recovered from their spleens as tissue associated L-microcolonies . An occasional in vivo revertant was identified as B . suis, biotype 1 . These data provide one possible explanation for earlier failures to detect the presence of atypical bacteria in clinical or experimental Brucella infections.

J Reprod Fertil, 1981 May, 62(1), 193 - 7
Factors affecting the quality of boar semen stored by means of dialysis; Bamba K et al.; The effects of dialysis fluids containing blood serum, serum albumin or activated charcoal on the storage of boar serum were examined . The effects of antibiotics were also tested by including them in the dialysis fluids and semen samples . Undiluted semen was stored for 7 days at 15 degrees C by means of dialysis across a cellulose membrane . A combination of sulbenicillin and streptomycin was superior to that of penicillin and streptomycin in reducing bacteria and maintaining sperm motility and normal acrosomes . Serum albumin exerted a beneficial effect on the stored spermatozoa which may be due to its capacity to adsorb the metabolic products from bacteria and spermatozoa; it could be replaced with activated charcoal.

South Med J, 1981 May, 74(5), 530 - 3
Cellulitis: analysis of 101 cases and review of the literature; Ginsberg MB; A retrospective study of 101 patients with cellulitis of the head and neck and extremities showed that cellulitis, predominantly a disease of males, occurred at all ages; the lower extremities were affected more frequently in the elderly, whereas upper extremity involvement prevailed in young adults . A clinical prodrome, most often including chills, was less common than is widely believed . Redness, heat, swelling, and tenderness were consistently present, and lymphangitis and lymphadenitis were less frequent . Fever was generally mild, and WBC counts were modestly elevated, if at all . Because needle aspirates and blood cultures were rarely helpful, delineation of specific cause was difficult . Therapy included rest, elevation, moist heat, analgesia, antibiotics (usually penicillinase-resistant penicillin or penicillin itself), and incision and drainage when indicated . Most patients improved rapidly . Prolonged course and complications were unusual and there were no deaths.

Z Hautkr, 1981 May 1, 56(9), 563 - 9
{Sexually transmitted diseases in a crew of a destroyer on a voyage to Far East (author's transl)}; Adams HA; 21 cases of gonorrhea, some with very long incubation periods, were treated either with 3 x 4 Mega Clemizol-Penicillin G (13 cases) or with 2 x 2 gr . Spectinomycin (8 cases) . Thereby a complete cure was achieved in 14 cases (66, 6%), whereas in 2 cases after treatment with Penicillin no complete cure could be accomplished . A non-gonorrhean urethritis (NGU) occurred in the case of 5 patients (24%) . Treatment by Doxycyclin was successful but in one case 10 days of treatment proved to be too short so it was necessary to extend the period to 14 days for reasons of safety . The same applies to treatment of nongonorrhean urethritis . In the therapy of granuloma venereum Cotrimoxazol proved to be even more effective than tetracycline . However, it has to be taken into consideration that the disease had been yet in a process of healing.

Am Fam Physician, 1981 May, 23(5), 123 - 6
Treating gonorrhea; Fiumara NJ; The records of 1,381 patients with gonorrhea were examined by the Massachusetts Department of Public Health to determine the efficacy of their treatment schedules . Urethritis, cervicitis and pharyngitis were treated with 4.8 million u . of aqueous procaine penicillin G intramuscularly, without probenecid . Cure rates were 98 percent in urethritis, 97 percent in pharyngitis and 98 percent in cervicitis . Patients allergic to penicillin were treated with tetracycline orally or spectinomycin intramuscularly . In patients with proctitis, a 98 percent cure rate was achieved with one intramuscular injection of procaine penicillin G, followed by ampicillin orally for four days.

Can J Ophthalmol, 1981 Apr, 16(2), 79 - 83
Inactivation of aminoglycoside-penicillin combinations after subconjunctival injection; Ellis PP et al.; A study was undertaken to determine the extent of inactivation of gentamicin, tobramycin, ticarcillin and carbenicillin when given subconjunctivally in amino-glycoside-penicillin combinations . Rabbits were injected with such a combination in either the same or opposite subconjunctival sites . The aqueous humor was aspirated and bioassayed for antibiotic activity at 1 and 4 hours after injection . The influence of the aqueous humour upon antibiotic inactivation was studied by in vitro experiments . Ticarcillin penetrated into the aqueous humour better than carbenicillin . Some chemical inactivation of all the antibiotics given in combination occurred . There was less inactivation of the aminoglycosides at 4 hours when the antibiotics had been injected at opposite poles . The inactivation occurred primarily within the aqueous humour but to a lesser extent in the subconjunctival space . The degree of inactivation is likely of little clinical significance with the doses usually used.

J Antibiot (Tokyo), 1981 Apr, 34(4), 452 - 8
Delayed type hypersensitivity for penicillin in mice . I . Induction and characterization of delayed type hypersensitivity for penicillin in mice; Shiho O et al.; The delayed type hypersensitivity (DTH) for benzylpenicilloyl (BPO) group was observed in the footpad swelling reaction (FSR) in mice . Mice were subcutaneously immunized with 300 microgram of BPO-human serum albumin (HSA) conjugate and Freund's complete adjuvant and challenged into footpads with 25 microgram of BPO-bovine gamma globulin (BGG) conjugate 2 weeks after the immunization . The strongest FSR was observed 24 hours after the challenge . This FSR was typical DTH . Namely, the kinetics of FSR and the histological study showed the pattern of the DTH . Furthermore, the FSR could be transferred to normal syngenic mice by transfer of antigen-primed spleen cells and could not be transferred by anti-Thy-1,2-serum treated cells . The DTH for BPO was observed on day 4 after the immunization and reached the maximum on day 11 to 14 . Thereafter, the DTH for BPO decreased gradually in proportion as the IgG antibodies for BPO were produced . C57BL/6 and C3H/He mice high responders, A/J mice moderate, and BALB/c and DBA/2 mice were low responders . Penicillins were broad cross-reactive in FSR and its desensitization test because the DTH for penicillins contained the common reactivity for the penicilloyl moiety . The DTH for BPO was suppressed by intravenous preadministration of HSA and this suppression was sensitive to cyclophosphamide.

Sex Transm Dis, 1981 Apr-Jun, 8(2), 79 - 81
Eradication of Chlamydia trachomatis from the urethras of men with nongonococcal urethritis by treatment with amoxicillin; Bowie WR et al.; Twenty men with nongonococcal urethritis were treated orally with amoxicillin (750 mg three times daily for 10 days) . One man had herpes simplex virus infection of the urethra . Chlamydia trachomatis was isolated from the urethras of six (32) of the remaining men . Urethral specimens cultured for C . trachomatis became negative during amoxicillin therapy for all six men and remained negative for all five men who were followed for 24-48 days . Amoxicillin did not eradicate Ureaplasma urealyticum from any of 13 colonized men . Nongonococcal urethritis persisted or recurred at greater than or equal to 14 days after initiation of treatment in one of five men with, and ten of twelve men without initial C . trachomatis infection (P = 0.06) . Since multiple-dose penicillin regimens are used for the treatment of acute pelvic inflammatory disease and epididymitis, which are frequently caused by C trachomatis, the apparent efficacy of high-dose amoxicillin therapy for chlamydial urethritis in this study is of interest . However, until the results of further study of the efficacy of multiple-dose penicillin regimens for infections due to C . trachomatis are known, tetracyclines remain the treatment of choice for the majority of such complications.

Antimicrob Agents Chemother, 1981 Apr, 19(4), 571 - 4
Isolating specific auxotrophic mutants of Mycobacterium smegmatis by using vancomycin; Woodley CL et al.; After inducing mutagenesis with nitrosoguanidine, we used vancomycin enrichment in isolating auxotrophic mutants of Mycobacterium smegmatis . Compared with cycloserine and penicillin G, which are also cell wall inhibitors, vancomycin, with 24 h of exposure, produced less cell lysis and a greater reduction in viable cell numbers . With vancomycin enrichment, 13 specific auxotrophs were isolated after nitrosoguanidine-induced mutation, whereas only two mutants were isolated without enrichment.

Eur J Biochem, 1981 Apr, 115(3), 579 - 84
On the DD-carboxypeptidase enzyme system of Streptomyces strain K15; Leyh-Bouille M et al.; Streptomyces K15 possesses a set of exocellular and cell-bound D-alanyl-D-alanine carboxypeptidases . Four of them have been isolated to the stage where each enzyme preparation contains on single penicillin-binding protein . The exocellular 54000-Mr enzyme is extremely sensitive to benzylpenicillin and performs low transpeptidase activity on the carbonyl-donor/amino-acceptor tetrapeptide ACLLys(Gly)-DAla-DAla . The exocellular 40 000-Mr enzyme and the two lysozyme-releasable 40 000-Mr and 38 000-Mr enzymes are moderately sensitive to benzylpenicillin and have a high propensity to catalyse dimer formation from the aforementioned tetrapeptide monomer.

J Urol, 1981 Apr, 125(4), 549 - 50
Current management of iatrogenic splenic injuries in children; McCool RE et al.; Recent clinical observations indicate that children who have undergone splenectomy for trauma have a significantly increased incidence (about 2 per cent) of subsequent fata sepsis, particularly with pneumococcus organisms . Some protection against fatal sepsis may be afforded by immunization with the newly developed pneumococcal vaccine in children more than 2 years old or by the use of prophylactic penicillin . However, splenectomy should be avoided whenever possible . The vast majority of iatrogenic splenic injuries that occur during renal operations in children are usually minor capsular lacerations that can be managed conservatively, using suturing techniques and drainage, and do not require splenectomy.

J Antimicrob Chemother, 1981 Apr, 7(4), 319 - 30
Penicillin susceptibility testing of gonococci by disc diffusion; Jacobs MR et al.; This study investigated the use of various beta-lactam discs in the detection of penicillin sensitive, intermediate resistant and resistant strains (minimal inhibitory concentrations of penicillin G of less than 0.06, 0.06 to 0.25, and greater than 0.25 mg/l respectively) . Discs containing 0.15 and 0.6 microgram of penicillin G, and 5 microgram of methicillin were the most useful in separating the three groups . Cut-off zones between sensitive, intermediate resistant and resistant strains are 12 and 24 mm for 0.15 microgram penicillin discs; 24 and 32 mm for 0.6 microgram penicillin discs; and 20 and 30 mm for 5 microgram methicillin discs . Oxacillin discs (1 microgram) were useful in separating resistant from both sensitive and intermediate resistant strains at a cut-off zone of 8 mm . Use of a combination of discs provides the best index of susceptibility group, and at least two should be used

Epilepsia, 1981 Apr, 22(2), 217 - 24
Activating effects of homotaurine and taurine on corticoreticular epilepsy; Fariello RG et al.; Homotaurine and taurine are two powerful inhibitory aminoacids with anticonvulsant properties against various experimental models of focal epilepsy . This study reports on their effects in the feline model of corticoreticular epilepsy induced by parenteral administration of large amounts of penicillin . Both aminoacids, but particularly homotaurine, remarkably potentiate epileptiform discharges in cats . Brainstem transection at the precollicular level does not modify the activation, thus ruling out the intervention of mesoromboencephalic structures in the observed effect . The opposing action of these two amino acids on focal epilepsy as compared to corticoreticular epilepsy suggests that the two types of epileptiform activity stem from very different pathophysiological mechanisms . Homotaurine is a powerful GABA agonist that exerts a central action upon parenteral administration . Other GABA analogs such as muscimol, imidazole acetic acid, and gamma-hydroxybutyrate have been reported to potentiate experimental models of spike and wave epilepsy . Thus, the activating effects of homotaurine in this epilepsy model are in keeping with the demonstrated GABAmimetic properties of the compound.

Antimicrob Agents Chemother, 1981 Apr, 19(4), 532 - 3
Effects of sodium piperacillin on platelet function in normal volunteers; Gentry LO et al.; Piperacillin is a new semisynthetic penicillin which is similar in structure to carbenicillin and ticarcillin . Since the latter antibiotics have been shown to cause abnormalities in hemostasis, we studied the effects of piperacillin on blood coagulation and platelet function . Fifteen healthy volunteers received the drug in doses of either 100, 200, or 300 mg/kg per day for a period of 7 days . Serial studies showed no abnormalities in blood coagulation in any subject . Decreased platelet aggregation responses to adenosine diphosphate, epinephrine, collagen, and achidonic acid were commonly noted, but prolongation of the bleeding time occurred in only 3 of 15 subjects after 7 days of piperacillin administration . These results suggest that although piperacillin also induces platelet dysfunction, these effects may be less than those caused by ticarcillin or carbenicillin at an equivalent dosage.

Brain Res, 1981 Apr, 227(2), 269 - 81
Development of receptive field properties in the visual cortex of rabbits subjected to early epileptiform cortical discharges; Crabtree JW et al.; We examined the effects of early epileptiform activity on development of visuocortical receptive fields in the rabbit . Aqueous penicillin was injected twice a day into a cannula implanted over the monocular area of one visual cortex . Drug administration was begun on postnatal day 8-9 and continued until postnatal day 24-30 . Concomitant with the penicillin injections a mixture of penicillin and penicillinase was similarly applied to the monocular area of the contralateral control cortex . Interictal discharges were routinely observed only from the penicillin-treated or epileptic cortex . Single-unit recordings made on postnatal day 25-31 revealed that in the neuronal population adjacent to the cortical penicillin focus percentages of receptive field types were severely altered relative to control cortex percentages . Epileptic cortex showed an abnormally high percentage of no response type cells together with an abnormally low percentage of complex and oriented-directional type cells . These abnormalities were greater closer to the penicillin focus than further from it . Epileptic visual cortex receptive field percentages are compared with those for the neonatal rabbit and the rabbit subjected to early monocular deprivation . One interpretation of our results is that development of complex and oriented-directional type cells is impeded by epileptogenic disruption of organized geniculostriate activity.

Am J Gastroenterol, 1981 Apr, 75(4), 309 - 10
Whipple's disease, successful response to sulfamethoxazole-trimethoprim; Viteri AL et al.; Because of allergy to penicillin and intolerance to tetracycline, a 47-year old man, known to have Whipple's disease, was treated with sulfamethoxazole-trimethoprim, one tablet two times a day for six months . The patient has remained in remission one year after medication was discontinued . Sulfamethoxazole-trimethoprim may be the treatment of choice for Whipple's disease.

Electroencephalogr Clin Neurophysiol, 1981 Apr, 51(4), 393 - 402
Pattern of intracortical potential distribution during focal interictal epileptiform discharges (FIED) and its relation to spinal field potentials in the rat; Elger CE et al.; The pattern of intracortical potential distribution during focal interictal epileptiform discharges (FIED) was analysed with respect to the occurrence of descending neuronal activity to the spinal cord recorded as spinal field potentials (SFPs) . The experiments were performed in rats . Epileptiform activity was elicited by application of penicillin to the motor cortex . The spread of active penicillin was limited by penicillinase in part of the experiments . (1) When penicillinase was applied 10--20 sec before penicillin to the cortical surface typical FIED appeared in the epicortical lead . During well-established focal activity they were accompanied by negative field potentials at a depth of 300 micrometers and 600 micrometers and by positive field potentials in deeper records . This pattern of intracortical potential distribution was not associated with characteristic SFPs . (2) When penicillinase was applied simultaneously with penicillin, the fully developed epicortical FIED were accompanied by negative intracortical field potentials which in this case reached a depth of 900 micrometers . In the layers below predominantly positive potential fluctuations occurred . This pattern of intracortical potential distribution was associated with characteristic SFPs . (3) Intracortical application of penicillin at a depth of 800--900 micrometers led to negative field potentials of large amplitude in all intracortical records, with the concomitant epicortical potentials being positive in polarity . In this case SFPs occurred throughout the interictal activity . Since seizure activity can be restricted to only a few cortical laminae, descending neuronal activity to the spinal cord need not be correlated with definite epicortical potentials . A prerequisite for cortical output is intracortical activity reflected negative potentials at a depth of approx . 900 micrometers.

Brain Res, 1981 Mar 23, 209(1), 61 - 76
Visuocortical epileptiform discharges in rabbits: differential effects on neuronal development in the lateral geniculate nucleus and superior colliculus; Baumbach HD et al.; We have studied the effects of interictal epileptiform discharges originating from the striate cortex on the development of the receptive field characteristics of neurons in the lateral geniculate nucleus (LGNd) and superior colliculus (SC) in neonatal rabbits . The paroxysmal discharges were generated by twice-daily injections of penicillin into an implanted cannula . Control injections of penicillin + penicillinase were given to the other striate cortex of the same animal . Similar experimental procedures were used to study the effect of such projected discharges on the LGNd neurons in adult rabbit . The results of the first experiment show that cortical epileptiform discharges, initiated in neonatal rabbits 7--9 days of age and continuing to 20--25 days of age, retard the normal development of LGNd cells . There was an abnormal increase of indefinite cells, cells failing to respond to any light stimulation, and a concurrent decrease of cells with concentric cells was still present in adult rabbits which had interictal discharges in the striate cortex limited to the period of 7--9 days to 21--25 days of age . The fourth experiment shows that the interictal discharges in neonatal rabbits do not affect the normal receptive field development of neurons in the SC . The present results demonstrate that asymptomatic interictal epileptiform discharges, produced without focal structural damages in immature brain, can affect the development of neuronal connectivity . These results may have some clinical implications in relation to our understanding about the learning and developmental disabilities exhibited in children who had episodic seizure discharges.

Eur J Biochem, 1981 Mar 16, 115(1), 53 - 7
Chemical modifications of the active site of Streptomyces R61 DD-carboxypeptidase; Georgopapadakou NH et al.; The DD-carboxypeptidase of Streptomyces R61 is an exocellular enzyme related to the bacterial peptidoglycan cross-linking enzymes, and, like them, is inhibited by penicillin . The active-site reagents methanesulfonyl fluoride and diisopropylfluorophosphate inhibit catalytic activity and binding of penicillin G indicating the involvement of a serine residue in both processes . For methanesulfonyl fluoride the second-order rate constant (0.7 M-1 min-1) is comparable to that of classical serine proteases . For diisopropylfluorophosphate, which binds to the enzyme stoichiometrically, the second-order rate constant (1.5 M-1 min-1) is at least two orders of magnitude smaller . The arginine-specific reagents methylglyoxal, 2,3-butanedione and phenylglyoxal inactive DD-carboxypeptidase in borate buffer with second-order rate constants of 70, 70 and 120 M-1 min-1, respectively . Inactivation correlates with stoichiometric binding to the enzyme . Peptidase and esterase activities are similarly affected, suggesting that substrate binding in both cases requires an arginine-carboxyl group interaction . Penicillin binding is also inhibited, but the degree of inhibition depends on the alpha-dicarbonyl side chain . Binding of alpha-dicarbonyls to DD-carboxypeptidase facilitates subsequent binding of diisopropylfluorophosphate suggesting that interaction of these compounds with the active site might induce a conformational change on the enzyme making the serine residue more accessible to the modifying reagent.

Neurosci Lett, 1981 Mar 10, 22(2), 159 - 63
Effects of intracellular injections of chloride and EGTA on postepileptiform-burst hyperpolarizations in hippocampal neurons; Hablitz JJ; Intracellular recordings were obtained from CA1 neurons of hippocampal slices maintained in vitro . Epileptiform activity was induced by bath application of either penicillin (3.4 mM) or picrotoxin (5 X 10(-4) M) . The afterhyperpolarizations (AHPs) following evoked epileptiform events induced by penicillin were inverted by diffusion of chloride ions from KCl electrodes but were insensitive to injection of EGTA . Picrotoxin produced epileptiform events qualitatively similar to those seen with penicillin, but the AHPs were reduced or abolished by injection of EGTA and were chloride insensitive . AHPs that were evoked directly by depolarizing-current pulses when penicillin or picrotoxin was present were sensitive to EGTA . These results indicate that hippocampal CA1 neurons are capable of generating two types of hyperpolarizing events and that penicillin is apparently ineffective in completely blocking the chloride-mediated event.

Br J Haematol, 1981 Mar, 47(3), 443 - 52
Antibody-dependent cell-mediated cytotoxicity (ADCC) of penicillin-treated human red blood cells; Yust I et al.; Penicillin-treated human red blood cells (RBC) were lysed by the cooperation of autologous nonsensitized peripheral blood mononuclear cells and human anti-penicillin serum . Using a rapid (3 h) assay of antibody-dependent cell-mediated cytotoxicity (ADCC), lysis was proportional to serum (anti-penicillin antibody) concentration, to incubation time and to the concentration of attacking cells, which were obtained from normal human peripheral blood by Ficoll-Hypaque separation . Incubation of these lymphoid effector cells on a nylon column prior to the tests depleted the number of phagocytic (latex positive) cells in the effluent; there was a concomitant drop in cytotoxic activity . Enrichment of mononuclear phagocytes in the attacking cell population by albumin gradient separation led to an increase in cytotoxicity . Granulocytes separated by Ficoll-Hypaque were not active in this system . Using specific antisera the antibody was found to be of the IgG1 sub-class . Anti-penicillin antibody activated the complement system in vitro, but failed to induce lysis of penicillin-treated RBC in the presence of complement without attacking cells . These results suggest that ADCC may participate in the destruction of RBC in penicillin-induced haemolysis in vivo.

Poult Sci, 1981 Mar, 60(3), 631 - 6
Effect of dietary cereal grain, citrus pectin, and guar gum on liver fat in laying hens and young chicks; Patel MB et al.; One laying hen and three chick experiments were conducted to study the effect of cereal grains, citrus pectin, and guar gum on liver fat of chicks and hens and on serum cholesterol of chicks . Feeding of wheat, rye, or 2% pectin in place of corn reduced liver fat content . The decrease in liver fat of hens fed wheat or rye was larger than that of those fed 2% pectin (P less than .05) . The smallest amount of liver fat was found in livers of hens fed the rye diet . Wheat or pectin did not affect egg production of egg weight, but rye caused a significant decline in egg production in comparison with other treatments . Addition of 4% pectin or 2% guar gum to the corn control diet lowered liver fat, serum cholesterol (P less than .05), and body weight in chicks (P less than .05) . Penicillin added to the diets containing 2% guar gum gave an increase in body weight (P less than .05) but had no effect on body weight of chicks fed diets containing 4% pectin . In contrast, pectinase prevented growth depression by pectin and guar gum . Pectinase also increased liver fat and serum cholesterol of birds fed the diet containing pectin or guar gum . When the corn control diet was pair-fed to the pectin diet, growth of the pair-fed chicks was better than that of the pectin-fed birds but was lower than that of birds fed the control diet ad libitium . Pectin-fed birds again had lower liver fat the serum cholesterol than the control birds . The reduced feed intake of chicks pair-fed the corn control diet had no effect on liver fat content.

Comput Programs Biomed, 1981 Mar-Jun, 13(1-2), 19 - 26
Real-time analysis of hippocampal neural activity in the intervals between interictal spikes; Horowitz J et al.; Previously the electroencephalogram (EEG) was modeled as consisting of faster, smaller waves superimposed on larger, slower waves . The intent of this study is to modify the program to sample neural activity over specific intervals of time following detection of a distinct wave pattern . The use of conditional sampling is illustrated by considering wave detection following epileptic interictal spikes in the rabbit hippocampus . To create an epileptic focus, small pellets of sodium penicillin suspended in agar were placed on the rabbit hippocampus . This produced regularly recurring, spontaneous, large amplitude discharges, or interictal spikes, at the site of application . Following detection of an interictal spike, the program delayed the onset of a sample period for either 1.0 s or 6.0 s . The neural activity was then sampled for 5.1 s, and fast and slow waves were detected over the sample period . The frequency distribution of waves in four of these 5.1 s intervals was calculated . Comparison of the frequency distributions following the 1.0 s and 6.0 s delays showed no discernible differences . The data illustrate that not all types of neural activity are markedly modified by interictal spikes and suggest that hippocampal cellular populations generate similar waves 1.0 s and 6.0 s after such a spike . Moreover, this experiment illustrates adaptation of the program to sample activity over a limited period of time following detection of a specific cortical waveform.

Z Rheumatol, 1981 Mar-Apr, 40(2), 54 - 61
{Current status of D-penicillamine therapy in chronic polyarthritis}; Franke M et al.; Long-term-treatment of rheumatoid arthritis (RA) with D-Penicillamine (DPA) is well established . In several controlled clinical studies, DPA-therapy has been shown to be effective, even in lower dosage (450--600 mg/day) than used in first years after introduction of this drug . As the dosage has been reduced there was a marked decrease in unwanted drug effects . Nevertheless proteinuria, agranulocytosis and LED-like syndromes remain serious side-effects . Therefore a close supervision of patients under DPA is still necessary . The limitations for DPA-treatment are age, disease activity and LED-like symptoms . RA-patients with renal insufficiency, penicillin-allergy, hematopoietic dysfunction, cancer and chronic infections should never be treated with DPA.

Farmakol Toksikol, 1981 Mar-Apr, 44(2), 136 - 40
{Effect of pyridoxal-5-phosphate on epileptic activity in the cerebral cortex}; Kryzhanovskii GN et al.; It has been shown in acute experiments on cats that pyridoxal-5-phosphate (PALPh) injected intravenously in doses of 5-20 mg/kg suppresses the epileptic activity in solitary foci caused by penicillin and strychnine local application as well as in the complex of loci created in different zones of the brain cortex . Under the influence of PALPh the complex was destabilized and suppressed, and the epileptic activity first disappeared in the dependent foci and then in a determinant one . It is concluded that PALPh has antiepileptic activity . This effect seems to be more pronounced in the penicillin-induced epileptic foci.

Trop Geogr Med, 1981 Mar, 33(1), 8 - 13
Childhood rheumatic heart disease in Nigeria; Jaiyesimi F et al.; Eighty Nigerian children (mean age = 8.8 years) with rheumatic heart disease (RHD) were studied prospectively . The initial acute rheumatic fever (ARF) was recognized in 34 of them (42%) while 18 patients (23%) had recurrent ARF . 76 patients (95%) had mitral incompetence, either alone or in combination with other lesions . Symptomatic mitral stenosis was present in 21 patients (26%), occurred early in life, and appeared to be causally related to recurrent ARF and intense host reactions . Aortic and tricuspid valve diseases were uncommon and pulmonary valve disease was rare . 94% of the patients presented in heart failure, and, 4 years after, 20% of those re-examined had improved, 32% remained about the same, and 48% had deteriorated . The high cumulative mortality at 6 years (20%) was attributable to heart failure and subacute bacterial endocarditis . We suggest that in developing countries, all episodes of pharyngitis in children susceptible to ARF should be treated with penicillin, the only exception being pharyngitis associated with definite viral illnesses like measles.

Prikl Biokhim Mikrobiol, 1981 Mar-Apr, 17(2), 203 - 9
{Intracellular ribonucleases from Penicillin brevicompactum and their natural inhibitors}; Zigel' M et al.; The ability of the fungus Penicillium brevi-compactum for the synthesis of intracellular ribonucleases and their inhibitors was examined . Activities of ribonucleases and their inhibitors were found to vary with the culture growth . As a result of isopropanol precipitation of the cell-free homogenate, ion-exchange chromatography on DEAE-cellulose and gel filtration on Sephadex G-75, two fractions were obtained, they being inhibitor complexes with acid and alkaline intracellular ribonucleases.

Pediatrics, 1981 Mar, 67(3), 387 - 8
Cerebrospinal fluid concentrations of aqueous procaine penicillin G in the neonate; Speer ME et al.; Simultaneous serum and CSF samples were obtained following the intramuscular administration of 50,000 units/kg of aqueous procaine penicillin G in 25 neonates . Penicillin activity was detected in the sera and CSF of all patients . Peak serum levels were noted at four hours (mean +/- SEM, 17.1 +/- 6.3 micrograms/ml) . Peak CSF levels were noted at 12 hours (0.70 +/- 0.35 microgram/ml) . The serum level at 24 hours was 2.1 +/- 0.98 microgram/ml (range, 0.2 to 5.8 micrograms/ml); the CSF level at 24 hours was 0.12 +/- 0.05 micrograms/ml (range, 0.03 to 0.27 microgram/ml) . These results demonstrate that spirocheticidal levels (greater than or equal to 0.03 microgram/ml) are achieved for at least 24 hours in the CSF following the intramuscular administration of aqueous procaine penicillin G in neonates.

Pharmacol Biochem Behav, 1981 Mar, 14(3), 273 - 81
The stereotyped behavior syndrome: a new model and proposed therapy; Kryzhanovsky GN et al.; The stereotyped behavior syndrome was induced in rats through local impairment of inhibitory GABA-ergic mechanisms in both caudate nuclei by bilateral microinjection of tetanus toxin, penicillin, or picrotoxin into the rostral part of the caudate nucleus . Intraperitoneally injected haloperidol suppressed the syndrome; this effect was dose-dependent . The same effect on the tetanus toxin-induced stereotyped behavior was produced by GABA microinjected bilaterally into the rostral part of the caudate nucleus of unrestrained rats . It was found in this model of tetanus toxin-induced stereotyped behavior that lithium chloride and diazepam can suppress the syndrome . Combined application of lithium chloride, diazepam, and haloperidol in minimal effective doses resulted in a much more complete and longer-lasting suppression of the syndrome than the separate use of these drugs . This effect is attributed to the joint specific actions of the drugs on pathogenetically interrelated components of a hyperactive determinant structure that arises in the caudate nuclei after impairment of the GABA control and this is responsible for the stereotyped behavior syndrome.

J Bacteriol, 1981 Mar, 145(3), 1293 - 8
Topographical distribution of penicillin-binding proteins in the Escherichia coli membrane; Buchanan CE; The penicillin-binding proteins (PBPs) found in the membranes of Escherichia coli X925 minicells (primarily cell ends or septa) were compared with those found in rod-shaped cells (primarily sidewalls) in an effort to determine whether certain PBPs are unevenly distributed over the bacterial cell membrane . The seven major PBPs of E . coli were all present in minicell membranes . PBP 1B was altered in minicells, however, appearing as two bands on sodium dodecyl sulfate-polyacrylamide gels rather than the usual three . PBP 2, which is needed for longitudinal growth of the cell but not for septum formation, was significantly reduced in minicell membranes . This observation is consistent with the fact that minicells contain very little sidewall material and raises the possibility that the specialized function of PBP 2 may be determined or regulated by its uneven topographical distribution in the membrane . None of the PBPs appeared to be selectively enriched in minicell membranes.

Farmakol Toksikol, 1981 Mar-Apr, 44(2), 143 - 6
{Changes in the activity of an epileptogenic focus in the hippocampus of rats treated with the chief metabolites of tryptophan}; Mikhailov IB; It has been shown in rats, as previously on frogs, with electrochemotrodes chronically implanted into dorsal hippocampuses that some kynurenine metabolites of tryptophan (quinolinic acid, d, 1-kynurenine) can provoke an increase in the pathological activity of the penicillin-induced epileptogenic focus in the hippocampus . Unlike kynurenines, serotonin, another tryptophan metabolite, and the serotoninomimetic 5-methoxytryptamine suppress the pathological activity of the epileptogenic focus . The results obtained support the hypothesis about a certain role of kynurenines and serotonin in the pathogenesis of epilepsy.

Clin Allergy, 1981 Mar, 11(2), 155 - 60
Diagnosis of penicillin allergy by means of Phadebas RAST penicilloyl G and V and skin tests; Jarisch R et al.; Fifty patients with suspected allergy to penicillin were tested . Skin tests were done with Na-penicillin G and penicilloyl-polylysin . Specific IgE antibody assays were done with penicilloyl G and V conjugates by means of RAST . The overall agreement between skin test and RAST results was 87%, borderline cases not included . In one case, skin tests were positive to penicillamine only, while RAST for penicilloyl G and V both proved to be positive . One case of penicillin allergy could be diagnosed in vitro post mortem only . Two cases of Hoigne syndrome showed no evidence of allergy . Patterns of skin manifestations varied but urticaria was the most commonly seen feature . Twenty patients without adverse reactions to penicillin treatment and seven patients who had not received penicillin over the last 10 years served as controls . None of them were positive in either skin tests of RAST . Two or our twenty control patients developed penicillin allergy during the study . Both showed positive RAST results.

J Neurosci, 1981 Mar, 1(3), 259 - 70
Snake alpha-toxin effects on cholinergic and noncholinergic responses of Aplysia californica neurons; Ono JK et al.; The effects of alpha-toxins from Bungarus multicinctus (alpha BuTX) and Naja naja siamensis (alpha NTX) were studied on synaptic responses and on extrasynaptic responses to focally applied acetylcholine (ACh), histamine (Hm), gamma-aminobutyric acid (GABA), and glutamate (glu) in neurons of the marine mollusc, Aplysia californica . Binding of 125I-alpha BuTX to Aplysia ganglia homogenates was pharmacologically characterized and compared with the pharmacological sensitivity of 125I-alpha BuTX binding to rat brain membrane preparations . Both alpha BuTX and alpha NTX at 10(-5) M reversibly inhibited the ACh-induced increase in Cl- conductance (GCl) without affecting ACh responses mediated by an increase in Na+ conductance (GNa) or an increase in K+ conductance (GK) . In addition, both alpha-toxin reversibly inhibited the GCl responses induced by Hm and, in some cases, glu . GABA-induced GCl responses were not affected by either toxin even at concentrations as high as 10(-3) M . Both toxins also inhibited synaptic cholinergic GCl responses as well as the GCl component of postsynaptic potentials mediated by noncholinergic presynaptic neurons . Studies of 125I-alpha BuTX binding to Aplysia ganglia homogenates demonstrated the presence of a single saturable, high affinity site with a dissociation constant (KD) of 3.6 X 10(-9) M . The pharmacological profile of agents which inhibit 125I-alpha BuTx binding to Aplysia ganglia was similar to the profile of vertebrate ganglionic and brain preparations; d-tubocurarine, nicotine, and carbamylcholine effectively and competitively inhibit binding, whereas hexamethonium and decamethonium are less effective and noncompetitive . Strychnine and bicuculline, agents known to block responses to a variety of agonists in Aplysia, were effective competitive inhibitors of toxin binding in Aplysia and in rat brain . Strychnine is not as potent in inhibiting toxin binding to electric organ preparations . Chloride channel blockers, such as penicillin and picrotoxin, and noncholinergic agonists, such as Hm and glu, had no effect on toxin binding . The alpha-toxins appear to inhibit noncholinergic GCl responses through a cholinergic receptor associated with the Cl- conductance mechanism for the noncholinergic agonist.

Nouv Presse Med . 1981 Feb 28;10(9):712.
{Erythema nodosum and oral contraception . Demonstration of an anti-ethinyl estradiol antibody}; Touboul JL et al.; PIP: The article reports a case of a 23 year old patient on combined oral contraception (OC) for 2 1/2 years, hospitalized for persistent fever . Sural phlebitis and extended erythema nodosum were diagnosed . OC treatment was discontinued and the patient, treated with penicillin and calcium heparinate, left the hospital after 1 week . While thrombotic accidents during OC treatment are well documented, there have been only 13 cases of erythema nodosum . The case presented here is of particular interest because of the association between phlebitis and erythema nodosum, and because the antiethinyl estradiol antibodies found in the patient's serum are those usually found during thrombosis caused by OCs . An immunologic mechanism may be the cause of such an accident .

Arch Intern Med, 1981 Feb 23, 141(3 Spec No), 301 - 4
Therapeutic implications of drug interactions with acetaminophen and aspirin; Hayes AH Jr; Only drug-drug interactions that are believed clinically important and that are primarily pharmacokinetic in nature are discussed in this article . Drugs reported to interact with aspirin are oral anticoagulants, methotrexate, probenecid, and sulfinpyrazone; those that are believed to interact with acetaminophen are propantheline bromide, narcotics, and metoclopramide hydrochloride, as well as food (carbohydrates) . Ethyl alcohol, ammonium chloride, antacids, oral antidiabetic agents, corticosteroids, and heparin sodium probably interact with aspirin . Fenoprofen calcium, gold sodium thiomalate, indomethacin, naproxen, penicillin, phenylbutazone, phenytoin sodium, and spironolactone may also cause such interactions . Ethyl alcohol, beta-adrenergic blockers, oral anticoagulants, chlorpromazine hydrochloride, and miscellaneous mutual toxicities may cause interactions with acetaminophen . The concomitant use of drugs that are believed to interact importantly with either aspirin or acetaminophen should be avoided when designing a treatment regimen . The remaining agents discussed here (of doubtful importance in man) demand careful monitoring in difficult clinical situations and must be submitted to further controlled studies.

Biochem J, 1981 Feb 15, 194(2), 645 - 7
Conversion of isopenicillin N into penicillin N in cell-free extracts of Cephalosporium acremonium; Jayatilake GS et al.; In a cell-free system prepared by osmotic lysis of protoplasts of Cephalosporium acremonium, isopenicillin N is converted into penicillin N . The epimerase activity of the system is labile.

Lancet, 1981 Feb 7, 1(8215), 315 - 9
Biological effects of sexual freedom; Catterall RD; PIP: It is difficult to determine the true incidence of sexually transmitted diseases (STD) . Underreporting of STD is widespread . In the United Kingdom the available figures exclude patients treated by general practitioners or patients in the armed forces . The incidence of STDs is rising . In 1979 the figure for the United Kingdom was about 500,000 new cases . The most common STD in England and Wales is non-specific urethritis or non-specific genital infection . The increase in gonorrhea has been less dramatic in England and Wales than it has been in other industrial and urbanized countries . Regardless, between 1960 and 1979 the incidence of the disease doubled to 60,000 new cases a year . Recent research has shown another group of sexually transmissible infectious agents which are now more common than the older venereal infections . Viruses are responsible for reversal of this 2nd generation of STDs . Their manifestations range from local discomfort to chronic disability, infertility, ectopic pregnancy, stillbirth, and neonatal death . There are many medical, social and economic factors which contribute to this increase in the incidence of STD and the recognition of the 2nd generation of sexual infections . Some of these are known, others unknown . The introduction of penicillin and other antibiotics has had a great effect on some STDs, notably syphilis . Pelvic inflammatory disease has been the most important cause of increases in female infertility and ectopic pregnancy . The new generation of STDs has serious and potentially dangerous effects on both expectant mothers and their infants .

Can J Psychiatry, 1981 Feb, 26(1), 68 - 70
Neurosyphilis in a young man; Hoffman BF; New cases of neurosyphilis are comparatively rare . The epidemiology and clinical presentation of neurosyphilis are described . The article describes the presentation of general paresis in a 34 year old man, 10 years after he had been ineffectively treated with penicillin for secondary syphilis . The various laboratory tests for syphilis are reviewed . The Venereal Disease Research Laboratories (VDRL) is currently the best screening test and the Fluorescent Treponema Antibody-Absorption test (FTA-ABS) is the current recommended specific test for syphilis . Central nervous system involvement is confirmed in the laboratory by a positive VDRL on the cerebrospinal fluid . Physicians should be on the alert for this cause of dementia which may, once again, be increasing in frequency.

Arch Dermatol, 1981 Feb, 117(2), 73 - 6
White sponge nevus; Jorgenson RJ et al.; White sponge nevus (WSN) is one of a number of white lesions of the oral mucosa . It is an autosomal dominant disorder of wide variability and high penetrance . White sponge nevus is characterized by white, spongy lesions of the oral mucosa, although extraoral mucosae may also be affected . Onset is early in life, and both sexes are affected equally . There are no extramucosal lesions associated with WSN . The plaques of WSN are benign and may undergo alternate periods of remission and exacerbation . In two of our cases from an affected family, penicillin precipitated remission of the plaques.

Am J Ophthalmol, 1981 Feb, 91(2), 261 - 3
A case of syphilitic uveitis; Kranias G et al.; A 38-year-old man had anterior uveitis that failed to respond to increasingly aggressive therapy with topical and systemic corticosteroids and mydriatrics . His disease progressed to panuveitis and neuroretinitis and was finally cured with penicillin injections for acquired syphilis . He suffered secondary optic nerve atrophy . Because of the resurgence of the incidence of syphilis in the general population and the dire consequences for the patient in the absence of appropriate therapy, the ophthalmologist needs to consider the possibility of syphilis in his patients with uveitis . He should obtain serologic studies for syphilis.

Drug Intell Clin Pharm, 1981 Feb, 15(2), 99 - 102
Actinomycosis: the disease and its treatment; Robbins TS et al.; A case of pulmonary actinomycosis is described in a patient who presented with fever, weight loss, and a painful mass on his lower anterior left rib cage . Gram-stain and culture and sensitivity tests performed on the fluid drawn of the chest wall mass revealed Actinomyces israelii as the infecting organism . The patient was successfully treated with long-term penicillin therapy . A review of this rare bacterial disease is presented, emphasizing its treatment and its similarities and differences to other bacterial and fungal diseases.

Biull Eksp Biol Med, 1981 Feb, 91(2), 178 - 81
{Effect of mebikar on focal epileptic activity}; Rekhtman MB et al.; Effect of mebicar on the epileptic activity (EA) and frequency of interepileptic activity discharges (IEAD) was studied in experimental focal cortical epilepsy induced by penicillin application to the sensomotor cortex of conscious rats . Mebicar in a dose of 300--100 mg/kg induced a dose-dependent suppression of EA in the presence of the increased frequency of IEAD . During rhythmic stimulation of some areas of the thalamus mebicar completely abolished high-frequency EA, promoting consecutive alternating on the electrocorticogram of periods of responses to each stimulus with dead bands . The antiepileptic effect of mebicar was compared with that of diazepam in the similar model of epilepsy . It is suggested that the action of mebicar on the focus of epileptic activity in the cerebral cortex is related to the potentiation of synaptic inhibition of the neurons in the focus of epileptic activity.

Neurology, 1981 Feb, 31(2), 202 - 4
Spinal epidural abscess due to Actinomyces israelii; Kannangara DW et al.; A 31-year-old man had back pain, weight loss, fever, and paraplegia, with radiographic evidence of a left upper lobe lesion and lytic lesions in ribs and vertebral bodies . Gallium uptake was increased over the spine . At surgery we found a paraspinal abscess due to Actinomyces israelii . The patient responded to surgery and penicillin therapy . This is the first report of a case of actinomycotic spinal epidural abscess necessitating emergency surgery since the advent of penicillin.

Aust J Ophthalmol, 1981 Feb, 9(1), 63 - 7
Evaluation of the safety of storage medium for corneal transplants; Thyer W et al.; The results of 27 keratoplasties done at the Royal Adelaide Hospital were analysed . The success rate of the graft was similar whether storage was as whole eyes (60%) or corneo-scleral rims (65%) . A modified McCarey-Kaufman medium has been used for 2 years to store the corneo-scleral rims . Phenol red has been added as an indicator of pH change and probable bacterial contamination . Laboratory experiments contaminating this medium with potential pathogens have shown that the indicator is valueless for this purpose . Several antibiotics, alone and in combination, and at varying temperatures of storage, were tested in experiments . None could be relied on to sterilise the media of the inoculated bacteria . Whole eyes are stored in moist chambers containing normal saline with penicillin plus streptomycin which is less able to support bacterial growth . Similar challenge experiments showed that normal saline is not sterilised by the penicillin plus streptomycin.

Br J Vener Dis, 1981 Feb, 57(1), 15 - 9
Treponema-specific and antilipoidal 19S(IgM) antibodies in penicillin-treated and untreated rabbits after infection with Treponema pallidum; Muller F et al.; The titres of treponema-specific and antilipoidal 19S(IgG) antibodies were determined in rabbits infected intratesticularly with Treponema pallidum . One group of rabbits was treated with penicillin the other served as control . Using different serological tests it was shown that 19S(IgM) antibodies were still detectable eight months after infection at about the same titres in both groups . In contrast, 19S(IgM) antibody titres in patients with syphilis became undetectable within three to six months after penicillin treatment . It is suggested therefore that the rabbit is not a reliable model for studying the effect of penicillin in human T pallidum infections.

Int J Pept Protein Res, 1981 Feb, 17(2), 211 - 8
Secondary structure relations between beta-lactamases and penicillin-sensitive D-alanine-carboxypeptidases; Moews PC et al.; The sequence homology found by Waxman & Strominger between penicillin-sensitive D-alanine-carboxypeptidases and penicillin-inactivating beta-lactamases is shown to extend to the level of secondary structure as predicted by the method of Chou & Fasman or by the informational method of Garnier et al . Thermodynamic similarity of homologous segments of these proteins is demonstrated by means of a sequence-independent parameter, the hydration potential of Wolfenden at al . Although the 40- to 70-residue amino-terminal sequences examined contain a common serine reactive with penicillins and (in the case of the carboxypeptidases) an R-D-alanyl-D-alanine substrate analog, no homology in secondary structure or hydration potential could be found with a serine protease such as alpha-chymotrypsin.

J Gen Microbiol, 1981 Feb, 122(Pt 2), 339 - 43
Intergeneric cosynthesis of penicillin by strains of Penicillium chrysogenum, P . chrysogenum/notatum and Aspergillus nidulans; Makins JF et al.; A number of mutants impaired in penicillin production have previously been isolated from Penicillium chrysogenum and Aspergillus nidulans . During cofermentation of osmotically fragile mycelia derived from these strains, in the presence of inhibitors of cell wall regeneration, intergeneric cosynthesis has been demonstrated between mutants which are probably impaired in different parts of th penicillin biosynthetic pathway.

Semin Arthritis Rheum, 1981 Feb, 10(3), 173 - 97
Disseminated gonococcal infection (DGI) and gonococcal arthritis (GCA): II . Clinical manifestations, diagnosis, complications, treatment, and prevention; Masi AT et al.; This is the second part of an integrated review of disseminated gonococcal infection (DGI) and gonococcal arthritis (GCA) . It covers clinical manifestations, spectrum of GCA, diagnosis and treatment . These disorders are important since DGI may be the most frequent form of acute arthritis in sexually active younger females, and other selected groups . Although the spectrum of disease is varied, it may be classified into stages and clinical subgroups . N . gonorrhoeae strains causing DGI in the U.S . have been highly sensitive to penicillin . Such findings require revision in beliefs that high-dose intravenous penicillin is needed for effective initial therapy of GCA . Recommended treatment protocols for localized gonorrhea and DGI are reviewed as well as the occurrence and implications for treatment of penicillinase-producing N . gonorrhoeae (PPNG) infection in the U.S.

Br J Dermatol, 1981 Feb, 104(2), 157 - 9
Repeated patch testing in penicillin allergy; Bruynzeel DP et al.; Fifteen patients with positive patch test reaction to penicillin preparations were retested several times . This resulted in increasing reactions in eight out of fifteen patients and in decreasing reactions in five patients.

J Pharm Sci, 1981 Feb, 70(2), 127 - 30
Utility of chloranil in assay of naphazoline, clemizole, penicillin G sodium, and piperazine; Belal S et al.; A simple and sensitive spectrophotometric method is described for the assay of naphazoline, clemizole, penicillin G sodium, and piperazine . The method was based on the formation of a charge transfer complex between these drugs as n-donors and chloranil, the pi-acceptor . Conformity to Beer's law enabled the assay of dosage forms of these drugs . Compared with official methods, the results obtained were of equal accuracy . A more detailed investigation of th naphazoline-chloranil complex was made with respect to its composition, association constant, and free energy change.

Vet Rec, 1981 Jan 31, 108(5), 90 - 3
Characterisation of Brucella abortus strain 19 cultures isolated from vaccinated cattle; Thomas EL et al.; Thirty-four cultures recovered from material of bovine origin in England, Scotland and Wales were identified unequivocally as Brucella abortus strain 19 (S19) . All had the properties of carbon dioxide-independent B abortus biotype 1 strains, were inhibited by penicillin G and thionin blue at standard concentrations and behaved in oxidative metabolism and guinea pig virulence tests as typical S19 . Their sensitivity to i-erythritol varied somewhat between cultures as did reference subcultures of S19 . Of the total number of isolates, 11 were recovered from abortion material or cyetic products, 10 were from calves which died from a hypersensitivity reaction within 24 hours of S19 vaccination and the remainder were from milk or internal organs . From the evidence available, there is little to suggest that calfhood vaccination with S19 has resulted in persistent systemic infection in other than a very small proportion of the animals inoculated.

Science, 1981 Jan 16, 211(4479), 294 - 7
Giant synaptic potential hypothesis for epileptiform activity; Johnston D et al.; According to one hypothesis, the paroxysmal depolarizing shift observed in the penicillin model of epilepsy results from a giant excitatory postsynaptic potential . This hypothesis has recently been questioned, primarily because it has never been subjected to rigorous experimental examination . Four quantitative predictions were derived from this hypothesis and tested in CA3 pyramidal neurons of the hippocampus . The four critical predictions concern the behavior of the paroxysmal depolarizing shift under current- and voltage-clamp conditions as a function of membrane potential . The experiments confirmed all four predictions.

Brain Res, 1981 Jan 5, 204(1), 226 - 30
Voltage clamp study of cat spinal motoneurons during strychnine-induced seizures; Schwindt PC et al.; Cat spinal motoneurons were examined by the technique of somatic voltage clamp during strychnine-induced spinal seizures . No clear alteration of voltage-dependent ionic currents was required in order for typical strychnine-induced paroxysmal depolarization shifts (PDSs) to develop in contrast to results previously obtained during penicillin-induced spinal seizures . Voltage clamp of evoked and spontaneous PDSs indicates these are generated by a synchronized mixture of excitatory and inhibitory synaptic currents wih excitation predominating.

Ann Otol Rhinol Laryngol, 1981 Jan-Feb, 90(1 Pt 1), 21 - 4
Electronystagmography in congenital and acquired syphilitic otitis; Wilson WR et al.; This study is an analysis of the electronystagmogram (ENG) changes in 17 patients with luetic vestibular disease with early and late acquired syphilis and congenital syphilis . Vestibular disturbances occurred in 80% of patients with luetic otitis . Among these patients the ENG gives signs of peripheral rather than central vestibular injury, and reduced vestibular response to caloric stimulation is the most common finding . Congenital syphilis patients have the greatest dysfunction, both in degree of ENG changes and incidence of bilaterality . We found no correlation between FTA-ABS levels and the amount of hearing impairment or vestibular injury . Treatment with penicillin and steroids had a beneficial subjective effect upon the symptoms of vertigo in over half the patients.

Int Arch Allergy Appl Immunol, 1981, 64(2), 195 - 200
Evaluation of circulating immune complex-like material for development of skin reactions in connection with penicillin therapy; Ahlstedt S et al.; The levels of immune complex-like material in serum from 18 patients in connection with skin eruptions appearing during penicillin therapy were determined with a modified ELISA . Immune complex-like material could only be shown in the serum of 3 out of the 17 patients . However, according to ELISA results, the complexes appeared without the simultaneous presence of penicilloyl-specific antibodies . Neither could penicilloyl-specific antibodies be recorded in 9 patient treated with parenteral penicillin without adverse reactions . 3 of these patients had immune complex-like material in their serum . It was concluded that immune complex-like material with penicilloyl specificity is not likely to contribute to the development of skin eruptions often seen in connection with penicillin treatment.

Am J Clin Pathol, 1981 Jan, 75(1), 113 - 6
Infections caused by Actinomyces viscosus; Eng RH et al.; Two cases of Actinomyces viscosus infection of the lungs were seen in nonimmunosuppressed patients . One patient had a peripheral actinomycotic lung mass resembling a tumor . Both patients responded to a long course of penicillin therapy . Reports of A . viscosus infections are rare, although the organism colonizes the mouths of most adult humans . Only ten cases have previously been described . There is no characteristic of A . viscosus infection that can distinguish it from Actinomyces israelii or Actinomyces bovis infections . The illness usually manifests as a chronic disease weeks to months before the diagnosis, which can only be made by identification of the organism from a clinical specimen uncontaminated by sputum or mouth flora . Ignorance of the biochemical reactions and growth characteristics of this organism have in the past hindered its isolation and identification . At least three weeks of antibiotic therapy using agents to which A . viscosus is sensitive in vitro are required for cure.

Surg Gynecol Obstet, 1981 Jan, 152(1), 27 - 9
The management of transpharyngeal gunshot wounds to the cervical spine; Schaefer SD et al.; Management to prevent cervical osteomyelitis in transpharyngeal gunshot wounds which involve the cervical spine consists of triple endoscopy to identify the pharyngeal injury, anteroposterior and lateral view roentgenograms to localize the injury to the cervical spine, administration of penicillin and gentamicin intravenously, exploration of the neck and repair of pharyngeal wounds, debridement of the cervical spine and external immobilization of the spine for six weeks . This management protocol has proved successful in five patients.

Gastroenterology, 1981 Jan, 80(1), 159 - 65
Protein secretion in suspensions of isolated rat hepatocytes: no influence of acute ethanol administration; Morland J et al.; The effect of ethanol on the secretion of proteins was studied in hepatocytes isolated from 24-h fasted rats and from fed rats . Hepatocytes were isolated after collagenase disruption of the liver and incubated in a standard medium containing amino acids, bovine albumin, glucose, penicillin and streptomycin in HEPES buffer . Cell viability was determined by urea production and trypan blue exclusion . When studying protein export, a model had to be chosen in which the labeling is accomplished before the addition of the test agents . Cells were incubated with {3H}valine for 2.5 and 7.5 min followed by a 15-mM valine chase and the incubates were adjusted to final concentrations of ethanol of 50 mM, 100 mM, colchicine 5-50 microM or cycloheximide 18 microM . Cells and media were harvested at various times, and counts incorporated into medium and cell protein were determined . Cycloheximide inhibited protein synthesis by 99%, decreased protein secretion by 10-20%, but did not further inihibit protein labeling when given after the chase confirming the chase's effectiveness . Colchicine inhibited protein release by 27-54% depending on the dose . With control cells labeled protein and specifically albumin appeared in the medium 20 min from the start of the pulse and this release of protein was not inhibited by 50 mM or 100 mM ethanol incubated with cells from the same animal whether the donor has been fed or fasted . The values for the ethanol-treated cells ranged from 94.0 to 113% of the control values from 30 to 120 min after the addition of the pulse . Lactate levels were markedly elevated, and urea synthesis decreased in the presence of either 50 mM EtOH or 100 mM EtOH . Thus using a method that can distinguish the effect of ethanol on synthesis from secretion, it is concluded that acute exposure to EtOH does not interfere with protein secretion.

J Pediatr Orthop, 1981, 1(2), 215 - 8
Case report . The pathogenesis of neurovascular complications following penicillin injection; Meyer S et al.; A 12-year-old patient presented following inadvertent intraarterial injection of benzathine penicillin . Complications manifested as an incomplete cauda equina lesion with ischaemia and necrosis over the buttock in the distribution of the injected artery . Angiography confirmed damage to the superior gluteal artery while histology revealed severe ischaemic damage without evidence of an allergic process . Spasm of the injected vessel with retrograde flow and occlusion by particulate matter can explain the clinical manifestations . The prognosis for these complications is poor and the best approach lies in prevention.

Pharmatherapeutica, 1981, 3(1), 14 - 7
Penetration of penicillin into the cerebrospinal fluid of patients with latent syphilis; Goldmeier D et al.; Eighteen patients with latent syphilis were treated with 360 mg, 720 mg, 1080 mg or 1440 mg intramuscular procaine penicillin daily for 14 days . Penicillin was assayed in serum and cerebrospinal fluid collected 3 hours after the second injection in each patient . Penicillin was present in all sera in concentrations greater than the generally accepted fully treponemacidal level, but none was detected in cerebrospinal fluid from 11 patients . The significance of these results is discussed, particularly with a view to changes in standard treatment regimens for latent syphilis.

J Hyg Epidemiol Microbiol Immunol, 1981, 25(4), 449 - 64
Rheumatic fever situation in Czechoslovakia with special reference to long-term prognosis for rheumatic carditis; Sramek J et al.; In a prospective study (1961-1972) the incidence of rheumatic fever (RF), development of rheumatic heart disease (RHD) and penicillin prophylaxis efficacy were investigated in 300 000 children and 70 000 adults . Only patients whose index attack met the modified Jones' criteria were included; all were enrolled in a prophylaxis programme (i . m . benzathine-penicillin) . The RF incidence decreased from an initial 61.2 attacks per 100 000 in children and 42.9 in adults to below 10 by 1969 and remained low thereafter . In total, 541 children (209 with carditis) and 176 adults (108 with carditis) were followed up for 5.5 years (average) after an index attack . At final examination, no valvular involvement was detected where previous attacks had been without clinical carditis . Patients studied from time of the primary attack with carditis (211) had a very favorable prognosis: only up to 3.5% had developed a moderate to severe heart lesion by the end of the study . However, of 68 adult patients followed up only from the time of recurrence with carditis and often having had a prolonged rheumatic history: 23.5% had a moderate to severe heart lesion and a further 20.6% had died of RHD by the end of the study . Prophylaxis efficacy calculated as a cumulative attack-recurrence rate per 100 patients and over a 5-year interval was 2.72 in protected as against 64.75 in unprotected children (mostly failing to comply with prophylaxis); in adults, the respective values were 1.3 and 24.92 . The prevalence of serious residual RHD may be expected to decrease substantially in the future, starting with the younger age groups.

Arch Psychiatr Nervenkr, 1981, 231(1), 81 - 91
The effects of focal epileptic activity on the somatosensory evoked potentials in the rat; Takahashi H et al.; The cortical somatosensory evoked potential (SEP) of the rat, evoked by contralateral forepaw stimulation, consisted of early (P 1 and N 1) and the late components (P 2 and N 2) . Microelectrode recording yielded evoked unitary responses of short latencies in the range of the early components and responses of longer latencies in the range of P 2 . During the development of focal epilepsy after topical application of penicillin, the late components of SEP were enhanced and the enhanced late negativity corresponded to a surface negative cortical spike . The prominent enlargement of later components was associated with prolonged, often recurrent discharges of long latency unitary responses and with enlarged local field potentials . Early components of SEP remained relatively unaffected and so did unitary responses with short latencies . Epileptic spike-conditioned SEPs in the cuneate nucleus, thalamic sensory relay nucleus and sensory cortex were depressed from 100 ns (cuneate nucleus) to about 300 ms (thalamus and cortex) subsequent to spike discharge . Transmission in the cuneate nucleus was least affected . Thalamic and cortical early components of SEP had similar time courses of recovery, which differed markedly from hat of cortical late components . Our findings suggest that two different neuronal activities generate different components of SEP and are differentially involved in the epileptic activities, which results in the different amplitude recovery following spontaneous epileptic spike discharges.

Acta Physiol Pharmacol Bulg, 1981, 7(2), 43 - 52
Anticonvulsant properties of two new 3,3-diethyl-2,4-pyridinedione derivatives . I . Effects in two experimental models of generalized epilepsy in cats; Belcheva I et al.; The anticonvulsant properties of two N-aminomethyl derivatives of 3,3-diethyl-2,4-pyridinedione (persedon) are studied on two experimental models of generalized (pentylenetetrazol and penicillin) epilepsy in cats . N-aminomethylmorpholine 3,3-diethyl-2,4-pyridinedione (DKMM) applied in doses of 100 mg/ng i . v . in cases of pentylenetetrazol epilepsy leads to a rise in the convulsive thresholds (n, N) by 1.5 and two times, respectively . Administration of the drug in the same dose on developed penicillin epilepsy in cats reveals slight to moderate suppression of the generalized paroxysms, lasting until the 90th-120th min . N-aminomethylpiperazine 3,3-diethyl-2,4-pyridinedione (DKMP), injected in a dose of 100 mg/kg i . v., raises the pentylenetetrazol threshold ("n") 3.5 to 4 times and 8-10 times the N-threshold, approaching the effect of diazepam (10 mg/kg i . v.) . On the background of injected DKMP it is difficult to attain epileptic status, and in the case of developed epileptic status DKMP in a dose of 50 mg/kg suppresses completely the seizure manifestations . Injection of DKMP in the cases of developed penicillin epilepsy results in complete suppression of the generalized paroxysmal activity, lasting until the 100th-120th min.

Biochem J, 1981 Jan 1, 193(1), 83 - 6
The penicillin-binding site in the exocellular DD-carboxypeptidase-transpeptidase of Actinomadura R39; Duez C et al.; Heat denaturation and Pronase degradation of the complex previously formed between benzylpenicillin and the exocellular DD-carboxypeptidase-transpeptidase of Actinomadura R39 yields a heptapeptide H-Leu-Pro-Ala-Ser-Asn-Gly-Val-OH, where the benzylpenicilloyl group is ester-linked to the serine residue . This linkage is very labile and its hydrolysis causes the release of benzylpenicilloate . In contrast, the native benzylpenicilloyl-enzyme complex is very stable (half-life 70 h at 37 degrees C) and its breakdown proceeds via fragmentation of the bound benzylpenicilloyl group {Fuad, Frere, Ghuysen, Duez & Iwatsubo (1976) Biochem . J . 155, 623-629}.

Ann Med Interne (Paris), 1981, 132(5), 328 - 32
{Disseminated actinomycosis presenting with multiple subcutaneous abscesses (author's transl)}; Brion N et al.; The case report describes a patient hospitalized for multiple subcutaneous abscesses who presented a four-year history of recurrent skin lesions and a fifteen-year history of non specific bronchopulmonary infections requiring segmental resection . The diagnosis of actinomycosis, A . israeli species, was established by culture of surgical drainage material from a thoraco-abdominal wall abscess . Muscle and bone involvement of the right thigh was subsequently demonstrated . There was no evidence of pulmonary infection at the time of hospitalization . Treatment with Penicillin G was curative . A review of the literature is presented together with a summary of thirteen reported cases . Although disseminated actinomycosis has become very rare since the introduction of antibiotic therapy, patients share similar features and a common clinical pattern which are highly evocative of the disease . All patients described had preceding pleuropulmonary disease, characteristically chronic . Evolution of cutaneous lesions was subacute or chronic . In all cases, there was significant delay (months to years) between the initial appearance of skin lesions and subsequent diagnosis . In most cases, actinomycosis had not been suspected . Diagnosis was usually established by isolation and identification of the micro-organism in cultures of purulent material obtained from cutaneous lesions . Despite the probability of hematogenous disease dissemination, pleuro-pulmonary foci were only rarely demonstrated . Prolonged antibiotic therapy was curative in all treated cases.

Zh Nevropatol Psikhiatr Im S S Korsakova, 1981, 81(6), 812 - 5
{Increase in the peroxidation of neuron membrane lipids, one of the pathogenetic mechanisms of epileptic activity}; Nikushkin EV et al.; It was found that the development of the epileptic activity focus induced in rats by application of penicillin to the sensomotor cortex surface was accompanied by an activation of lipid peroxidation in the focus area . An analogous effect was also observed in the development of general convulsive seizures induced in rats by injection of bemegride . Preliminary administration of antioxidants (alpha-tocopherol and ionol) to the animals prevented the effect of lipid peroxidation activation and sharply lowered the penicillin-induced epileptic activity . This manifested itself in a diminution of the number and frequency of the seizures and a prolongation of the latent period of their development . The protective action of alpha-tocopherol also manifested itself in a considerable reduction of the animals' mortality on administration of lethal doses of bemegride . It is supposed that lipid peroxidation in the neuronal membranes takes part in the mechanisms of epileptic activity development.

Scott Med J, 1981 Jan, 26(1), 24 - 6
Tetanus prophylaxis and accidental wounds; Morgan WJ et al.; Of 400 consecutive patients who had wounds treated in the Accident Department, 200 remembered receiving either booster injections or a full course of tetanus toxoid in the last 10 years . During this period, 182 patients received their initial toxoid injection in association with treatment of a wound in an accident department . Only 71 (38%) of these patients attended for a full course of injections . From our assessment of the wounds and the patient's anti-tetanus immunity, 79 patients (20%) were considered to be at risk of developing tetanus . By further considering the time interval elapsed between injury and treatment, a 'high risk' group of 13 patients (3%) was recognised . It is recommended that the use of human immunoglobulin should be reserved for the 'high risk' group, and that the remainder of the 'at-risk' patients should receive penicillin prophylaxis only.

Nephron, 1981, 27(6), 313 - 5
Acute interstitial nephritis due to amoxicillin therapy; Appel GB et al.; Acute interstitial nephritis (AIN) has been reported in association with therapy with a number of drugs . We report a patient who developed drug-related AIN while receiving intravenous amoxicillin therapy . The patient developed rash, secondary temperature elevation, and eosinophilia in association with nonoliguric renal failure . Renal biopsy showed evidence for AIN and the renal failure was responsive to corticosteroid therapy . AIN may occur in patients receiving any drug of the penicillin class . This reversible form of acute renal failure must not be overlooked in patients with other forms of renal disease.

Eur Neurol, 1981, 20(3), 188 - 93
A double tracer autoradiographic technique for simultaneous measurement of cerebral blood flow and cerebral metabolism in rats; Mies G et al.; Double tracer autoradiographic measurement of cerebral blood flow and glucose consumption was performed in rats using 131I-iodo-antipyrine and 14C-deoxyglucose, respectively . Local coupling of blood flow and metabolism was studied under different types of anesthesia (barbiturate, halothane), following experimental tumor implantation, and during penicillin seizures or spreading depression . Both coupling and uncoupling of flow and metabolism was observed on the same tissue section, indicating a considerable degree of variability in local coupling mechanisms.

J Antibiot (Tokyo), 1981 Jan, 34(1), 72 - 8
IgE antibodies for penicillins and cephalosporins in rats . I . Characteristics of the IgE antibodies for penicillins and cephalosporins in rats; Shiho O et al.; Rats immunized with sulbenicillin-ovalbumin (SBPC-OvA) in combination with aluminum hydroxide (alum) and thimerosal-killed Bordetella pertussis produced high levels of anti-SBPC antibodies . Anti-SBPC antibodies were first detected on day 8, reaching the maximum titer on day 12 and rapidly declined thereafter . Anti-SBPC sera obtained on day 13 were sulfhydryl-labile and heat-labile . The optimal latent period in the passive cutaneous anaphylaxis (PCA) reaction was 60 approximately 72 hours . These results indicate that anti-SBPC antibodies were IgE antibodies . Sprague-Dawley (SD), Wister and F344 rats were equally productive of anti-SBPC antibodies, while SD rats were more productive of anti-cephaloridine (CER) antibodies than Wister and F344 rats did . In SD rats, the IgE antibodies for penicillin G (PCG), ampicillin (ABPC) and SBPC were more easily produced than the IgE antibodies for CER, cefazolin (CEZ) and cephacetrile (CEC).

Scand J Infect Dis, 1981, 13(1), 78 - 9
Subacute bacterial endocarditis due to Actinobacillus actinomycetemcomitans; Hofstad T et al.; A case of infective endocarditis in a 59-year-old female caused by Actinobacillus actinomycetemcomitans is reported . The organism was recovered from 9 blood cultures . Despite treatment with penicillin and gentamicin the illness led to destruction of the aortic valve.

Am J Vet Res, 1981 Jan, 42(1), 51 - 3
A swine dysentery model for evaluation of drug prophylaxis: efficacy of various drugs in the control of swine dysentery; Raynaud JP et al.; A swine dysentery (SD) model that produces consistent, homogeneous, and severe SD was used in 2 experiments to compare the prophylactic effectiveness of 5 commercially available swine feed additive products . Under the conditions of these studies, carbadox and carbadox + sulfamethazine proved to be the most effective agents in preventing SD during the infection + medication and postmedication periods . Olaquindox was effective in preventing SD in the infection + medication period; however, SD recurrence was high during the postmedication period . Nithiamide and chlortetracycline + sulfamethazine + penicillin were least effective in preventing SD during the infection + medication and postmedication periods.

Int Arch Allergy Appl Immunol, 1981, 64(3), 332 - 7
Chronic pruritic dermatitis in asthmatic monkeys: a subhuman primate analogue of atopic dermatitis?
Patterson R, Harris K.
In a group of adult normal rhesus monkeys and monkeys with IgE-mediated asthma observed over a period of 15 years, 2 of the latter group were found to have chronic, generalized pruritus and dermatitis . The skin lesions were recurrent and located on the flexural surfaces of the forearms leading to the thickened, scaling, lichenified dermatitis in that area in the skin of 1 monkey . The pruritus and skin lesions subsided following therapy with depot methylprednisolone but recurred after this therapy was discontinued . Both animals had recurrent severe cutaneous infections in excoriated lesions following scratching without infections in other organs . The cutaneous infections responded to penicillin therapy but recurred with scratching . No deficiencies in immunoglobulin levels, or lymphocyte responses to phytohemagglutinin were found in these 2 monkeys . The 2 animals differed from normal animals by their high titers of immediate skin reactivity to ascaris antigen, persistent and severe asthmatic responses to ascaris antigen, high IgG antibody levels to ascaris antigen but all of the latter findings were also present in asthmatic monkeys without dermatitis . Cutaneous biopsies of lesions were nonspecific but provided no evidence for other explanations for the dermatitis which appears to be an analogue of human atopic dermatitis.

Neurosci Lett, 1981 Jan 1, 21(1), 93 - 7
The action of glycine on rat epileptic foci; Cherubini E et al.; The action of glycine (Gly) intravenously injected on rat epileptic foci induced by strychnine or penicillin topically applied, was compared with that of GABA . Gly (450 mg/kg i.v.) produced a complete block of the spiking activity . The inhibitory action of GABA (80 mg/kg), in terms of threshold and duration, was stronger than the action of Gly . The same inhibitory effect was also observed if these amino acids were applied topically or intracisternally . These results are consistent with the possibility that Gly has a role in the rat cortical inhibition.

Int Arch Allergy Appl Immunol, 1981, 66(4), 382 - 90
Antibody responses in man after single or repeated treatment with intramuscular ampicillin; Ahlstedt S et al.; Antibody responses to the penicilloyl moiety were recorded in patients treated intramuscularly with ampicillin for respiratory infections . For practical reasons this was performed at two clinics . At each clinic, two commercially available ampicillin preparations were used in a single-blind, randomised study . One of the preparations at each clinic was of high-grade purity and the other was slightly contaminated, according to a radioimmunoassay . There was the same heterogeneity in the patient material between the two clinics . The results showed a slight but significant (p less than 0.001) increase in IgM penicilloyl antibodies in the group of patients treated with the pure penicillin but not in those treated with the contaminated penicillin . When the patients in the two studies were analysed jointly, the increase in IgM antibodies was significantly greater (p less than 0.05) in the group treated with pure penicillin than in that treated with impure penicillin . The difference in antibody formation between the patient groups treated with pure or contamined ampicillin at each clinic was not significant, however . An immunological activity of the impurities suppressing the IgM antibody response is suggested.

Derm Beruf Umwelt, 1981, 29(5), 131 - 4
Dermatologic hazards from hidden contacts with penicillin; Boonk WJ; The unbridled use of penicillin after its discovery by Fleming has resulted in possible hazards to human health due to traces of the drug being present in food and other hidden sources . These hazards may include toxic effects, hypersensitivity reactions and possibly a raising of the frequency and duration of allergy to penicillin.

Med Cutan Ibero Lat Am, 1981, 9(3), 221 - 8
{Critique of the basic elements on which various syphilis treatments are founded}; Collart P et al.; Certain basic treatments of syphilis depend on the following theories: 1) All treponema divide every 30 to 33 hours . Experiments have shown that this idea is only valid during the phase of exponential growth, i.e . it corresponds to the period lyinu between penetration of the germ into the organism and the onset of the initial lesion . One should also be reserved about a whole series of factors which may interfere with the rate of multiplication of treponema . 2) Blood penicillin levels of 0.03 U./ml . would destroy all treponema during cell division . It seems that the efficacy of penicillin mainly depends on levels, at the time of multiplication of the spirochetes . This level of 0.03 U./ml., according to Eagle, should be considered as an average serum concentration, the concentration of maximum efficacy is much higher, about 0.825 U./ml . In any case, it is not possible to obtain with a single dose, equal for all subjects, fixed and certain penicillin levels . For a given quantity injected, serum levels vary from one subject to another and, in the same individual, from one time to another . 3) The epidemiological results do not seem to confirm the optimistic forecasts of certain venereologists who thought that with a standard therapeutic method, it would be possible to eradicate syphilis.

Eur Neurol, 1981, 20(5), 424 - 8
Tabetic lightning pains: high-dosage intravenous penicillin versus carbamazepine therapy; Gimenez-Roldan S et al.; The relief of tabetic lightning pains (LP) by carbamazepine (CBZ) was questioned as in some instances penicillin was given simultaneously . Only 1 out of 6 cases became pain-free on high-dosage intravenous penicillin, while CBZ rapidly abolished LP in those unresponsive to penicillin . Gastric crises were similarly abated by CBZ in 1 case under a placebo-controlled study . Inflammatory and degenerative changes in the posterior nerve root and ganglia may be the underlying pathologic basis that explains these two different responses to penicillin.

Antimicrob Agents Chemother, 1981 Jan, 19(1), 117 - 21
Evaluation of rosaramicin phosphate in treatment of experimental syphilis in rabbits; Baughn RE et al.; The in vivo activity of rosaramicin phosphate in disseminated and localized Treponema pallidum infections in rabbits was compared with that of penicillin G benzathine . Rabbits were injected either intradermally or intravenously to establish infection . Groups of four animals each then received either two weekly injections of 200,000 U of penicillin G benzathine, injections of 12.5 or 25 mg of rosaramicin per kg of body weight twice a day for 10 days, or no antibiotic therapy . Treatment of the intradermal and intravenous infections was initiated on days 7 and 14 postinfection, respectively . With both infection models, striking differences were noted between the untreated control rabbits and the three groups receiving treatment; no discernible differences, however, were detected among any of the treated groups . Rabbits that had been infected intravenously did not develop disseminated lesions or orchitis after treatment, and chancres produced by intradermal infection regressed and healed rapidly after the initiation of therapy . Continued increases in treponemal and nontreponemal antibody titers posttreatment did not occur in any of the treated rabbits . Infectivity studies also suggested that the lymph nodes and testes of treated animals were free from infectious organisms . Overall, at the dosage regimens employed, both rosaramicin and penicillin G benzathine appeared to effect complete control of the experimental disease.

Med Hypotheses, 1981 Jan, 7(1), 43 - 9
Malariotherapy and cancer; Greentree LB; Malariotherapy merits a clinical trial as an adjuvant to conventional cancer therapy . This particular modality of treatment is a most potent stimulus of macrophage activity . These scavenger cells are widely believed to be an essential arm in the host's immune defenses against malignant disease, both as regards the processing of antigens and as killers of tumor cells . Significant too, malariotherapy, as formerly used to effectively treat some 16,000 patients with paretic neurosyphilis in one institution alone, before the advent of the penicillin age, has proved to be a particularly safe modality of treatment.

Acta Derm Venereol Suppl (Stockh), 1981, 96, 1 - 14
The profile of neurosyphilis in Denmark A clinical and serological study of all patients in Denmark with neurosyphilis disclosed in the years 1971-1979 incl . by Wassermann reaction (CWRM) in the cerebrospinal fluid; Perdrup A et al.; 55 cases of neurosyphilis, probably all that has been disclosed in Denmark in the nine year period 1971 to 1979 are submitted . 55 case histories and 10 tables illustrate the variegated clinical features and the differential diagnoses, the serological data, and CSF findings, the treatment and its results . As the symptomatology of the series fits well into the classification of neurosyphilis of the past our cases are classified accordingly in five clinical groups with seven subgroups . Penicillin treatment was applied to all the patients in current dosages and proved beneficial in most patients with regard to clinical symptoms and to laboratory parameters . The outcome here registered seem, however, to be related more to the character of the disease than to the types or amounts of penicillin . Eleven of the patients had a history of previous positive serology and two of them had been treated with penicillin for early syphilis but their neurosyphilis was evidently due to an untreated reinfection . Ten of the patients had aortitis.

Rev Stomatol Chir Maxillofac, 1981, 82(6), 366 - 71
{Gas gangrene of dental origin . Report on four cases (author's transl)}; Baron D et al.; Four patients developed diffuse cervicofacial cellulitis following an acute circumscribed infection of dental origin . Necrosis of skin, subcutaneous and muscle layers was associated with a severe generalised toxic infective syndrome, producing a clinical picture and following a course identical with that observed in gas gangrene of the limbs . Anaerobic germs, normally present in the buccodental region, were at the origin of the affection in all four cases, chronic dental lesions providing favourable anaerobic conditions for an increase in their virulence . Three factors appear to be of importance for the development of gas gangrene from dental abscesses: insufficient or lack of suitable surgical treatment, the use of antibiotics not active against anaerobic germs, treatment with corticoids or anti-inflammatory drugs . Once gas gangrene has developed, possible intramediastinal spread should be investigated . Treatment is essentially surgical (with excision of necrotic tissue and wide drainage), plus penicillin therapy and hyperbaric oxygen . The prophylaxis of these gas gangrene lesions is discussed.

Z Exp Chir, 1981, 14(4), 166 - 74
{Organ cultures from isolated pancreatic islets of rats and their transplantation into streptozotocin-diabetic rats}; Kojima Y et al.; Islets of Langerhans were isolated from the adult wistar rat by means of the collagenase method and cultivated in an incubator at a temperature of 37 degree Celsius and with a mixture of 95% air and 5% CO2 . With that each two of the islets were put into every drill hole of multi-dish trays . 1 ml Eagle medium modified by Dulbecco with admixtures of 20% foetal calf serum, 100 microgram/ml Streptomycin and 100 u/ml Penicillin G was the nutrient medium . This medium was exchanged every third day and the released insulin quantity was measured by a radio immunologic test (Phadebas insulin test) . Results: 1 . The insulin quantity in the nutrient medium runs to 1097 to 1434 microu/ml two islets if a change took place every third day during an 80 days duration of the culture . 2 . The cultivated islets had a demonstrable reactivity of the insulin secretion to glucose and glucagon . 3 . Diabetic rats with transplants of nearly 400 cultivated islets recover from diabetic state within one week after transplantation and keep healthy for 8 weeks.

Physiologie, 1981, 18(2), 99 - 104
A comparative study of the immunogenicity of some penicillins and of their cross reactions; Cirstea M et al.; The immunogenicity of four penicillin preparations was comparatively investigated by titration of penicilloyl (PO) specific hemagglutinating antibodies found in sera of rabbits inoculated with equimolecular amounts of these penicillins incorporated in Freund incomplete adjuvant . Benzylpenicillin (BP) was shown to be endowed with the highest immunogenicity, while oxacillin (OX), ampicillin (AM) and Amoxil (AX) were found significantly less immunogenic . By examining comparatively the titers of hemagglutination reactions given by the sera of each animal with erythrocytes coated with the penicillin used for its immunization as well as with the other penicillins investigated, important cross immunological reactions were found in all of the cases . Interestingly, the cross reactions produced by AM- and AX-specific antisera with heterologous penicillins were apparently higher than the reactions obtained with the homologous penicillin . No significant differences were found concerning the ability of the four penicillins to form PO conjugates with BGG . Thus, the differences in immunogenicity exhibited by the four penicillin preparations may not be explained in this way.

J Int Med Res, 1981, 9(3), 189 - 90
Absorption of penicillin V from mixture formulations . Comparison of potassium and benzathine salts; Heikinheimo M et al.; The absorption rate and serum level curves of two commercial phenoxymethylpenicillin mixture preparations were compared in adult volunteers . Both the potassium salt (Primcillin) and the benzathine salt (V-Pen ped forte) of V-penicillin were rapidly absorbed and the mean peak serum levels were obtained with both preparations within the first hour after single dose administration . The mean peak level obtained with the potassium salt was several-fold higher (p less than 0.001) and was also reached within a shorter time than that of the benzathine preparation . These results confirm the earlier evidence, obtained with other formulae, for the superior bioavailability of the potassium salt of V-penicillin as compared to most other derivatives used in V-penicillin mixtures.

Zh Nevropatol Psikhiatr Im S S Korsakova, 1981, 81(6), 801 - 9
{Use of nicotinamide and pyridoxal-5-phosphate to treat experimental epilepsy}; Kryzhanovskii GN et al.; In experiments on cats it was shown that nicotinamide injected intravenously in a dose of 300 to 500 mg per kg body weight depressed singular epileptic foci and groups of foci with synchronized activity induced in the animals' brain cortex by application of strychnine (0.1 ml of 3% solution) . The vitamin was also effective, though to a lesser degree, in depressing foci induced by application of penicillin (2% solution) . Pyridoxal-5-phosphate (Pyr-5-Ph) injected intravenously in a dose of 10 mg/kg depressed singular foci and groups of foci with synchronized activity induced by application of 2% solution of penicillin, but was less effective in depressing strychnine-induced foci . Combined application of both drugs even in lower doses (nicotinamide, 200 mg/kg; Pyr-5-Ph, 5 mg/kg) resulted in depression of groups of epileptic foci induced by combined application of strychnine and penicillin . Mechanisms of the effects discovered are discussed . A question on possible use of combined nicotinamide and pyridoxal-5-phosphate in the treatment of epilepsy is raised.

Dermatologica, 1981, 163(2), 151 - 9
Skin testing in chronic urticaria; Boonk WJ et al.; In 164 patients with chronic recurrent urticaria, the value of skin tests was investigated, Patch tests carried out with the standard series of the International Contact Dermatitis Research Group and with a series of penicillins revealed positive reactions in 22 (35/162) and 6.9% (11/158), respectively . IN 21.5% (33/152) positive intracutaneous tests to cilligen and/or penicillin G were observed . 35% (51!147) of the patients had one or more positive intracutaneous tests with inhalants . Scratch tests with food allergens showed positive reactions in 12.5% (12/95) . There was no difference in results between patients with idiopathic urticaria or angio-oedema and those with physical urticaria . The value of these findings is discussed . Most of the patients with penicillin allergy, were recommended to be on a diet free from milk and milk products . In 50% this was successful.

J Int Med Res, 1981, 9(4), 268 - 73
Clinical evaluation of piperacillin in bronchopulmonary infection; Marlin GE et al.; Piperacillin sodium, a new semi-synthetic penicillin, was administered to eleven patients with acute bronchial infection and to fourteen patients with pneumonia . Piperacillin dosage was either 8 g/day (twenty-one patients) or 16 g/day (four patients) intravenously for periods of between 5 and 15 days . Clinical assessment was determined by diminution of sputum purulence, eradication of pathogen from sputum, clinical and radiological progress . There was a beneficial response in all but six patients, two of whom had severe chronic infective bronchial disease and four had underlying pulmonary malignancy . The low toxicity of piperacillin was confirmed, although one patient with chronic renal failure had a significant decline in renal function . Dosage should be reduced in patients with renal impairment.

Physiol Bohemoslov, 1981, 30(1), 63 - 71
Effect of phenobarbital on cortical epileptogenic foci in the rat; Mares P et al.; The activity of epileptogenic foci was studied in acute experiments on adult male rats without general anaesthesia; the animals first received an intraperitoneal injection of phenobarbital {40 mg/kg} and 30 min later a cortical focus was induced by the local application of penicillin . These foci, which were induced in the sensorimotor area, had a lower discharge frequency than in the controls and the formation of projected discharges was delayed . In two symmetrical and asymmetrical cortical foci, activity was synchronized significantly more slowly after phenobarbital than in the controls . The cortical interhemispheric response was not influenced by the administered dose of phenobarbital . In these experiments, phenobarbital had an anti-epileptic effect both on the primary focus and on the spread of epileptic activity from this focus.

Biull Eksp Biol Med, 1981, 91(1), 42 - 5
{Further study of the antiepileptic properties of nicotinamide}; Kryzhanovskii GN et al.; Acute experiments on cats have shown that nicotinamide (100-500 mg/kg) injected intravenously suppresses the epileptic activity in solitary foci produced in the cortex by application for several seconds of a 0.5% solution of penicillin as well as in the complex of foci produced by application of a 0.1--3% solution of strychnine to various cortical zones . Nicotinamide (500-100 mg/kg) does not affect the character of the epileptic activity of foci created by application of 1% penicillin to the cerebral cortex or on the generalized epileptic activity produced by application of concentrated solutions of strychnine or penicillin . In an epileptic focus produced by application of 5-10% acetylcholine and 0.5% proserine, injection of nicotinamide leads at first to the disappearance of after-effect discharge and then of spike potential . It is concluded that nicotinamide has an antiepileptic activity.

J Bacteriol, 1981 Jan, 145(1), 333 - 40
Evidence for involvement of penicillin-binding protein 3 in murein synthesis during septation but not during cell elongation; Botta GA et al.; Furazlocillin (1 microgram/ml) and piperacillin (5 microgram/ml) bound specifically to penicillin-binding protein 3 (PBP-3) and not to the other major PBPs in intact Escherichia coli cells . The effect of this specific binding to PBP-3 on murein synthesis of elongating and synchronously septating cells was investigated in two thermosensitive division mutants, E . coli BUG6 and E . coli JE10730, the latter possessing a thermolabile PBP-3 . Synchronous cell division was induced by shifting the cultures from the nonpermissive temperature (42 degrees C) to 30 degrees C . Both {14C}diaminopimelic acid incorporation into murein of intact cells and {14C}N-acetylglucosamine incorporation into murein of cells permeabilized with ether was inhibited by an average of 42% in septating cells . In filaments growing at the nonpermissive temperature, we detected no inhibition and, frequently, a 10 to 15% stimulation of murein synthesis . The two drugs, at concentrations used in the above experiments, bound exclusively to PBP-3 both in elongating and septating intact cells and in ether-treated cells . These results support the hypothesis that PBP-3 activity is exclusively required for septal murein synthesis.

Acta Physiol Scand, 1981, 113(3), 355 - 62
Monosynaptic transmission during epileptiform activity induced by penicillin in hippocampal slices in vitro; Gjerstad L et al.; Synaptic transmission was studied in the CA1 region of transverse hippocampal slices in vitro before and after the addition of the epileptogenic agent sodium benzyl penicillin . The presynaptic fibre volley and the field potential associated with the intracellular EPSP, 'field EPSP', were recorded from the layer of the activated synapses . Addition of penicillin did not change either response . The rising phase of the intracellularly recorded EPSP did not change . However, the peak amplitude and, particularly, the duration of the EPSP both increased . The prolongation of the EPSP may be of importance for the triggering of epileptiform bursts.

Acta Physiol Acad Sci Hung, 1981, 57(2), 191 - 6
Effects of drugs influencing the cAMP level on hippocampal seizure activity; Ludvig N et al.; Changes of hippocampal EEF seizure activity elicited by electrical stimulation of the hippocampus or penicillin injection into the hippocampus were investigated under the effect of locally applied drugs influencing the cAMP level in the brain . It was observed that some drugs which elevate the cAMP level such as papaverine, histamine +K+ and dibutyryl cAMP elevated the electric seizure threshold while in penicillin-induced epilepsy they reduced the occurrence of ictal activity and the interictal spike frequency . These drugs when applied before penicillin prolonged the time necessary for development of the epileptic focus . The effect of imidazole was the opposite in every respect . On the basis of these data the possible role of cAMP in the pathomechanism of epilepsy is discussed.

J Antibiot (Tokyo), 1981 Jan, 34(1), 79 - 83
IgE antibodies for penicillins and cephalosporins in rats . II . Antigenic specificity of rat anti-penicillin-OvA IgE sera; Shiho O et al.; Sprague Dawley (SD) rats were immunized with various penicillin-ovalbumin (OvA) in combination with aluminum hydroxide (alum) and thimerosal-killed Bordetella pertussis for the purpose of obtaining rat anti-penicillin IgE sera . In the rat 60-hour passive cutaneous anaphylaxis (PCA) reaction and the hapten inhibition test, a weak cross reaction between penicillin G (PCG) and ampicillin (ABPC) was observed, but not cross reaction was observed between sulbenicillin (SBPC) and other penicillins . Rat anti-6-formamidopenicillanic acid (FPC) IgE serum reacted with PCG-bovine gamma globulin (BGG), ABPC-BGG and SBPC-BGG, but FPC-BGG did not react with rat anti-PCG, anti-ABPC and anti-SBPR IgE sera and the PCA reaction between anti-FPC IgE sera and FPC-BGG was inhibited by FPC, PCG, ABPC and SBPC . These results indicate that the antigenic active sites of PCG, ABPC and SBPC are limited to the acyl side chain moiety of penicillins, while the antigenic active site of FPC is confined to the penicilloyl moiety of the penicillin.

Int Arch Allergy Appl Immunol, 1981, 64(2), 210 - 6
Induction of immunological tolerance to the penicilloyl antigenic determinant . III . Suppression of benzylpenicilloyl-specific IgE antibody formation by cleavable penicilloylated dextran; Nakagawa T et al.; The suppressive effect of cleavable penicilloylated dextran (BPO-DEX), whose directly bound penicilloyl groups undergo hydrolytic cleavage within 3 days under physiological conditions, on murine IgE antibody formation against the benzylpenicilloyl (BPO) determinant was investigated in BALB/c and C3H mice . Intraperitoneal administration of BPO-DEX during either primary or secondary IgE responses to BPO ascaris produced a reversible suppression of BPO-specific IgE, while not affecting carrier-specific IgE antibody formation . Suppression of longer duration, at least 10 weeks, was achieved, however, by repeated administrations of BPO-DEX . BPO-DEX itself did not generate detectable BPO-specific IgE antibodies . These results suggest that BPO-DEX might be one of the promising tolerogens in the prevention of penicillin allergy.

Wien Med Wochenschr, 1981, 131(8), 213 - 5
{Single dose treatment of primary syphilis with Benzathine penicillin (author's transl)}; Pehamberger H; Out of 40 male patients with primary syphilis diagnosed microscopically by dark field preparations and by serological tests 20 patients were treated with a single intramuscular injection of 4.8 millions I . U . Benzathine penicillin and 20 patients with a daily intramuscular injection of 1 million I . U . Clemizol penicillin over a period of 21 days . In all patients success of treatment was verified by complete remission of the clinical symptoms and by serological tests over a period of 2 years . Single dose treatment with Benzathine penicillin represents a simple and reliable method of treatment of primary syphilis.

J Biol Chem, 1980 Dec 10, 255(23), 11173 - 80
Purification and properties of penicillin-binding proteins 5 and 6 from Escherichia coli membranes; Amanuma H et al.; Penicillin-binding proteins (PBPs) 5 and 6 in the cytoplasmic membranes of Escherichia coli K12, which had previously been co-purified as a penicillin-sensitive D-alanine carboxypeptidase IA (Tamura, T., Imae, Y., and Strominger, J . L . (1976) J . Biol . Chem . 251, 414-423), were each purified to protein homogeneity . Purification involved selective solubilization of PBPs 1a, 5, and 6 from membranes by Triton X-100 at low ionic strength, covalent penicillin affinity chromatography, and CM-cellulose column chromatography . Purified PBP 5 and PBP 6 each catalyzed a D-alanine carboxypeptidase I activity using various natural and synthetic substrates including linear uncross-linked peptidoglycan . PBP 5 showed 3- to 4-fold higher specific activities toward these substrates than PBP 6 . Both PBPs also catalyzed a model transpeptidase activity using glycine as a transpeptidation acceptor, and showed similar pH profiles and MgCl2 sensitivities for their D-alanine carboxypeptidase I activities . Both PBPs bound a stoichiometric amount of {14C}penicillin G at saturation . Peptide mapping by sodium dodecyl sulfate-polyacrylamide gel electrophoresis after partial proteolysis by proteases and cyanogen bromide demonstrated that these PBPs are distinct polypeptides.

Biochim Biophys Acta, 1980 Dec 4, 616(2), 283 - 9
Substrate specificity of penicillin amidase from E . coli; Margolin AL et al.; 1 . The kinetic parameters of 12 substrates of penicillin amidase (penicillin amidohydrolase, EC 3.5.1.11) from E . coli have been determined . Most of the penicillin amidase amide substrates containing a phenylacetyl group in the acyl moiety have been shown to have similar catalytic constants of 50 s-1 . Substitution of the phenylacetyl group b 2-thienylacetyl group (cephalothin, cephaloridine) having a similar structure leads to a slight decrease in kcat . 2 . Nonspecific penicillin amidase substrates, which contain a free amino group in their acyl moiety, are characterized by a strong dependence of kcat, on the structure of the leaving group with Km being constant . To investigate the free amino group influence on the reaction kinetics, pH-dependences of kcat/Km of enzymatic hydrolysis of phenylacetic and D-(-)-alpha-aminophenylacetic acid p-nitroanilides have been studied . It has been shown that enzyme binds the deprotonated form of the substrate only . 3 . Under thermodynamically favourable conditions for the synthesis of beta-lactam antibiotics (at low pH), a concentration of the deprotonated substrate form is very low, and the reaction proceeds in the bimolecular regime . The value of the second-order rate constant for the substrate having a free amino group is small even at pH 7.5, and sharply decreases as does the pH . Hence, despite the favourable thermodynamic conditions for the production of all beta-lactam antibiotics, low reaction rate is the basic hindrance for enzymatic synthesis of penicillins and cephalosporins having a free amino group in the acyl moiety.

Biull Eksp Biol Med, 1980 Dec, 90(12), 696 - 8
{Anticonvulsive effect of the antioxidant ionol}; Nikushkin EV et al.; The influence of the antioxidant ionol on the intensity of epileptic activity in rats has been studied . The epileptic activity was induced by penicillin application to the sensorimotor cortex . It was established that preliminary injection to rats of ionol abolished the effect of lipoperoxidation in the focus of hyperactivity and decreased by a factor of 10(1) the number of seizures recorded on the electrocorticogram in the course of the focus existence.

Arch Intern Med, 1980 Dec, 140(12), 1668 - 70
In vivo inactivation of gentamicin by carbenicillin and ticarcillin; Kradjan WA et al.; Inactivation of aminoglycosides by carbenicillin and ticarcillin is a well-recognized in vitro phenomenon . Isolated case reports of in vivo inactivation of gentamicin by either carbenicillin or ticarcillin exist . We report a case of nearly complete in vivo inactivation of gentamicin by both ticarcillin and carbenicillin in the same patient . In the absence of either of the penicillin derivatives, the patient demonstrated predictable plasma concentrations and elimination characteristics of both gentamicin and tobramycin . As in previous reports, the interaction was intensified by high-dose carbenicillin-ticarcillin therapy in the face of underlying renal impairment . When using ticarcillin or carbenicillin along with gentamicin in renally impaired patients, special attention must be paid to both the gentamicin and carbenicillin-ticarcillin doses used and the plasma concentrations obtained.

Br J Vener Dis, 1980 Dec, 56(6), 368 - 71
Tabes dorsalis progressing to general paresis after 20 years despite routine penicillin therapy; Giles AJ; A man with a history of treatment for early syphilis presented with tabes dorsalis . Despite receiving a course of penicillin accepted as adequate by the World Health Organisation the illness progressed to tabo-paresis after 20 years . Reinfection cannot be excluded.

Br J Vener Dis, 1980 Dec, 56(6), 355 - 62
Kinetic study of serum penicillin concentrations after single doses of benzathine and benethamine penicillins in young and old people; Collart P et al.; In a comparative kinetic study of the serum concentrations of two penicillin complexes--medium-long-acting (benethamine penicillin) and long-acting (benzathine bipenicillin)--after a single injection in young adults and elderly people, the following results were confirmed statistically: (a) age was a major factor in the variations in serum penicillin concentrations and in their persistence in the serum; (b) the penicillin was absorbed faster in young than in elderly subjects even when a long-acting complex was used; (c) serum concentrations below the level regarded as lethal for treponemes appeared much earlier and more frequently in young than in old people; and (d) the bioequivalence between penicillin preparations could not be estimated solely for the number of units of the agent used but from the bioavailability of the chosen formulation . Thus a uniform and standard penicillin dosage allowing no safety margin may help in the superficial healing of a syphilitic chancre or the resolution of a roseola but it will certainly be insufficient to kill Treponema pallidum . It seems essential therefore to provide an antibiotic cover at high dosage over a long period of time.

Br J Ophthalmol, 1980 Dec, 64(12), 892 - 5
Branhamella keratitis; Wilhelmus KR et al.; Three cases of suppurative keratitis caused by Branhamella catarrhalis are described . Each presented as a localised stromal infiltrate in a previously scarred cornea . The condition responded to penicillin G and to gentamicin treatment.

Epilepsia, 1980 Dec, 21(6), 587 - 96
Effects of artificially induced increases in intracranial pressure on epileptic activity; Caldarelli M et al.; The effects of induced increases in intracranial pressure (ICP) on epileptic activity following topical application of penicillin on the cerebral cortex or dorsal hippocampus were investigated in rabbits . Enhanced basal epileptic activity was brought about by the rise in the ICP, obtained with repeated lumbar infusions of saline . In some animals, this increased activity was already evident during the test, while in others it became obvious only at the end of the procedure . When induced, the increased epileptic activity could persist even after the ICP had returned to within normal limits.

Epilepsia, 1980 Dec, 21(6), 571 - 85
Changes in the number, size, and shape of synaptic vesicles in an experimental, projected cortical epileptic focus in the rat; Fischer J et al.; A projected epileptic focus was induced in the brains of experimental rats by applying penicillin G sodium to the contralateral hemisphere . Synapses of type I (after Gray) in the second cortical layer of the mirror area were analyzed morphometrically in the electron microscope 30 min after application of the epileptogenic drug . The number of agranular synaptic vesicles was counted per 0.01 micron2 over the active zone of the presynaptic membrane in an area 0.1 micron wide adjacent to the active zone and in an area of the same width 0.1 micron distant from the active zone . A statistically significant increase in the number of synaptic vesicles was found in the experimental animals as compared with the controls . The number of synaptic vesicles per 0.01 micron2 area was evaluated along the inactive presynaptic membrane, both in the area adjacent to the active zone of the presynaptic membrane and in other areas at successively greater distances from the active zone . The counts in some of these latter areas were statistically significantly higher in the experimental animals . The size and shape of synaptic vesicles were evaluated in three zones, each 0.1 micron wide, parallel to the membrane of the synaptic cleft . Zone I was directly adjacent to the membrane of the synaptic cleft; zone II was 0.1 micron distant; and zone III 0.1 micron distant from the membrane . The results show that the synaptic vesicles of both the experimental and control animals are significantly smaller in zone I than in the more distant zones . This trend is more marked in the controls than in the experimental animals . Histograms of vesical areas of zones II and III in the controls point to two populations of vesicles . The volumes of vesicles are approximately 10% greater in zone I of experimental animals than in the controls . The elongation of the vesicles in the three zones does not differ statistically either in controls or in experimental animals . Experimental animals, however, have statistically more rounded vesicles than the controls . Assuming that the synpatic vesicles contain the transmitters, our results might contribute to a better understanding of the increased excitability of the epileptic focus area.

Poult Sci, 1980 Dec, 59(12), 2754 - 9
Growth depression of chicks fed a crude rye extract containing pectic substances; Day RM et al.; A crude extract with a high proportion of pectic substances was prepared from rye . This was fed to chicks in two studies to determine if rye pectic substances are responsible for the growth depression of chicks fed rye . The growth of chicks was significantly (P greater than .01) depressed when fed a diet containing this extract . Addition of penicillin to the diet improved the growth of chicks . Increasing the concentration of the extract in the diet produced an incremental depression in weight gain . The intestines of chicks fed this extract contained large quantities of gas that were reduced by penicillin supplementation . These results suggest that rye pectic substances may be responsible for the growth depression of chicks fed rye.

Acta Pathol Microbiol Scand {B}, 1980 Dec, 88(6), 317 - 22
Resistance types in Escherichia coli . II . Transfer of ampicillin resistance; Sogaard P; The ability to transfer resistance traits was investigated in 49 E . coli strains isolated from clinical specimens . The strains were divided into the three groups according to sensitivity to penicillin derivatives . Group 1 contained 8 ampicillin-carbenicillin sensitive (A-s/Ca-s) strains, group 2 contained 16 ampicillin resistent-carbenicillin sensitive (A-r/Ca-s) strains and group 3 contained 25 ampicillin-carbenicillin resistant strains . In group 3, 17 strains could transfer A-resistance (range of transfer frequency was 10(0.0) to 10(-7.5) . The 16 strains in group 2 that did not transfer A-resistance more often than mutants arose from the recipient (10(-8.8) . The mutants of the recipient selected on A-plates were A-r/Ca-s/cephalothin-resistant, exactly as the strains in group 2 . The A-resistance in group 3 was probably based on plasmids, and that of group 2 was based on mobilizable plasmids and/or chromosomal resistance . The frequencies of transfer of sulphonamide-, tetracycline- and streptomycin resistance of the strains in groups 1 and 2 did transfer, were in the same range as the frequencies of transfer in group 3.

Antibiotiki, 1980 Dec, 25(12), 914 - 21
{Penicillin amidase from E . coli . The determination of the ionization constants of the Michaelis complex ionogenic groups in the enzymatic deacylation reactions of the phenacetyl derivatives of phenylglycine and 7-aminodesacetoxychephalosporanic acid}; Nys PS et al.; pH and temperature relationships of the maximum rate of the reaction of enzymatic hydrolysis of phenacetyl derivatives of phenylglycine (PPG) and 7-aminodesacetoxycephalosporanic acid (7-PADCA) catalysed by immobilized penicillinamidase (IPA) (penicillinamidohydrolase CE 3.5.1.11) were studied . A possibility of applying for the routine methods used in determination of electrochemical properties of ampholites for estimation of the ionization constants of the functional groups of both the enzyme and the enzyme-substrate complex was shown . The applicability of various methods for estimation of the ionization constants is discussed and the ways of determination of the ionization constants and the means of quantitative description of the bell-like pH relationship of the kinetic and equilibrium parameters of the biocatalytic reaction are presented . The equations described were used in analysis of the pH relationship of the immobilized penicillinamidase enzymatic activity in the reactions of 7-PADCA and L-PPG hydrolysis . The estimated ionization constants of the ionogenic groups of the Michaelis complexes were used in quantitative description of the electrochemical state of the complexes at wide pH ranges . The acid properties of the PA and IPA complexes with a number of substrates, such as benzylpenicillin, 7-PADCA, L-PPG and PANAB were compared . The effect of the immobilization procedure, electrochemical properties of the substrates and the reaction products on the electrochemical state of the Michaelis complexes is discussed.

Am J Obstet Gynecol, 1980 Dec 1, 138(7 Pt 2), 1088 - 90
Problems and approaches in the surveillance and control of sexually transmitted agents associated with pelvic inflammatory disease in Africa; Nsanze H; The problems in surveillance of sexually transmitted disease (STD) in Africa are numerous and are based mainly on socioeconomic barriers . Policies for controlling STD are either inadequate or nonexistent in many African countries . Gonococci are becoming increasingly insusceptible to penicillin and other drugs because of widespread use of inadequate therapy . Gonorrhea is recognized as the major pathogen of pelvic inflammatory disease in Africa . The magnitude of the PID problem is so great that current efforts are directed at case treatment rather than surveillance and control . The formation of the African Union Against Venereal Diseases and Treponematoses is an important step, and its suggestions and resolutions form a sound basis for improved STD control in Africa.

J Bacteriol, 1980 Dec, 144(3), 1190 - 2
Deletion of the penicillin-binding protein 5 gene of Escherichia coli; Spratt BG; A strain of Escherichia coli that has a deletion of the entire dacA gene has been constructed . The complete lack of penicillin-binding protein 5 in this strain establishes that the activity of this protein is not essential for the growth of E . coli.

Ann Thorac Surg, 1980 Dec, 30(6), 550 - 7
Aortocoronary bypass with homologous saphenous vein: long-term results; Bical O et al.; Between February 1973, and February, 1979, 27 homologous saphenous veins were used in 20 patients (mean age, 54 years) . Seven fresh grafts were used less than 24 hours after severance . They were kept at a temperature of 4 degrees C in saline solution containing penicillin . Twenty cryopreserved grafts were used within a period of eight days to 2 months from severance . They were preserved in glycerol at a temperature of -40 degrees C . One patient (5%) died postoperatively . A perioperative myocardial infarction developed in 3 patients (15%) . Average follow-up is 27 months . No late mortality was registered . Fifteen patients are free from symptoms, and 3 patients have residual angina with exercise . Control angiograms were made in 13 patients 1 to 68 months after operation; 17 homografts were seen . Early occlusion of 1 graft and late occlusion of 8 grafts were registered . The poor late patency rate does not seem to be related to either histocompatibility or technical conditions . Conversely, microscopic examination of several cryopreserved grafts showed that the mode of preservation resulted in deterioration of intimal and medial tissues of the vein . Therefore, it appears to us that the use of homologous saphenous veins should be avoided for coronary bypass.

Allergy, 1980 Dec, 35(8), 657 - 64
Antigenicity of semisynthetic penicillin preparations to evoke systemic anaphylactic reactions in animal models; Koizumi K et al.; Four commercially available penicillin preparations (benzylpenicillin, aminobenzylpenicillin, carbenicillin and sulbenicillin) and two kinds of the new semisynthetic penicillin preparations (mezlocillin and piperacillin) evoked systemic anaphylactic reactions in guinea pigs immunized with one of the following penicillin-Ascaris extract (As) conjugates in aluminum hydroxide gel (alum), i.e., benzylpenicilloyl (BPO)-As, aminobenzylpenicilloyl (ABPO)-As, carbenicilloyl (CBPO)-As, sulbenicilloyl (SBPO)-As, mezlocillin-As conjugate (MEZ-As) and piperacillin-As conjugate (PIP-As) . The tracheal chains prepared from the tracheas of the guinea pigs immunized with BPO-As, MEZ-As, or PIP-As revealed anaphylactic contractions in vitro on addition of benzylpenicillin, mezlocillin, or piperacillin preparations . These results indicated that the semisynthetic penicillin preparations as well as benzylpenicillin preparation have enough antigenicity to evoke systemic anaphylactic reactions in guinea pigs immunized with penicillin-As conjugate . Such guinea pigs seem to be suitable animals for investigations of penicillin allergy.

Ann Neurol, 1980 Dec, 8(6), 564 - 73
Correlation of intracellular redox states and pH with blood flow in primary and secondary seizure foci; Tenny RT et al.; Epileptogenic foci were created by topical application of penicillin to the cerebral cortex in 40 paralyzed and artificially ventilated cats receiving halothane anesthesia . The animals were divided into two equal groups to compare primary and secondary foci . The following variables were recorded at normocapnia, hypocapnia, and hypercapnia prior to and during seizure activity: cerebral blood flow (CBF), determined by clearance of xenon 133; cortical redox states, measured by the fluorescence of reduced pyridine nucleotides (PN); brain pH, measured using a lipid-soluble, pH-sensitive fluorescent indicator; and electroencephalograms (EEG) . Mean arterial blood pressure, arterial pH, arterial carbon dioxide tension (PaCO2), and arterial oxygen tension (PaO2) were monitored in each animal . All animals had a normal PaCO2-CBF response prior to the creation of a seizure focus, assuring the presence of autoregulation and normal metabolic function . CBF increased equally with seizures in the primary and secondary hemispheres . The relative increase was related to the PaCO2 but approximated 68% at normocapnia . There was an alteration in the PaCO2-CBF response with seizures, but the ability of the cerebral vasculature to constrict and dilate with hypocapnia and hypercapnia was retained . There was no significant difference in the reduced PN signal with variations in PaCO2 prior to seizures, but there was an apparent 10 to 15% fall with seizures . The "equivalent" intracellular pH fell to 6.94 at normocapnia in the primary focus but remained essentially unchanged from the control value of 7.10 in the secondary focus . These differences in pH were consistent with the greater degree of seizure activity observed in the primary focus . We conclude that a nonhypoxic acidosis existed in the primary focus and that changes in CBF were not related to it because the CBF changed equally in both hemispheres.

J Bacteriol, 1980 Dec, 144(3), 869 - 76
Inhibition and repression of homocitrate synthase by lysine in Penicillium chrysogenum; Luengo JM et al.; Homocitrate synthase in the first enzyme of the lysine biosynthetic pathway . It is feedback regulated by L-lysine . Lysine decreases the biosynthesis of penicillin (determined by the incorporation of {14C}valine into penicillin) by inhibiting and repressing homocitrate synthase, thereby depriving the cell of alpha-aminoadipic acid, a precursor of penicillin . Lysine feedback inhibited in vivo the biosynthesis and excretion of homocitrate by a lysine auxotroph, L2, blocked in the lysine pathway after homocitrate . Neither penicillin nor 6-aminopenicillanic acid exerted any effect at the homocitrate synthase level . The molecular mechanism of lysine feedback regulation in Penicillium chrysogenum involved both inhibition of homocitrate synthase activity and repression of its synthesis . In vitro studies indicated that L-lysine feedback inhibits and represses homocitrate synthase both in low- and high-penicillin-producing strains . Inhibition of homocitrate synthase activity by lysine was observed in cells in which protein synthesis was arrested with cycloheximide . Maximum homocitrate synthase activity in cultures of P . chrysogenum AS-P-78 was found at 48 h, coinciding with the phase of high rate of penicillin biosynthesis.

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