Penicillin

Int Arch Allergy Appl Immunol, 1976, 52(1-4), 248 - 56
Penicillin allergy studies by a modified red-cell-linked antigen-antiblobulin reaction; Kraft D et al.; A red-cell-linked antigen-radioactive antiglobulin reaction (RCLA AR) is reported which may be combined with the conventional red-cell-linked antigen-antiglobulin reaction (RCLAAR) to measure antibodies of all five immunoglobulin calsses against the same determinant at the same time . The method has been applied to sera from penicillin-allergic patients and controls . Human erythrocytes coated with rabbit antibodies carrying penicilloyl groups were incubated with the serum to be tested, then washed . 125I-labelled anti-human IgE was added and, after further incubation and washing, the radioactivity retained by the cells was counted . This gives a measure of the specific IgE in the test sample . Other aliquots of the coated cells were treated with specific antiglobulin reagents in the usual manner of the RCLAAR in order to determine antibodies of other classes . The sensitivity for IgE was similar to that of the radioallergosorbent test . Information was also obtained about specific IgG subclasses.

Acta Histochem, 1976, 55(1), 14 - 8
Use of chellators in the electron microscopic detection of mitochondrial adenosine triphosphatase; Sotonyi P et al.; Even when using modified WACHSTEIN-MEISEL procedure for the detection of mitochondrial ATP-ase it is difficult to avoid the non-specific reaction . Separation of the artefact from the precipitate of citric hydrolysis can be carried out only with difficulty . 20 mM of penicillin G amine or 40 mM of ascorbic acid in the incubation solution leads to selective localization . Ascorbic acid can also be used in the form of a 0.2 M tris and 0.05 M ascorbic acid buffer . With the use of chellators it is possible to eliminate factors which under pathological conditions greatly favour the formation of the artefact.

Int J Gynaecol Obstet, 1976, 14(3), 239 - 45
Pelvic actinomycosis; Cohen A et al.; Case report of tubo-ovarian abscess due to Actinomyces israeli is presented with revision of the literature with regard to pathogenesis, diagnostic difficulties and treatment . Diagnosis was established by culturing the organism from exudate obtained during surgery . The pathogenesis of pelvic actinomycosis is still controversial . Penetration of the GI tract with subsequent infection of the pelvic viscera seems to be the most likely mode of infection . Penicillin has an important role in the treatment of this disease . It does not cure, but retards the course of the infection . Surgical extirpation of infected tissue in combination with penicillin offers the best therapeutic results . When chronic pelvic inflammatory disease does not respond to therapy, when the sedimentation rate remains high, and the patient's general debility is progressive, an actinomycotic infection should be suspected.

Ann Anesthesiol Fr, 1976, 17(3), 281 - 4
{A study of allergy to local anesthetics using the lymphoblast transformation test}; Sabbah A; The lymphocyte transformation test (LTT) confirms the classical concept that Novocain is three times as potent as Xylocaine as a sensitizing agent . This sensitization to Novocaine is more common in patients with an allergic constitution and in those treated with several drugs . The LTT made it possible to identify the responsible drug, which was not always a local anesthetic, but sometimes Penicillin G and aspirin.

Antibiotiki, 1976 Jan, 21(1), 31 - 4
{Study of the penicillin amidase from E . coli . An ultrasonic method of studying the ph- and temperature-conformational transitions in the active center of the enzyme}; Berezin IV et al.; pH and temperature conformation transitions in the active center of penicillin amidase i.e . penicillinamidohydrolase E.C . 3.5.I.II were investigated by means of the kinetic method and a new ultrasonic method . It was shown that the catalytic activity of the enzyme was controlled by 2 ionogenic groups with pK 6.1 and 10.2 . The study of penicillinamidase by means of the ultrasonic method showed that the ionogenic group with pK 10 was responsible for maintaining the catalytically active conformation of the enzyme active center . Investigation of the temperature relation between the kinetic parameters of the enzymatic hydrolysis of benzylpenicillin catalyzed by penicillin amidase and the data on the effect of ultrasound on the enzyme showed that the enzyme was subjected to the temperature conformation transiton . The temperature and thermodynamic parameters of the conformation transition were determinded (T=318 degrees K, delta H=81 kcal/mole and delta S=255 e.u.) . The structure of the active center of the enzyme is discussed on the basis of the data obtained.

Brain Res, 1975 Dec 26, 100(3), 589 - 97
Effect of penicillin on an excitatory synapse; Futamachi KJ et al.; When penicillin, an epileptogenic agent, was applied to the neuromuscular junctions of the superficial flexor muscles of crayfish, the excitatory junctional potential (EJP) amplitudes were increased by 50-200% . This effect of the drug was not due to changes in the passive electrical properties of the muscle cell membrane or to an increase in its chemical sensitivity to acetylcholine (ACh), the presumed transmitter at the junction studied . Inactivating the penicillin with the enzyme penicillinase, or substituting acetate for penicillin in the test solutions eliminated the effect on EJPs, showing that the penicillin ion was the active agent . Penicillin ions did decrease the frequency of spontaneous miniature EJPs and increase the amplitude or presynaptic spikes recorded extracellularly, suggesting that augmentation of EJPs may have been due to alterations at the presynaptic nerve terminals.

J Gen Microbiol, 1975 Dec, 91(2), 287 - 94
The inheritance of penicillin titre in crosses between lines of Aspergillus nidulans selected for increased productivity; Merrick MJ; Selection for increased penicillin production among the progeny of pairwise crosses between wild-type isolates of Aspergillus nidulans resulted in the production of high-titre strains . Three crosses were made between strains with increased titre derived from independent selection lines . Significant genetic variation was found among the progeny of each cross, indicating that different genes for increased titre had been selected in each line . Gene action was additive in each cross . Renewed selection from the progeny of one 'between-line' cross resulted in further increases in titre, over three successive generations.

J Gen Microbiol, 1975 Dec, 91(2), 278 - 86
Hybridization and selection for increased penicillin titre in wile-type isolates of Aspergillus nidulans; Merrick MJ; Repeated hybridization and selection among wild-type isolates produced strains of Aspergillus nidulans with increased penicillin titre . Four independent selection lines were established, each originating from a sexual cross between two different heterokaryon-incompatible wild-type isolates . In each generation, two selected high-titre sister strains were crossed to produce the next generation . An initial increase in titre was obtained in each line, but after four or five generations of selection the genetic variation was considerably reduced and the rate of response to selection had decreased . From a base population of wild-type isolates with a mean titre of 8-6 units/ml the progeny mean titre was raised to between 16 and 20 units/ml in each line . The gradual nature of the response suggests that a number of genes determine penicillin titre in the wild-type isolates used . The gene action throughout the selection programme was predominantly additive.

J Gen Microbiol, 1975 Dec, 91(2), 278 - 86
Hybridization and selection for increased penicillin titre in wild-type isolates of Aspergillus nidulans; Merrick MJ; Repeated hybridization and selection among wild-type isolates produced strains of Aspergillus nidulans with increased penicillin titre . Four independent selection lines were established, each originating from a sexual cross between two different heterokaryon-incompatible wild-type isolates . In each generation, two selected high-titre sister strains were crossed to produce the next generation . An initial increase in titre was obtained in each line, but after four or five generations of selection the genetic variation was considerably reduced and the rate of response to selection had decreased . From a base population of wild-type isolates with a mean titre of 8-6 units/ml the progeny mean titre was raised to between 16 and 20 units/ml in each line . The gradual nature of the response suggests that a number of genes determine penicillin titre in the wild-type isolates used . The gene action throughout the selection programme was predominantly additive.

Mutat Res, 1975 Dec, 33(2-3), 299 - 310
A cytogenetic study in women who had used oral contraceptives and in their progeny; Bishun N et al.; PIP: A recent publication has suggested that exposure to sex steroids and oral contraceptives (OCs) during pregnancy may possibly cause congenital defects in human infants exposed in utero . Chromosome numbers and characteristics of leukocytes cultured from mothers who had taken OCs over long periods and of their progeny were studied . Results were compared with control subjects . At the delivery of the baby, 10 ml of venous blood was collected from the mother and 5 ml of cord blood was collected . Whole blood was incubated with Eagle's Minimal Essential Medium, with added penicillin and streptomycin and phytohemagglutinin at 37 degrees C for 3 days, with periodic agitation . 3 hours before harvesting the leukocytes, colcemid was added to arrest cells in metaphase . For each metaphase, a chromosome count was made . Each chromosome was then examined for breaks and other structural disorders . Breaks and gaps were scored only from cells with a full complement of chromosomes . Chromosome counts and examinations were obtained from 114 blood cultures from the test mothers, 153 from the test babies, 126 from control mothers, and 157 from control babies . 92-93% of cells had 46 chromosomes . Polypoid cells were 0-.1% . Structural aberrations were mainly gaps (.1-.5%) and breaks (.1-.6%) . 295 cells were found with an abnormal chromosome count, excluding cells with structural alterations . 131 cells were tetraploid with 92 chromosomes, of which 47 tetraploid cells were from control babies . There were 6 triploid cells in the test babies' group to only 1 found in the control babies . There were many hypodiploid cells with chromesome counts of less than 46, probably due to broken cells being counted . The overall figures show no significant differences (p less than .05) between control and test subjects for either mothers or their babies . Findings of this, and of other studies quoted, suggest that there is no chromosomal damage in human subjects who have taken OCs before conceiving . Although the potential of a chemical substance for mutagenicity is not the same as its potential for carcinogenicity, no overt risk of carcinogenicity to women taking the pill is obvious .

Biochem J, 1975 Dec, 151(3), 741 - 6
Behaviour of tritium-labelled isopenicillin N and 6-aminopenicillanic acid as potential penicillin precursors in an extract of Penicillum chrysogenum; Fawcett PA et al.; 1 . 3H was incorporated into solvent-soluble penicillin from isopenicillin N and 6-aminopenicillanic acid 3H-labelled in the 2beta-methyl group when the labelled compounds were incubated with a crude extract of Penicillum chrysogenum . 2 . With a soluble protein fraction of the extract incorporation from isopenicillin N occurred on addition of phenyl-acetyl-CoA . 3 . Labelled benzylpenicillin was isolated after incubation of the crude extract with phenylacetyl-CoA and isopenicillin and the addition of unlabelled benzylpenicillin as a carrier . 4 . No incorporation of 3H into solvent-soluble penicillin was detected on incubation of these extracts with penicillin N.

Biochem J, 1975 Dec, 151(3), 729 - 39
Synthesis of tritium-labelled isopenicillin N, penicillin N and 6-aminopenicillanic acid; Usher JJ et al.; 1 . Phenoxymethylpenicillin sulphoxide 4-methoxybenzyl ester was labelled with 3H in its 2-beta-methyl group . Its specific radioactivity was 362 mCi/mmol . 2 . Removal of the side chain of this compound yielded the corresponding ester of 6-aminopenicillanic acid sulphoxide and coupling of the latter with the appropriate protected alpha-aminoadipic acid gave 4-methoxybenzyloxycarbonylisopenicillin N sulphoxide di-4-methoxybenzyl ester or the corresponding derivative of penicillin N . 3 . Removal of the protective groups by hydrogenolysis and reduction of the sulphoxide group yielded 3H-labelled isopenicillin N or penicillin N . 4 . 3H-labelled phenoxymethylpenicillin sulphoxide was obtained by hydrogenolysis from its 4-methoxybenzyl ester . Reduction of its sulphoxide group and subsequent removal of the side chain gave 3H-labelled 6-aminopenicillanic acid.

J Immunol, 1975 Dec, 115(6), 1577 - 83
Measurement of absolute amounts of antigen-specific human IgE by a radioallergosorbent test (RAST) elution technique; Schellenberg RR et al.; A technique for the absolute quantification of antigen-specific human IgE is described . It employs elution of a calculable amount of antigen-specific IgE from an allergosorbent-antibody complex by means of alkaline pH treatment, followed by measurement of the IgE content of the eluate with a modified radioimmunosorbent test (RIST) . With this method IgE antibody directed against the benzylpenicilloyl determinant of penicillin (BPO) was measured quantitatively in sera from seven penicillin allergic patients . IgE specific for ragweed antigen E was measured in sera from 33 ragweed allergic patients . Values obtained for IgE anti-BPO ranged from 19 to 1806 ng/ml and comprised from 1.3 to 27.5% of total serum IgE . Values of IgE anti-antigen E ranged from 9 to 1807 ng/ml, comprising from 3 to 84% of total serum IgE . Excellent correlation (r = 0.99; p less than 0.001) was obtained for both antigen systems between values determined by the RAST elution technique and by simple RAST assay with interpolation from a reference serum of known specific IgE content as determined by the elution technique may be needed only for primary standardization of reference sera.

Albrecht Von Graefes Arch Klin Exp Ophthalmol, 1975 Nov 25, 197(2), 107 - 17
{Transport of 131J-iodo-o-hippurate and 22Na out of the retroretinal space in experimental non rhegmatogenous detachment of the retina (author's transl)}; Gloor BP et al.; A model of an experimental arhegmatogenous retinal detachment is presented, to allow the measurement of the transport of radioactive labeled substances out of the subretinal space . Experiments were performed on 19 male cats . 131I-iodo-o-hippurate and 22Na were used as test substances . There was no significant difference between the rate of disappearance of 131I-hippurate if injected retroretinally or intravitreally . The rate of disappearance of 131I-hippurate could be slowed down by intravenous infusion of penicillin-G . The rate of disappearance of 22Na following retroretinal injection is not only slower than the rate of disappearance of 22Na injected intravitreally, but significantly slower than the rate of disappearance of 131I-hippurate . For graphic analysis ("curve peeling") of the terms embodied in the curves, more densly situated points of measurements will be necessary . Then the experimental model will serve well to analyze the components influencing the transport of labeled sodium out of the subretinal space.

Laryngoscope, 1975 Nov, 85(11 pt 1), 1888 - 97
Hearing loss of acquired syphilis: diagnosis confirmed by incudectomy; Nadol JB Jr; Syphilis, both congenital and acquired, may cause sensori-neural hearing loss . Congenital syphilis presents in two forms: early (infantile), and late (tardive) . Acquired syphilis, both secondary and tertiary, may cause deafness . The clinical course of the acquired and congenital forms are similar . Sensori-neural hearing loss with low discrimination scores may affect both ears simultaneously or sequentially, and vestibular complaints are common . A clinical diagnosis can be made on the basis of history, the presence of other stigmata of syphilis, and serological tests, including the FTA-ABS . The histopathology of acquired and congenital forms is indistinguishable and is essentially twofold: first, syphilis may cause a miningo-neurolabyrinthitis with round cell infiltration of the labyrinth and VIIIth nerve as the predominant lesion in early congenital syphilis and the acute meningitides of secondary and tertiary acquired syphilis . Second, syphilis may cause a perivascular round cell osteitis of the temporal bone with secondary involvement of the membranous labyrinth in both late congenital and acquired late latent or tertiary syphilis . Endolymphatic hydrops may be seen in both the congenital and acquired forms . A case of bilateral sequential sudden deafness due to acquired syphilis is presented . A histological diagnosis of syphilitic involvement of the temporal bone was made by incudectomy . Treatment with prednisone and penicillin over a three-month period resulted in return of good cochlear function in one ear.

JAMA, 1975 Nov 10, 234(6), 618 - 9
Cephalexin-related nephropathy; Verma S et al.; Hematuria and eosinophilia developed in two patients being treated for bacterial endocarditis with 20 or 24 gm/day of cephalexin given orally together with probenecid (Benemid) . One patient had a concurrent transient increase in serum creatinine; both patients had a history of penicillin allergy and had previously received cephalexin intravenously . All abnormalities promptly remitted following discontinuation of therapy.

Med J Aust, 1975 Nov 8, 2(19), 743 - 5
Erysipelothrix endocarditis; Baird PJ et al.; This communication describes the second reported Australian case of erysipelothrix endocarditis; after treatment with penicillin, the patient survived . It also gives up-to-date summary and brief discussion of the literature.

Lancet, 1975 Nov 8, 2(7941), 896 - 9
Early syphilitic hepatitis; Feher J et al.; 17 out of 175 cases of early syphilis had clinical, biochemical, and immunological evidence of liver damage . Before penicillin therapy the histological appearance of the liver was abnormal in 14 of the 15 patients from whom biopsy specimens were obtained . In 7 cases, treponemes were seen in the liver . After two months' penicillin therapy the extent and severity of the histological abnormality was reduced . In the repeat liver-biopsy specimens obtained after penicillin treatment no treponemes could be demonstrated . It is suggested that the hepatitis found in these 17 cases of early syphilis was produced by treponemes.

Acta Allergol, 1975 Nov, 30(5), 250 - 8
Production of rat homocytotropic antibodies using low dose, long term oral exposure to penicillin G; Perelmutter L et al.; Sera from 15 patients with immediate hypersensitivity reactions to penicillin G gave positive responses in the rat mast cell test (RMCT) indicating the presence of IgE-type antibodies in the sera . Five sera were from patients who had had reactions to penicillin 15 to 22 years previously without known re-exposure to this antigen . To explore the possibility that non-therapeutic exposure to penicillin may have produced continued sensitization in these patients, an animal model system was developed to explore the efficacy of low dose, long term oral exposure to penicillin G in rats for producing homocytotropic antibodies in these animals . It was found that when rats were given penicillin G in their drinking water at concentrations of 0.1 to 1 U/ml over a period of 1 to 3 months they produced serum IgE and IgGa antibodies . In addition, IgE antibodies were actively bound to the peritoneal mast cells of these animals . The presence of circulating or cell bound antibodies was detected using the rat mast cell test . It was also shown that rats given penicillin G orally for 1 month were more prone to antibody production after a single intramuscular injection of penicillin G compared to a control group receiving only the intramuscular injection of this antigen . The results of this study are discussed in terms of possible non-therapeutic sensitization towards penicillin G in the human population.

Am J Med, 1975 Nov, 59(5), 614 - 28
Acute interstitial nephritis . A clinical and pathologic study based on renal biopsies; Ooi BS et al.; To define interstitial nephritis without preselection bias, 25 consecutive renal biopsy specimens from patients with tubular damage, interstitial damage and interstitial inflammation were analyzed in detail . In four patients (all with acute renal failure), tubulitis, and interstitial eosinophil and lymphocyte infiltration were found, but no glomerular abnormalities . In four others, the findings were similar but some glomerular abnormalities were noted . Two patients had probable healed interstitial nephritis . The clinical presentation varied from transient renal insufficincy to oliguric renal failure . Three of the patients with glomerular abnormalities had significant proteinuria . When the 10 patients with interstitial nephritis were compared with the other 15 serving as controls, striking features in the former group were skin rash, eosinophilia, the absence of hypertension and the frequency of administration of penicillin and its analogs . Serum immunoglobulin E (IgE) levels were elevated in three of the patients . The striking eosinophilia, interstitial eosinophil infiltration and increased IgE levels suggest that allergen-reaginic complexes may be involved in the pathogenesis of the lesion.

South Med J, 1975 Nov, 68(11), 1333 - 6
Gonococcal arthritis in pregnancy: a ten-year review; Chapman DR et al.; Thirty-two cases of gonococcal arthritis in pregnant women admitted to Jackson Memorial Hospital between 1962 and 1971 are reviewed . Our specific aim is to reinforce awareness of this serious complication in pregnancy . The incidence of gonococcal arthritis is higher in women, but more significantly, it appears that the pregnant patient is at greater risk . The incidence of skin lesions seems to be higher in pregnancy . Penicillin was universally effective, since penicillin-resistant strains appear not to involve joints.

Epilepsia, 1975 Nov, 16(4), 583 - 92
Actions and interactions of dipropylacetate and penicillin on evoked potentials of excised prepiriform cortex of guinea pig; Voskuyl RA et al.; Slices from guinea pig brain containing the lateral olfactory tract (LOT) and the prepiriform cortex were studied in vitro . Field potentials, evoked by stimulation of the LOT, were recorded extracellularly . This field potential comprises a compound action potential, a surface negative wave (identified as EPSP), and superimposed positive peaks ("population spikes" or PSs) reflecting postsynaptic activity . In a previous article the penicillin-induced increase of EPSP and of both amplitude and number of PSs was described . Now we are reporting the slight depression of EPSP and PSs and the prevention of the appearance of penicillin-induced PSs by an antiepileptic drug sodium dipropylacetate (Depakine) . The effect was dose-dependent . Models explaining the effects of penicillin and dipropylacetate are discussed.

Allergol Immunopathol (Madr), 1975 Nov-Dec, 3(6), 391 - 402
{Study of drug allergies with special reference to skin manifestations}; Dieguez I et al.; One hundred and forty four patients, with dermal reactions to different drugs, were chosen from our clinic . The selection criteria was based on a detailed and careful anamnesis in order to be certain of the specific drug responsible for the reaction . We tried to establish a drug-specific reaction pattern for each of the drugs studied . Intradermal skin tests were performed with all drugs to be studied, except with pyrazolones and aspirin, for which patch tests were applied . The drug concentrations were established prior to the tests in order to avoid unwanted unspecific reactions . In every case, immediate and delayed reaction readings were carried out . A three crosses reaction (+++) was considered positive . The skin tests were positive in 44% of the cases, a value higher than those referred to by most authors . The delayed reactions to skin tests and the chloramphenicol-mediated delayed-type "dermatitis-like" manifestations are compared . It is noteworthy to mention that positive delayed reactions were observed more frequently with chloramphenicol than with any of the other studied drugs . The same applies for those patients with a positive history to chloramphenicol . The most common reaction pattern to penicillin and streptomycin in our series (20%) were urticaria and Quincke's edema . Penicillin, pyrazolones and streptomycin were the most common drugs responsible for urticarial patterns, being the pyrazolones related to fixed erythema in many cases . The age group 25-50 was the most frequently involved . No sex predominance was observed . The value of the classic skin tests is discussed, so are history recording and the in vitro tests.

Electroencephalogr Clin Neurophysiol, 1975 Nov, 39(5), 499 - 506
Suppression of cortical epileptiform activity by generalized and localized ECoG desynchronization; Wagner R 2nd et al.; The effects of high frequency electrical stimulation of both diffusely projecting brain regions and regions of more restricted projection were studied on penicillin-induced cortical epileptiform focal activity in the cat . Results obtained were contingent on the level of focal activity present at the time of stimulation . Very active foci (spike rates above 0.5/sec) were uniformly driven by stimulation of all structures under study . Foci exhibiting weak to moderate levels of activity were, on the other hand, inhibited both during and following stimulation . Episodes of spike suppression induced through stimulation of diffusely projecting structures were typically followed by an intensified "rebound" of interictal activity . Episodes of suppression induced through stimulation of regions of limited projection were not followed by such rebounds, an effect most dramatically apparent with caudate stimulation and motor cortex foci . Results are discussed in terms of the interaction between naturally occurring brain rhythms in sleep and arousal with the epileptic process.

Antibiotiki, 1975 Nov, 20(11), 984 - 90
{Properties of penicillin amidase covalently bound to cellulose matrices}; Nys PS et al.; Properties of penicillinamidase (PA) covalently bound with the cellulose matrix were studied . The efficiency of the binding depended on the bind type and purity of the native enzyme taken for binding . Stability of the immobilized PA (IPA) was studied at wide pH ranges . The effect of the ion strength, substrate concentration and purity of the native PA on stability of IPA was also investigated . The maximum stability of the enzyme was observed at pH 6.5-7.0 Stability of IPA depended on the purity of the native enzyme . When PA of the diazotized ether of cellulose containing amino groups was used, the enzyme was destabilized . IPA prepared on chlortriazinylcellulose was more stable than the respective native PA almost by I order.

J Pharm Sci, 1975 Oct, 64(10), 1711 - 3
Plasma protein binding of drugs as a function of age in adult human subjects; Bender AD et al.; The intent of this study was to determine what influence, if any, increasing age has on the binding of drugs by plasma proteins . Plasma from healthy subjects ranging in age from 21 to 94 years was used . The binding of phenytoin (diphenylhydantoin) (acid), penicillin G potassium (benzylpenicillin potassium), and phenobarbituric acid was determined by equilibrium dialysis of 14C-labeled compounds . No differences were found in total protein concentration; however, albumin was reduced in subjects over 50 years of age . Plasma binding of each drug studied was not related to age; this finding suggests that age per se is not a factor in the binding of drugs by plasma proteins.

Orthop Clin North Am, 1975 Oct, 6(4), 923 - 34
Septic arthritis in children; Morrey BF et al.; When septic arthritis involves the hip, the prognosis is much worse than with any other joint . Approximately 50 per cent of the results were unsatisfactory with hip involvement compared to 12 per cent unsatisfactory results with involvement of the other joints . The erythrocyte sedimentation rate is a much more helpful diagnostic test than the leukocyte count or differential cell count . The most important prognostic factors are the duration of symptoms prior to treatment, a penicillinase-producing organism (penicillin-resistant) as the etiologic agent, and evidence of associated metaphyseal osteomyelitis . Early decompression and cleansing of the joint by aspiration or arthrotomy are essential for a good result . Long-term parenteral antibiotic therapy improves the prognosis when osteomyelitis is an assoicated feature . Arthrotomy with continuous irrigation appears to be more effective in decreasing long-term residual effects than arthrotomy alone . Almost all secondary surgical procedures are directed toward correcting the sequelae of septic arthritis of the hip.

Endocrinol Jpn, 1975 Oct, 22(5), 465 - 9
Mouse prolactin obtained by pituitary organ culture in a serum-free medium; Kohmoto K; Mouse prolactin was purified by organ culture of pituitaries and electrophoresis of the medium . Mouse pituitaries were organ-cultured in 9-cm Petri dishes containing Waymouth's medium (MB 752/1) supplemented with penicillin (50 units/ml), streptomycin (100mug/ml), and bovine insulin (0.12 I.U./ml) for 8 days . Prolactin-rich culture medium was half-saturated with ammonium sulfate and centrifuged . The pellet was subjected to analytical disc electrophoresis (10% acrylamide) . Gels were sectioned into 2-mm segments . Prolactin was eluted in 0.04M phosphate buffer (pH 7.2), dialyzed and lyophylized . Two hundred and forty ml medium in which 360 pituitaries were cultured yielded 29.3 mg lyophylized mouse prolactin . Although the preparation contained 2 other bands on acrylamide gel disc electrophoresis, a single precipitin line was seen in immunodiffusion and immunoelectrophoresis, showing the identity of their antigenicity . From these results, two other proteins in the preparation were suggested to be deamidated prolactin.

Antibiotiki, 1975 Oct, 20(10), 921 - 4
{Study of the possibility of using penicillin and a specific globulin for treating the anthracic infectious process in an irradiated organism}; Strel'nikov VA et al.; Comparative efficacy of the specific globulin and penicillin in the treatment of Siberia ulcer infection was studied on 160 guinea pigs and 400 albino mice irradiated with Co60 gama-rays in sublethal doses . It was found that penicillin preserved its efficiency, while the curative effect of the specific globulin significantly decreased in the irradiated animals.

Klin Monatsbl Augenheilkd, 1975 Oct, 167(4), 600 - 4
{Drainage of the vitreous body space in cases of intra-ocular infection (author's transl)}; Ritzinger I et al.; In the last 2 years we saw eight cases with massive i.o.infection (panopht-almitis) following perforating injuries . We took measures as follows: After trepanation of the sclera we washed out the space of the vitreous body with diluted solution of Gentamycin and simultaneously we used massive systemic therapy of Gentamycin and of Penicillin . In this way we stopped the infection in four eyes and we were successful in maintaining in various degree the function of these eyes.

Br J Obstet Gynaecol, 1975 Oct, 82(10), 831 - 5
Postpartum renal failure associated with eclampsia and penicillin hypersensitivity; Down PF et al.; A case of acute renal failure associated with disseminated intravascular coagulation occurring immediately post partum is reported . The aetiological role of the associated eclampsia together with evidence for a hypersensitivity reaction to ampicillin is discussed.

J Pharmacol Exp Ther, 1975 Oct, 195(1), 16 - 21
Pharmacodynamic analysis of substrate stimulation of p-aminohippurate transport by newborn rabbit kidney; Pegg DG et al.; Penicillin pretreatment of 2-week-old New Zealand White rabbits significantly increased the ability of renal cortical slices to transport p-aminohippuric acid (PAH) . The PAH slice/medium ratio increased with dose to a maximum at 90,000 I.U . of procaine penicillin G . Sodium penicillin G (180,000 I.U.) produced no greater increase . Stimulation was maximal after four penicillin injections at 12-hour intervals . The maximal response was observed 24 hours after the final injection, whereas after 72 hours the capacity of slices from treated animals to transport PAH was no different than control . To determine the effect of a maximal substrate challenge on the development of transport capacity, pregnant does were treated with 90,000 I.U . of procaine penicillin i.m . twice daily through the last half of gestation . Young animals received four penicillin injections before sacrifice . The PAH slice/medium ratio from pups 3 days, 1 and 2 weeks old were not significantly different from that normally observed at 4 weeks . Animals 4 weeks old did not respond to penicillin treatment . Thus, intrinsic transport capacity for PAH is mature at 4 weeks of age . Only before this age may transport be enhanced by substrate . Maximal enhancement of PAH transport capacity occurs when four injections of 90,000 I.U . of procaine penicillin G are administered at 12-hour intervals followed by sacrifice 24 hours after the final injection.

J Am Vet Med Assoc, 1975 Oct 1, 167(7), 561 - 4
Dermatophilosis in two polar bears; Newman MS et al.; Dermatophilosis was diagnosed in 2 of 13 captive polar bears (Thalarctos maritimus), causing generalized dermatitis of 3 years' and 6 months' duration, respectively . Progressive clinical signs included yellowing and darkening of the hair, pruritus, encrustation of skin, and reluctance to bathe . Dramatic resolution of lesions occurred during 8 weeks of twice-weekly intramuscular treatment with long-acting penicillin.

Am J Surg, 1975 Oct, 130(4), 496 - 8
Cervicofacial actinomycosis; Leafstedt SW et al.; Cervicofacial actinomycosis is a disease that is currently encountered as a pseudotumor entity or cold abscess . The frequent use of antibiotics in treatment of masses in the cervicofacial region may either delay its appearance or disguise the diagnosis . The surgeon must be highly suspicious when making the diagnosis since precautions in handling the biopsy specimens are necessary . Treatment consists of incision biopsy and drainage or aspiration to establish the diagnosis, followed by prolonged penicillin therapy . In those patients allergic to penicillin, clindamycin should be the initial drug of choice . Either medication must be administered for a prolonged period of time, even after the disease is clinically controlled.

Farmaco {Sci}, 1975 Oct, 30(10), 807 - 14
A new product of rearrangement of penicillin V (S)-sulphoxide; Valcavi U et al.; Penicillin V (S)-sulphoxide (I), treated with methanesulphonic acid in benzene and dimethylacetamide, gives the decarboxylated increment3-cephem compound (IV) and a new product of rearrangement to which the structure of the 4-{N-(1'-carboxy-2'-methylenepropyl)carbamoyl}-2-phenoxymethylthiazole (VIII) is ascribed.

Antibiotiki, 1975 Oct, 20(10), 917 - 21
{Study of the interaction of human serum albumin with penicillins by means of spin labels}; Kharakhonycheva NV et al.; Interaction of 8 penicillin preparations with human serum albumin was studied with the spin-labels method and a probe . Correlation between the binding level of penicillins with human serum albumin and their effect on the spectrum of EPR of the spin-label attached to albumin was observed only with the use of a hydrophobic probe (radical III) . The covalent attached marks and the hydrophobic probe may be used for rapid orienting estimation of pencillin interaction with albumin.

Biochim Biophys Acta, 1975 Sep 22, 403(1), 256 - 65
Determination of heat changes in the proximity of immobilised enzymes with an enzyme thermistor and its use for the assay of metabolites; Mosbach K et al.; A device, the enzyme thermistor, is described which is capable of measuring changes in heat due to enzymic reactions . The sensor, a thermistor, is in direct contact with the site of reaction through its placement in a microcolumn filled with an immobilised enzyme preparation . The substrate solution flows past the thermistor tip, and as much as approx . one half of the total heat evolved can be registered as temperature change, deltat . Glass-bound glucose oxidase (EC 1.1.3.4), penicillinase (EC 3.5.2.6), trypsin (EC 3.4.21.4) and urease (EC 3.5.1.5) were used for the determination of glucose, penicillin G, benzoyl-L-arginine ethyl ester and urea respectively . Linear relationships between the deltat recorded and the concentration of substrate were obtained in all cases.

Med Klin, 1975 Sep 12, 70(37), 1469 - 73
{Syncopal convulsions with myocarditis in childhood . A case contribution to the transitory pacemaker treatment of myocarditis-induced heart block}; Tamm D et al.; A ten-year-old girl was admitted to hospital with convulsions due to Adams-Stokes syndrome as a complication of complete heart block . A rheumatic myocarditis was causing the conduction defect . As a temporary measure a pacemaker was used to treat the extremely serious condition . In addition, cortisone, antibiotics and antiphlogistics were given for treatment of the underlying disease . The child was discharged from hospital in good condition with a long-term therapy of penicillin.

Schweiz Med Wochenschr, 1975 Sep 6, 105(36), 1147 - 51
{Diagnosis and therapy of liver actinomycosis}; Clavadetscher P et al.; A 47-year-old man who had undergone gastrectomy for duodenal ulcer required repeated hospitalization due to recurrent fistulas in the region of the laparotomy scar and increased cholestasis and cachexia . An intrahepatic and subphrenic abscess was diagnosed clinically and by liver scan and confirmed by laparotomy . The histologic findings revealed actinomycosis . Through early surgical drainage and administration of 20 million units penicillin G daily it proved possible to discharge the patient completely cured after 2 months . The pathogenesis of liver actinomycosis is discussed.

MMW Munch Med Wochenschr, 1975 Sep 5, 117(36), 1405 - 8
{Penicillin V potassium in tonsillar tissue and serum (author's transl)}; Backmann H et al.; 1.2 mega U Penicillin V potassium was given to 20 patients 2 hours (group 1) and another 19 patients 3 hours (group 2) before tonsillectomy . After the operation biological determinations of the levels of active principle were made from tonsillar tissue and serum with statistical evaluation of the results (Spearman's rank correlation) . There was a significant connection between the serum and tonsillar tissue concentrations (in children and adults) in both groups . The level of the active principle in group 2 was only slightly lower than in group 1 . Many of the micro-organisms responsible for tonsillitis can be influenced by the concentrations found here, so that application of Penicillin V can often be expected to have a good therapeutic effect.

Zh Evol Biokhim Fiziol, 1975 Sep-Oct, 11(5), 497 - 502
{Age peculiarities in the effect of M- and N-cholinolytics on the activity of the epileptogenic zone in the rabbit hippocampus}; Grigor'eva ON et al.; In experiments on 6-10, 16-20-day and adult rabbits, electrochimiotrodes were chronically implanted into the dorsal hippocamp . Direct application of a M-cholinolytic, metamizyl, or N-cholinolytic, gangleron, to penicillin-induced epileptogenic zone in the hippocamp inhibited seizures in rabbits of all age groups . The intensity of interseizure epileptiform discharges in the EEG did not change under the action of cholinolytics in adult and 6-10-day rabbits, and decreased in 16-20-day ones . Parenteral administration of gangleron caused the same effect on the activity of epileptogenic zone, as its direct application to the hippocamp . Parenteral administration of metamizyl inhibited seizures in young animals (similarly to its direct application to the hippocamp), but increased the seizures and interseizure discharges in adult rabbits . Therefore, already to the 6th day of postnatal life of rabbits, blocking of the cholinoreactive system of the hippocamp may inhibit circulation of seizural discharges along closed neuronal circuits, which is necessary for the formation of the seizure.

Prostaglandins, 1975 Sep, 10(3), 383 - 93
Effect of PGF2 alpha and 15(S)-15-methyl PGE2 methyl ester on feline generalized penicillin epilepsy; Quesney LF et al.; The effect of PGF2alpha and 15(S)-15-methyl PGE2 methyl ester on transient generalized epilepsy in the cat induced by penicillin was examined . Epileptic activity before and after administration of the prostaglandins by several routes was determined from continuous EEG recordings and expressed in epileptic bursts per min . The PGE2 analogue given in single non-toxic doses (1.6-3 mug/kg) by intramuscular or intravenous routes at the peak of epileptic activity significantly reduced epileptic activity for up to four hours . Subcutaneous administration was less effective . PG2alpha given by the intramuscular route (0.3 mg/kg) also markedly reduced the number of epileptic bursts . Increasing the dosage 4-fold almost completely suppressed epileptic activity . Intracarotid infusion of PGF2alpha for one hour (10 mug/min) almost abolished all epileptic activity . Neither prostaglandin given in non-toxic doses induced EEG abnormalities in non-epileptic cats . Toxic doses of the E2 analogue (greater than 16 mug/kg) caused bilaterally synchronous high voltage slow wave activity . It is concluded that these prostaglandins reduce penicillin epilepsy in the cat . The findings are consistent with either a direct excitatory action on neurones of the medial reticular formation or anatagonism of the depressant action of norepinephrine on Purkinje cells.

Poult Sci, 1975 Sep, 54(5), 1689 - 92
Deamination of amino acids in the small intestine of chickens fed meat meal; Skurray GR et al.; The loss of amino acids by bacterial deamination in the small intestine of chicks fed heated and unheated meat meal was studied by incubating the intestinal contents in vitro . The loss of amino acids by bacterial deamination was found to take place mainly in the lower small intestine . Deamination of amino acids was significantly higher in the contents of the small intestine of chicks fed a meat meal compared to the freeze-dried raw materials, and this deamination was reduced by the addition of 50 p.p.m . penicillin to the meat meal.

Epilepsia, 1975 Sep, 16(3), 469 - 76
Neuroexcitatory and depressant effects of penicillin at the cat soleus neuromuscular junction; Raines A et al.; Penicillin administered intraarterially in a dose of 200 units per kg produced high frequency (ca 300 Hz) repetitive discharges originating in motor nerve endings in response to single stimuli applies to the cat soleus nerve . The high frequency repetitive discharges were antidromically conducted and recorded on ventral root filaments . Simultaneously each repetitive burst was transmitted to the muscle, producing an increase in contractile strength by converting a twitch into a brief tetanic contraction . Posttetanic potentiation in this system, which is mediated by repetitive discharges originating in nerve terminals after high frequency stimulation, is augmented by penicillin; larger doses depressed posttetanic potentiation, and still larger doses produced varying degrees of neuromuscular block . Events similar to those observed after intraarterial injections were recorded when penicillin was administered intravenously in larger doses . These data suggest that in the presence of penicillin the motor nerve terminals remain depolarized for a prolonged period after excitation by the stimulus, thus providing a current sink for the parent axon . Under the influence of this constant cathodal focus the axon fires repetitively at the high frequency.

Acta Paediatr Scand, 1975 Sep, 64(5), 718 - 24
Asymptomatic bacteriuria in school girls . V . The clinical course and response to treatment; Lindberg U; The short-term prognosis of 116 school girls with asymptomatic bacteriuria (ABU) treated or left untreated is reported . In untreated girls a spontaneous remission was obtained in 11% within one year . A short course of nitrofurantoin eliminated the bacteriuria in 93% of the girls in the treatment group . The recurrence rate was 30% in one year in the patients that became abacteriuric spontaneously, after a bladder washout test or after treatment with penicillin or nitrofurantoin . The first recurrence occurred withn 3 months in 79% (19/24) . Nineteen of the 24 patients with recurrences (79%) had a third infection within 9 months . In patients with parenchymal reduction or reflux the renal concentrating capacity increased significantly after treatment of the bacteriuria . All the girls left untreated had normal renal concentrating capacity on detection and this remained unchanged during the year of follow-up . One of 28 untreated girls attracted a symptomatic pyelonephritis caused by a strain different from that at detection of ABU . Of 81 girls cured from the bacteriuria 24 recurred, 5 with a symptomatic pyelonephritis and 3 with cystitis . It is concluded that strains isolated from girls with ABU do not commonly cause symptomatic pyelonephritis.

J Bacteriol, 1975 Sep, 123(3), 916 - 20
Role of the cell surface in bacterial mating: requirement for intact mucopeptide in donors for the expression of surface exclusion in R+ strains of Escherichia coli; Beard JP et al.; Two derivatives of the F-like R factor R1drd19 carrying mutually exclusive resistance determinants were used to study the role of the mucopeptide in the expression of conjugal functions . The use of metabolically active penicillin spheroplasts in R+ times R- matings had no effect on the ability of the cells to donate or accept a plasmid . However, in R+ times R+ matings it was found that surface exclusion was totally abolished if the donor, but not the recipient, was a spheroplast . This result implies that the traS gene, expressed by the excluding plasmid, is dependent for its action on an intact mucopeptide layer in the donor cell, and that this interaction is independent of the transfer ability of the excluding plasmid.

J Bacteriol, 1975 Sep, 123(3), 888 - 97
Attachment of lipoprotein to murein (peptidoglycan) of Escherichia coli in the presence and absence of penicillin FL 1060; Braun V et al.; In vivo studies on the attachment of lipoprotein to the murein (peptidoglycan) of Escherichia coli showed that it takes several generations of growth until the amount of lipoprotein on newly made murein is equilibrated . The technique used involves degradation of the sodium dodecyl sulfate-insoluble murein-lipoprotein complex (sacculus, rigid layer) with lysozyme and separation of the labeled products on paper . No lipoprotein was found on murein subunits incorporated during a pulse of {3H}diaminopimelate for 1 min in logarithmically growing cells at 37 C . Even after one doubling of the cell mass, only 4 to 8% of the labeled murein was isolated as bound to lipoprotein . With uniformly labeled murein, 30% remains bound to lipoprotein after lysozyme treatment, corresponding to three murein subunits . Therefore it can be concluded that during pulse labeling either no lipoprotein is incorporated into the newly synthesized murein or no murein subunits are inserted into existing murein around lipoprotein attachment sites . Longer pulse and pulse-chase experiments argue for the latter interpretation . It is therefore concluded that incorporation of murein subunits into the growing murein polymer is not at all a random process . Instead, quite large areas of murein, on which lipoprotein is situated, seem to be preserved . Under the influence of penicillin FL 1060 murein synthesis is 50% inhibited . The rate of lipoprotein attachment is less affected so that increasing amounts of lipoprotein become attached during spheroplast formation . By the time the stationary growth phase has been reached, the lipoprotein content of the murein has doubled . Diaminopimelate auxotrophic mutants require, in the presence of penicillin FL 1060, more diaminopimelate for full growth than in the absence of penicillin FL 1060 . This finding and the fact that murein synthesis is always inhibited by 50% over a wide range of penicillin concentration (1 to 1,000 mug/ml) point to the inhibition of an enzymatic step of murein synthesis which can be partially bypassed by a second enzyme, less efficient but resistant to penicillin FL 1060.

Klin Monatsbl Augenheilkd, 1975 Sep, 167(3), 465 - 9
{Bacteria and resistance examination in bacterial conditions of the conjunctiva (author's transl)}; Junker FK; The optimal treatment of any inflammation within the area of conjunctiva, after recognition of pathogen and determination of resistance, is not always feasible in the daily practice of the ophthalmologist because usually immediate treatment is necessary . To test the (in vitro) efficacy of the medications available, determinations of pathogen and resistance were made in 100 conjunctival swabs taken from patients with inflammations of the conjunctiva and lacrimal duct . The relatively high incidence of resistance to penicillin, chloramphenicol and tetracycline should be the reason for using more effective substances such as gentamycine and rifamycin . The pathogens and resistance found at present are important criteria for the selection of appropriate chemotherapeutic agents.

South Med J, 1975 Sep, 68(9), 1147 - 52
Trimethoprim-sulfamethoxazole in the treatment of gonorrhea: comparison with standard treatment schedules; Duncan WC et al.; Several treatment regimens of trimethoprim-sulfamethoxazole (TMP-SMZ) were compared to the USPHS-recommended schedules for treatment of uncomplicated gonorrhea with ampicillin plus probenecid, tetracycline, or aqueous procaine penicillin G in both men and women . TMP-SMZ, six tablets as a single oral dose daily for 3 days, was as effective as the ampicillin or tetracycline schedules . The drug was well tolerated.

Antibiotiki, 1975 Sep, (9), 846 - 53
{Possibility of the intrauterine sensitization to benzylpenicillin and ampicillin in Syrian hamsters}; Solov'ev VN et al.; Immunization of Syrian female hamsters with benzylpenicillin and ampicillin resulted in positive skin reactions of the retarded type and decreased titers of the blood antihistamine factor (AHF) in a part of the posterity . Penicillin allergy was in particular observed in the posterity of the female hamsters immunited before the pregnancy . The state of allergy to penicillins was found in the posterity of the female hamsters with both the positive and negative skin reactions on immunization during the 2nd half of the pregnancy.

Epilepsia, 1975 Sep, 16(3), 449 - 55
Epileptogenic effects of several penicillins and penicillin-related compounds in rat neocortex; Van Hartesveldt C et al.; Several penicillins and penicillin-related compounds were tested for their ability to produce epileptiform activity in rat neocortex . (1) Alterations in the side chain of penicillin G decreased epileptogenic capability in all the compounds tested in this study: Phenoxymethylpenicillin produced a primary focus but no mirror focus, suggesting a dissociation of the mechanisms underlying these two processes . Ampicillin, 6-aminopenicillanic acid, and potassium 6-aminopenicillanic acid, and potassium 6-aminopenicillanic acid produced little or no epileptiform activity . All these compounds have free amino grounds and are amphoteric . (2) Breaking the beta lactam ring of penicillin G (potassium penicillin G penicilloate) eliminated epileptogenic capability . (3) Potassium salts of penicillin or its derivatives (potassium penicillin G, propicillin, potassium 6-aminopenicillanic acid, potassium penicillin G penicilloate) consistently suppressed cortical activity, regardless of the ability of the compound to produce spike discharges . Thus, mechanisms underlying these two properties can be dissociated . (4) Antibiotic activity of penicillins bears no relationship to epileptogenic capability.

Antibiotiki, 1975 Sep, (9), 810 - 3
{Determination of the penicillin acylase activity of E . coli cultures using a method of gas-liquid chromatography}; Tochenaia NP et al.; Penicillinacylase activity was determined in E . coli by the product of benzylpenicillin destruction, i.e . phenylacetic acid formed under the effect of the enzyme . The determination was performed on a chromatograph . The immobile phase consisted of 10 per cent of ethylenglycol edipate on chromosorb A, modified with 2 per cent H3PO4 . Nitrogen was used as the gaseous carrier . The method is rapid and handy for mass testing of the cultures with a purpose of detecting penicillinacylase-producing strains . It provided reliable determination of penicillinacylase in the cultures producing simultaneously beta-lactamase, another penicillin-destroying enzyme.

Z Immunitatsforsch Exp Klin Immunol, 1975 Sep, 150(2), 138 - 60
Clinical trial of Ro 6-0787, a monovalent specific hapten inhibitor of penicillin allergy; De Weck AL et al.; A second clinical trial of the compound Ro 6-0787, which is a specific monovalent penicilloyl hapten inhibitor of allergic reactions to penicillin has been conducted by investigators from 9 different European groups in 90 patients allergic to penicillin . The effect of a combined Ro 6-0787-penicillin therapy was considered as clinically successful in the large majority of cases, since treatment with penicillin could be pursued or resumed without allergic manifestation in 42 from 46 cases (91 percent) . The effect of Ro 6-0787 alone on acute allergic manifestations after interruption of penicillin therapy was more difficult to evaluate but was nevertheless considered satisfactory in 17 from 26 patients (65 percent) . A depression of skin hypersensitivity to PPL and/or penicillin and penicillin derivatives sometimes persisting for weeks and months was obvious in numerous allergic patients submitted to combined Ro 6-0787-penicillin treatment . A depressing effect on antipenicillin antibody titers detected by passive hemaglutination was also manifest in some patients . Failure to suppress allergic manifestations was reported in 11 cases, among which some may have been due to insufficient dosage of inhibiting hapten . The overall tolerance of Ro 6-0787 in allergic patients has been very good . Nevertheless, the major obstacle to a wider general use of Ro 6-0787 at the present time appears to be the occurrence of positive skin reactions to that compound in approximately 5 percent of patients allergic to penicillin . It is not yet ascertained whether the occasional positive skin reactions and urticaria to Ro 6-0787 may have been due to aggregation, or incomplete dissolution of the compound or whether it reflects hypersensitivity to another antigenic determinant . With the reservation that patients with positive skin test to Ro 6-0787 have for the time being to be excluded from combined treatment, this monovalent hapten certainly offers a new possibility to resume and/or pursue penicillin therapy in patients demonstrably allergic to that drug.

Antibiotiki, 1975 Sep, (9), 807 - 10
{Electron microscopic study of the localization of penicillin acylase in E . coli cells}; Chaikovskaia SM et al.; The paper describes the studies on definition of penicillinacylase localizations in the cells of E . coli with the help of ferritin labeled immune sera and electron microscopy . Both the intact cells and the cells treated with the substances affecting the cell wall intactness were used . The study showed relation between penicillinacylase and the surface structures of the cell, i.e . the cell wall and the periplasmic areas . It was found that penicillinacylase got into the environmental medium with the splitted cell fragments which corresponded to the general mechanism of excretion of large high molecular compounds by gramnegative organisms.

MMW Munch Med Wochenschr, 1975 Aug 29, 117(35), 1383 - 6
{Blood-CSF kinetics of penicillin G in neurosyphilis (author's transl)}; Ritter G et al.; Measurements of the penicillin concentration in serum and cerebrospinal fluid patients with neurosyphilis showed that conventional therapy can attain effective treponemocidal levels for only a short time or not at all in the CSF and brain-tissue, the regions where the treponemas are found in this particular stage of disease . Intravenous infusions with high doses (0,5 mega unit penicillin-G/kg body weight in 24 hours) over more than one generation phase of the treponemas (35-43 hours) considerably improve the recovery . 16 patients were treated in this way and been followed over 2-3 years clinically and immunologically.

Schweiz Med Wochenschr, 1975 Aug 23, 105(34), 1065 - 72
{Drug allergy damage to the blood }; Muller U; Drug induced blood dyscrasias, leukocytopenia, thrombocytopenia and hemolytic anemia were observed in 7% of 643 adverse drug reactions registered by drug monitoring in Bern, Switzerland, in the period 1970-1973 . Life threatening reactions were consistently more frequent in hematological side effects (22%) than in the total of adverse drug reactions (6%) . Blood dyscrasias induced by drug allergy are generally believed to belong to the allergic reactions of type II . Antigen-antibody reaction evolves in connection with cells of the blood, either by fixation of the drug itself or a metabolite on the cell surface, or by adsorption of primarily formed antigen-antibody complexes on the cell . In drug induced immune hemolytic anemia three types may be distinguished: 1 . the innocent bystander type, caused by quinine, PAS, rifampicin and others, 2 . the penicillin-type, caused by penicillins and cephalosporins, and 3 . the autoimmune type caused by alpha-methyl-dopa etc . Agranulocytosis in Europe is most frequently due to pyrazolones, while phenothiazines play the leading role in the USA . In pyrazolone agranulocytosis an allergic pathogenesis is very probable, whereas phenothiazines probably induce agranulocytosis by a direct toxic effect on bone marrow cells . The clinical course in pyrazolone agranulocytosis is acute, whereas it is rather insidious in the phenothiazine type . The main drugs causing allergic thrombocytopenia are thiazide diuretics, quinine, quinidine and sulfonamides . Clinical aspects and therapy of drug induced blood dyscrasias are discussed.

Dtsch Med Wochenschr, 1975 Aug 8, 100(32), 1634 - 8
{Severe side-effects of treatment with D-penicillamine (author's transl)}; Hennemann HH et al.; In a 53-year-old woman an acute allergic thrombocytopenia (acute Werlhf's disease) occurred after treatment with D-penicillamine for one month which led to death . In two further patients transitory platelet deficiencies were observed after six and two months which regressed completely in six months and four weeks, respectively . One of the patients had nephrotic syndrome and a retrobulbar neuritis at the same time . Both symptoms were equally transitory and could not be demonstrated five weeks after cessation of therapy . In a further case a lethal Lyell syndrome developed three weeks after therapy was started . These observations show that during D-penicillamine treatment weekly, and later fornightly, blood counts should be performed . In the occurence of thrombocytopenia, leucopenia or anaemia treatments should be stopped; Signs of drug intolerance together with exanthemata should also led to a critical review of the indications and the dosage . D-Penicillamine should not be used when hypersensitivity to penicillin exists or when cell deficiencies have occurred after anti-reheumatic medication . The development of proteinuria should also result in withdrawal of the drug . Therapy with D-penicillamine requires conscientious follow-up urinalyses and blood counts as well as attention to allergic rashes.

JAMA, 1975 Aug 4, 233(5), 432 - 5
Penicillin-induced immune hemolytic anemia . Occurrence of massive intravascular hemolysis; Ries CA et al.; A patient with penicillin-induced immune hemolytic anemia had massive intravascular hemolysis with hemoglobinemia and hemoglobinuria . Substantial amounts of complement components C3 and C4 were detected on the patient's red blood cells (RBCs), in addition to the usual IgG antibody to penicillin . The patient's serum demonstrated a high titer of antibody to penicillin (8,000), which did not cause hemolysis in vitro, but did cause complement fixation when incubated with normal serum . The presence of complement components on the patient's RBCs, and the finding that the serum fixed complement in vitro suggests that penicillin-antipenicillin immune complexes may have been present in the serum . We attribute the severity of the hemolysis to participation of the complement system in the hemolytic process and to the high titer of antibody to pencillin.

Biochem J, 1975 Aug, 149(2), 357 - 64
The reaction of penicillin with proteins; Corran PH et al.; The mode of reaction of benzylpenicillin with two proteins was studied, with particular reference to the allergenicity of penicillin . These reactions, with pig insulin, and with hen's-egg-white lysozyme, were carried out in neutral solution at 37 degrees C . High concentrations of penicillin are needed to label the proteins, owing to concurrent hydrolysis of penicillin . Evidence has been obtained that the penicillin-reactive sites on the insulin molecule are the alpha-amino group at the N-terminus of the A chain and the epsilon-amino group of the lysine residue; whereas a site of reaction with lysozyme appears to be the epsilon-amino group of lysine-116.

Gann, 1975 Aug, 66(4), 417 - 9
Adjuvant action of garlic sugar solution in animals immunized with Ehrlich ascites tumor cells attenuated with allicin; Nakata T et al.; Ethanol-insoluble components were extracted from fresh garlic with 0.9% NaCl solution containing streptomycin and penicillin . This extract, containing approximately 10% sugar, 0.3% nitrogen, and 0.4% ash, was termed garlic sugar solution . This garlic sugar solution (Medium 1) was used as the suspending medium for Ehrlich ascites tumor cells attenuated with allicin, the main principle of garlic, and 0.9% NaCl solution containing streptomycin and penicillin (Medium 2) was also used as the suspending medium . Mice of DDD strain were immunized with the attenuated tumor cells suspended in Medium 1 or 2 . After immunization, the immunized and control mice were challenged intraperitoneally with viable Ehrlich ascites tumorcells . Animals immunized with the attenuated tumor cells suspended in Medium 1 acquired significantly stronger resistance against the tumor cells than animals immunized with those suspended in Medium 2.

Hautarzt, 1975 Aug, 26(8), 423 - 4
{The effect of pivampicillin and probenecid on experimental syphilis in rabbits}; Petzoldt D; The oral single-dose-treatment of the acute gonorrhoeal urethritis of the male with 1.4 g pivampicillin and 1.0 g probenecid is one of the possible alternatives to a parenteral penicillin treatment . Experiments were performed on rabbits to determine if this dose of pivampicillin and probenecid could cure a simultaneously acquired syphilis at a very early stage of incubation . 300 treponems (Nichols strain, T . pallidum) were inoculated intratesticularly and 3 days later pivampicillin and probenecid were administered in doses which produced antibiotic serum levels similar to those in patients who had received a single oral dose of 1.4 g pivampicillin and 1.0 g probenecid . Controls over a 15-weeks period showed that this dosage did prevent the development of syphilitic orchitis and reactivity to the quantitative FTA-ABS-test . It is concluded that the treatment of acute gonorrhoea with 1.4 g pivampicillin and 1.0 g probenecid in general is sufficient to cure a simultaneously acquired syphilis.

Neurology, 1975 Aug, 25(8), 785 - 64
Response of generalized penicillin epilepsy in the cat to ethosuximide and diphenylhydantoin; Guberman A et al.; The effects of ethosuximide and diphenylhydantoin sodium on feline generalized penicillin epilepsy, a model of human generalized corticoreticular (centreccephalic) epilepsy, were significantly reduced following administration of ethosuximide with plasma levels of 60 mug per milliliter, and there was a linear correlation between the plasma level and antiephilepileptic effect (p less than 0.01) . Diphenylhydantoin produced a lesser reduction in epileptic activity, and there was no correlation between the plasma level and effect . Four cats that received both drugs successively responded well to ethosuximide, while only two responded to diphenylhdantoin . The good response to ethosuximide is in accord with clinical experience in human generalized corticoreticular epilepsy.

Am J Dis Child, 1975 Aug, 129(8), 980 - 3
Pneumococcal endocarditis in a 7-week-old infant . A case complicated by congenital heart malformation with mitral valve perforation; Moodie DS et al.; A 7-week-old girl had pneumococcal endocarditis and perforation of the mitral valve . Pneumococcal endocarditis in children under 2 years of age is extremely rare, and is a prototype for endocarditis in general in infants less than 2 years of age . To our knowledge, this is the youngest reported patients with pneumococcal endocarditis in the penicillin era.

Surgery, 1975 Aug, 78(2), 202 - 10
Effects of drugs and parenteral solutions on vascular fibrinolytic activity; Johnston WE et al.; The effects of saline, D5W, D10W, dextran, penicillin, cephalothin, and the Renografin "dyes" on vascular fibrinolytic activity were evaluated in in vitro experiments and in caninne preparations . Saline, D5W, D10W, and dextran did not affect fibrinolytic activity . High concentrations of the Renografin "dyes" and penicillin decreased fibrinolytic activity in vitro . Cephalothin, with an increased association of postinfusion in vitro studies but demonstrated minimal effect during the in vivo studies during which sufficiently high local concentrations of drug may not have been obtained . It is concluded that, although intimal damage, stasis, and/or hypercoagulability are responsible for the development of post infusion thromboses, local hypofibrinolytic activity is induced by some infusions and might contribute to the persistence and propagation of the thromboses.

J Pharm Sci, 1975 Aug, 64(8), 1384 - 6
High-pressure liquid chromatographic analysis of penicillin G potassium and its degradation products; Blaha JM et al.; An anion-exchange high-pressure liquid chromatographic system capable of separating penicillin G potassium from five of its degradation products was developed . The retention times were: penicillin G potassium, 17.5 min; DL-penicillamine, 4.5 min; benzylpenilloic acid, 7.0 and 8.0 min; benzylpenamaldic acid, 13.0 min; benzylpenicilloic acid, 19.5 min; and benzylpenillic acid, 22.0 min . In addition, the system permits quantification using linear calibration curves.

Proc Natl Acad Sci U S A, 1975 Aug, 72(8), 2999 - 3003
Distinct penicillin binding proteins involved in the division, elongation, and shape of Escherichia coli K12; Spratt BG; The varied effects of beta-lactam antibiotics on cell division, cell elongation, and cell shape in E . coli are shown to be due to the presence of three essential penicillin binding proteins with distinct roles in these three processes . (A) Cell shape: beta-Lactams that specifically result in the production of ovoid cells bind to penicillin binding protein 2 (molecular weight 66,000) . A mutant has been isolated that fails to bind beta-lactams to protein 2, and that grows as round cells . (B) Cell division: beta-Lactams that specifically inhibit cell division bind preferentially to penicillin binding protein 3 (molecular weight 60,000) . A temperature-sensitive cell division mutant has been shown to have a thermolabile protein 3 . (C) Cell elongation: One beta-lactam that preferentially inhibits cell elongation and causes cell lysis binds preferentially to binding protein 1 (molecular weight 91,000) . Evidence is presented that penicillin bulge formation is due to the inhibition of proteins 2 and 3 in the absence of inhibition of protein 1.

J Pharm Sci, 1975 Aug, 64(8), 1378 - 80
Effect of self-association on rate of penicillin G degradation in concentrated aqueous solutions; Ong JT et al.; The apparent rate of degradation of penicillin G potassium micellar solutions of 500,000 units/ml, a concentration commonly encountered in vials reconstituted for storage in the refrigerator, was investigated and compared to that of nonmicellar solutions of 8000 units/ml at 25 degrees, ionic strength of 1.1 M, and pH range from 5.0 to 9.5 . In the micellar solutions the apparent rate of the H+-catalyzed degradation was increased twofold but that of water- and OH minus-catalyzed hydrolysis was decreased two- to three-fold . Consequently, the pH-rate profile of the micellar solutions was shifted to higher pH values and the pH of minimum degradation was found to be at 7.0 compared to 6.5 for the nonmicellar solution of the same ionic strength . Compared at their respective pH-rate profile minima, micellar penicillin G is 2.5 times as stable as the nonmicellar solution under the conditions of constant pH and ionic strength.

J Pharm Pharmacol, 1975 Aug, 27(8), 580 - 7
Chemical reactions involved in penicillin allergy: kinetics and mechanism of penicillin aminolysis; Tsuji A et al.; In view of the fundamental importance of the reaction of penicillins with amino groups of proteins to the penicillin allergy, the aminolysis of benzylpenicillin by various amines was kinetically investigated . The formation rate constants, kamide, of benzylpenicilloylamides were determined at 35 degrees, 45 degrees and 60 degrees (mu equals 0.5), and found to obey the general rate law: kamide equals k1{amine} + k2{amine H+} {amine} + k3{amine}2 + k4{amine}aoh . All of the amines exhibited the unassisted nucleophilic rate constant, k1 . The relative importance of the other kinetic terms depends on the basicity and the chemical structure of amines . The reaction mechanism of penicillin aminolysis was discussed . Bronsted relations for k1, k2 and k3, except for hydrazines, were satisfactory.

Schweiz Med Wochenschr, 1975 Jul 26, 105(30), 953 - 6
{Clinical and immunological analysis of 1,047 allergic reactions to penicillin}; Girard JP et al.; Of 1047 patients who had had an allergic reaction to penicillin established by clinical and laboratory findings, 224 were given penicillin therapy again later . One third of these patients developed a second allergic reaction to penicillin . In patients experiencing a second allergic reaction the most striking feature is a dramatic increase in the immediate reactions and especially of the anaphylactic type, and less markedly, an increase in the serum-sickness type of reaction . All the patients were skin tested with penicilloyl-polylysine (PPL) and benzylpenicillin (BPO) . Circulating hemagglutinating antibodies were determined and in vitro stimulation of peripheral blood lymphocytes was performed in all cases . Skin tests show little change for several years . In contrast, circulating hemagglutinating antibodies disappear in half the cases within 6 months . Finally, lymphocyte stimulation with penicillin was positive in only 50% three months after onset of the allergic reaction, whereas one year later there was a 73% positive response . The best test for prediction of an allergic reaction to penicillin appears to be determination of the (high) and (low) reactors among patients with a positive skin test to PPL and BPO.

J Neurol, 1975 Jul 2, 209(3), 199 - 215
DC potentials of temporal lobe seizures in the monkey; Mayanagi Y et al.; In 8 monkeys, made epileptic by alum or penicillin injection into temporal lobe structures, 40 seizures were studied by both DC cortical potential and subcortical EEG recordings . Eighteen seizures of lateral temporal origin had an abrupt negative DC potential shift of 0.5 to 2.0 mV in and around the focus . The frontal, parietal and occipital cortices did not develop DC potential changes, perhaps due to the limited propagation of the neocortical seizures . Twenty-two seizures of medial temporal origin showed a negative shift of the anterior, inferior or lateral temporal cortex in 85% of seizures . The other 15% had a positive or no shift . In hippocampal seizures, a positive displacement was sometimes seen prior to the main negative shift in the lateral temporal cortex . The remote cortex developed only a minimal positive shift in 30% of the mediotemporal seizures . A marked negative shift in the frontocentral cortex was the first sign of impending generalization, which may result from a series of chain reactions with seizure propagation, involving more and more structures of the brain . Registration of DC potentials in temporal lobe seizures may give insight into the nature of abnormal EEG activities and to some extent into the origin of seizures.

Zh Evol Biokhim Fiziol, 1975 Jul-Aug, 11(4), 410 - 8
{Age peculiarities of trace discharges of after-effect and of the activity of epileptogenic zone in the hippocamp of rabbits}; Gusel' VA et al.; Seizure activity in the hippocamp has been studied on 6-10-, 16-20-day and adult rabbits . The pattern and thresholds of trace discharges of after-effect evoked by the electrical stimulation of the hippocamp were found to be similar in animals of all age groups . However, the amplitude of after-discharges significantly increased during the development of the brain . After the formation of penicillin epileptogenic zone in the hippocamp, EEG of all animals exhibited the identical types of focal interseizure discharges and electrographic correlates of seizures, yet the amplitude of epileptifiorm discharges on the EEG increased with age . Contralateral hippocamp was involved into the pathological process more easily in young rabbits than in adult ones.

Acta Allergol, 1975 Jul, 30(2-3), 126 - 32
Morphological studies on allergen induced blast transformation of sensitized lymphocytes; Petrunov B et al.; The morphological and ultrastructural changes occurring in blast transformed lymphocytes, isolated from patients sensitive to grass pollen and penicillin, were studied . Certain differences in the appearance of the blast cells, as evidenced by light microscopic observation, were not found by electron microscopy . The blast cells showed foamy protoplasm regardless of the nature of the allergens employed . An increased number of either single or rosette-forming ribosomes was established . Numerous vesicles were visible in the cytoplasm . The endoplasmic sacs were more numerous . Golgi apparatus was well-developed; the mitochondria were increased and had a dense matrix.

J Bacteriol, 1975 Jul, 123(1), 75 - 82
Genetic and physiological analysis of an envB spherelike mutant of Escherichia coli K-12 and characterization of its transductants; Westling-Haggstrom B et al.; The envB1 mutation mediating a distorted cell morphology of Escherichia coliK-12 was cotransducible with strA, aroE, aspB, and argG . The mapping data is consistent with a gene location for envB around 62.5 min . In partial diploids envB1 was recessive to its wild-type allele . The original envB mutant contained a second mutation in a locus denoted sloB close to strA . The following gene order is suggested: sloB-strA-aroE-envB-aspB-argG . The sloB1 mutation caused a marked reduction in the growth rate of both envB and envB+ strains . Moreover, this mutation in the presence of envB1 appears to increase the ratio between deoxyribonucleic acid and protein in cells growing in rich medium . The phenotypic properties of envB1, sloB+ and envB+ transductants were characterized . Cells with envB1, sloB+ genotype were hypersensitive to several penicillins including the beta-lactam compound, amidino penicillin . Penicillin hypersensitivity could not be explained by increased outer membrane penetrability . The original envB mutant (envB1,SLOB1), as well as envB1, sloB1 or envB+, SLOB1 transductants were resistant to amidino penicillin . Resistance was explained by the slow growth rate mediated by the sloB1 mutation . The similarity between envB cells and wild-type cells treated with sublethal concentrations of amidino penicillin was emphasized.

Can J Comp Med, 1975 Jul, 39(3), 340 - 8
The effect of penicillin, dihydrostreptomycin and prednisolone treatment of experimental Candida krusei infections of the mammary glands of dairy cattle; Farnsworth RJ et al.; The growth of Candida krusei in quarters treated intramammary with penicillin, dihydrostreptomycin and prednisolone was compared with growth in untreated quarters . No clinical mastitis occurred in any of the quarters of either group . The number of yeast organisms isolated from the quarter during and after the treatment period appeared similar in both groups . The number of leukocytes in all treated quarters increased during the antibiotic and steroid treatment period but the number of yeast isolated remained the same or decreased as compared to the control quarters.

Med Klin, 1975 Jun 20, 70(25), 1090 - 4
{Clinical experiences with a new multi-effective penicillin "spectacillin", gained in the gynecological and obstetrical therapy (author's transl)}; Lehmann WD; With the new semi-synthetic ampicilline-derivate, we treated 28 female patients of gynecological, and 22 of obstetrical indications . Owing to bacterial infections by grampositive/gramnegative germs, in these cases an antibiotic therapy was indicated . The target therapy was based on clinical findings, the germ analysis and the antibiogram . Considering the degree of disease, the intravenous (3 x 2 grams per day) or the oral treatment (4 to 6 grams a day) has been effected during 6 days at least and 13 days as a maximum duration . The evaluation of the therapeutical results was made by means of the clinical cours as well as the germ findings . These two parameters showed the reliable effectiveness of "Spectacillin", whereas the low exanthemic rate must be emphasized.

Naunyn Schmiedebergs Arch Pharmacol, 1975 Jun 18, 289(1), 55 - 64
Cerebral toxicity of penicillins in relation to their hydrophobic character; Weihrauch TR et al.; The neurotoxic effects of ticarcillin, methicillin, phenthicillin, oxacillin, cloxacillin and dicloxacillin were studied in the conscious rabbit . During and after intravenous administration of 1.2 and 2.4 g/kg, resp., over 50 min the blood concentrations of the drugs were determined and the neurotoxicity assessed by continuous recording of the electroencephalogram . The hydrophobia of the penicillins was characterized by determination of their partition coefficients between isobutanol and buffer solution pH 7.4 . The penicillins showed quite different neurotoxic properties . A close correlation (r = 0.928) was found between the neurotoxic potency of the penicillins and their partition coefficients . With increasing hydrophobia the neurotoxic potency increased in the following sequence: Ticarcillin, methicillin, oxacillin, phenethicillin, cloxacillin, dicloxacillin . It can be concluded, therefore, that determination of the partition coefficient of a penicillin gives valuable information on the neurotoxicity to be expected . The introduction of a neurotoxicity quotient revealed that penicillins may be divided into two groups: less neurotoxic penicillins with a partition coefficient below 1.0 and highly neurotoxic penicillins with a partition coefficient above 1.0.

Can Med Assoc J, 1975 Jun 14, 112(13 Spec No), 40 - 2
Treatment of gonorrhea in the male with trimethoprim-sulfamethoxazole using a one- or two-dose regimen; Brathwaite AR; One hundred and eighty-four male patients with uncomplicated gonorrhea were treated in a randomized double-blind trial using two drug regimens . The combinations used were co-trimoxazole (trimethoprim, 80 mg and sulfamethoxazole, 400 mg) and TMP-SDZ (sulfadiazine, 400 mg and trimethoprim, 80 mg) . In 43 patients who received eight tablets of co-trimoxazole in a single dose the cure rate was 88% . In the 46 patients who received a second dose of eight tablets 24 hours later the cure rate was 100% . When TMP-SDZ was used according to the same schedule the respective cure rates were 85% (41 patients) and 86% (35 patients) . It is suggested that the two-dose regimen with co-trimoxazole is very effective in the treatment of uncomplicated urethral gonorrhea in the male and that the single-dose regimen, although less effective, may well prove adequate in patients defaulting after the initial treatment . At the present time, and with our local conditions, this form of treatment should be reserved for patients sensitive to penicillin or whose infections are resistant to this agent . The attack rate for patients having an episode of gonorrhea in the 12-month period immediately preceding the trial bore a direct relation to the outcome of therapy . It was highest (26%) in the group with an unsatisfactory outcome and lowest(4.3%) in the group with the highest cure rate . No adverse toxic reactions to the drug were recorded.

Can Med Assoc J, 1975 Jun 14, 112(13 Spec No), 83 - 6
Comparison of penicillin and trimethoprim-sulfamethoxazole in the treatment of ear, nose and throat infections; Quick CA; A double-blind trial of penicillin and the combination trimethoprim-sulfamethoxazole was undertaken in adult patients with active infection of the ears, nose or throat . The results indicated that the drug trimethoprim-sulfamethoxazole was as effective as penicillin in achieving clinical improvement and showed a broader spectrum than penicillin the the elimination of pathogenic organisms . The difficulties in obtaining positive cultures that were reflective of the clinical condition are described.

Can Med Assoc J, 1975 Jun 14, 112(13 Spec No), 43 - 6
Comparison of trimethoprim-sulfamethoxazole with penicillin and tetracycline in the treatment of uncomplicated gonorrhea in women; Nelson M et al.; In a collaborative prospective study 327 women with uncomplicated gonococcal cervicitis or proctitis were randomly assigned to one of four treatment groups: (1) aqueous procaine penicillin G, 4.8 million units IM in one session plus 1.0 g probenecide; (2) tetracycline HCI, 9 g over 4 days; (3) trimethoprim, 80 mg-sulfamethoxazole, 400 mg (TMP-SMX) six tablets once daily for 3 days; (4) TMP-SMX, six tablets wtice on 1 dat at a 6-hour interval . They were re-examined 4 to 8 days and 10 to 15 days after completion of therapy . There was no significant difference between the results of the four regimens in the 4- to 8-day period (P greater than 0.36) . However, at the 2-week point the results of TMP-SMX given for 3 days were less effective (P smaller than 0.05) than those obtained by penicillin plus probenecid . There was no significant difference between the results of the other regimens at this latter period.

Med Klin, 1975 Jun 13, 70(24), 1055 - 8
{Spectacillin-a new-developed multi-effective penicillin in treating chronic bronchoulmonary diseases author's transl}; Krause-Michel B; 50 patients with a chronic disease of the bronchopulmonary system, within the therapy of an acute exacerbation received in addition to bronchosecretolytics, spasmolytic substances, and corticosterones the substance 'Spectacillin' in a dosage ranging from 2 to 6 grams per day during the period of 2 weeks . The acute exacerbation has been stopped in 34 patients and there-by the recurrence could be prevented . Although in 9 patients a clinical improvement has been obtained, no germ elimination could be ascertained; 7 cases of disease remained uninfluenced . The evalution is documentated by the clinical and laboratory findings, the germ analysis and the test of pulmonary functions . The compatibality can be evaluated as well-effective; especially the low rate of exanthema (2 patients) is to be emphasized.

Antibiotiki, 1975 Jun, 20(6), 546 - 9
{Change in the alkaline phosphatase activity and glycogen content in the leukocytes of white rat blood under the influence of penicillin preparations}; Zabirov ISh et al.; The contents of alkaline phosphatase and glycogen in the neutrophils of the peripheral blood of unbred albino rats weighing 170-200 gm were determined . Benzylpenicillin and oxacillin in doses of 50000 and 20000 Units/kg respectively were administered intramuscularly once a day over a long period of time . Two-phase changes in the contents of alkaline phosphatase and glycogen under the effect of penicillin were found . An increase in their contents was observed on the 5-10th days then it was followed by a decrease . Increase in the contents of the metabolites proceeded simultaneously with enhancing of the digestive capacity of the leucocytes and activity of lysozyme in them.

Proc Soc Exp Biol Med, 1975 Jun, 149(2), 546 - 9
Substrate stimulation of para-aminohippuric acid transport: effect on uptake and runout; Pegg DG et al.; The ability of penicillin pretreatment to increase PAH accumulation by slices of newborn rabbit renal cortex was dissected into two components, uptake and runout . The oxygen-requiring component of the uptake process was significantly enhanced by penicillin treatment, whereas runout was unaffected . Kinetically, the data suggest that penicillin alters the affinity of the transport system for PAH . Due to the limitations of such a kinetic analysis, no conclusions may be drawn from such a suggestion . However, it may be concluded that penicillin pretreatment increases renal accumulation of PAH solely by stimulating the uptake process . Elucidation of the molecular changes involved will require techniques more sophisticated than uptake into renal cortical slices.

Epilepsia, 1975 Jun, 16(2), 257 - 67
Effects of acute and chronic paleocerebellar stimulation on experimental models of epilepsy in the cat: studies with enflurane, pentylenetetrazol, penicillin, and chloralose; Myers RR et al.; Effects of acute and chronic paleocerebellar stimulation were evaluated in four experimental models of epilepsy in 24 adult cats chronically implanted with bilaterally symmetric parasagittal electrocorticographic electrodes and anterior lobe cerebellar stimulation electrodes . Pentylenetetrazol was given intraveneously in 50-mg increments or 4% enflurane was inspired until grand mal seizures occurred spontaneously or were triggered by photic or auditory stimuli . Alpha-chloralose, 50 mg/kg, was injected intraperitoneally to produce a model of stimulus-sensitive myoclonus and sodium penicillin G, 350,000 units/kg, was injected intramuscularly to produce a model of petit mal epilepsy . One- to 250-Hz electrical stimulation of paleocerebellar cortical surfaces was performed with constant-voltage or constant-current stimulators at threshold and suprathreshold intensities with average intensities of 8 V and 2.5 mA, respectively . Acute or chronic, threshold or suprathreshold paleocerebellar stimulation did not predictably alter the electrographic or clinical manifestations in any of these four models.

Br J Vener Dis, 1975 Jun, 51(3), 183 - 7
Ampicillin plus probenecid compared with procaine penicillin plus probenecid in the treatment of gonorrhoea; Taylor PK et al.; 396 male patients with gonococcal urethritis were treated by one of three treatment schedules . Of 132 patients treated with 2.4 m.u . procaine penicillin plus 2 g . probenecid, 109 were followed . There were three (2.8 per cent) recurrences in the first week and none in the second . Of 132 patients treated with 2 g . ampicillin plus 2 g . probenecid, 112 were followed . There were four (3.6 per cent.) recurrences in the first week and three (2.6 per cent.) in the second (total of 6.2 per cent.) . Of 132 patients treated with 3 g . ampicillin plus 2 g . probenecid, 115 were followed . There was one (0.8 per cent.) recurrence in the first week and five (4.4 per cent.) in the second (total of 5.2 per cent.) . A close correlation was found between the sensitivities of gonococcal strains to ampicillin and to penicillin . The overall sensitivity pattern of N . gonorrhoeae to penicillin had not changed at The London Hospital since the last report in 1972, but there was further evidence of cross-resistance between penicillin and cotrimoxazole.

Br J Vener Dis, 1975 Jun, 51(3), 179 - 82
Single-dose treatment of gonorrhoea with cotrimoxazole . A report on 1,223 cases; Rahim G; 1,223 ambulant patients with gonorrhoea were each treated with a single dose of eight tablets of cotrimoxazole . 1,069 patients were followed up (794 males and 275 females) . Of these, only 46 (4%) failed to respond . Cotrimoxazole in the dosage used was well tolerated by all the patients, with very few side-effects . There was clear evidence that cotrimoxazole did not mask concomitant syphilitic infections; neither did it produce a gonococcal carrier state . The incidence of post-gonococcal non-specific urethritis was 6 per cent . At present cotrimoxazole seems to be the most useful alternative to penicillin in the treatment of gonorrhoea.

Nord Vet Med, 1975 Jun, 27(6), 337 - 9
Some recommendations concerning primary isolation of Mycoplasma suipneumoniae and Mycoplasma flocculare a survey; Friis NF; Two mycoplasma species of the porcine respiratory tract: Mycoplasma suipneumoniae and Mycoplasma flocculare, have been notoriously difficult to cultivate . In the present paper a description is given of a new medium with which primary isolation of these organisms is usually successful . The basal medium is made from commercial dehydrated products . Pig serum is added and phenol red used as pH indicator . Contrary to what is customary in the preparation of mycoplasma media, various inorganic salts (Hank's balanced salt solution) are included and penicillin-G replaced as a bacteriostatic by bacitracin and meticillin . The volume of water is adjusted so as to give isotonia . Various additives often recommended for mycoplasma cultivation have been examined for growth promoting effect; apparently, however, they were all without effect . Working procedures for primary isolation trials are briefly described.

J Med Chem, 1975 Jun, 18(6), 727 - 30
7-N-amidinocephalosporins; Altman J et al.; 7-Aminocephalosporanic acid tert-butyl ester reacts quantitatively at--20 degrees with iminium chlorides to give amidino derivatives . Removal of the tert-butyl protecting group with trifluoroacetic acid and treatment with 1 equiv of triethylamine yield the corresponding zwitterions . These compounds were less active than their penicillin analogs.

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