JAMA, 1980 Nov 28, 244(21), 2445 - 5 A novel approach to the temporary control of intractable bone pain; Zweig JI et al.; When treating patients with intractable bone pain secondary to bone metastasis from cancer, we have found that the injection of 2% lidocaine directly into the metastatic bone lesion will give prompt pain relief to some patients . Those who respond will then get prolonged pain relief lasting from 24 to 72 hours when reinjected with a mixture of 2% lidocaine and penicillin G procaine, 600,000 units/mL . Lesions of the spine should not be treated with this method. JAMA, 1980 Nov 21, 244(20), 2327 - 8 Dog bite wounds; Callaham M; Dog bite wounds are a common problem with an infection rate only slightly higher than that for lacerations in general . Wounds may be sutured after debridement and thorough irrigation, unless they are located on the hand, where infection is common . Infection is caused by a variety of organisms . A penicillinase-resistant penicillin or cephalexin monohydrate is the drug of choice; studies suggest prophylactic antibiotic therapy may be useful, especially in high-risk wounds. Clin Pharmacol Ther, 1980 Nov, 28(5), 624 - 8 Influence of prolonged recumbency on drug disposition; Kates RE et al.; The disposition of lidocaine and penicillin was studied in normal subjects before and after 7 days of total recumbency . Penicillin (1,000,000 U) and lidocaine (100 mg) were administered intravenously . Lidocaine protein binding was also followed . Total body clearance, elimination half-life, and volume of distribution were calculated . There were no statistically significant differences in these disposition parameters before and after 7 days of recumbency . The binding of lidocaine also was not changed after bed rest . We conclude that the physiologic changes that occur during prolonged bed rest do not affect distribution or elimination of lidocaine or penicillin. Arch Intern Med . 1980 Nov;140(11):1552. Oxacillin nephritis; Tillman DB et al.; Acute interstitial nephritis secondary to administration of antibiotics is a well-described entity . Oxacillin, however, has never been directly implicated . An 80-year-old man had a rising creatinine level and eosinophiluria while receiving oxacillin sodium . These findings disappeared when use of the drug was discontinued . We conclude that oxacillin is an additional penicillin that can cause interstitial nephritis. Arch Dis Child, 1980 Nov, 55(11), 857 - 60 Penicillin allergy: anti-penicillin IgE antibodies and immediate hypersensitivity skin reactions employing major and minor determinants of penicillin; Chandra RK et al.; 300 children considered to have had adverse reactions to penicillin were examined . Informed consent was obtained from the parents . Skin tests were conducted by the scratch/prick and intradermal techniques, using benzylpenicilloyl polylysine conjugate and a mixture of minor determinants of penicillin . Specific anti-penicillin IgE antibodies were estimated by the radioallergosorbent test . There was a good correlation between the two methods . The overall frequency of positive tests was 19% . 11 children showed cutaneous reactivity only to the minor determinants mixture . Positive results were found more often in those with accelerated adverse reactions, particularly anaphylaxis, serum sickness, angio-oedema, or urticaria . The validity of penicillin-negative results was confirmed by drug challenge in 56 subjects, only 2 of whom showed a slight skin rash . Of 5 patients with positive tests, inadvertent administration of penicillin produced accelerated urticaria in all . 14 of 42 children with positive tests had lost hypersensitivity to penicillin one year later . In a separate group of 50 children with a history of adverse response to ampicillin, the overall frequency of positive tests was 12%; 38% showed evidence of recent E-B virus infection . It was concluded that penicillin allergy is often overdiagnosed . The diagnosis can be reliably confirmed by skin tests using major and minor determinants of benzylpenicillin and by the radioallergosorbent test; such hypersensitivity is not permanent. Transfusion, 1980 Nov-Dec, 20(6), 662 - 8 Streptomycin-specific antibody coincident with a developing warm autoantibody; Florendo NT et al.; The presence of an antibody with specificity against streptomycin-sensitized red blood cells in the serum of a patient with tuberculous pericarditis is reported . Hemolysis and significant anemia were absent . The antibody appeared to develop together with an evolving warm autoantibody, but was clearly separable from the latter . The streptomycin-specific antibody was "penicillin-like" by being totally neutralized in the presence of streptomycin . Red blood cells had to be separately sensitized with streptomycin prior to incubation with the antibody . The antibody cross-reacted with neomycin-sensitized cells and was also neutralized by the presence of neomycin . In addition, a possible cross-reactivity of the streptomycin-specific antibody and the warm autoantibody is suggested . The association of a drug-induced antibody and autoimmune antibody of IgG type is most unusual . In our experience, we have encountered only one similar example. J Neurosurg, 1980 Nov, 53(5), 726 - 7 Nonsurgical resolution of a brain-stem abscess . Case report; Vaquero J et al.; A case of solitary mesencephalic abscess in a 13-year-old boy is presented . The computerized tomography and clinical pictures, indicating a Weber syndrome and obstructive hydrocephalus, resolved totally 20 days after implantation of a ventriculoatrial shunt and treatment with intravenous chloramphenicol and penicillin . This is the fifth reported case of survival in a patient with a brain-stem abscess, and the first in which this outcome has been achieved without surgical drainage of the abscess. J Antibiot (Tokyo), 1980 Nov, 33(11), 1363 - 8 Penicillin-binding proteins in Streptomyces cacaoi and Streptomyces clavuligerus . Kinetics of {13C}benzylpenicillin binding, temperature sensitivity and release of {14C}benzylpenicillin from the complex; Horikawa S et al.; On the membrane-bound penicillin-binding proteins (PBP) of Streptomyces cacaoi and S . clavuligerus, the kinetics of {14C}benzylpenicillin binding, the temperature sensitivity, the release of {14C}benzylpenicillin from the {14C}benzylpenicillin-PBP complexes and the changes of the PBP patterns during the growth cycle were examined . All the PBP in both strains, especially PBP in S . clavuligerus, had very low affinity for benzylpenicillin, comparing with other bacteria . As for the temperature sensitivity of the binding ability, all the PBP in S . cacaoi were highly sensitive to heat, while PBP-3 in S . clavuligerus retained the binding activity after incubation at 60 degrees C for 10 minutes . The release of {14C}benzylpenicillin from the complexes with PBP-1, PBP-2 in S . cacaoi and PBP-3 in S . clavuligerus was relatively fast initially . However, this soon reached a plateau and the complexes retained {14C}benzylpenicillin even after prolonged incubation . During the growth cycle, the PBP patterns in S . cacaoi did not change significantly . However, in S . clavuligerus, a band of molecular weight of about 120,000 daltons was observed only in the membrane fraction of early log phase, and PBP-1 (Mr=83,000) and PBP-2 (Mr=79,000) appeared only slightly in this phase. J Gen Microbiol, 1980 Nov, 121(1), 5 - 16 Genetics of penicillin titre in lines of Aspergillus nidulans selected through recurrent mutagenesis; Simpson IN et al.; Genetic analyses of mutations for increased penicillin titre were carried out on two strains of Aspergillus nidulans isolated after independent programmes of recurrent mutation and selection, similar to those used industrially for strain improvement . Both selected strains were stable in terms of colony morphology and penicillins titre . Backcrosses to the unselected ancestor indicated that the increased yield of each strain was due to an induced polygenic system with both additive and non-additive gene action . The titre-increasing mutations in one strain (A6-9) were recessive to their wild-type alleles, while those in the other (B6-27) were either semi-dominant or showed ambidirectional dominance . The diploid between A6-9 and B6-27 had a titre less than either component haploid, suggesting that the mutations in the two strains involved different genes . Strain B6-27 carried a translocation between chromosomes III and VII which had been induced during the selection programme . This investigation complements previous work on the genetics of penicillin production in A . nidulans and Penicillium chrysogenum and the results are directly relevant to industrial strain improvement by hybridization of divergent strains. Antimicrob Agents Chemother, 1980 Nov, 18(5), 675 - 9 Quantitative correlation between penicillin resistance and beta-lactamase activity specified by the R plasmids R1, R1 bla-45, and RP1 in Escherichia coli K-12; Crowlesmith I et al.; A mutant of the R plasmid R1 which synthesizes a beta-lactamase with altered kinetic characteristics was isolated . The level of penicillin resistance specified by this plasmid was correctly predicted from the properties of the wild-type R1 according to a simple theoretical model published by Zimmermann and Rosselet (Antimicrob . Agents Chemother . 12:368--372, 1977) . The model also accounts for the high level of penicillin resistance specified by the R plasmid RP1. Antimicrob Agents Chemother, 1980 Nov, 18(5), 667 - 74 Characterization of beta-lactamase-deficient (bla) mutants of the R plasmid R1 in Escherichia coli K-12 and comparison with similar mutants of RP1; Crowlesmith I et al.; Thirty-eight mutants of R1, an R plasmid specifying the type IIIa (TEM) beta-lactamase, were isolated; these mutants are partially or totally unable to synthesize the type IIIa beta-lactamase . The loss of beta-lactamase activity was associated with a reduction in the level of penicillin resistance conferred by the mutants upon their host strain . At least two of the mutants synthesized a beta-lactamase with altered substrate specificity . These properties are compared with those of two beta-lactamase-deficient mutants of plasmid RP1 . The results suggest that, for both R plasmids, penicillin resistance is entirely attributable to the presence of beta-lactamase activity . The properties of two R1 derivatives, pUB251 and pUB252, which have phenotypes similar to that of RP1, support this conclusion. Antibiotiki, 1980 Nov, 25(11), 808 - 15 {Penicillin amidase from E . coli . The kinetic and equilibrium parameters of the enzymatic hydrolysis of 7-phenylacetamidodesacetoxycephalosporanic acid catalyzed by an immobile enzyme}; Nys PS et al.; The kinetics of 7-phenylacetamidodesacetoxycephalosporanic acid (7-PADCA) catalyzed by immobilized penicillinamidase was studied . The kinetic and equilibrium parameters of the reaction were determined by analysis of the kinetic curves of the reaction product accumulation . Inhibition of the enzymatic reaction by the substrate and hydrolysis products was studied . It was found that the Michaelis complex completely lost its activity after attachment of the substrate second molecule to it . The values of the Michaelis constants, catalytic constant and constants of inhibition by the substrate and reaction products were determined: Km = (9.3 +/- 1.1) . 10(-5) M, kcat = (65 +/- 5) c-1, Ks = (1.4 +/- 0.1) . 10(-2) M, K1 (FAA) = (2.5 +/- 0.3) . 10(-4) M, K1 (7-ADCA) = (1.4 +/- 0.1) . 10(-1) M . The diffusion effect in the kinetic reaction catalyzed by immobilized penicillinamidase is discussed . The values of the Thiele modulus and the actual value of Km were calculated. Rev Infect Dis, 1980 Nov-Dec, 2(6), 867 - 79 Epidemiologic, clinical, laboratory, and therapeutic features of an urban outbreak of chancroid in North America; Hammond GW et al.; An epidemic of 135 cases of chancroid occurred in Winnipeg, Manitoba, Canada, from July 1975 to September 1977 . Probable contributing factors for development of chancroid lesions included male sex, lack of circumcision, and genital trauma . A previous history of venereal disease, sexual contact with a person from a bar or hotel in the core city area, unemployment, alcoholism, American Indian or Metis (mixed American Indian and Caucasian) race, and unstable domestic relationships were often accessory findings for infected patients . The tracing and treatment of lesion-free contacts of patients with chancroid may have contributed to the restriction of the outbreak to the core city area . Nineteen isolations of Hemophilus ducreyi were made, most by the use of a new selective medium . Treatment with a short course of penicillin antibiotics was ineffective for 10 of 16 patients, whereas an adequate course of sulfonamide or tetracycline antibiotics, combined when necessary with drainage of fluctuant inguinal abscesses, was effective therapy for most patients. Sex Transm Dis, 1980 Oct-Dec, 7(4), 193 - 4 Type I allergic reaction to orally administered tetracycline hydrochloride: a case report; Steinbruegge JM et al.; A 26-year-old man experienced a Gell-Coombs type I allergic reaction to tetracycline hydrochloride, which had been given as therapy for nongonococcal urethritis . The patient had a history of allergy to penicillin and of asthma . The allergic response to tetracycline resolved after administration of epinephrine and diphenhydramine . Since tetracycline is often used for treatment of sexually transmitted diseases, physicians should be aware of the possibility of an allergic response to this drug. Ginekol Pol, 1980 Oct, 51(10), 935 - 40 {Actinomycosis of the genital organs as a complication of intrauterine devices}; Bieda W et al.; PIP: A case of actinomycosis of the genitals is described . It occurred in a woman after insertion of an IUD . The paper presents the diagnostic difficulties resulting from the rarity of such complication, and the noncharacteristic signs and symptoms of the disease, leading to initial therapeutic failure . In the described case, the signs of inflammation of the genital organs were accompanied by a hard infiltration of the bladder wall . Results of ultrasonographic and microscopic examinations permitted finally to pose the correct diagnosis . Full recovery was observed after a 28 day curative period including injections of 22 million units of penicillin and 4 grams of ampicillin per day . (Author's modified) J Bone Joint Surg Am, 1980 Oct, 62(7), 1168 - 75 The transcapillary passage and interstitial fluid concentration of penicillin in canine bone; Bloom JD et al.; Using {14C} benzyl penicillin, we determined the ability of penicillin to cross capillary membranes in the tibiae of dogs, the degree of protein-binding of penicillin in serum and tibial bone tissue, and the concentration of penicillin in the interstitial fluid space of tibial bone . Extraction studies demonstrated that the capillary membranes in bone were readily traversed by benzyl penicillin . Penicillin concentrations in filed cortical and crushed cancellous bone samples, measured by both isotopic and biological assays, ranged from 1.0 to 8.7 per cent of the simultaneous concentrations of penicillin in plasma . Twenty-one per cent of the penicillin in plasma was protein-bound, while 39 per cent of the penicillin in cortical bone was tissue-bound and not biologically active . Studies of the distribution of benzyl penicillin showed that it was distributed in equal concentrations in the plasma and in the interstitial fluid spaces of bone . The concentration of biologically active penicillin in the interstitial fluid spaces of bone correlated closely with the simultaneously observed plasma level in animals in which a steady-state equilibrium had been achieved. Ann Allergy, 1980 Oct, 45(4), 253 - 5 Allergological risk factors as predictors of radiographic contrast media hypersensitivity; Kalimo K et al.; An in-depth allergy history was obtained from 830 consecutive patients who were subjected to intravenous radiographic contrast medium (RCM) examinations . During the RCM examination 47 patients reacted with symptoms of hypersensitivity . In 26 of these (55.3%) a positive previous allergy history had been obtained . Although this finding was statistically significant, its practical value is severely hampered by the lack of selectivity, many of RCM non-reactors also giving positive allergy histories . A positive history of a previous reaction to RCM or to penicillin, however, was found to have more specificity in predicting a forthcoming hypersensitivity reaction to RCM. J Clin Invest, 1980 Oct, 66(4), 821 - 31 Riboflavin transport in the central nervous system . Characterization and effects of drugs; Spector R; The relationship of riboflavin transport to the transport of other substances including drugs in rabbit choroid plexus, the anatomical locus of the blood-cerebrospinal fluid barrier, and brain cells were studied in vivo and in vitro . In vitro, the ability of rabbit choroid plexus to transport riboflavin from the medium (cerebrospinal fluid surface) through the choroid plexus epithelial cells into the extracellular and vascular spaces of the choroid plexus was documented using fluorescence microscopy . These studies provided further evidence that riboflavin is transported from cerebrospinal fluid to blood via the choroid plexus . The transport of {14C}riboflavin by the isolated choroid plexus was inhibited by thiol agents, ouabain, theophylline, various flavins (lumiflavin and lumichrome > sugar containing flavins), and cyclic organic acids including penicillin and fluorescein . Riboflavin inhibited {14C}penicillin transport competitively and the inhibition constant (K1) for riboflavin equaled the concentration of riboflavin at which the saturable transport system for riboflavin is 50% saturated (KT) . These and other data suggest that riboflavin, penicillin, and possibly fluorescein are transported by the same transport system in choroid plexus . In vivo, the intra-ventricular injection or riboflavin and {14C}penicillin inhibited {14C}penicillin transport from cerebrospinal fluid . In vitro, various flavins (riboflavin > other sugar-containing flavins > lumiflavin > lumichrome) inhibited {14C}riboflavin accumulation by brain slices . These studies support the notions that: (a) riboflavin accumulation by choroid plexus (active transport) is quite different from that in brain cells (facilitated diffusion and intracellular trapping), and (b) therapeutically important cyclic organic acids (e.g., penicillin) are transported fom cerebrospinal fluid by the riboflavin transport system in choroid plexus. Jpn J Exp Med, 1980 Oct, 50(5), 365 - 74 In vitro cultivation of Metastrongylus apri; Hata H et al.; The 3rd stage larvae of Metastrongylus apri were successfully cultured in vitro to the nearly maturity adult worms which possessed the sperm and immature eggs, though the worms were smaller in size than those grown in vivo . The most excellent medium for the development was relatively simple and consisted of chemically defined NCTC 109 supplemented with 20% calf serum, penicillin (200 unit/ml) and streptomycin (100 micrograms/ml) . Standing culture with a larval concentration of 100 to 200 worms per tube containing 2 ml medium and wih a gas phase of 5% CO2 in air at 37 to 28 degrees c was found to be sufficient twice a week using aseptic techniques . Under these conditions a relatively uniform development was obtained, attaining 85 +/- 6.7% of larvae to the 5th stage. Sex Transm Dis, 1980 Oct-Dec, 7(4), 188 - 90 Cefuroxime compared with penicillin for the treatment of gonorrhea; Morrison GD et al.; One hundred seventy-eight men and women with acute gonorrhea were treated by intramuscular administration of cefuroxime . Use of 1 g of cefuroxime plus 1 g of probenecid gave a cure rate of 95.5%, which compared well with that of a standard treatment of 5 x 10(6) units of intramuscularly administered benzyl penicillin plus 1 g of probenecid . The latter gave a cure rate of 97.2% in a concurrent series of 178 patients . A subsequent comparison of 163 patients who received 750 mg of cefuroxime plus 1 g of probenecid with 145 patients who received 1.5 g of cefuroxime alone showed cure rates of 95.1% and 97.2%, respectively . Only two cases of possible hypersensitivity to cefuroxime were found . It is concluded that cefuroxime is a valuable drug for single-session treatment of acute gonorrhea in both men and women. Arch Microbiol, 1980 Oct, 127(3), 297 - 9 Differentiation of mycoplasmatales from bacterial protoplast L-forms by assay for penicillin binding proteins; Martin HH et al.; Membrane proteins with the specific ability for binding penicillin with high affinity (penicillin binding proteins) were found to be present in two strains of the cell wall-less protoplast L-form of P.Mirabilis and were absent from different species of Mycoplasma and from Acholeplasma laidlawii . Thus, the assay for penicillin binding proteins appeared to be suitable for the differentiation of the cell wall-less procaryotes . The absence of penicillin binding proteins from the mycoplasmatales further confirmed the unrelatedness of this group to the bacteria. Br J Vener Dis, 1980 Oct, 56(5), 291 - 6 Quantitative microhaemagglutination assay for Treponema pallidum antibodies in experimental syphilis; Tight RR et al.; The quantitative microhaemagglutination assay for Treponema pallidum antibodies (MHA-TP) was studies in 52 untreated and treated rabbits with experimental syphilis . Rabbits with incubating experimental syphilis were cured or inadequately treated with penicillin G and some cured rabbits were later reinfected . MHA-TP conversion occurred within 45 days in untreated rabbits . Titres reached peak levels about four months after inoculation and remained relatively high for up to two years . The quantitative MHA-TP test differentiated between rabbits cured of experimental incubating syphilis and those untreated and inadequately treated . MHA-TP titres decreased after treatment given six or 12 months after inoculation but reversion did not occur . MHA-TP conversion or significant increases in titre occurred as soon as seven days after reinfection and preceded corresponding changes in a quantitative non-treponemal test . The MHA-TP is useful as a screening test for treponemal antibodies in rabbits . The quantitative MHA-TP in humans after treatment for syphilis and reinfection deserves further study. Br J Vener Dis, 1980 Oct, 56(5), 308 - 10 Sensitivity to penicillin of gonococci in different racial groups; Rodin P et al.; The distribution of the sensitivity to penicillin of gonococci isolated from 631 men and 290 women was analysed in relation to the racial origin of the patients and the type of source contact alleged by the men . No difference in the sensitivity patterns was found between strains from white patients from the United Kingdom and those from immigrants from the Caribbean area . Asian men harboured significantly more insensitive strains than men of other racial groups . Men of Caribbean stock who had been born in this country had significantly more infections due to fully sensitive strains . The reasons for these variations are not known, but one contributory factor may be differences within the racial groups in the proportions of infections contracted from prostitutes. Antibiotiki, 1980 Oct, 25(10), 730 - 4 {Nitrogen metabolism characteristics of P . chrysogenum in relation to penicillin biosynthesis}; Lur'e LM et al.; Quantitative correlation between the nitrogen level in the mycelium of P . chrysogenum and biosynthesis of penicillin was shown . With an increase in the nitrogen level of the mycelium, its productivity with respect to the formation of the antibiotic also increased . The high level of nitrogen in the mycelium is an obligatory but not sufficient parameter characterizing the penicillin production capacity of the mycelium . The content of acid soluble compounds in the mycelium was found to be important for estimation of its productivity . Intensively aerated mycelium contained much greater numbers of nitrogen labile forms and had higher productivity levels as compared to the mycelium grown under poor aeration. J Clin Gastroenterol, 1980 Sep, 2(3), 281 - 5 Salicylate hepatotoxicity: the potential role of hypoalbuminemia; Gitlin N; Seventeen patients suffering from an initial attack of acute rheumatic fever were studied during treatment with phenoxymethyl penicillin and salicylates (600 mg orally every 4 or 6 hours) . Elevated transaminase (SGOT) levels occurred in nine patients . The SGOT levels were directly related to serum salicylate levels (r = 0.668) and inversely to the serum albumin level (r = -0.418) . SGOT response was greater in patients with a serum albumin of less than 3.5 g/dl (P < 0.001) . In hypoalbuminemia, the ratio of free salicylate to bound salicylate rises and the free salicylate might be more active and thus more hepatotoxic even at relatively low total serum salicylate levels . In all patients with hypoalbuminemia of less than 3.5 g/dl, close monitoring the SGOT is advisable, especially if the level of total serum salicylate is 15 mg/dl or higher. Postgrad Med, 1980 Sep, 68(3), 207 - 10 Late sequelae of splenectomy for trauma; Neilan BA; Hematologic and immunologic changes following splenectomy for trauma include abnormal RBC morphology, leukocytosis, thrombocytosis, impaired clearance of blood-borne particulate antigens, and reduced antibody formation . These abnormalities may be the bases for overwhelming bacterial infection, the most serious delayed complication of splenectomy for trauma . The state of knowledge at present indicates that splenectomized patients should receive pneumococcal vaccination, but whether penicillin prophylaxis should be given daily in addition is less clear . However, penicillin may be advisable for young children, particularly those under 2 years of age, in whom the efficacy of pneumococcal vaccine has not been established . To prevent sepsis, various surgical alternatives to total splenectomy have been proposed, including deliberate autotransplantation of splenic tissue at the time of splenectomy. Biull Eksp Biol Med, 1980 Sep, 90(9), 367 - 70 {Ultrastructural characteristics of the dorsal hippocampus in rabbits with epileptiform seizures}; Semenov SP et al.; An increase in the medium size of mitochondria in synapses, postsynaptic dendrites and neurons of the dorsal hippocampus was recorded after single and 3fold intracortical injection of penicillin (1000 IE) to rabbits . An increase in the size of vacuoles was found in astrocytes, synapses and postsynaptic dendrites . Mitochondrial hypertrophy indicates the energy output intensification in the form of ATP, while the increased size of vacuoles points to a greater permeability . The changes disclosed evidence an activation of synapses, postsynaptic dendrites and neurons. Klin Padiatr, 1980 Sep, 192(5), 488 - 91 {A case of juvenile priapism (author's transl)}; Stosch M et al.; A case of juvenile priapism is presented following cortisone and penicillin treatment for a traumatic lesion of the oesophagus . Increased coagulability from such treatment is discussed as causative factor . The importance of early surgical intervention is stressed and the methods of choice presented. Am J Ophthalmol, 1980 Sep, 90(3), 380 - 4 Secondary syphilis with iris papules; Schwartz LK et al.; A 30-year-old man developed bilateral iridocyclitis with iris roseolae and papules three months after the rash of secondary syphilis . The inflammation resolved after treatment with penicillin, intramuscularly, topically given corticosteroids, and cycloplegics . The serum immune-complex levels were slightly increased . Iris angiography showed leakage of fluorescein in the region of the papules and roseolae and from the vessels of the pupillary margin . When the eye was clinically uninflamed, a follow-up angiogram showed leakage of fluorescein from the same areas, suggesting that the inflammatory effect on the iris vessels persisted in the region of the roseolae, the papules, and the sphincter vessels. Antibiotiki, 1980 Sep, 25(9), 655 - 9 {Determination of penicillins by means of an enzymatic electrode}; Kulis IuIu et al.; Penicillin sensitive enzyme electrodes were prepared on the basis of native penicillinase (EC 3.5.2.6) and penicillinamidase (CE 3.5.1.11), as well as penicillinase entrapped in a complex of polyethylenimine and polyacrylic acid or linked with albumin and lattice entrapped penicillinase . The time of the electrode response is 2-10 minutes . The electrode potential change within a minute is linear at 1-20 mM of benzylpenicillin and depends on the electrode type . The electrodes prepared on the basis of the native enzymes lost their sensitivity within the first 10 days . Sensitivity of immobilized penicillinase did not change for 15 days . The electrodes prepared on the basis of albumin-linked penicillinase preserved their high stability for 60 days . The sensitivity of these electrodes is slightly dependent on the phosphate buffer concentration (from 0.001 to 9 mM). MMW Munch Med Wochenschr, 1980 Aug 29, 122(35), 1184 - 90 {Drug-induced disturbances of the coagulation system (author's transl)}; Hiller E; Side-effects of longterm therapy on the coagulation system become manifest either as hemorrhages or as an increased risk of thromboembolism . The most frequent drug-induced coagulation defect is thrombopathia . The most important drug-induced plasmatic coagulation disorders are caused by anti-coagulants and therefore predictable . In patients exposed to hemorrhage risk, non-steroidal antiphlogistics are not contraindicated since they entail inhibition of platelet aggregation and prolonged hemorrhage time . High doses of penicillin G and the semisynthetic penicillins can lead to hemorrhage in patients with renal insufficiency . Corticosteroids and contraceptives however tend to induce hypercoagulability. Biochim Biophys Acta, 1980 Aug 11, 619(2), 258 - 66 Phosphatidylserine biosynthesis in mitochondria from Ehrlich ascites tumor cells; Baranska J; 1 . Isolated mitochondria of Ehrlich ascites tumor cells incorporated {14C}serine into phosphatidylserine and partly into its decarboxylation product, phosphatidylethanolamine, while phosphatidylserine was the sole product with microsomes . 2 . The incorporation of {14C}serine into mitochondrial phospholipids was stimulated by Ca2+ which indicated the operation of the Ca2+-dependent base-exchange mechanism, virtually absent in mammalian tissue mitochondria . The finding cannot be attributed to microsomal contamination . 3 . The incorporation of {14C}serine into mitochondrial phospholipids was also stimulated by ATP, both in the presence and in the absence of calcium-complexing agents . The stimulation by ATP was insensitive to penicillin and streptomycin, thus pointing that this process was not of bacterial origin . 4 . The latter process was further stimulated by phosphatidic acid and phosphatidic acid precursors, but not by CDP diacylglycerol . 32P from neither {gamma-32P}ATP nor {32P}phosphatidic acid was incorporated into phosphatidylserine in the presence of CTP and L-serine . The release of {14C}CMP from {14C}CDP diacylglycerol was not stimulated by l-serine . 5 . It is concluded that {14C}serine incorporation into mitochondrial phospholipids by ATP-dependent process does not fit to any of the pathways of phopholipid biosynthesis described so far. Dtsch Med Wochenschr, 1980 Aug 8, 105(32), 1121 - 3 {Administration of D-penicillamine instead of penicillin with fatal results: allergy of the delayed type with protracted shock as fatal complication of treatment with D-penicillamine for rheumatoid arthritis in a child (author's transl)}; Erkrath KD et al.; Following one-week treatment with D-penicillamine for rheumatoid arthritis a seven-year-old girl died with the clinical features of protracted circulatory shock . Several doctors had mis-diagnosed the skin changes and mistakenly prescribed penicillamine, given for the rheumatoid arthritis, instead of plenicillin at the latter's dosage . By the administration of penicillamine a hypersensitivity reaction of the delayed type had been induced which ended fatally due to severe shock. Hautarzt, 1980 Aug, 31(8), 444 - 6 {Simultaneous therapy of gonorrhea with penicillin and probenecid . Serum penicillin picture}; Petzoldt D et al.; 19 patient received penicillin and probenecid . The resulting serum concentrations of penicillin was determined . In regimen I 4 mill . IU depot penicillin was given i.m . simultaneously with 1 g probenecid orally . In regimen II probenecid was given 30 min prior to the administration of penicillin . In both series the average serum concentrations of penicillin were not significantly different (p = 0.01). Am J Gastroenterol, 1980 Aug, 74(2), 170 - 2 Diffuse enlargement of gastric folds as a manifestation of secondary syphilis; Morin ME et al.; A case of gastric lues with diffuse enlargement of gastric rugae is presented . Confirmation of the etiological role of the spirochete in producing this very unusual roentgen manifestation of syphilitic gastropathy was provided by recovery of the organism from the gastric mucosa and reversal of the clinical and roentgenographic aberrations by penicillin therapy alone . Diffuse hyperrugosity and erosive gastritis occurring in a patient with a reactive serologic test for syphilis should raise the possibility of luetic gastritis. J Physiol, 1980 Aug, 305, 297 - 313 Reduced inhibition during epileptiform activity in the in vitro hippocampal slice; Dingledine R et al.; 1 . Intracellular recordings were made from CA1 pyramidal cells in the hippocampal slice in vitro . The responses to orthodromic and antidromic activation and to ionophoretically applied GABA were studied . 2 . The epileptogenic agent sodium benzyl penicillin reduced the recurrent i.p.s.p . evoked by subthreshold antidromic stimulation . Reversal potential studies of the i.p.s.p . and resistance measurements showed that this reduction was mainly due to a decrease in i.p.s.p . conductance . 3 . Penicillin also reduced the conductance and associated membrane potential changes induced by ejecting GABA near the soma or into the apical dendritic region . 4 . The mixed e.p.s.p.-i.p.s.p . evoked by orthodromic stimulation was converted to a pure depolarizing potential as the i.p.s.p . was blocked . Concurrently the probability of discharge to a constant orthodromic stimulus was increased . Similar changes were seen in a low chloride solution . 5 . The time course of the reduction of inhibition was similar to that of the enhanced orthodromic response seen after penicillin treatment . 6 . We conclude that reduction of postsynaptic inhibition is partly responsible for the increased probability of orthodromic discharge caused by penicillin . The longer latency all-or-nothing burst seen in some cells, however, seems to require an additional mechanism, although reduced inhibition may facilitate the triggering of this burst. Tsitologiia, 1980 Aug, 22(8), 998 - 1000 {Controlled cell cultivation . V . The effect of various rubbers on the isolated neurons of Limnaea stagnalis in culture}; Arkhipov VV et al.; Various domestic rubbers were tested for toxicity to cultured isolated neurons of Lymnaea stagnalis, the survival time of these cells, and their morphological differentiation being used as criteria . According to the effect towards the neurons, the tested materials could be divided into inert, low-toxic, and toxic ones . Type 52336/4 silicon rubber, the rubber of surgical gloves, and dry rubber of "b" type produce no unfavourable effect on isolated neurons . Stoppers of penicillin bottles, baby's dummies, and silicon-based BgO-1 "Germetic" paste are low-toxic rubbers . By contrast, silicon rubbers of 52336 and 14p-6 types, KLT-30 silicon paste and black rubber of HO-68-1 type decreased sharply the survival time of the neurons and depressed their morphological differentiation in culture. Ann Allergy, 1980 Aug, 45(2), 100 - 3 The use of stereoisomers in patch testing; Voorhorst R et al.; A patient is described with a clinical picture resembling that of relapsing scarlatina . The complaints were found to be based on two types of delayed-type allergy: one to the equatorially bound hydroxyl grouip at the 6 position of the basic phenanthrene structure as occurs in morphine and codeine, and the other to the D(-)-alpha-position of the amino group as occurs in some penicillin derivatives. Epilepsia, 1980 Aug, 21(4), 369 - 78 The role of the corpus callosum in bilateral interhemispheric synchrony of spike and wave discharge in feline generalized penicillin epilepsy; Musgrave J et al.; In this study on interhemispheric synchrony of spike and wave discharges in feline generalized penicillin epilepsy, four groups of cats were treated in the following manner: Group A underwent complete section of the corpus callosum and anterior commissure; group B underwent division of the massa intermedia alone; group C underwent partial section of the corpus callosum; and in group D, a slab of the cortex on one side, comprising the middle parts of the lateral and suprasylvian gyri, was severed from all its subcortical inputs, without disturbing its connections with the opposite hemisphere through the corpus callosum . Two weeks after surgery or later the cats received an i.m . injection of penicillin . Bilateral synchrony of the epileptic discharges was abolished in group A, but not in group B . In group C, bilateral synchrony of the epileptic bursts was impaired, but not abolished . In group D, epileptic bursts synchronous with those occurring in the intact hemisphere continued to occur in the slab, but at lower amplitude . It is concluded that the corpus callosum is the main, if not the exclusive, pathway ensuring bilateral synchrony of the epileptic discharges of feline generalized penicillin epilepsy. Arch Intern Med, 1980 Aug, 140(8), 1117 - 8 Failure of penicillin G benzathine in the treatment of neurosyphilis; Greene BM et al.; Although penicillin remains highly effective in syphilis, important questions exist regarding the optimal regimen for syphilitic involvement of the nervous system . Progression of neurosyphilis despite 7.2 million units of penicillin G benzathine occurred in the case reported here, with subsequent resolution following high-dose intravenous aqueous penicillin therapy . This and other recent reports support the conclusion that neurosyphilis should be treated with higher amounts of penicillin than is provided by the benzathine regimens. Proc Natl Acad Sci U S A, 1980 Aug, 77(8), 4499 - 503 On the process of cellular division in Escherichia coli: isolation and characterization of penicillin-binding proteins 1a, 1b, and 3; Tamura T et al.; Multiple mutants of Escherichia coli defective in penicillin-binding proteins (PBPs) were constructed, and into these strains Co1E1 plasmids carrying the genes for PBP-1a, -1b, or -3 were introduced . From these plasmid-carrying strains, PBP-1a and -1b were purified by ampicillin-Sepharose affinity chromatography and PBP-3 by cephalexin-Sepharose affinity chromatography . Improved purification was achieved by differential elution with NH2OH . Purified PBP-1b synthesized murein when added to the membrane fraction of a PBP-1b-defective mutant, which by itself failed to support murein synthesis in vitro . The PBP-1b preparation was able to synthesize murein from the lipid intermediate extracted with chloroform/methanol but was unable to utilize UDP-linked precursors for murein synthesis . Murein synthesis was inhibited by vancomysin, ristocetin, moenomycin, and enduracidin, but not by beta-lactam antibiotics . The synthesized murein was shown to contain crosslinked muropeptides . Their crosslinking was abolished by action of beta-lactam antibiotics . The PBP-1a and -3 preparations showed substantially no activity for murein synthesis in the same reaction system . None of the three PBPs showed D-alanine carboxypeptidase activity with UDP-N-acetylmuramoyl-pentapeptide as substrate or endopeptidase activity with bis(disaccharide-peptide) as substrate. J Infect Dis, 1980 Aug, 142(2), 265 - 72 Direct stimulation of lymphokine production by cephalothin; Larson SE et al.; Cephalothin significantly suppressed in vitro DNA and total protein synthesis in human peripheral blood lymphocytes stimulated by antigens or mitogens . However, similar concentrations of this antibiotic enhanced streptokinase-streptodornase-stimulated production of the lymphokine leukocyte-migration-inhibition factor (LMIF) and directly stimulated production of this lymphokine by otherwise unstimulated lymphocytes from 10 of 12 normal human subjects . Penicillin did not appear to produce these effects . Cephalothin did not interfere directly with neutrophil migration or the interaction of preformed LMIF with neutrophils . Stimulation of LMIF production by cephalothin required viable lymphocytes and was inhibited by puromycin . These results suggest that cephalothin is capable of inducing lymphokine production by human lymphocytes in a manner that appears to be nonspecific in nature . This type of effect could be the basis of some apparently immunologic reactions to this antibiotic. J Clin Invest, 1980 Aug, 66(2), 243 - 53 Cerebrospinal fluid outflow resistance in rabbits with experimental meningitis . Alterations with penicillin and methylprednisolone; Scheld WM et al.; Acute bacterial meningitis may be associated with increased intracranial pressure, neurological sequelae such as communicating hydrocephalus, and a slow response to antibiotic therapy . Alterations in cerebrospinal hydrodynamics are at least partially responsible for these complications . Constant, low-flow short-duration manometric infusion studies through a hollow-bore pressure monitoring device in direct continuity with the supracortical subarachnoid space were performed in rabbits with experimental meningitis . Maximal resistance to cerebrospinal fluid (CSF) outflow from the subarachnoid to vascular space was markedly increaed in acute pneumococcal meningitis when compared to control, uninfected animals (6.77 +/- 3.52 vs . 0.26 +/- 0.04 mm Hg/microliter per min, P less than 0.001) . Similar elevations (8.93 +/- 4.15 mm Hg/microliter per min were found in experimental Escherichia coli meningitis . Despite eradication of viable bacteria from the CSF by penicillin therapy during the acute stage of pneumococcal meningitis, resistance remained elevated (6.07 +/- 4.68 mm Hg/microliter per min) and had not returned to normal up to 15 d later . Administration of methylprednisolone during the early stages of acute pneumococcal meningitis reduced mean peak outflow resistance towards control values (0.59 mm Hg/microliter per min) and no "rebound" effect was apparent 24 h later . These hydrodynamic alterations in experimental meningitis prevent normal CSF absorption and decrease the ability of the bran to compensate for changes in intracranial volume and pressure. Br J Vener Dis, 1980 Aug, 56(4), 230 - 4 Induction of a cell wall variant of the gonococcus by human amylase; Mellersh A et al.; Human amylase has been shown to be an effective and powerful inhibitor of the gonococcus in vitro . Its action appears to be on the bacterial cell wall . When tested in osmotically stabilised liquid media the organism was not inhibited; however the organisms which grew in such cultures appeared to be cell wall variants, which were less sensitive to penicillin than the parent strains . Studies on these variants suggest that they are "transitional-phase variants." Since cervical mucus has much in common with an alkaline osmotically stabilised liquid medium and also contains a high concentration of amylase, it seems possible that these variants may occur in vivo. Riv Neurol, 1980 Jul-Aug, 50(4), 253 - 68 {Effect of gamma-amino-beta-hydroxybutyric acid (GABHB) on experimentally-induced epileptic activity}; Chemello R et al.; Effects of GABOB on experimental induced epileptiform activities . Antiepileptic activity of gamma-amino-beta-hydroxybutyric acid (GABOB) has been tested on different models of either generalized or focal epilepsy induced by penicillin in cat . In acute experiments, topical application to the cortex of GABOB (from 1% to 10%) during feline generalized epilepsy produced a reverse in polarity of the spike and wave complex, while in the so called "epileptogenic corticopathy" it induced a decrease in voltage as well as in frequency of the bilateral spikes and polyspikes . A similar effect was seen after parenteral injection of GABOB in acute preparations in which a penicillin focus was created . In chronic animals, in which feline generalized penicillin epilepsy had been produced, a single i.v . injection of GABOB induced a significant decrease of the epileptic bursts during the first 30' after the antiepileptic drug was injected . Finally in 4 animals chronic administration of GABOB leaded to a mean decrease of the epileptic bursts higher than 50% . These data support the antiepileptic activity of GABOB . However the high doses used in this study to achieve the antiepileptic effect could make difficult its use in human patients. Can J Surg, 1980 Jul, 23(4), 343 - 5 Symposium on trauma . 3 . Major problems in blunt and penetrating abdominal trauma; Walt AJ; Many pitfalls exist in treating patients with blunt and penetrating wounds of the chest and abdomen . The thoracic and abdominal cavities should not be dissociated in the examiner's mind because apparently trivial lesions of one may be associated with serious lesions of the other . Constellations of injuries should be sought, especially in blunt and seat-belt injuries . Life-threatening damage may not be clinically obvious for days or even weeks . Peritoneal lavage, while valuable, should be carefully interpreted . Splenic injury is treated much more conservatively today than in the past with strenuous attempts made to preserve all or part of the organ . When splenectomy is unavoidable, decisions about the need for penicillin and pneumococcal vaccine are important and should include dose and frequency . Liver injuries are also treated more conservatively . Lobectomy is seldom necessary as assiduous local hemostasis and debridement (accompanied in about 3% of cases by ligation of the hepatic artery) are effective when good exposure and preliminary measures to achieve temporary hemostasis are obtained. Psychiatr Neurol Med Psychol (Leipz), 1980 Jul, 32(7), 443 - 6 {Embolitic lumbar artery occlusion following benzathinpenicillin (penduran) . A case contribution to Nicolau syndrome in adults}; Gebert K; On the basis of a case report, Nicolau's syndrome after I . M . injection of benzathine penicillin to a 33-year-old woman is dealt with . Pathogenetic mechanisms of this extremely rare complication in adults are discussed. Chem Biol Interact, 1980 Jul, 31(1), 113 - 32 cis-Platinum(II) amine complexes: some structure-activity relationships for immunosuppressive, nephrotoxic and gastrointestinal (side) effects in rats; Broomhead JA et al.; A local graft-versus-host reaction was established to elicit lymphoid hypertrophy in F1 hybrid PVG X Lew rats . cis-Di(amine)platinum(II) complexes were given i.p . on days 1--4 in divided doses . Overnight proteinuria and measurements of renal hypertrophy on day 5 reflected the nephrotoxicity of the test compound . Stomach weights indicated the peculiar effect on pyloric stasis causing gastric distension . Weights of thymus' and spleens together with lymph-nodes showed the lymphodepressant/immunosuppressive properties of platinum compounds . Structure activity relationships for immunosuppressant, nephrotoxic and gastric-distending activities were investigated with: (a) cis-diaquo, cis-hydroxyaquo- and cis-dichlorodi(amine)platinum(II) complexes; (b) dinuclear mu-dihydroxo-bridged di(amine)platinum(II) complexes; (c) carboxylatodi(amine)platinum(II) complexes . Nephrotoxicity was minimised (with retention of immunosuppressant activity) by (a) the use of certain N-substituted amines e.g . Dach, Me4en; (b) co-administration of selected adjuncts e.g . citrate, salicylate; (c) auxiliary treatment with a penicillin mixture (Triplopen) . In vitro effects of some platinum(II) compounds on isolated rat kidney tubules were also investigated. J Bacteriol, 1980 Jul, 143(1), 531 - 4 A mutant of Escherichia coli defective in penicillin-binding protein 5 and lacking D-alanine carboxypeptidase IA; Nishimura Y et al.; A mutant of Escherichia coli defective in penicillin-binding protein 5 activity was isolated . The mutation (pfv) was shown to be located at 14.0 min on the E . coli chromosome map . Loss of penicillin-binding protein 5 in the pfv mutant was associated with the loss of D-alanine carboxypeptidase IA activity and increased sensitivity to beta-lactam antibiotics . We conclude that penicillin-binding protein 5 catalyzes the major D-alanine carboxypeptidase IA activity and that the enzyme activity, in vivo, protects E . coli cells from killing by low inhibitory concentrations of beta-lactam antibiotics. Oral Surg Oral Med Oral Pathol, 1980 Jul, 50(1), 30 - 2 Dental drugs and anaphylactic reactions . Report of a case; Gill C et al.; The patient described here experienced an acute anaphylactic reaction after receiving parenteral lidocaine, oral aspirin, codeine, and penicillin following routine dental treatment . The patient had taken all of the drugs previously with no untoward effects . The incidence and mechanisms of drug-induced hypersensitivity reactions are discussed . The importance of monitoring the patient following drug administration, even in the case of a negative medical and drug history, is discussed. Antimicrob Agents Chemother, 1980 Jul, 18(1), 69 - 76 Biliary elimination of mezlocillin: an experimental and clinical study; Brogard JM et al.; The biliary elimination of mezlocillin, a new semisynthetic penicillin of the acyl-ureido-penicillin group, was investigated in vitro in rabbit liver preparations and in vivo in humans . Experimentally, mezlocillin recovery in the bile during perfusion of isolted rabbit liver (3 h; n = 5) averaged 20.3% of the administrered dose (10 mg) . The mean peak concentration in the bile (758 +/- 129.3 micrograms/ml) was reached between 0.5 and 1 h . Biliary clearance was 169 ml/h . In healthy subjects (n = 5), the concentrations of antibiotic measured in the duodenal fluid during a period of 4 h after intravenous administration of 5 g of mezlocillin ranged between 440 and 637 micrograms/ml . In 10 cholecystectomized patients provided with a T-tube, intramuscular injection of 1 g of mezlocillin resulted in a biliary peak concentration of 295.7 +/- 58.1 micrograms/ml . Mean total amount of antibiotic eliminated in the bile over 12 h corresponded to 2.6% of the administered dose . Assays performed during surgery after intravenous administration of 2 g of mezlocillin (n = 10) showed antibiotic activity of 895 +/- 196 micrograms/ml in the common duct bile and 402 +/- 133 micrograms/ml in the gallbladder bile . These data were compared with the values determined for 11 other beta-lactamines studied under identical conditions. Neurosci Lett, 1980 Jul, 18(3), 309 - 12 Inhibition of GABA and benzodiazepine receptor binding by penicillins; Antoniadis A et al.; Penicillins are thought to be GABA receptor antagonists . In order to determine the affinities of various penicillin derivatives for the GABA receptor, their potencies as inhibitors of specific {3H}GABA binding to rat brain membranes were investigated . All investigated penicillins inhibit specific {3H}GABA binding, with IC50 values ranging from 2 to 60 mM . The results are consistent with the assumption that penicillins are weak GABA receptor antagonists. Ann Neurol, 1980 Jul, 8(1), 71 - 3 Benzodiazepine receptor interactions may be involved in the neurotoxicity of various penicillin derivatives; Antoniadis A et al.; The interaction of seven penicillin derivatives with specific {3H}flunitrazepam binding to benzodiazepine receptors was investigated . The affinities of the penicillins for benzodiazepine receptor seemed to depend on the lipophilia of the derivatives . The concentrations of the penicillins which inhibit specific {3H}flunitrazepam binding are consistent with penicillin levels found in the central nervous system of patients developing penicillin induced convulsions . The results suggest that penicillins inhibit GABAergic transmission not only at the GABA receptor, but also at the benzodiazepine receptor, which is thought to be part of a neuronal system facilitating GABAergic transmission . Both mechanisms may account at least in part for the convulsive not neurotoxic properties of penicillins. JAMA, 1980 Jun 27, 243(24), 2500 - 2 Treatment of primary and secondary syphilis . Serological response; Fiumara NJ; One hundred thirty-eight patients with primary syphillis and 161 patients with secondary syphilis were treated with penicillin G benzathine, 2.4 million units given intramuscularly weekly for two weeks, for a total of 4.8 million units . All 138 patients with primary syphilis had a rapid resolution of their lesions, and all became seronegative within one year . Similarly, the 161 patients with secondary syphilis were cured clinically, and all achieved seronegativity within 24 months. Brain Res, 1980 Jun 23, 192(2), 495 - 512 The effects of convulsant doses of penicillin on primary afferents, dorsal root ganglion cells, and on 'presynaptic' inhibition in the spinal cord; Kinnes CG et al.; Intracellular recordings were made from neurons in dorsal root ganglia (DRG) of rats, isolated in vitro . The depolarization of DRG cells caused by the application of gamma-aminobutyric acid (GABA) diminished reversibly when penicillin (0.08--2.0 mM) was added to the bathing fluid . The decrease of the input resistance of DRG cells measured during GABA perfusion was also depressed in the presence of penicillin, but no evidence of a shift of the reversal potential of the GABA-induced depolarization was found . Nor did penicillin (up to 10 mM) cause a change in the voltage-current function, in electrical excitability, in the inclination to repetitive firing, bursting discharge, or after discharge . In decapitate cat preparation the amplitude of the negative dorsal root potential (DRP or DR V) diminished by 0--50% after the i.v . administration of 0.5--1.0 X 10(6) I.U./kg (the convulsant dose) of penicillin . Post-tetanic depression of the DRP was aggravated by penicillin . The degree of depression of the DRP bore no relationship to the promptness of the eruption, and to the intensity, of the seizure activity induced by penicillin . The rates of rise and fall of the negative DRP (DR V) were consistently slowed, the positive DRP (DR VI) reduced, and the dorsal root reflex (DRR) blocked by penicillin . Inhibitory reflex effects presumed to be presynaptic were either enhanced or unchanged, never depressed by penicillin . This was seen when inhibitory function was gauged by monosynaptic reflex amplitude, and also from the inhibition of ventral root electrotonic excitatory postsynaptic potentials (VP EPSPs) . Possible explanations of these seemingly paradoxical findings are discussed, with arguments in favor and against each. Science, 1980 Jun 13, 208(4449), 1264 - 5 Kindling induces long-lasting alterations in response of hippocampal neurons to elevated potassium levels in vitro; Oliver AP et al.; The cellular basis of kindling was studied electrophysiologically with slices of guinea pig hippocampus . Normally, epileptiform activity can be induced in the slices only by combined exposure to elevated potassium levels and a chemical convulsant such as penicillin . In hippocampal slices from pentylenetetrazole-kindled animals, however, elevated potassium alone can induce seizures . These data suggest that kindling elicits long-term changes in neuronal excitability that may involve ionic mechanisms. Jpn J Antibiot, 1980 Jun, 33(6), 690 - 2 {Effectiveness of amoxicillin as a potent antiluetic in the treatment of syphilis (author's transl)}; Munemitsu H et al.; A daily dose of 1.0 approximately 1.5 g of amoxicillin, a synthetic penicillin, was tried as an antiluetic in 9 cases of syphilis . Oral administration for 4 weeks makes up one course of treatment . One of the patients was given two courses of treatment . Amoxicillin showed effect in 6 patients out of 9 (66.7%) . Constipation and diarrhoea were observed in two cases and one case as side effects, and they were controlled easily . Amoxicillin could be a very effective and safe antiluetic. Acta Orthop Scand, 1980 Jun, 51(3), 451 - 7 Acute haematogenous osteomyelitis and septic arthritis in childhood . A 10-year review and follow-up; Petersen S et al.; Seventy-three children, who were admitted to hospital during the period 1965-1976 with osteomyelitis or septic arthritis, were included in a retrospective study as well as a clinical and radiological follow-up . Ten cases of osteomyelitis occurred during the neonatal period and about half of the cases of osteomyelitis and septic arthritis occurred before the age of 2 years . Staph . aureus was the dominating pathogen isolated and half of the strains were penicillin-resistant . The group of children with osteomyelitis who were given early treatment, i.e . within 1 week, against penicillin-resistant Staph, aureus had a higher clinical cure rate after 1 month (0.01 < P < 0.025) compared with the rest of the children . Five children developed recurrent or chronic osteomyelitis . An early follow-up in 69 children 1-11 years after the disease showed that none had any complaints or invalidity . However, one patient with neonatal septic arthritis presented severe dysplasia and subluxation of the hip and four children with osteomyelitis had severe, but asymptomatic, radiological changes. South Med J, 1980 Jun, 73(6), 745 - 8 Neutropenia induced by semisynthetic penicillin; Carpenter J; The semisynthetic penicillins, like the parent drug penicillin G, are remarkably safe drugs . However, a significant number of patients have been reported in whom profound neutropenia has developed . This is a side effect of these drugs not appreciated by a significant number of physicians . I report two more cases of neutropenia due to nafcillin and review the literature on neutropenia induced by semisynthetic penicillin . The relative risk of each individual drug is evaluated, and the two proposed mechanisms of production of the neutropenia are discussed. J Allergy Clin Immunol, 1980 Jun, 65(6), 465 - 6 Acute laryngeal hemorrhage with laryngeal obstruction initially confused with penicillin anaphylaxis; Grammer L et al.; A case of acute laryngeal obstruction was considered to be penicillin anaphylaxis because the onset followed penicillin administration . The laryngeal obstruction was found to be the result of laryngeal hemorrhage in a patient on chronic anticoagulant therapy . The hemorrhagic lesions appeared to be induced by coughing due to bronchitis for which the penicillin was given. Neurology, 1980 Jun, 30(6), 575 - 81 Anticonvulsant effects of muscimol; Collins RC; Muscimol is a potent agonist at GABA-inhibitory synapses in mammalian brain . Given systemically at 7 mumol per kilogram, it blocks topical penicillin seizures and delays the onset of generalized metrazol convulsions in rats . It has no effect against generalized seizures caused by picrotoxin or strychnine . Higher doses of muscimol cause bradykinesia, ataxia, catatonic posturing, and slowing of the electroencephalogram . When applied topically to cortex, muscimol blocks focal penicillin, bicuculline, and picrotoxin discharges in a dose-response relationship . It has no effect against topical strychnine . Muscimol offers a potential new approach to the treatment of epilepsy. Int J Oral Surg, 1980 Jun, 9(3), 166 - 72 Value of penicillin in the prevention of pain, swelling and trismus following the removal of ectopic mandibular third molars; Macgregor AJ et al.; A double-blind randomised placebo-controlled study of the value of systemic penicillin in preventing pain, swelling and trismus following the removal of impacted mandibular third molars and indicates that penicillin may be used justifiably in the more difficult cases. Plast Reconstr Surg, 1980 Jun, 65(6), 798 - 804 Evaluation of burn blister fluid; Heggers JP et al.; Although edema is evident immediately after a burn, the diffusion of nutrient chemical constituents of the body is not impaired . Blister fluid, not unlike plasma or serum, contained all substances found in the body, including parenterally administered penicillin . The elevation of potassium and the cation to anion imbalance is primarily due to the Na/K cellular pump malfunction, and the destruction of the permeability of the cell membrane is most likely a direct result of complement and other cellular enzymes, which include the prostaglandins and thromboxanes . The elevated SGOT, CPK, and LDH indicated severe trauma to the cells in the immediate area of burn and possibly to the skeletal muscle . The presence of immunoglobulins indicated that high-molecular-weight proteins diffuse equally well during this edematous phase (IgM, 900,000; IgG, 190,000) . Evidence of this nature strongly suggests that the integrity of the burn blister by maintained. Sem Hop, 1980 May 18-25, 56(19-20), 979 - 82 {Inflammatory rheumatic disorders during the course of secondary syphilis (author's transl)}; Taillandier J et al.; A 46-year-old man presented signs of secondary syphilis, including a skin eruption, multiple adenopathies, and alopecia . The diagnosis was confirmed by positive serological and Nelson's tests . Inflammatory arthritic signs developed in a few joints two weeks after the onset of the skin eruption, affecting mainly the left wrist, right sternoclavicular joint, lumbar spine, and right shoulder and hip joints, which were painful and stiff . Tests for a rheumatic origin, especially urethral smears and HLA B27 antigen, were negative . The articular manifestations disappeared completely after 8 to 10 days of penicillin . Rheumatic disorders from secondary syphilis affect one or several of the large joints, and quite frequently the sternoclavicular joints, the clinical, radiological, and biological characteristics showing no particular features . Diagnosis is based on the exclusion of other causes for the rheumatic disorder, total rapid regression after penicillin alone, and the simultaneous appearance of the affections. Philos Trans R Soc Lond B Biol Sci, 1980 May 16, 289(1036), 285 - 301 The active centres in penicillin-sensitive enzymes; Ghuysen JM et al.; The interaction between beta-lactam antibiotics and the penicillin-sensitive enzymes is a multiple-step process . Binding of the beta-lactam ring of the penam (or 3-cepham) nucleus occurs at binding site no . 1 . Interaction between the N-14 substituent of the bound molecule and binding site no . 2 induces changes in binding site no . 1 . In turn, the catalytic site thus created increases the chemical reactivity of the beta-lactam amide bond . As the beta-lactam ring opens and acylates an enzyme serine residue, the interaction between the thiazolidine (or dihydrothiazine) ring and binding site no . 3 stabilizes the acyl-enzyme complex . Enzyme regeneration slowly proceeds either by direct elimination of the penicilloyl moiety or via C-5-C-6 splitting of the bound metabolite . The fragment arising from thiazolidine yields free N-formyl-D-penicillamine while the enzyme-linked N-acylglycyl fragment is immediately attacked by an exogenous nucleophile correctly positioned on the acceptor site . Similarly, the enzyme action on L-X-D-Ala-D-Ala terminated peptides is mediated via a binding site no . 1 that combines with D-Ala-D-Ala, a binding site no . 2 that interacts with the side chain of the preceding L-residue, an inducible catalytic site and an acceptor site . Enzymes are known that form a transitory L-X-D-Ala-enzyme complex where the acyl group is ester-linked to the same serine residue as that involved in the formation of the penicilloyl-enzyme complex (Waxman et al., this symposium) . Other enzymes, however, may function as catalyst templates . Depending on the enzymes, the independence of the beta-lactam and L-X-D-Ala-D-Ala active centres is more or less pronounced. Philos Trans R Soc Lond B Biol Sci, 1980 May 16, 289(1036), 273 - 83 Biochemical and genetical approaches to the mechanism of action of penicillin; Spratt BG; Since the discovery in 1965 that penicillin inhibits the transpeptidation reaction in peptidoglycan synthesis, a considerable effort has been put into the purification of enzymes that catalyse this reaction . This has resulted in the recognition that bacteria possess multiple forms of these penicillin-sensitive enzymes and has made it difficult to identify the precise target that penicillin inactivates to kill the organism . Recently penicillin-sensitive enzymes have been detected and studies as penicillin-binding proteins on sodium dodecyl sulphate polyacrylamide gels . The availability of this convenient method for identifying penicillin-sensitive enzymes has allowed biochemical and genetical approaches to be used to dissect their roles in the lethal effects of penicillin and other beta-lactam antibiotics . Three penicillin-binding proteins (1 B, 2 and 3) have been identified as killing targets for penicillin in Escherichia coli, whereas four other binding proteins are not implicated in the mechanism of action of the antibiotic . The complex biological effects that beta-lactam antibiotics produce on the growth of E . coli can be explained by their interaction with the three killing targets . Progress in the correlation of penicillin-binding proteins with penicillin-sensitive enzymes and in the development of strains of E . coli that overproduce penicillin-binding proteins is discussed. J Am Vet Med Assoc, 1980 May 15, 176(10 Spec No), 1054 - 60 Pharmacotherapeutics of newer penicillins and cephalosporins; Powers TE et al.; The beta-lactam group of compounds includes a large number of biologically active substances . Some are important as antibiotics (penicillin and cephalosporins) or antibiotic precursors (6-aminopenicillanic acid) and some are important due to their inhibitory action on several beta-lactamases . The pharmacologic features of these compounds are discussed on the basis of their structure, mechanism of action, pharmacokinetics, therapeutics, toxicologic properties, interaction, and incompatibilities. J Biol Chem, 1980 May 10, 255(9), 3824 - 5 Cation/proton antiport systems in Escherichia coli . Absence of potassium/proton antiporter activity in a pH-sensitive mutant; Plack RH Jr et al.; Alkaline-sensitive strains of Escherichia coli were selected by mutagenesis followed by penicillin killing in medium at pH 8.3 . One such strain was found to lack K+/H+ exchange . At neutral pH, the doubling time of the mutant was not significantly different from that of the parent, but at pH 8.3 the doubling time of the mutant increased over 5-fold . No energy-dependent uptake of 204Tl+ was observed in the mutant, but addition of the K+/H+ exchanger Nigericin resulted in identical 204Tl+ uptake in the mutant and parent . These results are consistent with the hypothesis that the K+/H+ antiporter is responsible for regulation of cytosolic pH in E . coli . In the absence of antiporter, the organism would be unable to grow at alkaline pH due to alkalinization of the cytosol. Dtsch Med Wochenschr, 1980 May 2, 105(18), 635 - 9 {Clinical significance of positive penicillin test reactions (author's transl)}; Haneke EG et al.; Epicutaneous, scratch and intracutaneous tests with various penicillins and their major as well as minor determinants were performed on 495 patients either because they were suspected of having a penicillin allergy, or in order to exclude such allergy, or before starting penicillin treatment, or because they suffered from chronic recurrent urticaria . A positive test reaction occurred in 25%: 44% among those with a history pointing to penicillin allergy and 17.8% among those who were tested before treatment to exclude penicillin allergy . Positive reactions also occurred in 11% of patients with chronic recurrent urticaria, but in practically all instances were clinically without significance . D-Penicillamine (Metalcaptase) and penicilloyl-polysine in the intracutaneous test, penicillin-G-sodium and ampicillin in the epicutaneous test gave the highest incidence of positive reactions. Acta Physiol Scand, 1980 May, 109(1), 27 - 36 Topical application of penicillin into hippocampal in vitro slices: A methodological study using benzyl (14C) penicillin; Olofsson S et al.; A gas pressure system is employed for topical application of pico/nanolitre volumes of 9 mmol/l benzyl (14C) penicillin into guinea-pig in vitro transverse hippocampal slices . Control of pressure pulse parameters enables ejectates, computed after liquid scintillation, from 10 micrometer, 5 micrometer and 2 micrometer pipettes with high reliability of ejection . A detailed study was done on the ejection performance of 5 micrometer and 2 micrometer pipettes . It shows that for the 5 micrometer tips, with the chosen ejection parameters, feeding pressure = 0.5 MPa, feeding pulse duration 50 ms, a 99% ejection incidence was obtained (n = 200) . The mean volumes ejected were 0.12 and 0.5 nl (n = 50) for one and four pulses delivered respectively . The corresponding ejectate means obtained from five 2 micrometer pipettes given a feeding pressure of 1.5 MPa, and a feeding pulse duration of 70 ms, were 0.04 and 0.13 nl . Statistical evaluation of the individual pipette ejection performances gave characteristic regression slopes within each pipette group . A comparison between visually controlled injection into oil and injection into slice, showed a close correspondence . The applicability of the ejection method is discussed in relation to functional studies on the conversion of single neurones into "epileptic" ones. J Am Acad Dermatol, 1980 May, 2(5), 388 - 92 Secondary syphilis with acute meningitis and quadriparesis; Lichten GD et al.; This report describes a case of secondary syphilis presenting with an atypical cutaneous eruption and acute spastic quadriparesis . The etiology of the cutaneous and neurologic manifestations was obscure until cerebrospinal fluid (CSF) studies revealed pleocytosis, elevated protein, and a positive CSF, VDRL, and fluorescent treponemal antibody (FTA) . These findings, correlated with the histologic presence of plasma cells in the dermal infiltrate, indicated secondary syphilis with acute syphilitic meningitis as the cause of the patient's illness . Therapy with intravenous penicillin, 20 million units daily for 3 weeks, resulted in almost complete recovery. Fiziol Zh SSSR Im I M Sechenova, 1980 May, 66(5), 650 - 7 {Suppression of epileptiform activity by micropolarizing brain structures}; Tsukunov SG et al.; Penicillin administration elicited epileptiform responses whereas micropolarization (MCP) affected the epileptogenic foci in cats with indwelled electrodes and chemotrodes . Three types of experimental epilepsy models were obtained: focal petit mal seizures, adversive, and grand mal seizures . The MCP of amygdala and caudate nucleus completely suppressed all three types of seizures whereas MCP of hippocampus enhanced the pathology . Two mechanisms of seizure suppression seem to exist: the inhibitory and the activating ones. Brain Res, 1980 Apr 7, 187(1), 165 - 82 Extracellular calcium and potassium changes in hippocampal slices; Benninger C et al.; Ca2+ and K+ ion sensitive microelectrodes were used to measure changes in ionic activities in the CA1 region of hippocampal slices during orthodromic (stratum radiatum) stimulation . Baseline levels of {K+}o and {Ca2+}o were those of the bathing medium which contained 5 mM K+ and 2.0 mM Ca2+ . During stimulation {K+}o rose to maximal levels of 12 mM while {Ca2+}o decreased to as low as 1.4 mM . Systematic alterations in extracellular field potentials in stratum pyramidale accompanied the ionic shifts . Following stimulation K+ undershoots occurred . An active K+ uptake mechanism was demonstrated using iontophoretic K+ pulses . {K+}o and {Ca2+}o changes occurred in parallel and in a laminar distribution with maximal changes recorded in stratum pyramidale . Maximal {K+}o changes occurred from baselines of 5 mM and declined progressively at higher baseline levels . During epileptiform activity produced by exposure of slices to penicillin, larger ionic shifts with a more rapid onset occurred . The alterations in {K+}o and {Ca2+}o in the hippocampal slice are similar in some respects to those obtained by stimulation in vivo, making this preparation a potentially useful one for determination of mechanisms and effects of alterations in the ionic microenvironment. Poult Sci, 1980 Apr, 59(4), 758 - 69 The utilization of rye by growing chicks as influenced by calcium, vitamin D3, and fat type and level; Antoniou T et al.; Four experiments were conducted with growing chicks to study the effects of feeding rye and wheat diets supplemented with different calcium levels, two types and two levels of fat, and increasing levels of vitamin D3 and to study the interrelationships of these dietary ingredients on chick performance . In Experiment 1, feed conversion efficiency was reduced to a much greater extend (10% vs . 1%) when tallow replaced soybean oil in a rye-based diet containing only .6% calcium compared to a wheat-based diet . When the dietary calcium was increased to 1.1% the replacement of tallow by soybean oil resulted in only a small reduction in feed efficiency for chicks fed either the rye-(3%) or wheat- (1%) based diets . The retention of fat, particularly tallow, was depressed in rye as compared to wheat-fed birds . Fat retention was also influenced by calcium levels . Increasing the dietary calcium from .6 to 1.1% improved tallow (16%) and depressed (7%) soybean oil retention in rye-based diets, whereas in wheat-based diets the retention for both fats was slightly decreased . Experiment 2 showed that the efficiency of utilization of rye diets containing 7.5% tallow was improved by 10% when the level of dietary calcium was increased from .6 to 1.1% while the corresponding improvement in similarly formulated wheat diets was only 1% . The improvement of 2.5% fat, however, was only about 3% for both wheat and rye diets . The results from Experiment 3 showed that in the presence of a large excess of vitamin D3, the depression in the efficiency of utilization of the wheat diet was 13% but was less than 1% for the rye diet . This indicates that rye contains a factor that depresses vitamin D3 absorption . In Experiment 4, when dietary calcium was increased from .80 to 2.00% or when penicillin (200 mg/kg) was added, the improvement in efficiency of feed utilization was greater in chicks fed a rye diet (7%) compared to those fed a wheat diet (1%) . The rye diets, however, were always less efficiently utilized than the corresponding wheat diets . Vitamin D supplementation, in contrast, did not affect chick performance . These results show that the performance of chicks fed rye diets is markedly influenced by type and level of dietary fat and the level of dietary calcium. J Chromatogr Sci, 1980 Apr, 18(4), 186 - 90 A GLC and GC/MS study of the reaction between benzylpenicillin and BF3-methanol; Hoyt AM Jr et al.; A study of the reaction of BF3-methanol with benzylpenicillin showed that penicillin could be converted to a form suitable for gas-liquid chromatography . This study indicated possible use of the reaction in an analytical method for penicillin, by determining the methyl phenylacetate product . A reaction rate and yield study was conducted using gas-liquid chromatography employing an internal standard for improved measurement accuracy . The reaction gave a relatively constant yield of 70 +/- 2% and was complete in less than 1 minute . Investigations of the identity of side products were conducted using GC/MS, UV, and IR . A variety of products, including penicillenates, penillates, penilloates, and acrylic acid esters, were indicated at very mild reaction conditions. Anesthesiology, 1980 Apr, 52(4), 330 - 4 Ketamine-induced changes in regional glucose utilization in the rat brain; Nelson SR et al.; Ketamine appears to induce both excitatory and depressant actions in the brain; however, it is not clear which regions are affected . The 2-deoxyglucose functional mapping method of Sokoloff et al . was used to determine regional variations in metabolic activity of rat brain caused by injection of ketamine, 25-75 mg, intramuscularly . To compare the effects of ketamine with those of hippocampal-induced seizures, the 2-deoxyglucose method was used, following injection of penicillin G, 400-800 units, into the hippocampus . The findings from five control, seven ketamine-treated, and three penicillin G-treated rats are given . Ketamine caused a significant increase of metabolic activity in the hippocampal sulci and a decrease of activity in the medial geniculate and the inferior colliculus . Similar changes were found with hippocampal seizures caused by penicillin . The inhibition of the regions associated with sensory systems (medial geniculate and inferior colliculus) may account in part for the anesthetic action of ketamine, while the intense activity of the hippocampus may be related to the excitatory manifestations . The results indicate that ketamine produces seizures in the hippocampus, which in turn inhibit auditory and visually associated nuclei . Thus, the anesthesia may follow from the sensory depression and the cataleptic phenomena may be related to the hippocampal excitation. Clin Pharmacol Ther, 1980 Apr, 27(4), 563 - 6 Intravenous azlocillin kinetics in patients on long-term hemodialysis; Aletta JM et al.; The kinetics of the antipseudomonas penicillin, azlocillin, was studied after intravenous injection in 9 patients with creatinine clearance under 7 ml/min . All were on long-term hemodialysis; 3 were also studied during a dialysis-free period . Kinetic parameters were derived using a 2-compartment open model . The mean serum azlocillin half-life (t 1/2) was 1.93 hr in patients on dialysis and approximately 5 hr off dialysis . Thirty percent of the dose was recovered in the dialysate during a 4-hr period . An approach to the use of azlocillin in patients undergoing dialysis is presented. Z Gesamte Inn Med, 1980 Apr 1, 35(7), 304 - 8 {Diagnosis and therapy of the extragenital manifestations of gonorrhea}; Rytter M et al.; Among the several infections gonorrhoe occupies the first place . Long-term complications are rare . The arthritis gonorrhoica, the perihepatitis acuta gonorrhoica (Fitz-Hugh-Curtis-syndrome) and the gonococci sepsis, the clinical picture differential diagnosis of which were discussed, possess clinical relevancy . Apart from few exceptions penicillin even nowadays is still the remedy of choice. Arch Otolaryngol, 1980 Apr, 106(4), 237 - 8 Oropharyngeal tularemia; Everett ED et al.; A case of oropharyngeal tularemia mimicking a peritonsillar abscess is presented . This diagnosis should be entertained in patients who are seen initially with ulcerative-exudative pharyngitis with or without tonsillitis and whose routine cultures are negative and/or are unresponsive to penicillin . Institution of appropriate therapy depends largely on the clinical diagnosis because cultures on ordinary media are routinely negative, and it takes several days for antibody titers to reach diagnostic significance. Br J Vener Dis, 1980 Apr, 56(2), 88 - 91 Prolonged use of the Greenland method of treatment of gonorrhoea; Evans AJ et al.; Of 1081 patients with gonorrhoea treated with probenecid 1 g orally and benzyl penicillin 5 megaunits intramuscularly, 96.7% were cured and no complications were encountered . This treatment regimen was associated with a pronounced reduction in the proportion of gonococcal strains showing diminished sensitivity to penicillin, from 51% to between 4% and 14% over a period of four years . When this treatment method was abandoned, however, the percentage of less sensitive strains rose to 33% over the following 18 months. Eur J Cell Biol, 1980 Apr, 21(1), 48 - 52 Formation of intracytoplasmic membranes in chemotrophic mecillinam sphaeroplasts of Rhodospirillum rubrum; Golecki JR et al.; Chemotrophically growing cells of Rhodospirillum rubrum were transformed into sphaeroplasts of irregular shape under the influence of the penicillin antibiotic mecillinam . On a cell protein basis, respiratory activities of whole sphaeroplasts were slightly decreased as compared with the untreated control . But, on a membrane protein basis various activities of the respiratory chain were largely identical in membrane preparations from untreated cells and sphaeroplasts, respectively . Chemotrophically cultured sphaeroplasts did not produce detectable quantities of bacteriochlorophyll . Nevertheless, electron-microscopic examination of thin sections and freeze fractures revealed the presence of vesicular intracytoplasmic membranes in the major portion of sphaeroplasts . The diameter of these vesicles was smaller (35-40 nm) than that of the vesicles formed under phototrophic conditions (60-70 nm) . A minor portion of the sphaeroplasts contained large amounts of membraneous extrusions in the enlarged periplasmic space . Upon removal of mecillinam, the sphaeroplasts were reverted into normal cells exhibiting no intracytoplasmic membranes under chemotrophic conditions . Only a few sphaeroplasts were unable to revert; these sphaeroplasts, however, still increased the cellular amounts of membraneous structures. Biull Eksp Biol Med, 1980 Apr, 89(4), 418 - 20 {Role of calcium ions in the evolution of the anticonvulsant effect of taurine}; Gurevich VS et al.; The decreased microsomal Ca++Mg++ATPase activity and lowered level of Ca++ binding by the brain cortex microsomes in seizure prone rats as compared with normal animals have been revealed . Taurine increases these parameters in experiments in vitro . Injection of taurine into the penicillin-provoked epileptogenic focus prevents the seizure reaction in rabbits . This effect is not observed after injection of taurine together with EGTA . The data obtained demonstrate the important role of calcium ions in the anticonvulsant action of taurine. Electroencephalogr Clin Neurophysiol, 1980 Apr, 48(4), 447 - 60 Focal interictal epileptiform discharges (FIED) in the epicortical EEG and their relations to spinal field potentials in the rat; Elger CE et al.; To study the relations between epileptiform potentials in the surface EEG and motor phenomena, focal interictal epileptiform discharges (FIEDs) were induced by the combined application of penicillin and penicillinase to the cortical surface of the rat . Spinal field potentials (SFPs) served as an indicator of descending activity . The following results were obtained . (1) The focus induced by the technique generated epileptiform activity within a very restricted cortical region . (2) FIEDs were accompanied by synchronized SFPs in the cervical and lumbar cord if the focus was located in the corresponding cortical motor area . With FIEDs in non-motor areas SFPs failed to occur . A unilateral focus led to SFPs on both sides of the spinal cord . (3) The transverse distribution of field potentials within the spinal cord revealed that the early negative peak of the SFP reached its maximum in the dorsal horn . (4) After the application of the drugs the development of FIEDs preceded that of SFPs by ca . 5 min . When the drug effect ceased SFPs remained often fully developed up to 10 min after the FIEDs had disappeared . (5) The temporal relationship between the cortical and spinal events showed individual and interindividual variations . (6) Anodal and cathodal electrical polarization of the cortical surface by currents sufficient to alter the shape, amplitude and polarity of the FIEDs failed to change the SFPs . The present investigations demonstrate that the cortical output from a restricted focus does not correspond to a definite epicortical field potential. JAMA, 1980 Mar 21, 243(11), 1143 - 4 Treatment of anorectal gonorrhea infections in men; Sands M; The charts of 606 men with anorectal gonorrhea infections treated using the current Public Health Service recommendations were reviewed . There were 3.3% failures in the group treated with penicillin--14.4% in those treated with tetracycline hydrochloride, 14.8% in the ampicillin trihydrate group, and none among those treated with spectinomycin hydrochloride . The intramuscular (IM) injection of penicillin G procaine, 4.8 million units, with 1 g of probenicid given orally is the treatment of choice for anorectal gonorrhea . An IM injection of 2 g of spectinomycin hydrochloride was effective but should be reserved for patients allergic to penicillin and for penicillin treatment failures. Biochem J, 1980 Mar 15, 186(3), 881 - 7 Syntheses of penicillin N, {6 alpha-3H}penicillin N and {10-14C,6 alpha-3H}penicillin N; Baldwin JE et al.; 1 . Penicillin N was synthesized by coupling alpha-amino-alpha-p-nitrobenzyl-N-p-nitro-benzyloxycarbonyl-D-adipate with 6-aminopenicillanic acid benzyl ester, followed by removal of the protecting groups through hydrogenolysis . 2 . alpha-Amino-alpha-p-nitrobenzyl-N-p-nitrobenzyloxycarbonyl-D-{5-14C}adipate was prepared by treating alpha-p-nitrobenzyl-N-p-nitrobenzyloxycarbonyl-D-glutamic acid with {14C}diazomethane followed by rearrangement with silver trifluoromethanesulphonate . 3 . Coupling of alpha-amino-alpha-p-nitrobenzyl-N-p-nitrobenzyloxycarbonyl-D-{5-14C}adipate with 6-aminopenicillanic acid benzyl ester gave triprotected {10-14C}penicillin N . 4 . 3H was introduced at C-6 of the Schiff's base derivative (10) by oxidation followed by reduction with NaB3H4 . 5 . The so-derived (6 alpha-3H)-labelled Schiff's base was hydrolysed to give 6-amino {6 alpha-3H}penicillanic acid benzyl ester p-toluenesulphonic acid salt, which after coupling as the free amine with alpha-amino-alpha-p-nitrobenzyl-N-pnitrobenzyloxycarbonyl-D-adipate and then hydrogenolysis, yielded {6alpha-3H}penicillin N . 6 . Triprotected {10-14C}penicillin N and triprotected {6alpha-3H}penicillin N in admixture were hydrogenolysed to give {10-14C,6alpha-3H}penicillin N. Experientia, 1980 Mar 15, 36(3), 333 - 4 Effects of probenecid on plasma/tissue distribution of 14C-benzylpenicillin in rats; Bergholz H et al.; Probenecid (50 mg . kg-1) was found to induce an increase of the plasma concentration of 14C-benzylpenicillin with a decrease of the concentration in liver and kidney . Accumulation in corresponding tissue slices was reduced by probenecid . Therefore, the well known increase of penicillin in plasma after probenecid seems to be not only due to an inhibition of renal excretion but also to a reduced tissue uptake in liver and kidney. Biochem J, 1980 Mar 15, 186(3), 889 - 95 Incorporation of 3H and 14C from (6 alpha-3H)penicillin N and (10-14C,6 alpha-3H) penicillin N into deacetoxycephalosporin C; Baldwin JE et al.; 1 . In a cell-free system prepared by lysis of protoplasts of Cephalosporium acremonium mutant M-0198, 3H and 14C were incorporated from singly- and doubly-labelled penicillin N into deacetoxycephalosporin C . 2 . The deacetoxcephalosporin C obtained from the above feeding experiments was converted into two different crystalline derivatives, namely N-phthalimidodeacetoxycephalosporin C bisbenzhydryl ester and N-phthalimidodeacetoxycephalosporin C bisdicyclohexylamine salt and recrystallized to constant specific activity or constant ratio of specific activity . 3 . That 3H is incorporated at C-7 in the biosynthesized deacetoxycephalosporin C was shown by the loss of radioactivity (95.2%) after methoxylating the derived N-phthalimidodeacetoxycephalosporin C bisbenzyhydryl ester . 4 . Deacetoxycephalosporin C was also the product of the cell-free reaction conducted in the presence of ferrous ions and ascorbic acid, as shown by two-dimensional paper electrophoresis-chromatography; these additives appreciably improved the efficiency of conversion. Brain Res, 1980 Mar 3, 185(1), 169 - 81 Effects of TEA on hippocampal neurons; Schwartzkroin PA et al.; The effects of the potassium channel blockers, tetraethylammonium (TEA) and tetramethylammonium (TMA) on behavior of hippocampal CA1 neurons were studied in the in vitro slice preparation . Intracellular injections of TEA produced marked spike broadening, increased input resistance, and a prolongation of a putative slow calcium-activated afterhyperpolization (AHP) . Little effect was seen on synaptic potentials . Bursting activity induced by TEA in hippocampal neurons was qualitatively different from the epileptiform bursting induced by raising extracellular potassium concentrations or by including penicillin in the bathing medium . Effects of TMA were qualitatively similar to those of TEA, but much slower and less dramatic . The results suggested that there were at least two different potassium channels in the membranes of hippocampal CA1 neurons, and that both were important in determining normal neuronal activity . TEA appeared to preferentially block a fast, voltage-dependent potassium conductance (gk); however, it also modified the slow, calcium-activated gk . Although cell bursting activity may have resulted from blockade of a gk produced by TEA treatment, the epileptiform bursts produced by penicillin exposure appeared to be independent of this mechanism. Ann Sclavo, 1980 Mar-Apr, 22(2), 116 - 24 {Transient bisalbuminemia induced by penicillin and gentamicin . Immunoelectrophoretic study and thorough examination of bibliography (author's transl)}; Soffiati G et al.; The Authors report a case of transient bisalbuminemia due to the administration of large doses of penicillin and gentamicin . Cellulose acetate electrophoresis showed an abnormal fraction of normal albumin . The IEB showed a better result . Transient bisalbuminemia may indicate saturation of albumin sites with beta-lactamines, requiring interruption of therapy . The Authors point out the utility of IEB in disclosing this alteration induced by antibiotics. Allergol Immunopathol (Madr), 1980 Mar-Apr, 8(2), 105 - 10 Allergy to penicillin . Comparison of "in vivo" and "in vitro" tests; Olive A et al.; Skin tests (SKT) and Lymphocyte Transformation Test (LTT) utilizing sodium penicillin G (PNG) and penicilloyl polylysine (PPL) and Rast to penicilloyl G were carried out on forty patients with a history of allergic reactions to penicillin, the results obtained indicated no statistically significant difference between the use of SKT or LTT in the diagnosis of allergy to penicillin (X2, p > 0,05), while the use of Rast showed a statistically significant difference (X2, p < 0,001) in favour of LTT and SKT . The use of either type of allergen (PNG or PPL) in LTT or SKT showed a significant difference in favour of the former (X2, p < 0,01). J Pharm Sci, 1980 Mar, 69(3), 346 - 8 Colorimetric determination of procaine hydrochloride in pharmaceutical preparations; Salama RB et al.; A new rapid, specific, and convenient colorimetric method for the determination of procaine hydrochloride in pharmaceutical preparations is described . This method is based on measurement of the intensity of the orange-red color developed when procaine hydrochloride is allowed to react with 1,2-naphthoquinone-4-sulfonic acid sodium salt in aqueous solution . Beer's law is followed over 6.0--20.0 micrograms/ml . The method was applied to the determination of procaine hydrochloride in procaine hydrochloride, procaine hydrochloride injection with or without epinephrine, penicillin G procaine, penicillin G procaine injection, and fortified procaine penicillin injection (BP) . The results were comparable to those obtained by official procedures . Because of its simplicity, sensitivity, and accuracy, this method is particularly suited for routine analysis of official preparations of procaine hydrochloride. J Comp Neurol, 1980 Mar 1, 190(1), 1 - 13 Prefrontal system in the rat visualized by means of labeled deoxyglucose--further evidence for functional heterogeneity of the neostriatum; Divac I et al.; An epileptic focus was formed in the anteromedial part of the prefrontal cortex in rats by means of intracortical injection of penicillin, and radioactively labeled deoxyglucose was immediately injected intravenously . Auto-radiograms revealed that, in addition to the injected cortical area, a number of formations increased their consumption of deoxyglucose . The labeled formations were the posterior medial and perirhinal cortical areas, the anteromedial part of the neostriatum, the anterior and intermediodorsal part of globus pallidus, the entopeduncular nucleus, the reticular portion of the substantia nigra, the claustrum, and the basolateral nucleus of amygdala . In addition, several thalamic nuclei were activated, including the entire parataenial, paraventricular, anteromedial, and axial nuclei, as well as distinct parts of the mediodorsal and lateral nuclei and, in the instances of spread of cortical activity to the dorsal surface, of the ventral nucleus . In some animals, activation of the ventral tegmental area of Tsai was also found . All these formations have previously been shown by neuro anatomical techniques to be directly connected with the anteromedial cortex of the neostriatum . Some of them were included in the "prefrontal system." The present findings, in agreement with earlier neurobehavioral studies, indicate that, in the rat, the anteromedial part of the neostriatum, but not other neostriatal regions, is functionally related to the anteromedial part of the prefrontal cortex . The present and earlier similar studies suggest that the mammalian forebrain contains a number of "systems," each of which consists of a neocortical area and a set of associated subcortical sites. Vet Rec, 1980 Mar 1, 106(9), 190 - 3 Non-surgical transfer of bovine eggs: investigation of some factors affecting embryo survival; Christie WB et al.; In an investigation on the effect of position of deposition of the egg within the uterus, surgical transfer of single eggs to the tip of the horn resulted in a significantly higher pregnancy rate than transfer to the base . To determine embryo survival at differing times after transfer single eggs were transferred non-surgically to the base of the uterine horn . The highest pregnancy rate occurred in a group of heifers slaughtered 16 to 17 days after oestrus followed by heifers slaughtered on days 24 to 26 . The lowest pregnancy rate occurred in a group where pregnancy diagnosis was on day 42 by rectal palpation . The pregnancy rates of the highest and the lowest groups were significantly different . The pregnancy rate was increased in a group of heifers which were treated with human chorionic gonadotrophin from day 13 to 24 and palpated per rectum on day 42 to determine pregnancy . The presence or absence of penicillin and streptomycin in the medium and of passing differing volumes into the uterus after non-surgical transfer of single eggs using a glass pipette had no effect on pregnancy rate and there was no significant difference in pregnancy rate and there was no significant difference in pregnancy rate between the groups using different volumes of transfer media . The position of the egg within the uterine lumen after transfer contributes to the reduced pregnancy rate achieved after nonsurgical transfer when compared with the surgical method . The greatest proportion of embryonic death after non-surgical transfer occurs after day 17 and there is some evidence that human chorionic gonadotrophin treatment can improve embryo survival . The use of comparatively small volumes of medium to eject the egg into the uterus may be preferable to achieve maximum pregnancy rates. Neurology, 1980 Mar, 30(3), 315 - 8 Ketamine activation of experimental corticoreticular epilepsy; Black JA et al.; Generalized corticoreticular epilepsy was established in adult cats by parenteral penicillin, and electroencephalographic monitoring was carried out . Ketamine HCl was injected intravenously in doses of 2.5 to 20 mg per kilogram . If doses of penicillin were inadequate to establish typical spike-wave activity, ketamine induced the spike-wave pattern typical of much higher doses of penicillin . At doses of penicillin that established the spike-wave pattern, ketamine potentiated the spike-wave activity and sometimes induced spike-and-wave status . These findings suggest caution in the clinical use of ketamine in patients with corticoreticular epilepsy . Because analogous effects have been observed upon administration of GABA-mimetic agents, GABA systems may play a role in ketamine anesthesia and corticoreticular epilepsy . Precollicular brain transections failed to modify ketamine effects, excluding a possible influence of mesencephalic centers on the observed potentiation. Clin Orthop, 1980 Mar-Apr, (147), 203 - 6 Septic arthritis in a Charcot joint; Rubinow A et al.; Two patients with Charcot joints developed septic arthritis . The infection in the first patient was treated successfully by repeated needle aspirations and parenteral oxacillin administration . In the second patient closed drainage and parenteral penicillin were not successful in eradicating the infection, and surgical incision with suction drainage was required . Technical difficulties achieving arthrodesis in a Charcot joint suggest that repeated needle aspirations are the preferred method of initial joint drainage . Surgical drainage is advised for loculated, grossly purulent parts of the joint. J Bacteriol, 1980 Mar, 141(3), 1115 - 21 Genetic and physiological characterization of Escherichia coli mutants deficient in phosphoenolpyruvate carboxykinase activity; Goldie AH et al.; Mutants doubly deficient in phosphoenolpyruvate carboxykinase (pck) and phosphoenolpyruvate synthetase (pps) were unable to grow with succinate as the sole carbon source . A number of pck mutations isolated from pps strains by penicillin selection mapped at 74 min on the Escherichia coli chromosome, between glpD and aroB . Several of the strains containing these mutations had a protein antigenically related to phosphoenolpyruvate carboxykinase, and therefore, the mutations probably represented mutations in the structural gene for this enzyme . Phosphoenolpyruvate carboxykinase was regulated at the level of transcription by catabolite repression . Enzyme levels also increased in stationary-phase cultures by a mechanism independent of cyclic adenosine monophosphate or the product of the relA gene. Ann Dermatol Venereol, 1980 Mar, 107(3), 153 - 61 {Lymphocytic infiltrations of the nipple . The benign cutaneous lymphocytoma of the breast areola (author's transl)}; Grosshans E et al.; Benign lymphocytic infiltrations may often occur in the skin of nipple and areola: 55 cases have been described in literature especially in Scandinavia and in Germany, sometimes in correlation with tick bites or erythema chronicum migrans, but until now no cases have been reported in France . In a retrospective study of 30 cutaneous lymphocytomas, we found 8 cases localized on the breast-3 children and 5 older patients-, associated with a erythema chronicum migrans in 3 patients and following a tick bite in another patient . The course of the disease is always benign and the healing can be accelerated by penicillin therapy . The pathogenesis still remains unclear but some data argue for an infectious mechanism: frequency of tick bites (20 p . 10), geographical occurrence in the spreading area of common ticks in Europe, affinity of ticks for the breast in all mammals, carriage of viruses by some tick species, efficiency of penicillin in tick-transmitted viral infectious and in benign skin lymphocytomas, positive inoculations in volunteers, general course of an infectious disease (seasonal variations, frequency of satellite lymph-node swelling, spontaneous healing). Antimicrob Agents Chemother, 1980 Mar, 17(3), 506 - 9 Effects of penicillin G on mesosome-like structures in Agmenellum quadruplicatum; Balkwill DL et al.; Agmenellum quadruplicatum was treated with lethal doses of penicillin G (15 and 75 U/ml) and then examined by electron microscopy to observe changes that took place before lysis . Treatment for 30 min led to increases in the frequency and size of mesosome-like structures within the cells . There was a direct correlation between the magnitude of these increases and the concentration of penicillin G . The mesosome-like structures often were associated with division septa, and they resembled mesosomes reported in other cyanobacteria . It is suggested that these structures appeared and enlarged because synthesis of membrane material continued after wall (peptidoglycan) synthesis was inhibited by the drug. Ann Neurol, 1980 Mar, 7(3), 222 - 9, 236-7 Effects of manipulation of the sensorimotor system on focal motor seizures in the monkey; Hosokawa S et al.; During focal motor seizures induced by injecting penicillin into the face-hand area of the right motor cortex of 24-month-old monkeys, the sensorimotor system was manipulated by three methods . Elimination, by a paralytic agent, of proprioceptive input from contracting muscles and joints did not alter the electrographic expression of the seizure or the pattern of local glucose utilization in cortical or subcortical components of the sensorimotor system . An overall increase in the rate of energy metabolism occurred in the paralyzed monkeys with electrographic seizures . Cryogenic destruction of up to 90% of the ipsilateral ventral caudal globus pallidus had no effect on electrographic or clinical expression of the seizure . Electrical stimulation of the ipsilateral ventral caudal globus pallidus caused reproducible maximum expression of electrographic and clinical seizure phenomena for the 90-second duration of the stimulus. Ann Neurol, 1980 Mar, 7(3), 204 - 12, 230-2 Local cerebral glucose utilization in newborn and pubescent monkeys during focal motor seizures; Kato M et al.; The {14C}deoxyglucose method was used to determine the rate of local cerebral glucose utilization (LCGU) in newborn and pubescent monkeys during focal motor seizures induced by injecting penicillin into the face-hand area of the right motor cortex . Seizures were studied in 3 newborn and 6 pubescent monkeys, and 3 newborn and 4 pubescent monkeys were used as controls . In controls, the pattern of glucose utilization within structures of the sensorimotor system was quite differenet at the two age levels; newborns showed far less activity, especially in the neocortex and striatum . In the monkeys with seizures, the unilateral increase in LCGU relative to the controls was greater in newborn than in pubescent monkeys except in the cerebral and cerebellar cortices . The increased glucose utilization in cortical and subcortical structures of the newborns was ipsilateral to the discharging lesin and lacked the well-defined pattern seen in the pubescent monkeys . In general, newborn brain was capable of supporting a focal motor seizure but lacked the precise clinical and electrographic expressions or efficient energy metabolism that accompany maturation of the brain at puberty. Antimicrob Agents Chemother, 1980 Mar, 17(3), 316 - 21 Moxalactam (6059-S), a new 1-oxa-beta-lactam: binding affinity for penicillin-binding proteins of Escherichia coli K-12; Komatsu Y et al.; Moxalactam (6059-S) is a new beta-lactam derivative with a structure markedly different from those of penicillins or cephalosporins . The binding activity of 6059-S to penicillin-binding proteins (PBPs) in Escherichia coli K-12 was tested . {14C}benzylpenicillin- or {14C}6059-S-bound inner membrane proteins of E . coli K-12 were rapidly detected without using fluorography . 6059-S had the highest affinity for PBP-3 and -7/8, had a higher affinity than benzylpenicillin for PBP-1A, -1Bs, -4, and -5/6 and a lower affinity for PBP-2, 609134, the 1-thiacephem analog of 6059-S, showed as high an affinity for PBP-1A, -1Bs, -3, and -4 as 6059-S but a lower affinity for PBP-5/6. Allergy, 1980 Mar, 35(2), 135 - 8 Allergological examination of cystic fibrosis patients with skin reactions during carbenicillin treatment; Moller NE et al.; Sixteen of 84 cystic fibrosis patients developed skin manifestations during intensive carbenicillin therapy . The possibility of allergic drug reactions was examined . None of the patients showed any significant levels of antibodies of IgE, IgG or IgM classes against carbenicillin and different penicilloyl determinants as recorded with RAST, sandwich-radioimmunoassay and double antibody assay . The leukocytes of the patients did not release histamine on in vitro provocation with carbenicillin . Furthermore, none of the patients responded to prick test or to peroral penicillin provocation . The negative findings indicated that the recorded reactions were most probably not due to antibody-mediated allergy of type I or type III. Biochim Biophys Acta, 1980 Feb 14, 611(2), 351 - 7 Inhibition kinetics of three R-factor-mediated beta-lactamases by a new beta-lactam sulfone (CP 45899); Labia R et al.; A new beta-lactam sulfone, CP 45899, has been proved to be a time-dependent irreversible inhibitor of three R-factor-mediated beta-lactamases (penicillin amido-beta-lactamhydrolase, EC 3.5.2.6): TEM-1 (pI = 5.4), TEM-2 (pI = 5.6) and Pitton's type 2 (pI = 7.7) . This inhibition occurs in two principal steps: (1) formation of a reversible enzyme-inhibitor complex (characterized by a Ki); (2) evolution of this complex into one, or more, inactive protein(s) (kinact) . With the three beta-lactamases CP 45899 shows, respectively, Ki of 0.9, 0.8 and 1.8 microM and kinact of 1.2 . 10(-3), 0.8 . 10(-3) and 1 . 10(-3) s-1; the turnover numbers are: 525, 2280 and 1220 . These results are compared to those previously obtained with clavulanic acid. Brain Res, 1980 Feb 3, 183(1), 61 - 76 Changes in excitatory and inhibitory synaptic potentials leading to epileptogenic activity; Schwartzkroin PA et al.; The effects of the epileptogenic agent, penicillin, on excitatory and inhibitory postsynaptic potentials (EPSPs and IPSPs) were studied in the hippocampal in vitro slice preparation . The actions of penicillin were compared to those of bicuculline, an antagonist of gamma-aminobutyric acid . Neither substance enhanced monosynaptic EPSP amplitude in CA1 pyramidal cells, but both penicillin and bicuculline depressed IPSPs . Large depolarizations that gave rise to cellular bursting activity did develop after addition of penicillin or bicuculline to the bathing medium . There was also an increase in the incidence of fast prepotentials of 'd-spikes.' These observations are interpreted according to the hypothesis that penicillin and bicuculline block cellular IPSPs, and consequently allow remote intrinsic excitatory events to invade the cell soma and trigger act