Rev Esp Cardiol, 1991 Oct, 44(8), 556 - 9 {The management by medical treatment of an intracranial mycotic aneurysm in a patient with infectious endocarditis with negative blood cultures and hypertrophic myocardiopathy}; Anguita M et al.; A case of intracranial mycotic aneurysm due to culture-negative infective endocarditis involving a patient with hypertrophic cardiomyopathy is reported . The patient, a 22-year-old woman with no history of known prior disease, had fever, headache and focal neurologic symptoms 3 days before admission . An echocardiogram performed after admission disclosed an obstructive hypertrophic cardiomyopathy and a gross vegetation on septal leaflet of mitral valve . Cerebral angiography revealed a mycotic aneurysm involving a peripheral branch of the left middle cerebral artery . Causal agent was not identified, and empiric treatment with penicillin G and streptomycin achieved medical cure and disappearance of the aneurysm 2 weeks later . Four months after endocarditis had been cured, the patient was electively operated because of progression of mitral regurgitation . Six months later, she is asymptomatic. Otolaryngol Head Neck Surg, 1991 Oct, 105(4), 578 - 85 Mucosal changes induced by experimental pneumococcal otitis media are prevented by penicillin V; Hermansson A et al.; Penicillin V (pcV) was administered to 50 rats, either before bacterial challenge (prevention group), or after bacterial challenge but before fulminant purulent acute otitis media (AOM) was established (early treatment group) . Five animals from each group were killed on days 4, 8, and 12, and 2 and 6 months after challenge . Middle ear mucosa was sampled at six different sites and studied in the light microscope . Untreated pneumococcal AOM in the rat has been shown to cause persistent structural changes of the middle ear mucosa . Both in the early treatment group and in the prevention group, the structural changes were diminished, as compared with those of untreated infected controls . The persistent structural changes seen after 6 months in untreated controls were not seen in animals that had received pcV in conjunction with the AOM episode . Though the beneficial effect on the mucosal changes during the first 2 weeks was more pronounced when pcV was given prophylactically, its use as early treatment would seem to be almost as effective in preventing the persistence of mucosal changes. J Microsc, 1991 Oct, 164 ( Pt 1), 29 - 41 A preparation method of specimens of the fungus Penicillium chrysogenum for ultrastructural and immuno-electron microscopical studies; Muller WH et al.; A combination of cryofixation without pre-treatment, freeze-substitution and low-temperature embedding was used to prepare specimens of Penicillium chrysogenum for electron microscopy . To produce specimens which are thin enough for appropriate cryofixation, the P.chrysogenum colonies were grown between dissected-dialysis tubing on an agar plate, which in addition allowed longitudinal sectioning . In contrast to classical chemical fixation, this preparation procedure resulted in excellent preservation of ultrastructure . Furthermore, the penicillin biosynthetic enzyme acyltransferase could be unequivocally located by immunogold labelling, indicating a preservation of antigenic properties of the specimen . Labelling density was not conspicuously affected when using different freeze-substitution media, but it was reduced after embedding in Epon 812. Acta Paediatr Scand, 1991 Oct, 80(10), 944 - 52 Monitoring of drug prescriptions for children in the county of Jämtland and Sweden as a whole in 1977-1987; Wessling A et al.; One individual-based (Jamtland) and one population-based (Sweden) monitoring system provided information on the prescription sales of drugs for children in ambulatory care . The overall prescription rate decreased between 1977 and 1987 and it was 20-25% lower in Jamtland than in Sweden as a whole . Antibiotics, drugs for ear, nose and throat diseases and respiratory drugs accounted for three out of four prescriptions . Penicillin V dominated among antibiotics and the prescription rate was stable whereas that of other antibiotics increased . During their first year of life one out of ten children in Jamtland had at least one prescription of antibiotics, during their first five years three out of four children . Prescribing of decongestants, especially systemic, decreased during the study period whereas that of anti-asthmatics increased, partly due to the non-approved use of these drugs for common cough . The results from our study underline the need for pharmaco-epidemiological studies linking prescription data to clinical data in order to answer questions on the rational of present drug treatment practices. Dtsch Tierarztl Wochenschr, 1991 Oct, 98(10), 393 - 4 {A method for the treatment of oviduct obstruction in cattle using CO2 insufflation into the uterus}; Boitor I et al.; The investigations were carried out on 59 cows from Holstein half-breed, establishing that 8 cows suffered salpinx obstruction (5 cases with unilateral obstruction and 3 cases with bilateral obstruction) . The authors are using an apparatus made by themselves, for insufflation of air in the obstructed uterus, and which is useful in desobstruction treatment, too . For diagnosis, CO2 was introduced inside of uterus . The authors used for treatment PBS (saline phosphate buffer) in addition with penicillin G, hydrocortisone and trypsin . Before air insufflation in uterus there will be infused 10-20 ml 2% Lidocaton . The cows must be examined in oestrus period, or 2 days after PGF2 alfa administration . The gas must be introduced under rectal palpation, and pressure must not be higher than 500 mm H2O column . If there is a permeable oviduct, after 15-20 sec . from gas introduction, ist is possible to palpate the filled oviduct . From ovary we can perceive a rustle produced by gas crossing in abdominal cavity . In case of salpinx obstruction, the treatment must be start as soon as possible . The utilized liquid for treatment will be introduce by gas pressure, inside of uterus and oviducts . Using this method, it managed the repermeability of oviducts at 3 from 8 treated cows . In each case, there were used 3 treatments at 48 h interval . After the second insemination (I.A.) 2 cows remained pregnant. Biochemistry, 1991 Sep 17, 30(37), 9034 - 40 Refolding and assembly of penicillin acylase, an enzyme composed of two polypeptide chains that result from proteolytic activation; Lindsay CD et al.; The in vitro folding and assembly of penicillin acylase (EC 3.5.1.11) (PA) to active enzyme has been studied . PA is a large bacterial protein (Mr = 86,000) comprising two peptides, alpha and beta, produced by proteolytic processing and activation of a 92-kDa precursor . Proteins that result from proteolytic processing are characteristically difficult if not impossible to refold . Different factors that affect folding and assembly of PA, including pH, ionic strength, and temperature, have been studied . Yields of 60% can be obtained, based on recovery of enzyme activity, together with another 20% of folded and associated monomer with conformation closely similar to that of the active enzyme but with the active site not formed . Evidence is presented for in vitro assembly proceeding via initial folding of the N-terminal alpha-peptide with subsequent collapse of the transiently folded beta-chain on to the surface of the former . A slow process of rearrangement follows association in vitro . Competition experiments support the proposal that the linker endopeptide in the precursor serves to increase the probability of productive collision between folded alpha- and beta-peptides . The effect of raised temperature is to interfere with the folding of the alpha-peptide, thus preventing proper folding of the precursor . This finding accounts for the basis of the temperature regulation of PA production in vivo. Biochem J, 1991 Sep 15, 278 ( Pt 3), 673 - 8 The mutation Lys234His yields a class A beta-lactamase with a novel pH-dependence; Brannigan J et al.; The lysine-234 residue is highly conserved in beta-lactamases and in nearly all active-site-serine penicillin-recognizing enzymes . Its replacement by a histidine residue in the Streptomyces albus G class A beta-lactamase yielded an enzyme the pH-dependence of which was characterized by the appearance of a novel pK, which could be attributed to the newly introduced residue . At low pH, the kcat, value for benzylpenicillin was as high as 50% of that of the wild-type enzyme, demonstrating that an efficient active site was maintained . Both kcat . and kcat/Km dramatically decreased above pH 6 but the decrease in kcat./Km could not be attributed to larger Km values . Thus a positive charge on the side chain of residue 234 appears to be more essential for transition-state stabilization than for initial recognition of the substrate ground state. Eur J Biochem, 1991 Sep 15, 200(3), 767 - 73 Purification of penicillin-binding protein 4 of Escherichia coli as a soluble protein by dye-affinity chromatography; Mottl H et al.; The dacB gene of Escherichia coli, coding for penicillin-binding protein 4 (PBP4) was cloned under the control of the phage lambda pR promoter and cro gene translation signals . Depression of the phage lambda promoter for 2 h at 42 degrees C in E . coli led to the maximum over-production of PBP4 to 3.8% of the total soluble protein . Expression at 42 degrees C but not at 40 degrees C or 37 degrees C led to incomplete processing and aggregation of the preform of PBP4 . Cibacron navyblue 2G-E was selected from a collection of triazine dyes as having a high affinity for PBP4 . The immobilised dye was used in a two-step procedure to isolated 374 mg PBP4 from the soluble fraction of 125 g (wet mass) cells of the over-producing strain, with a recovery of 63.2% and a final purity of 99% as determined by active-site titration with radiolabelled penicillin . Saturation of PBP4 with various beta-lactam derivatives did not abolish binding to the dye material, nor was PBP4 eluted by addition of beta-lactams from the dye matrix . PBP4 behaved as a soluble protein throughout the purification, that was performed in the complete absence of detergents . Furthermore, in flotation experiments on sucrose density gradients and in Triton X-114 fractionation experiments, it showed the characteristics of a soluble protein . Cibacron navyblue 2G-E showed class specificity for all E . coli PBP except PBP3 and could be used for the isolation of these PBP from membrane extracts. DICP, 1991 Sep, 25(9), 925 - 8 Comparative attitudes to verbal and written medication information among hospital outpatients; Harvey JL et al.; This study was undertaken to assess the comparative preference of pharmacy outpatients for verbal and written medication information and to identify factors that might influence these preferences . Two hundred forty-seven consecutive, literate outpatients presenting with a prescription for a penicillin were enrolled in the study and given standardized verbal counseling by a pharmacist and a medication information leaflet . Assessment was made at initial presentation and by a prepaid mail questionnaire completed anonymously by the patient at home . Preferences were analyzed by age, sex, and number of medications prescribed . A response rate of 63 percent (155/247) was obtained . Low recall of physician instruction (11 percent) was recorded . Respondent preferences were for pharmacist counseling (30.4 percent), leaflet (20.6 percent), both of these (44.5 percent), or neither/uncertain (4.5 percent) . The only factor having a statistically significant effect on these preferences was age (31-55 y), which influenced preference for a leaflet . Patient opinion of each leaflet section is presented . Patient preference for a leaflet or verbal counseling with a leaflet provides further evidence that leaflets should be widely used. Prostaglandins Leukot Essent Fatty Acids, 1991 Sep, 44(1), 37 - 46 Influence of chemotherapeutic agents on prostacyclin synthesis . II . Effects of tetracycline and penicillin G on prostacyclin synthesis by the rat thoracic aorta and myometrial tissues; el Tahir KE et al.; The influence of the two antibiotics tetracycline hydrochloride (T) and penicillin G sodium (P) on PGI2 synthesis by the male rat thoracic aorta and day-20 pregnant rat myometrium was investigated in vitro using a rat platelet antiaggregatory bioassay method . Pretreatment of the tissues for 30 min at 37 degrees C with T (21-168 microM) or P (28-224 microM) significantly inhibited PGI2 synthesis in absence or presence of exogenous arachidonic acid (AA) (16.6 microM), (P less than 0.01, n = 5-6) . Furthermore, pretreatment of rats with the two drugs (T 11 and P 175 mu mole kg-1 for 30 min) significantly antagonised AA (4 n mole kg-1)-induced hypotension in urethane-anaesthetised rats . They also (T 0.5-4 and P 1-6 microM) antagonised AA-induced aggregation in rabbit citrated platelet-rich plasma . T failed to affect ADP-induced aggregation to any significant level whereas P (3-6 microM) reduced ADP-induced aggregation . The drugs seemed to interfere with the action of the PG endoperoxide synthase (or PG cyclooxygenase) enzyme resulting in decreased formation of PGG2 and PGH2 . Such an effect may have resulted from the induced formation of toxic {OH-} radicals and/or inhibition of O2 uptake by the tissues under the influence of the drugs . The demonstrated inherent property of these two antibiotics to inhibit the synthesis of the potent vasodilator, platelet antiaggregatory, anticonvulsant and inhibitor of gastric acid secretion--PGI2, may partly contribute towards better understanding of the biochemical mechanisms that underlie some of the previously known but poorly understood actions of these antibiotics . Furthermore, since good evidence exists for the involvement of excessive uterine prostaglandin synthesis in dysmenorrhoea and premature deliveries, it is suggested that the potential benefits of T or P in these two disorders be investigated. Medicine (Baltimore), 1991 Sep, 70(5), 287 - 92 Purpura fulminans and symmetrical peripheral gangrene caused by Capnocytophaga canimorsus (formerly DF-2) septicemia--a complication of dog bite; Kullberg BJ et al.; We review the syndrome of Capnocytophaga canimorsus (DF-2) septicemia after exposure to dogs or cats . We describe a previously healthy patient who developed diffuse intravascular coagulation and symmetrical peripheral gangrene as a result of C . canimorsus septicemia after a dog bite . To our knowledge, this patient was the first to receive combined plasmapheresis and leukapheresis for C . canimorsus septicemia . Symmetrical peripheral gangrene is frequently associated with C . canimorsus septicemia and may lead to an early diagnosis in patients who become severely ill after a dog bite . Other complications include arthritis, meningitis, and endocarditis . These manifestations can also be found in previously healthy patients, although a prior splenectomy or other causes of impaired host defense clearly enhance the risk . Prompt treatment with penicillin G is required. Hosp Pract (Off Ed), 1991 Sep, 26 Suppl 5, 20 - 3; discussion 55 Ceftriaxone in treatment of serious infections . Sexually transmitted diseases; Harrison WO; The most recent CDC guidelines for treatment of STDs list a number of syndromes for which ceftriaxone is the recommended therapy, including those caused by N . gonorrhoeae and H . ducreyi . The drug has successfully eradicated incubating syphilis . Its use in primary, secondary, and latent syphilis is promising, although adequate data regarding optimal dose and duration of therapy are not yet available . It remains to be seen whether ceftriaxone represents the sun rising on a new era of successful STD treatment or the sun setting on the old penicillin era. Epilepsia, 1991 Sep-Oct, 32(5), 591 - 6 Aggravation of penicillin-induced epilepsy in rats with locus ceruleus lesions; Sullivan HC et al.; The rate and pattern of development of seizures induced by penicillin injected intraperitoneally were determined in rats that had been depleted of brain norepinephrine (NE) by bilateral injections of the neurotoxin 6-OH dopamine into the locus ceruleus . Behavioral observations and scalp electrographic recordings were made after injection and the efficacy of NE depletion was determined by high performance liquid chromatography measurement of cortical levels of NE and its metabolites . We found that in comparison to sham-operated control rats, NE-depleted rats had a significantly shorter latency to first observable myoclonic jerk, the first epileptic discharge, the first convulsion with sustained epileptic discharges, and a longer duration of convulsions . We observed a similar electrographic pattern of multifocal spikes with bilateral synchrony in both groups . However, more of the control rats (six of 12) had convulsions as compared to the lesioned rats (four of 12) . These findings are consistent with previous evidence that depletion of neocortical NE facilitates the development of epileptiform activity in the CNS; however, a convulsive state was not induced by NE depletion. J Bacteriol, 1991 Sep, 173(18), 5740 - 6 Penicillin-binding protein 1B of Escherichia coli exists in dimeric forms; Zijderveld CA et al.; A high-molecular-weight band has been detected in Western immunoblots of nonboiled Escherichia coli samples incubated with polyclonal antiserum against penicillin-binding protein 1B (PBP 1B) . This band was shown to be a dimer of PBP 1B . The dimer was more strongly associated with the envelope than the monomer, and it was still able to bind penicillin G . Analysis of the binding of fusion proteins of PBP 1B and beta-lactamase showed that the part of PBP 1B necessary for complex formation lies in the amino-terminal half of the protein. J Bacteriol, 1991 Sep, 173(18), 5668 - 76 Subcellular distribution of the soluble lytic transglycosylase in Escherichia coli; Walderich B et al.; The localization of the major autolytic enzyme, the soluble lytic transglycosylase, in the different cell compartments of Escherichia coli was investigated by immunoelectron microscopy . Ultrathin sections were labeled with a specific antiserum against purified soluble lytic transglycosylase, and the antibody-enzyme complexes were visualized with colloidal protein A-gold . A preferential localization of the lytic transglycosylase in the envelope was observed, with only 20 to 30% of the enzyme left in the cytoplasm . Most of the enzyme associated with the cell wall was tightly bound to the murein sacculus . Sacculi prepared by boiling of cells in 4% sodium dodecyl sulfate could be immunolabeled with the specific antiserum, indicating a surprisingly strong interaction of the lytic transglycosylase with murein . The enzyme-substrate complex could be reconstituted in vitro by incubating pronase-treated, protein-free murein sacculi with purified lytic transglycosylase at 0 degrees C . Titration of sacculi with increasing amounts of enzyme indicated a limiting number of binding sites for about 1,000 molecules of enzyme per sacculus . Ruptured murein sacculi obtained after penicillin treatment revealed that the enzyme is exclusively bound to the outer surface of the sacculus . This finding is discussed in the light of recent evidence suggesting that the murein of E . coli might be a structure of more than one layer expanding by inside-to-outside growth of patches of murein. J Clin Neuroophthalmol, 1991 Sep, 11(3), 139 - 43 Meningovascular syphilis with a gumma of the midbrain; Standaert DG et al.; We report a patient with meningovascular syphilis who had a dorsal midbrain syndrome, cognitive dysfunction, and a left peripheral seventh nerve palsy . Magnetic resonance imaging (MRI) disclosed a large lesion of the midbrain and thalamus with intense enhancement of the interpeduncular cistern, both of which resolved after treatment with intravenous penicillin . The clinical features, radiographic appearance, and response to therapy suggest that this lesion was a focal syphilitic inflammatory process, or gumma . We conclude that MRI with intravenous contrast may reveal the full spectrum of pathologic involvement in neurosyphilis and, in certain situations, may obviate the need for biopsy of an associated mass lesion. Arch Ital Biol, 1991 Sep, 129(4), 273 - 87 The contribution of diffusion to the termination of penicillin-induced convulsive activity in the awake rat; Horn E et al.; 1 . Experiments were performed to investigate the contribution of diffusion to the termination of PCN induced convulsive (epileptiform) activity in the awake rat . The basic question was whether convulsive activity terminates at the same critical concentration Ct of PCN independently of the concentration Co of PCN injected into the superficial layer of the foreleg field of the right motor cortex . Different concentrations Co were used, the lowest being 16 IU PCN/0.5 microliters saline, the largest 1000 IU PCN/0.5 microliters saline . The convulsive activity was recorded by means of the electroencephalogram (EEG) . 2 . Mathematical calculations concerning the diffusion of the substances were performed by using the diffusion equation with a PCN diffusion coefficient D = 3.52 x 10(-4) mm2/s and the tortuosity factor lambda = 1.62 . 3 . The lowest dose of PCN used was considered as a threshold dose for acute induction of convulsive activity because only 4 out of 9 rats treated with 16 IU PCN developed epileptiform activity . For the range of doses between 16 and 32 IU, the median frequency of convulsive potentials was dose-dependent, and increased from 7.9 to 13.8 pot./min, respectively . For higher doses covering the range between 63 and 1000 IU, there was only an insignificant increase from 19.2 to 22.7 pot./min, respectively . 4 . The median period of convulsive activity increased significantly (p less than 0.05 or less than 0.01) and monotonically from 19.5 min in rats treated with 16 IU PCN to 267 min after treatment with 1000 IU PCN . 5 . At the end of the convulsive activity, the median critical concentration Ct within the artificial focus ranged from 1.75 to 1.31 IU/0.5 microliters saline in rats treated with 16 to 125 IU PCN, while after induction of convulsive activity with doses of 250, 500 or 1000 IU PCN, Ct gradually increased to 2.01, 2.83, and 3.75 IU/0.5 microliters, respectively . This means that the brain became less sensitive for PCN the longer the epileptiform activity lasted . 6 . It is concluded that during long-lasting convulsive activity, the brain takes advantage of its plastic properties by eliciting counteracting mechanisms . These self-protective factors may utilize neuronal networks which needs some time to become effective in the control of the cortical activity. Appl Biochem Biotechnol, 1991 Sep, 30(3), 297 - 302 Adsorption and expression of penicillin G acylase immobilized onto methacrylate polymers generated with varying pore generating solvent volume; Kotha A et al.; Adsorption and expression of penicillin G acylase was studied on macroporous methacrylate polymer beads of differing pore volume, generated with kerosene . The absorption and expression of the penicillin G acylase was dependent on pore volume . Maximum expression of 57% of adsorbed enzyme was obtained on beads synthesized with 40 mL of kerosene, indicating minimum pore-diffusion limitations. Appl Biochem Biotechnol, 1991 Sep, 30(3), 265 - 72 Immobilization of penicillin acylase in porous beads of polyacrylamide gel; Prabhune A et al.; A procedure is described for the immobilization of benzylpenicillin acylase from Escherichia coli within uniformly spherical, porous polyacrylamide gel beads . Aqueous solutions of the enzyme and sodium alginate and of acrylamide monomer, N,N'-methylene-bis-acrylamide, N,N,N,N'-tetramethylethylenediamine (TEMED) and sodium alginate are cooled separately, mixed, and dropped immediately into ice-cold, buffered calcium formate solution, pH 8.5, to give calcium alginate-coated beads . The beads are left for 30-60 min in the cold calcium formate solution for polyacrylamide gel formation . The beads are then treated with a solution of glutaraldehyde and the calcium alginate subsequently leached out with a solution of potassium phosphate . Modification of the native enzyme with glutaraldehyde results in a slight enhancement in the rate of hydrolysis of benzylpenicillin at pH 7.8 and 0.05M substrate concentration . The enzyme entrapped in porous polyacrylamide gel beads shows no measurable diffusional limitation in stirred reactors, catalyzing the hydrolysis of the substrate at a rate comparable to that of the glutaraldehyde-modified native enzyme . The immobilized enzyme preparation has been used in batch mode over 90 cycles without any apparent loss in hydrolytic activity. Kansenshogaku Zasshi, 1991 Sep, 65(9), 1116 - 22 Virulence of Escherichia coli strains with R-plasmid mediated penicillin resistance in mice infections; Obana Y et al.; Penicillinase I-, II- and III-producing R-plasmid of Escherichia coli were transferred to Escherichia coli 177, KC-14, and 444 . These strains are highly virulent in mice . This study was conducted to investigate the influence of conjugative R-plasmid on the virulence of its host strains . Escherichia coli 177 after penicillinase I- or III-producing R-plasmids transfer retained parental levels of virulence . On the other hand, penicillinase II-producing transconjugants showed reduced virulence in mice . The virulence of its revertants, in which R-plasmid was eliminated by heat, were equivalent to that of the host strain . It is suggested that the decrease in the virulence of transconjugants was not due to transferred R-plasmid . The reduced virulence of the these transconjugants may be due to alterations in their components such as the lipopolysaccharides in the cell envelope. Biull Eksp Biol Med, 1991 Sep, 112(9), 260 - 2 {Antiepileptic effects of nifedipine}; Karpova MN et al.; In experiments on freely moving male Wistar rats it was shown that nifedipine in a dose 10 mg/kg (i.p.) suppressed the penicillin-induced focal epileptic activity in cerebral cortex . A similar suppressing effect of nifedipine was shown on acute generalized tonic-clonic pentylenetetrazol (PTZ) seizures (75 mg/kg, i.p.) . Nifedipine in the same dose was not effective on chronic PTZ administration (PTZ-kindling, 30 mg/kg i.p . during 28 days): when injected 30 min before each PTZ administration it didn't delay the development of kindling induced seizure susceptibility and had no effect on the severity of seizures . The administration of nifedipine in a dose of 10 or 30 mg/kg to control kindled animals which had not been treated with nifedipine had no influence on the severity of seizures provoked by a testing dose of PTZ (30 mg/kg i.p.): its intensity was similar to that of caused by PTZ injection along. Epilepsy Res, 1991 Sep, 9(3), 161 - 74 Preclinical profile of the anticonvulsant remacemide and its enantiomers in the rat; Garske GE et al.; Studies conducted by Fisons Pharmaceuticals and the Antiepileptic Drug Development Program (ADD Program) of the Epilepsy Branch (NINDS, NIH) revealed that 'remacemide' (FPL 12924, formerly PR 934-423) was effective orally in the prevention of maximal electroshock seizures (MES) in rats . In this context (-)stereoisomer (FPL 14145) was of equal potency to the racemate (remacemide), while the (+)stereoisomer (FPL 14144) was 54% less potent . With respect to neurotoxicity, remacemide and its enantiomers possessed more favorable therapeutic indices than phenobarbital and valproate and less favorable indices than phenytoin and carbamazepine . The duration of protection of rats in the MES test at the ED50 or 3 x ED50 of remacemide and the (+)isomer was better or on par with the best reference compounds, phenytoin and phenobarbital . After subchronic administration of either the ED50 or the ED97 of remacemide, no tolerance developed in the hexobarbital sleep test, however, the activities of 3 hepatic microsomal enzymes were elevated . In naive rats high doses of remacemide or its (-)isomer and low doses of phenobarbital caused an increase in spontaneous motor activity . Alternatively, motor activity was depressed subsequent to high doses of phenobarbital and phenytoin . Remacemide was inactive against pentylenetetrazol and 'kindling' seizures . It was without effect in 5 electrophysiological tests (evoked responses, recurrent inhibition, long-term potentiation, penicillin-induced discharge rate and veratridine-induced depolarization) employing the in vitro hippocampal slice technique . Moreover, remacemide failed to demonstrate potent binding in vitro to neuronal L-glutamate, gamma-amino-butyrate A, adenosine A1, benzodiazepine, N-methyl-D-aspartate (strychnine-insensitive glycine and ion channel subsites) or muscarinic receptors . In conclusion, remacemide specifically prevents seizures elicited by MES, an action predicting utility in patients with generalized tonic/clonic convulsions. Am Fam Physician, 1991 Sep, 44(3), 843 - 54 Syphilis--an STD on the increase; Kirchner JT; The number of reported cases of syphilis, including primary, secondary and congenital syphilis, has been rapidly rising since 1987 . The greatest increases have occurred in urban areas . An association between human immunodeficiency virus infection and syphilis has been established . Primary syphilis is manifested by a clean, painless ulcer called a chancre . Secondary disease often presents with constitutional symptoms and a maculopapular rash . Most infants with congenital syphilis are born without signs of infection . Serologic testing for both nontreponemal and treponemal antibodies is essential for diagnosis . Penicillin is the treatment of choice for all stages of syphilis . Case reporting and treatment of sexual contacts are two aspects of this disease that warrant greater attention from physicians. Brain Res, 1991 Aug 23, 557(1-2), 95 - 102 The electrophysiological basis of epileptiform magnetic fields in neocortex: spontaneous ictal phenomena; Barth DS et al.; In a previous report (Barth, D.S . and Di, S., Brain Research, 530 (1990) 35-39), electrical measurements of epileptiform cellular currents produced by physiologically evoked interictal penicillin spikes in rat somatosensory cortex were directly compared to the extracranial magnetic fields these currents generate . The present study uses the same methodology to extend these observations to spontaneous interictal and ictal phenomena in rat auditory cortex, and provides a more realistic empirical foundation for physical models with which to interpret non-invasive neuromagnetic recordings of human focal seizures . These data indicate that seizure foci under 1 x 1 cm2 in cortical surface area are capable of producing magnetic fields that may be recorded at extracranial distances similar to those used in humans . Furthermore, physical models based on the dipole approximation appear to be appropriate for the interpretation of ictal magnetic field phenomena in neocortex. FEBS Lett, 1991 Aug 5, 287(1-2), 31 - 3 Penicillin acylase-catalyzed protection and deprotection of amino groups as a promising approach in enzymatic peptide synthesis; Didziapetris R et al.; Penicillin acylase from E . coli is able to catalyze both the introduction and the removal of the phenylacetyl group . We have established that phenylacetyl derivatives of amino acids and peptides can be used in protease-catalyzed peptide synthesis . Here the synthesis of leucine-enkephalin using enzymes for N-terminal amino group protection, peptide bond formation and deprotection is described. J Natl Med Assoc, 1991 Aug, 83(8), 724 - 6 Chancroid: a review for the family practitioner; Jordan WC; Chancroid, as the name implies, is like a chancre . Unlike the painless chancre of syphilis, it is painful, darkfield negative, and does not respond to penicillin therapy . The number of cases have continued to rise in recent years . Because it can cause irreversible anatomical destruction, making the correct diagnosis is important and can prevent chronic morbidity. J Neurol, 1991 Aug, 238(5), 271 - 80 Acute and chronic neuroborreliosis with and without CNS involvement: a clinical, MRI, and HLA study of 27 cases; Kruger H et al.; Of the 96 serologically confirmed neuroborreliosis cases seen in our clinic between 1983 and 1988, 11 patients had mild to moderate and 4 patients had serious cerebral and/or spinal cord symptoms . Nine of these 15 patients with CNS involvement exhibited a primary chronic course of the illness . After high-dose intravenous therapy with penicillin, doxycycline or cefotaxime, given mostly in combination with cortisone, gradual recovery occurred with normalization of CSF findings characteristic of neuroborreliosis, and normalization of significantly elevated Borrelia burgdorferi IgG antibody titres in CSF and serum . Brain MRI and CT showed evidence of or were suggestive of vascular involvement which correlated with clinical symptoms in 11 of the 15 patients with CNS involvement . Brain MRI changes that were similar but much slighter in number and intensity were seen in 5 of 12 neuroborreliosis patients without clinical signs of CNS involvement (lymphocytic meningoradiculitis; Bannwarth's syndrome) . The frequencies of the HLA-DR7 (75%), HLA-B44 (50%) and HLA-A29 (33%) antigens in 12 neuroborreliosis patients with clinical symptoms of CNS involvement were significantly different from the frequencies in 12 neuroborreliosis patients without CNS involvement and in 100 control subjects . Diagnostic criteria of active neuroborreliosis are proposed. Arch Neurol, 1991 Aug, 48(8), 832 - 6 Borrelia rhombencephalomyelopathy; Kuntzer T et al.; Three patients, in whom the diagnosis of Borrelia burgdorferi infection was unknown for several years, developed a biphasic involvement of the central nervous system: an acute brain-stem dysfunction was followed up, in two patients, by a progressive, disabling myelitis and, in one patient, by further relapsing-remitting episodes of severe multifocal rhombencephalitis . The most consistent cerebrospinal fluid abnormalities in the analysis of sequential specimens were elevated total IgM levels that normalized after penicillin therapy . The neuropathologic findings in one patient showed microgliosis and meningovascular involvement of the central nervous system, resulting in two ischemic infarcts in the myelencephalon . Few spirochetes were localized in the leptomeninges and around subependymal vessels of the fourth ventricle . The vascular element consisted of an obliterative inflammatory vasculopathy in the medullary parenchyma . This study (1) provides pathologic evidence that a vascular disease induced by B burgdorferi is a pathogenetic mechanism for cerebrovascular diseases, and (2) emphasizes the similarities between neuroborreliosis and neurosyphilis. J Allergy Clin Immunol, 1991 Aug, 88(2), 213 - 7 Penicillin resensitization among hospitalized patients; Parker PJ et al.; The purpose of this study was to determine the frequency of resensitization to penicillin after oral or intravenous treatment with beta-lactam antibiotics in hospitalized patients with histories of penicillin allergy . Seventeen adults (aged 24 to 76 years) and one child (aged 10 years) were treated intravenously and/or orally with beta-lactam antibiotics after negative skin tests were obtained with benzylpenicilloyl polylysine, potassium penicillin G, and alkaline hydrolysis products of penicillin G as minor determinant mixture . Repeat skin testing was performed 1 to 12 months after the therapy . Three patients (16%) became skin test positive after the treatment . Two patients reacted to potassium penicillin G alone, and the other patient reacted to benzylpenicilloyl polylysine and minor determinant mixture . These three patients were among the 15 patients who were treated with intravenous antibiotics . This study reveals a high percentage of skin test conversion after intravenously administered penicillin therapy and confirms the present practice of advising patients with a history of penicillin allergy who have successfully completed penicillin treatment to have a repeat skin test before future exposure to beta-lactam antibiotics. Exp Neurol, 1991 Aug, 113(2), 249 - 54 Effects of applied currents on epileptiform bursts in vitro; Kayyali H et al.; In this study, results show that applied electric currents can be effective to control the neuronal bursting that characterizes epileptic activity . Recordings from the CA1 region of rat hippocampus treated with penicillin show that local inhibition of epileptiform bursts is possible by short anodic current pulses (50 ms duration) applied extracellularly . Inhibition was evidenced by a large reduction (greater than 90%) in the amplitude of field potential . Data collected from 20 slices with moderate field potentials (50-80% of maximum) showed that current needed for complete inhibition was on the order of 42 +/- 3 microA . Intracellular recordings in CA1 cells (n = 13) showed that the decrease in field potential amplitude was accompanied by suppression of intracellular neuronal firing caused by somatic hyperpolarization as measured by transmembrane potentials . The resulting hyperpolarization was on the order of 13 mv below resting potential for weakly epileptiform responses (less than 50% of maximum response), and 50 mv below resting potential for strongly epileptiform activity (greater than 50% of maximum response) . These results reveal the existence of a stimulation window within which inhibition of neuronal elements can be achieved without simultaneous excitation. J Bacteriol, 1991 Aug, 173(15), 4799 - 813 Cloning, mapping, and characterization of the Escherichia coli prc gene, which is involved in C-terminal processing of penicillin-binding protein 3; Hara H et al.; The prc gene, which is involved in cleavage of the C-terminal peptide from the precursor form of penicillin-binding protein 3 (PBP 3) of Escherichia coli, was cloned and mapped at 40.4 min on the chromosome . The gene product was identified as a protein of about 80 kDa in maxicell and in vitro systems . Fractionation of the maxicells producing the product suggested that the product was associated with the periplasmic side of the cytoplasmic membrane . This was consistent with the notion that the C-terminal processing of PBP 3 probably occurs outside the cytoplasmic membrane: the processing was found to be dependent on the secY and secA functions, indicating that the prc product or PBP 3 or both share the translocation machinery with other extracytoplasmic proteins . DNA sequencing analysis of the prc gene region identified an open reading frame, with two possible translational starts 6 bp apart from each other, that could code for a product with a calculated molecular weight of 76,667 or 76,432 . The prc mutant was sensitive to thermal and osmotic stresses . Southern analysis of the chromosomal DNA of the mutant unexpectedly revealed that the mutation was a deletion of the entire prc gene and thus that the prc gene is conditionally dispensable . The mutation resulted in greatly reduced heat shock response at low osmolarity and in leakage of periplasmic proteins. Oral Surg Oral Med Oral Pathol, 1991 Aug, 72(2), 167 - 77 Chemoprophylaxis of prosthetic joint patients during dental treatment: a decision-utility analysis; Jacobson JJ et al.; A decision-analytic model and a cost effectiveness analysis was performed on 1 million hypothetic prosthetic joint patients undergoing dental treatment, to determine the most cost-effective strategy to prevent late prosthetic joint infections . The cost per quality-adjusted life-year saved (QALY) was determined for three preventive strategies: no prophylaxis, oral penicillin, and oral cephalexin . The UCLA Pain-Walking-Function-Activity Scale was used to obtain quality-of-life adjustments (utility assessment) for the study population . Costs were derived from 70 patients hospitalized between July 1, 1982, and June 30, 1986, at the UCLA Center for Health Sciences . The most cost-effective preventive strategy was the no prophylaxis alternative ($196,500/QALY) . However, by recommending a 1-day strategy of oral cephalexin only to those dental patients at high risk for late prosthetic joint infections rather than a 3-day regimen to all patients, the cost effectiveness improved from $1.1 million/QALY to $446,100/QALY while maintaining a low risk of death (0.38 deaths per 10(6) dental visits). Comput Methods Programs Biomed, 1991 Aug, 35(4), 301 - 10 Distinguishing drug toxicity syndromes from medical diseases: a QMR computer-based approach; Mabry ME et al.; Drug effects can mimic a wide variety of diseases . Experts note that adverse drug reactions (ADRs) have become the 'greatest imitator' of disease in clinical medicine . Quick Medical Reference (QMR) is a decision support system providing diagnostic data about more than 600 medical diseases . Currently, QMR contains only limited drug information . Just as physicians have difficulty diagnosing ADRs, QMR has similar problems in differentiating natural disease manifestations from drug toxicity syndromes . To remedy this problem, two prototype Drug Syndromes (DS), Carbamazepine Toxicity and Penicillin Toxicity, were incorporated into the QMR Knowledge Base (KB) . Using detailed case reports, we demonstrated that a DS-augmented version of QMR was successful in discriminating these DS from the other diseases in QMR's KB . The addition of DS significantly improves QMR's diagnostic performance in cases in which some of the pathologic features are the consequence of drugs. Enzyme Microb Technol, 1991 Aug, 13(8), 676 - 82 Studies on improved techniques for immobilizing and stabilizing penicillin amidase associated with E . coli cells; Babu PS et al.; A method for catalyst development has been suggested for immobilizing whole E . coli cells containing penicillin amidase . Conventional methods have limitations, such as permeation of substrate and product through cellular membranes, leaching of protein and other cellular components into the reaction phase, lower specific activity compared to immobilized enzyme system, etc . The whole cell immobilization technique has been optimized for different process parameters . The most suitable conditions for this process were pH, 4.25; cell concentration, 3.75%; concentration of glutaraldehyde, 1.5%; level of bovine serum albumin as additional support, 2 mg ml-1 . The reaction was continued for 2 h . The granular catalyst has good mechanical strength, low protein leachability, and high retention of penicillin amidase activity. Fortschr Med, 1991 Jul 30, 109(22), 447 - 8 {Branhamella catarrhalis as a disease pathogen}; Simon C; Since 1980, numerous reports have been published throughout the world on the pathogenic role of Branhamella catarrhalis . Apparently, Branhamella infections have been increasing in many places . Although they can affect various organs, they are most commonly observed in the airways and eye (both in children and adults) . Not infrequently, Branhamella catarrhalis causes sepsis, in particular in immunosuppressed patients . The rapid increase in beta-lactamase-forming Branhamella strains results in frequent ineffectiveness of treatment with penicillin . In patients treated with penicillin for a primary infection by other bacteria, a secondary infection due to penicillin-resistant Branhamella organisms can subsequently occur . For treatment, therefore, beta-lactamase-stable antibiotics should be preferred. FEMS Microbiol Lett, 1991 Jul 15, 66(1), 113 - 6 Effect of a beta-lactamase inhibitor, tazobactam, on growth and penicillin-binding proteins of Borrelia burgdorferi; Urban C et al.; The effects of tazobactam, a relatively new beta-lactamase inhibitor, were investigated on growth and penicillin-binding proteins (PBPs) of Borrellia burgdorferi . A previous communication from our group demonstrated several proteins capable of binding labelled penicillin in this organism . Of these proteins, 94-kDa and 57-kDa PBPs possessed the highest affinity for penicillin and were assumed to be essential proteins involved in cell-wall synthesis . In these experiments, tazobactam was used in competition binding experiments as well as on whole spirochetes . Only the 94-kDa and 57-kDa PBPs were affected by increasing amounts of tazobactam during competition-binding experiments and growth of B . burgdorferi was also inhibited . These results may explain the in vitro activity of beta-lactamase inhibitors in general and suggest a utility for these compounds when examining PBPs with hydrolysing activity and/or organisms with beta-lactamases. J Biol Chem, 1991 Jul 5, 266(19), 12646 - 54 Delta-(L-alpha-aminoadipyl)-L-cysteinyl-D-valine synthetase from Aspergillus nidulans . Molecular characterization of the acvA gene encoding the first enzyme of the penicillin biosynthetic pathway; MacCabe AP et al.; The Aspergillus nidulans gene (acvA) encoding the first catalytic steps of penicillin biosynthesis that result in the formation of delta-(L-alpha-aminoadipyl)-L-cysteinyl-D-valine (ACV), has been positively identified by matching a 15-amino acid segment of sequence obtained from an internal CNBr fragment of the purified amino-terminally blocked protein with that predicted from the DNA sequence . acvA is transcribed in the opposite orientation to ipnA (encoding isopenicillin N synthetase), with an intergenic region of 872 nucleotides . The gene has been completely sequenced at the nucleotide level and found to encode a protein of 3,770 amino acids (molecular mass, 422,486 Da) . Both fast protein liquid chromatography and native gel estimates of molecular mass are consistent with this predicted molecular weight . The enzyme was identified as a glycoprotein by means of affinity blotting with concanavalin A . No evidence for the presence of introns within the acvA gene has been found . The derived amino acid sequence of ACV synthetase (ACVS) contains three homologous regions of about 585 residues, each of which displays areas of similarity with (i) adenylate-forming enzymes such as parsley 4-coumarate-CoA ligase and firefly luciferase and (ii) several multienzyme peptide synthetases, including bacterial gramicidin S synthetase 1 and tyrocidine synthetase 1 . Despite these similarities, conserved cysteine residues found in the latter synthetases and thought to be essential for the thiotemplate mechanism of peptide biosynthesis have not been detected in the ACVS sequence . These observations, together with the occurrence of putative 4'-phosphopantetheine-attachment sites and a putative thioesterase site, are discussed with reference to the reaction sequence leading to production of the ACV tripeptide . We speculate that each of the homologous regions corresponds to a functional domain that recognizes one of the three substrate amino acids. J Bacteriol, 1991 Jul, 173(13), 4021 - 6 Lysis of Escherichia coli by beta-lactams which bind penicillin-binding proteins 1a and 1b: inhibition by heat shock proteins; Powell JK et al.; The heat shock proteins (HSPs) of Escherichia coli were artificially induced in cells containing the wild-type rpoH+ gene under control of a tac promoter . At 30 degrees C, expression of HSPs produced cells that were resistant to lysis by cephaloridine and cefsulodin, antibiotics that bind penicillin-binding proteins (PBPs) 1a and 1b . This resistance could be reversed by the simultaneous addition of mecillinam, a beta-lactam that binds PBP 2 . However, even in the presence of mecillinam, cells induced to produce HSPs were resistant to lysis by ampicillin, which binds all the major PBPs . Lysis of cells induced to produce HSPs could also be effected by imipenem, a beta-lactam known to lyse nongrowing cells . These effects suggest the existence of at least two pathways for beta-lactam-dependent lysis, one inhibited by HSPs and one not . HSP-mediated lysis resistance was abolished by a mutation in any one of five heat shock genes (dnaK, dnaJ, grpE, GroES, or groEL) . Thus, resistance appeared to depend on the expression of the complete heat shock response rather than on any single HSP . Resistance to lysis was significant in the absence of the RelA protein, implying that resistance could not be explained by activation of the stringent response . Since many environmental stresses promote the expression of HSPs, it is possible that their presence contributes an additional mechanism toward development in bacteria of phenotypic tolerance to beta-lactam antibiotics. J Gen Microbiol, 1991 Jul, 137 ( Pt 7), 1653 - 60 Evidence for a compartmentation of penicillin biosynthesis in a high- and a low-producing strain of Penicillium chrysogenum; Affenzeller K et al.; Pulse-chase experiments using {U14C}valine were done with P2 and Q176, high- and low-penicillin-producing strains of Penicillium chrysogenum . The metabolic flux of this amino acid into protein and penicillin was measured, and compartmentation of penicillin biosynthesis was assessed . Strain P2 took up 14C-valine more slowly than strain Q176, but their rates of incorporation into protein were comparable . Incorporation of 14C-valine into penicillin occurred immediately with the high-producer P2, but exhibited a lag with Q176 . After 14C-valine had been removed from the medium, the specific radioactivity of penicillin continued to increase in Q176 but started to decrease immediately in P2 . The specific radioactivities of 14C-valine in protein and in penicillin were significantly different in both strains: Q176 had a higher specific radioactivity of valine in penicillin than P2, whereas P2 had a higher specific radioactivity of valine in protein than Q176 . Moreover, the specific radioactivity of 14C-valine in penicillin was 20-fold higher in strain Q176 than in P2 . These results indicate that penicillin and protein biosynthesis use different pools of cellular valine, and that exchange of valine between the two compartments is slow in the low-producer, but rapid in the high-producer strain . Hence these results indicate a further control point of penicillin biosynthesis in P . chrysogenum. J Reprod Med, 1991 Jul, 36(7), 543 - 5 Advanced actinomycotic pelvic inflammatory disease simulating gynecologic malignancy . A report of two cases; Hoffman MS et al.; Two women had large, solid, fixed pelvic masses simulating advanced ovarian cancer in one case and advanced cervical cancer in the other . Both patients had had plastic intrauterine contraceptive devices in situ for 7 and 17 years, respectively . Both patients required laparotomy to make the diagnosis . In both the surgery was markedly difficult because of the total absence of tissue planes . Both had obvious actinomycotic disease on routine histologic examination of the ovary and were treated with prolonged penicillin, with some, but not total, resolution of the pelvic fibrosis . The diagnosis of advanced actinomycotic pelvic inflammatory disease should be entertained in patients with a large, solid pelvic mass and an intrauterine device in situ or a recent history of intrauterine device use. Fam Plann Perspect, 1991 Jul-Aug, 23(4), 173 - 7 An ounce of prevention .. . STDs and women's health; Althaus FA; PIP: Using recent data from the U.S., the argument is reiterated that sexually transmitted diseases (STDs) have serious consequences on female morbidity, mortality, pregnancy outcome and that the cost of screening and treatment can afford significant savings . Since the rosy view of the 1950s that STDs had been eliminated with penicillin, new viral, parasitic and bacterial forms have emerged, and antibiotic-resistant classical STDs have increased yearly . 13 million new cases were reported in 1989, excluding non-reportable diseases and asymptomatic infections, such as over half of chlamydia cases . Mortality is possible from STDs, most notably from AIDS, now among the top 5 causes of death of women aged 15-44 . Other fatal outcomes are cervical cancer related to human papilloma virus, accelerated by HIV, pelvic inflammatory diseases (PID) its consequences, ectopic pregnancy . Symptomatic PID affects 1 million women, resulting in 210,000 hospitalizations per year . Ectopic pregnancy accounts for 12% of maternal mortality . STDs are involved in neonatal infections with HIV, syphilis, gonorrhea, chlamydia, cytomegalovirus, and herpes . Chorioamnionitis, a finding in many miscarriages, is caused by many of the same organisms . Several studies have projected sizeable potential savings, even within the current year, by providing STD screening and treatment in family planning clinics and prenatal care, in terms of prevention of hospitalization of women, and intensive care for low birth weight, premature and infected newborns . Antimicrob Agents Chemother, 1991 Jul, 35(7), 1517 - 9 Comparative study of various hydrogen ion buffers to assay Zn(2+)-dependent beta-lactamases; Benitez MJ et al.; The low Zn2+ complex formation constants, the capacity to degrade penicillin G in combination with Zn2+, and UV absorbance make 4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid, 3-{N-tris(hydroxymethyl)methylamino}-2-hydroxypropanesulfonic acid, 1,3-bis{tris(hydroxymethyl)methylamino}propane, and 1,4-piperazinediethanesulfonic acid convenient buffers to study Zn(2+)-dependent beta-lactamases. Monatsschr Kinderheilkd, 1991 Jul, 139(7), 425 - 8 {Borrelia infections from a dermatological viewpoint}; Vocks E et al.; Erythema migrans (EM), Borrelia lymphocytoma (BL) and acrodermatitis chronica atrophicans (ACA) are the established dermatological manifestations of borrelia infection, a complex multiorganic disease . Analogous to syphilis Borrelia infection can be classified by three stages, at which stage I (localized infection) and II (disseminated infection) are manifestations of early infection and stage III (persistent infection) a symptom of late infection . At all stages skin manifestations can be present, the above mentioned as stage-marker as well as other non-specific polymorphous skin lesions which sometimes appear at stage II . Because of its frequent (60-80%) occurrence in all borrelia infections EM has a pathognomonic importance for borrelia infection . In diagnosis serology is currently the only practical laboratory aid . False negative and false positive results must be considered . Treatment of choice is ceftriaxone, penicillin G (or amoxycillin) or tetracycline . Prophylactic antibiotic therapy for tick bites is not recommended . Congenital borrelia infections seem to be unusual, but it is likely that they can occur and cause different adverse fetal outcome or abortion. Infection, 1991 Jul-Aug, 19(4), 279 - 83 Penicillin G sodium and ceftriaxone in the treatment of neuroborreliosis in children--a prospective study; Mullegger RR et al.; A controlled clinical study was set up to examine whether penicillin G sodium (PG) or ceftriaxone (C) is superior in the treatment of acute neuroborreliosis in childhood . Within a time period of 18 months 77 children with symptoms indicative of Lyme borreliosis of the central nervous system (CNS) were seen . In 23 of these children Borrelia burgdorferi specific cerebrospinal fluid (CSF) parameters confirmed the diagnosis of a neuroborreliosis . These children were treated at random with intravenous (i.v.) PG 400,000-500,000 I.U./kg/day for 14 days (group I) or with i.v . ceftriaxone 75-93 mg/kg/day for 14 days (group II), respectively . Clinical examination and a set of diagnostic laboratory parameters were done at admission, right after therapy, three, six and partly 12 months after therapy . The general condition of all children in both groups improved dramatically during antibiotic therapy, and no relapse occurred within the observation period . Considering the clear and comparable decrease of B . burgdorferi serum titres and the clinical outcome (duration of disease and follow-up for at least six months) in children of both groups no difference between both antibiotic drugs can be demonstrated. Vet Microbiol, 1991 Jul, 28(2), 171 - 88 Biological properties of RB51; a stable rough strain of Brucella abortus; Schurig GG et al.; A rifampin-resistant mutant of Brucella abortus, designated RB51, was derived by repeated passage of strain 2308 on Trypticase soy supplemented with 1.5% agar and varying concentrations rifampin or penicillin . The RB51 colonies absorbed crystal violet and RB51 cell suspensions autoagglutinated, indicating a rough type colonial morphology for this strain . No O-chain component was detected in lipopolysaccharide (LPS) extracted from RB51 on SDS-PAGE gels stained with silver . Western blot analysis with the monoclonal antibody BRU 38, which is specific for the perosamine homopolymer O-chain of smooth Brucella LPS, indicated that the LPS of RB51 is highly deficient in O-chain when compared with the parenteral smooth strain 2308 or rough strain 45/20 . Biochemically, RB51 resembles parental strain 2308 in its ability to utilize erythritol . Intraperitoneal inoculation of RB51 into mice results in a splenic colonization which is cleared within four weeks post infection . RB51 does not revert to smooth colony morphology upon passage in vivo (mice) or in vitro . Mice infected with RB51 produce antibodies against B . abortus antigens including class 2 and 3 outer membrane proteins but not against the O-chain . Furthermore, rabbits, goats and cattle hyperimmunized with sonicates of RB51 develop antibodies to B . abortus cellular antigens but do not develop antibodies specific for the O-chain . Immunization of mice with 1 x 10(8) viable RB51 organisms confers significant protection against challenge with virulent B . abortus strain 2308. Transplantation, 1991 Jul, 52(1), 30 - 3 In vitro inhibition of platelet aggregation by the liver with UW solution as the preservation fluid; Himmelreich G et al.; The influence of UW preservation fluid in comparison with that of Euro-Collins and Bretschneider solutions on collagen, adenosine diphosphate and ristocetin-induced platelet aggregation was investigated in vitro using platelet-rich plasma of 4 healthy volunteers . The concentrations of the solutions tested were comparable to those that may be used in the transplant situation . 2UW solution inhibited ADP and collagen-induced platelet aggregation--an effect that could be attributed mainly to adenosine and secondarily to penicillin in UW solution--whereas ristocetin-induced aggregation was not affected . Euro-Collins and Bretschneider solutions did not alter platelet aggregation . The inhibition of platelet aggregation by UW may, on the one hand, contribute to bleeding complications after reperfusion and, on the other hand, be responsible for the observed lower incidence of hepatic artery thrombosis. J Laryngol Otol, 1991 Jul, 105(7), 588 - 90 Pseudoaneurysm of the internal carotid artery: a forgotten complication of tonsillitis? Watson MG, Robertson AS, Colquhoun IR. Pseudoaneurysm of the internal carotid artery is an uncommon but potentially lethal complication of tonsillar or peritonsillar sepsis, which appears to have occurred more frequently prior to the introduction of penicillin . Management of such a case is discussed, and a literature review presented. Epilepsia, 1991 Jul-Aug, 32(4), 446 - 53 Magnetic resonance imaging and 31P spectroscopy of an interictal cortical spike focus in the rat; Karlik SJ et al.; Magnetic resonance imaging (MRI) has proven to be an effective noninvasive technique for identifying lesions in patients with temporal lobe epilepsy . It has also been suggested that MRI may be sensitive to transient functional or metabolic changes in brain tissue . Increased brain electrical activity as monitored by electroencephalography causes changes in cerebral metabolism that may be responsible for focal or regional alterations in signal in the MRI of some patients . To test this hypotheses, experimental interictal cortical foci were produced in rats by topical application of penicillin to one hemisphere of the brain . In vivo MRI and phosphorous-31 (31P) spectroscopy of the focal and contralateral hemifield were performed in a 30-cm bore 1.89-T Bruker MSL system . 31P spectroscopy revealed no quantifiable differences in pH or in phosphocreatinine and ATP levels between the focal area and the contralateral hemisphere or between experimental and saline-treated control animals . There were also no differences in proton MRI . Similar areas of prolonged T2 were found near the cortex and in the deeper parenchyma in 55% of the experimental animals and 50% of the controls . These results suggest that the electrical activity from an interictal cortical spike focus is not severe enough to perturb cerebral metabolism sufficiently to be detectable by 31P spectroscopy or proton imaging techniques. Arch Neurol, 1991 Jul, 48(7), 700 - 2 Neurosyphilis in human immunodeficiency virus type 1-seropositive individuals . A prospective study; Berger JR; The prevalence of neurosyphilis in human immunodeficiency virus type 1 (HIV-1)-seropositive (HIV+) persons was assessed during the course of a study of the neurological complications of HIV-1 infection . One hundred sixty-six asymptomatic HIV+ subjects, 63 neurologically symptomatic HIV+ subjects, and six at-risk HIV-1-seronegative (HIV-) control subjects underwent cerebrospinal fluid (CSF) analysis on entry into this longitudinal study . Three (1.8%) of the asymptomatic HIV+ subjects had both a reactive CSF VDRL test and a reactive CSF fluorescent treponemal antibody-absorption (FTA-ABS) test . Two of these three subjects had a history of appropriately treated early syphilis, and all had a reactive serum rapid plasma reagin test . Of the 63 neurologically symptomatic HIV+ subjects, one patient with dementia had both a reactive CSF VDRL test and a fluorescent treponemal antibody-absorption test . Subjective improvement in cognitive skills followed high-dose, intravenous penicillin therapy . Another subject had a penicillin-responsive myelopathy accompanied by a reactive CSF fluorescent treponemal antibody-absorption test result, but a nonreactive CSF VDRL . Unsuspected neurosyphilis is relatively common in our population of asymptomatic HIV+ subjects and may be responsible for neurological disease in a significant minority of neurologically symptomatic HIV+ persons . Cerebrospinal fluid examination should be performed in all HIV+ persons with a history of syphilis or serological evidence of syphilis, regardless of prior treatment . Additionally, neurosyphilis should be considered in the differential diagnosis of neurological disease in any HIV+ person. Biull Eksp Biol Med, 1991 Jul, 112(7), 12 - 5 {Effects of activation and lesions of the superior colliculi of the lamina quadrigemina on epileptic activity in rats}; Kryzhanovskii GN et al.; In acute experiments on rats it was shown that activation of SC by bilateral microinjection of penicillin (5-15 IU) or bicuculline (25-50 ng) resulted in the increased latency and decreased severity of i.p . picrotoxin-induced seizures (2 mg/kg) . The suppression of behavioral convulsions and the decreased epileptic activity in the hippocampus and cerebral cortex were followed by occurrence of spike discharges in SC with an amplitude of 200-500 mcV and frequency of 5-12/sec which testifies to the formation of penicillin- or bicuculline-induced generator excitation in SC . The lesions of SC by kainic acid administration resulted in the decreased seizure threshold and, also, facilitated the development of seizure under conditions of picrotoxin kindling . The conclusion is made that SC activation plays an important role in the realization of functional integrative activity of the antiepileptic system. Allergy, 1991 Jul, 46(5), 379 - 85 Imbalance of CD45R and CDw29 helper cell subsets after seven days of culture from penicillin hypersensitive patients; Perez T et al.; Specific PBMC proliferation to penicillin represents one of the in vitro diagnostic procedures to show antigenic sensitization . Nine patients with suggestive clinical history of penicillin hypersensitivity, significant stimulation index in the lymphocyte transformation test (LTT), and increased CD25 expression were selected . Their phenotypic expression of T-cell subset markers was compared with that of six normal subjects after 7 days of culture . Higher percentages of CD45R and CDw29 positive cells were found in penicillin-hypersensitive patients . This group of patients showed a significantly (P less than 0.01) higher percentage of CD45R positive cells compared with normal subjects, after 7 days of culture . The percentage of CD45R cells did not differ between patients and normal subjects at day 0, and the progressive decrease of CD45R positive cells in culture of normal subjects was not observable in our patients . These results suggest that the patients with penicillin hypersensitivity have an imbalance of CD45R/CDw29 ratio after 7 days of culture, with a higher expression of CD45R positive cells. J Immunol Methods, 1991 Jun 24, 140(1), 85 - 92 A simple ELISA procedure for HIV-1 based on the enzyme beta-lactamase; Simon H et al.; The enzyme beta-lactamase (penicillin-amido-beta-lactam-hydrolase, EC 3.5.2.6.) has been shown to be suitable for use in ELISA procedures . The assay proposed requires a conjugate containing a beta-lactam-hydrolase as the enzymatic component, penicillin or one of its derivatives as substrate and an iodic complex (an iodine-starch or an iodine-polyvinylic alcohol complex) as the chromogenic component . Binding of conjugate molecules results in the transition of the iodic complex from dark blue to colourless . The transition is readily visualized without the aid of an EIA reader . The decolorization occurs specifically giving a clear-cut yes/no decision without a cut-off value . The rate of the colour transition strongly depends on the amount of bound conjugate . beta-lactamase-based ELISA techniques are of potential use in the immunological diagnosis of some virus diseases . The sensitivity and specificity of the assay were assessed on a panel of 670 negative and 141 positive HIV-1 sera, giving values of 100% and 99.85%, respectively. J Clin Pathol, 1991 Jun, 44(6), 459 - 63 Patterns of mortality in sickle cell disease in the United Kingdom; Gray A et al.; Eighteen of 384 patients entered on the Brent sickle cell disease register died between 1974 and 1989, a mortality of one per 128 years of follow up . Two children died from acute splenic sequestration and a third died from fulminant pneumococcal septicaemia: none was taking prophylactic penicillin . Acute chest syndrome was the cause of death in eight young adults and one child . Three deaths occurred after surgery . Cerebrovascular accidents contributed to the cause of death in three cases and there were two sudden unexplained deaths . Ten of the deaths occurred at home or within 24 hours of admission to hospital . Post mortem examinations were made in 14 cases, but the histological appearances of acute chest syndrome were often not recognised . In most cases for whom information was available, the cause of death (chest syndrome, pneumococcal sepsis, postoperative complications) could have been prevented. J Infect Dis, 1991 Jun, 163(6), 1201 - 6 Syphilis, neurosyphilis, penicillin, and AIDS; Musher DM; Early neurosyphilis, characterized by meningitis, cranial nerve abnormalities, and cerebrospinal accidents, was first described in patients with syphilis who received inadequate courses of arsphenamine . Although more effective, penicillin at conventional doses does not yield treponemacidal levels in the central nervous system and probably does not eradicate the infecting organisms, suggesting that it works synergistically with the host's immune response in preventing neurosyphilis . Neurosyphilis after penicillin therapy was almost unheard of in the United States until it began to appear in human immunodeficiency virus (HIV)-infected patients . Numerous cases of syphilitic meningitis, cranial nerve abnormalities, and strokes have been reported in the past decade; about one-half of reported patients had received penicillin therapy, often within the previous 6 months . Thus, more intensive diagnostic evaluation, perhaps including routine cerebrospinal fluid analysis, more intensive therapy, for example with at least three doses of benzathine penicillin, and far more rigorous follow-up are indicated in HIV-infected subjects with syphilis . Since the efficacy of conventional therapy is now uncertain, novel approaches to treatment deserve systematic evaluation. Sangre (Barc), 1991 Jun, 36(3), 211 - 5 {Syphilis and blood transfusion}; Serrano J; Along 17 years (1973-1989), syphilis screening has been performed on 146,355 blood units in the author's blood bank . A total number of 143 positive results (confirmed by MHA-TP) was registered, which means an incidence of 0.097% . Of the total number of blood units, 31,529 came from professional donors, 51 of them (0.16%) being positive, while of the 114,826 blood units from voluntary donors 92 were positive (0.08%) . With respect to voluntary donations, the highest incidence of positive reactions was found between 1980 and 1982, but this period registered also the highest number of blood units studied . Along this 17 year period 8 patients have received blood products with positive syphilis test . They were transfused on urgent request with fresh blood or platelet concentrates, the transfusion being performed before knowing the results of the screening for syphilis . No special measures were taken in 2 such cases, who died shortly after the transfusion on account of their disease . Two other were treated with penicillin at the time of transfusion . The remaining four patients received preventive penicillin . Even taking into account that positive screening tests are uncommon amongst blood donors, and that only under special circumstances the patients receiving contaminated blood may develop the illness, it seems advisable for every blood bank to perform the screening for syphilis on every blood donation. Hautarzt, 1991 Jun, 42(6), 356 - 65 {Borrelia infections of the skin--progress of knowledge since the discovery of Lyme disease}; Garbe C; The description of Lyme disease in 1976 and the detection of its causative agent, the spirochete Borrelia burgdorferi (B . burgdorferi), in 1982 led to an increase in our knowledge of the course of B . burgdorferi infection and its clinical manifestations . The classic tick-borne dermatoses erythema chronicum migrans (ECM), lymphadenosis benigna cutis (LABC) and acrodermatitis chronica atrophicans (ACA) were proven by isolation of the spirochete from skin lesions to be caused by B . burgdorferi infection . In early disease (less than 1 year) ECM and LABC can develop locally at the site of infection (stage I), but both these skin manifestations can also occur together with multiple lesions after dissemination of the causative organism (stage II) . ACA is typical for late infection (greater than 1 year, stage III) . High titres of B . burgdorferi antibodies have been found in patients with localized sclerodermalike lesions (circumscribed scleroderma, lichen sclerosus et atrophicus, anetoderma), and frequent simultaneous occurrence of ACA suggests an association with late B . burgdorferi infection . Similarly, we found four cases of cutaneous B-cell lymphoma possibly arising from LABC in association with the same markers of late B . burgdorferi infection . Additionally, some cases of Schonlein-Henoch purpura and of Shulman syndrome may be associated with Lyme borreliosis . The disease is endemic in central Europe, and almost exclusively ticks of the Ixodes ricinus complex seem to transmit B . burgdorferi to humans, whereas the reservoir of infection seem to be rodents, especially mice . The main diagnostic tool is serological examination for B . burgdorferi antibodies, which will become detectable 3-6 weeks after infection . Enzyme-linked immunosorbent assay (ELISA) and the indirect immunofluorescence test (IFT) revealed similar sensitivity . In early disease, sensitivity for antibody detection could be improved by immunoblot technique and by flagellum-ELISA, which is specific for this early sensitizing B . burgdorferi antigen . For treatments, penicillin is no longer recommended as the drug of first choice, because low sensitivity of B . burgdorferi has been observed in vitro and in vivo . Tetracycline, doxycycline and amoxicillin p.o . are now preferred for the treatment of Lyme borreliosis, and in neurologic and cardiac abnormalities ceftriaxone i.v . is recommended . Treatment duration should be 14 days in early disease and 30 days in late disease. J Paediatr Child Health, 1991 Jun, 27(3), 175 - 9 Failure of intravenous infusions in neonates; Hecker JF et al.; The median life expectancy (survival) of 286 peripheral intravenous infusion sites in 105 babies in a children's intensive care unit was 36 h . Unadjusted univariate survival analysis revealed that dextrose infusions and the initial infusions received by a baby had longer survival than total parenteral nutrition (TPN) infusions and later infusions respectively . Also infusions with cloxacillin and penicillin survived for longer than average while infusions with phenytoin had reduced survival . Gestational age, weight, infusion site, other drugs, co-infusion of Intralipid with TPN solutions and neutralization of TPN did not influence survival of infusions . Multivariate survival analysis confirmed the findings for TPN and penicillin but not for cloxacillin, phenytoin or later infusions . Multivariate analysis also suggested that survival was improved with ampicillin and aminophylline and worse for leg sites, for older babies and for infusions in which the fluids were given at greater rates . It also indicated that neutralization of TPN improved survival. Trends Biochem Sci, 1991 Jun, 16(6), 234 - 7 Semi-synthetic approaches to novel penicillins; Nayler JH; The first part of this account of the discovery of penicillin, published in last month's issue of TIBS, concluded with the detection of 6-beta-amino-penicillanic acid (6-APA), the nucleus of the penicillin structure . The exploitation of 6-APA led to the preparation of a range of clinically important semi-synthetic penicillins, which is described in this article. Changgeng Yi Xue Za Zhi, 1991 Jun, 14(2), 101 - 5 {The clinical observation and follow-up of acute rheumatic fever}; Liang CD et al.; There were 15 patients under 15 years of age with cases of acute rheumatic fever diagnosed by revised Jones criteria admitted to pediatric department, Chang Gung Memorial Hospital of Kaohsiung from Jan . 1986 through Dec . 1989 . There were 11 boys and 4 girls . The age of onset was more commonly between 13 and 15 years old . Carditis was the most common clinical presentation, noted in 13 cases . Eleven cases had valvular involvement: mitral regurgitation (MR) and mitral valve prolapse (MVP), 5 cases; MR and aortic regurgitation (AR), 4 cases; MR, 1 case; and MVP, 1 case . One case with MR + AR also suffered transient acute glomerulonephritis, which presented with gross hematuria but improved one week later . And one case with severe MR expired due to severe congestive heart failure . Eleven of the 14 survivors had regular follow-up at our clinic with an interval of 3 months to 38 months, and received parenteral benzathine penicillin for prophylaxis . During follow-up, the murmur in 4 cases with MR + MVP and 2 cases with MR + AR disappeared within 2 months . One of the three cases who had not received secondary prophylaxis had recurrence of rheumatic fever 3 years later after the initial diagnosis. J Trop Pediatr, 1991 Jun, 37(3), 100 - 5 A clinico-epidemiological study of sickle cell anaemia in Saudi Arabia; Mulik R et al.; Ninety-nine Saudi Arabian children aged between 3 months and 15 years attending the sickle cell anaemia (SCA) clinic were studied using a review of case notes and an interview at clinic visits . All the patients come from the southwest and west area of Saudi Arabia . Despite the lack of infant screening for SCA, 73 per cent were diagnosed before the age of 3 years, reflecting severe early symptoms of the disease . The serious complications of SCA were two times higher, the number of admissions were three times higher and the attack rate for pneumococcal meningitis was nine times higher in our study population than previously reported from the Eastern Province of the country . Hand-foot syndrome was the commonest complication affecting 58 per cent of the children . It has been stated previously that there is no need to give penicillin prophylaxis to SCA children in Saudi Arabia, based on the observations in the Eastern Province only . Our study shows that SCA in western and southwestern population of Saudi Arabia is as severe as is described in American blacks . Therefore, we recommend penicillin prophylaxis to be given to the SCA children in the southwest and west regions of the country. Rapid Commun Mass Spectrom, 1991 Jun, 5(6), 263 - 8 Investigation of collisional-activation decomposition process and spectra in the transport region of an electrospray single-quadrupole mass spectrometer; Voyksner RD et al.; The use of collisional-activation dissociation (CAD) in the electrospray transport region was evaluated for generating structural information on several pesticides and antibiotics . The collision energy used to generate the CAD spectra could be varied easily by changing the capillary/skimmer potential difference, imparting from 0 eV to above 16 eV internal energy to the near thermal ions generated by electrospray . The internal energy distribution for low-energy collisions (capillary/skimmer potential difference of 20 V) closely matches the curves generated by a triple-quadrupole mass spectrometer . Furthermore, the CAD spectra for selected compounds generated by electrospray in the transport region at a capillary/skimmer potential difference of 30-50 V closely resembled those obtained from the {M + H}+ ion by a triple quadrupole using 30 eV collision energy . The CAD of ions in the transport region resulted in 70% to 80% daughter-ion yields and minimal loss in overall ion current compared to the ion current for protonated or cationized parent molecules . The major daughter ions for 10 pg of Aldicarb and penicillin G could be detected (signal-to-noise ratio greater than 5) under full-scan CAD conditions. Jpn J Psychiatry Neurol, 1991 Jun, 45(2), 265 - 70 Propagation of acute seizure activities observed by local cerebral glucose metabolism; Kato M et al.; We studied the propagation of acute focal seizure activities in animals by means of the {14C}deoxyglucose method . Seizures were induced unilaterally by injecting penicillin in the neocortical area 4 and area 9 in the monkey, and by injecting kainic acid in the hippocampus of the rat and in the ventral posterolateral thalamic nucleus of the cat . The earliest and the most consistent propagation was the one to the target structures of the primary focus, mediated through the "preferential" projection pathways . At a more advanced stage, the propagation to the immediately adjoining brain regions occurred, followed by the secondary propagation to the target structures of the adjoining regions . Propagation to the contralateral homologous structure was not a major one at the early stage unless the structure of the primary focus had its own commissural connections. P N G Med J, 1991 Jun, 34(2), 122 - 8 Management of common potentially serious paediatric illnesses by aid post orderlies at Tari, Southern Highlands Province; Rogers S et al.; Systematic observations were made of a small number of aid post orderlies (APOs) managing children with the common but potentially serious symptoms of cough, fever and diarrhoea . On-site performance was evaluated against recommended management guidelines set out in Dr Keith Edwards' Diagnosis and Treatment of Common Childhood Illnesses for APOs . History taking at the aid post was brief and usually non-exploratory; examination of patients was often neglected . Drug prescription was generally appropriate for the diagnosis made, but drug dosages were often incorrect and treatment principles were rarely explained to guardians . Preventive health issues were rarely tackled . Our study reaffirms the need for on-site assessment of the performance of paramedical workers, sets priority demands for continuing education of health workers, and provides a framework for competency-based problem-solving activities within this contextPIP: This operational study of the performance of aid post orderlies (APOs) at Taril, Southern Highlands Province, Papua New Guinea, was conducted as a follow up to prior operations research workshops and specific research which highlighted the need for adequate medical care . The assessments of the clinical performance (medical history taking, examination, diagnosis, treatment, and advice) of APOs were made by a trained Huli observer in mid-1988 . 86 consultations were recorded for children brought to the aid posts for complaints of cough (40), fever (24), or diarrhea (22) and seen by 7 Tari APOs . Data were evaluated by a medical officer who used the recommended Health Department reference . Diagnosis and Treatment of Common Childhood Illnesses for APOs . Results for each illness are provided . APOs made an adequate diagnosis based on the mild and self limiting symptoms, but the medical histories and examinations were too superficial to assess the severity of the illness . Sometimes the level of treatment was inappropriate, i.e., 70% of the children received appropriate cough mixtures and antimalarials for coughs, but over 50% received inadequate doses of procaine penicillin for their age . Several children were not properly referred to the hospital for management of severe dehydration . Treatments were qualitatively correct for the diagnosis made, but inappropriate doses were often prescribed . Information was rarely given to guardians on the need for repeat medications or the signs of treatment failure . There was ample opportunity to reinforce the importance of immunization, adequate nutrition, malaria control, or personal and food hygiene but APOs did not take advantage of the situation . The results reinforce the need for on-site assessment of paramedical workers who are entrusted with frontline care of patients . It has been found that APOs are often neglected by senior staff; there are complaints from APOs that they feel unappreciated by Health Department staff and the community served . Reference is made to a study of rural health services which found that only 585 of officers in charge of health centers had made any supervisory visit in the 2 months preceding the survey . In some provinces APOs sometimes are given a 1-week inservice training period a year . Structural changes, APO selection procedures, education, inservice training, supervision, and support must be addressed in order to overcome some of the apparent weaknesses in the delivery system . The emphasis is on a problem-based approach and education and continued training . Lancet, 1991 Jun 1, 337(8753), 1308 - 10 Allergic reactions to long-term benzathine penicillin prophylaxis for rheumatic fever . International Rheumatic Fever Study Group. {Fungal toxin dihydroxyaflavinine inhibits non-competitively GABAA receptor channel expressed in Xenopus oocytes} Yao Y, Li Y. Shanghai Institute of Physiology, Academia SinicaDihydroxyaflavinine is an indole-derived metabolite of Aspergillus flavus . Its action on GABA-induced response was quantitatively studied on the GABAA receptor expressed in Xenopus oocytes after injection of chick brain mRNA under voltage-clamp conditions . Dihydroxyaflavinine inhibits GABA-induced current non-competitively with KI = 12 mumol/L . This blockage is rapidly reversible . In comparison, the inhibitory effect of penicillin on GABAA receptor is enhanced by increasing GABA concentration . Ro 15-1788 (a benzodiazepine ligand with KD = 0.6--2 nmol/L) of concentration as high as 1 mumol/L, does not mask the action of 10 mumol/L dihydroxyaflavinine, indicating that dihydroxyaflavinine acts on a site different from benzodiazepines . Dihydroxyaflavinine appears to expedite desensitization of the receptor, which is similar to the action of picrotoxin and in contrast with that of penicillin and bicuculline. Neuropharmacology, 1991 Jun, 30(6), 637 - 42 In vitro depressant effects of U-54494A, an anticonvulsant related to kappa opioids, in the hippocampus; Proietti ML et al.; The effects of cis-3,4 dichloro-N-2-(1-pyrrolidinyl)cyclo-hexyl-benzamide (U-54494A), an anticonvulsant related to kappa opioids, were studied in vitro on the extracellular electrical activity of the CA1 region of slices of hippocampus in the rat . The effects of U-54494A were compared to those of the kappa opioid agonist trans-3,4 dichloro-N-2-(1-pyrrolidinyl)cyclo-hexyl benzeneacetamide methane sulphonate (U-50488H) . Both U-54494A and U-50488H, in concentrations of 50 and 100 microM, respectively, reduced the magnitude of the orthodromically evoked CA1 population spikes after electrical stimulation of the stratum radiatum (100-200 microA, 70 microseconds, 0.1 Hz) . Naltrexone (25 microM), or the selective kappa opiate receptor antagonist, 1-cyclopenthyl-5-(1,2,3,4,5,6-hexahydroxy-3,6,11-trimethyl-2 -6-methano-3- benzazocin)-3-pentatone methane sulphonate (WIN 44441-3) (25 microM), prevented the depressant activity of U-54494A (200 microM) on the CA1 population spikes . High calcium (+3mM) solutions prevented the depressant activity of increasing concentrations of both U-54494A and U-50488H on the amplitude of CA1 population spikes . Up to 200 microM, both drugs were ineffective in depressing the epileptiform bursting in CA1, due to 1 mM penicillin or to perfusion of the slice in absence of magnesium ions . The results demonstrate: (1) the inability of U-54494A to show antagonistic activity in two in vitro models of interictal epilepsy; (2) a depressant effect of U-54494A on basal synaptic transmission in the CA1 region of the hippocampus, which may be related to an influence on transneuronal calcium currents and which may be involved in the reported antagonism of ictal epileptic seizures by drugs. BMJ, 1991 May 4, 302(6784), 1051 - 2 Allergy to penicillin: fable or fact? Surtees SJ, Stockton MG, Gietzen TW. OBJECTIVE--To assess whether, on the basis of one blood test, penicillin allergy might be excluded sufficiently for general practitioners to give oral penicillin to patients claiming a history of penicillin allergy . DESIGN--Prospective study of patients referred by general practitioners . SETTING--Outpatient allergy clinic in a district general hospital . PATIENTS--175 referred patients who gave a history of immediate type reaction to penicillin, of whom 144 attended as requested and 132 completed the investigations . MAIN OUTCOME MEASURES--History and examination, serum radioallergosorbent test to phenoxymethylpenicillin and benzylpenicillin, and oral challenge with penicillin . RESULTS--Of 132 patients, four were confirmed to have penicillin allergy by the radioallergosorbent test and 128 had an oral penicillin challenge without ill effect . CONCLUSIONS--Most patients who gave a history of penicillin allergy are not so allergic, and their actual allergic state should be substantiated whenever feasible . For patients reporting minor or vague reactions negative findings with a radioallergosorbent test to phenoxymethylpenicillin and benzylpenicillin provide sufficient evidence to give oral penicillin safely. J Am Acad Dermatol, 1991 May, 24(5 Pt 2), 832 - 5 Tertiary syphilis of the face; Chung G et al.; We report a case of noduloulcerative tertiary syphilis that had gone misdiagnosed as discoid lupus erythematosus for many years . This case is noteworthy for (1) a Jarisch-Herxheimer-like reaction, (2) a dramatic response to penicillin therapy despite the presence of long-standing disease, and (3) posttreatment granulomas of possible hypersensitivity origin. Ann Allergy, 1991 May, 66(5), 385 - 92 Current status of mold immunotherapy; Dhillon M; There is evidence to suggest that molds can cause IgE-mediated upper respiratory tract disorders and immunotherapy is efficacious in a select group . The environmental sampling studies show a remarkably small numbers of molds accounting for a majority of the mold load in various diverse locations . These are Cladosporium, Basidiospores, Aspergillus, and Alternaria-Penicillin families . Basidiospores have been underreported in the older studies because of difficulties in their identification . Whether the absolute mold level is the most important factor leading to IgE formation and induction of upper respiratory tract symptoms is uncertain . Certainly, the majority of the studies are based on the assumption that the absolute level of mold in the environment is the most important factor leading to the development of symptoms, but this is not based on strong evidence . A major problem in the majority of the studies is a lack of standardization of extracts which may lead to false negatives on skin testing and thus produce variable data in population evaluations comparing the prevalence of mold to its ability to induce IgE production and symptoms . The best current trials to document the efficacy of mold immunotherapy have been with the standardized Cladosporium extract . Unfortunately, these results cannot be extrapolated to the commercially available mold extracts available in the United States either for immunotherapy or for skin testing . These extracts are highly variable in their potency, prone to high false negative rates, and at best serve as poor skin testing reagents and possibly even worse immunotherapy reagents . Adequately standardized mold reagents are urgently needed to determine whether the Cladosporium data can be extrapolated to them in any meaningful way. Am J Physiol, 1991 May, 260(5 Pt 2), R934 - 40 Respiratory responses to focal and generalized seizures in cats; Paydarfar D et al.; We studied the effects on breathing of seizures induced by focal injection of penicillin G into the parietal cortex in 13 anesthetized cats . Electrocorticograms, ventilation, end-tidal PCO2, and intrapleural and arterial pressures were monitored; changes of these variables were related to the stages of motor seizure . The first respiratory responses, tachypnea and hyperpnea, usually occurred before any peripheral muscular contractions developed . Progression of the seizure was always accompanied by further tachypnea and hyperpnea . The hyperpnea associated with all stages of seizure activity resulted in hypocapnia, which was sustained even during prolonged tonic-clonic motor convulsions that caused a threefold increase of metabolic rate . The extreme tachypnea of tonic generalized convulsions led to increased end-expiratory lung volume because of dynamic hyperinflation associated with very short expiratory durations in the tonic phase . We suggest that the profound effects of seizures on respiration are by feedforward mechanisms from the cortical focus itself and from subcortical circuits, such as hypothalamus, that become involved during seizure propagation and generalization . Peripheral respiratory feedback mechanisms are not important for the genesis of seizure-induced hyperpnea. Rinsho Shinkeigaku, 1991 May, 31(5), 561 - 3 {Lyme disease with the triad of neurologic manifestations}; Shiokawa T et al.; A 40-year-old man developed progressive neurologic manifestations following a tick bite with subsequent localized erythema migrans . These manifestations included bilateral sensory radiculoneuritis (T7-12), rectovesical dysfunction, paraparesis, right facial palsy and nuchal rigidity . Both serum and cerebrospinal fluid titers of IgG antibody against Borrelia burgdorferi were 1:8,192 using indirect immunofluorescence assay . No IgM antibody was detected . With high-dose intravenous penicillin and corticosteroid treatment the neurologic symptoms and signs gradually subsided, with a corresponding decrease in the IgG antibody titers . Among the cases of Lyme disease reported so far in Japan, the present case seems to be typical and serious in terms of the severity of nervous system involvement and the intensity of the antibody response. J Assoc Off Anal Chem, 1991 May-Jun, 74(3), 497 - 501 Determination of penicillin G residues in edible animal tissues by liquid chromatography; Boison JO et al.; An improved method has been developed for the determination of benzyl penicillin in animal tissues . Tissues are fortified with a known amount of penicillin V (internal standard) and extracted with water . The extract is deproteinized with sulfuric acid and sodium tungstate, filtered, and concentrated on a conditioned C18 solid phase extraction column . Penicillin V and benzyl penicillin are then eluted from the column with 1 mL 60% acetonitrile-35% water-5% 0.2M phosphate buffer solution and derivatized with 1 mL 1,2,4-triazole-mercuric chloride solution at 65 degrees C for 30 min . An aliquot of this sample is analyzed by reverse phase liquid chromatography with UV detection at 325 nm . The limit of detection is 5 micrograms/kg (ppb) penicillin G (8.4 IU/kg) in liver, kidney, and muscle tissues). Am J Otol, 1991 May, 12(3), 184 - 7 Endolymphatic sac surgery for refractory luetic vertigo; Huang TS et al.; The clinical symptoms of otitic syphilis, either congenital or acquired, are indistinguishable from Meniere's disease . In most cases the symptoms can be controlled by long-term and intensive medical treatment with penicillin and steroids . However, in some cases, luetic vertigo is refractory to such medical regimens, and surgical intervention may become necessary . We report on endolymphatic sac procedures performed on 37 patients with presumed luetic vertigo refractory to medical treatment, between March 1980 and December 1987, with follow-up ranging from 2 years to 9 years and 9 months . Results show that vertigo was completely and substantially controlled in 81 percent of cases, with 2 patients showing improvement in hearing, as assessed with AAO-HNS criteria . It is concluded that endolymphatic sac surgery is appropriate in treating refractory luetic vertigo when intensive medical therapy is unsuccessful, particularly in cases of late or tertiary-acquired lues, such as in this series. Chin Med J (Engl), 1991 May, 104(5), 428 - 31 Hypothalamic encephalitis with oligodendrocytic glial nodules . Case report of a Chinese boy; Wang LN et al.; A case of hypothalamic encephalitis proved by postmortem examination is reported . The patient was a three-year-old Chinese boy who had complained of obesity for one year and fever for half a year . Three days after admission to a hospital, the patient suddenly died of allergic reaction to intramuscular penicillin, without additional complaints . Autopsy revealed severe bilateral outfall of neurons in the ventromedian hypothalamic nuclei with diffuse hyperplasia of astrocytes and some glial nodules consisting chiefly of oligodendroglias and perivascular cuffing . Similar changes were noticed in hypothalamus at the level of optic chiasm, but the posterior hypothalamic nuclei and lateral hypothalamic nuclei were intact . This article provides significant data for the study of hypothalamic function. J Neurol Sci, 1991 May, 103(1), 48 - 50 Syphilitic meningitis causing paraparesis in an HIV-negative woman; Byrne TN et al.; Syphilitic meningitis, which can occur near the time of secondary syphilis, is frequently asymptomatic . There has been one recent report of an HIV-positive patient who developed syphilitic polyradiculopathy following a recent history of secondary syphilis . We describe an HIV-negative woman in whom paraparesis occurred secondary to syphilitic meningitis . Complete recovery followed a course of high-dose intravenous penicillin therapy, emphasizing the treatable nature of this cause of paraparesis. Minn Med, 1991 May, 74(5), 15 - 9 Patients go home for care . But do their doctors make house calls? Teigen T. Caring for a patient at home no longer consists simply of a black bag and a stethoscope warmed in the physician's palm . No longer is it a quarantine sign the physician tacked up on the front door, or a thermometer and an injection of penicillin . Today, taking care of a patient at home often involves sophisticated equipment, a highly trained staff of nurses and allied professionals, and a set of skills and a body of knowledge with which many physicians are neither familiar nor comfortable. J Heart Lung Transplant, 1991 May-Jun, 10(3), 401 - 8 Functional studies of the heart during a 24-hour preservation using a new autoperfusion preparation; Chien SF et al.; Serial cardiac function studies were carried out during a 24-hour preservation in a new autoperfusion multiorgan preparation using adult Yorkshire swine (n = 8) . The heart was removed with the lungs, liver, pancreas, duodenum, and both kidneys while they were still perfused by the heart and oxygenated by the lungs . The organs were placed in a 32 degrees C bath solution containing lactated Ringer's, heparin, and neomycin . Fresh blood and a solution containing glucose (10%) with potassium chloride (2 gm/L), calcium chloride (1 gm/L), heparin sodium (100 mg/L), mannitol (12.5 gm/L), insulin (100 U/L), metronidazole hydrochloride (500 mg/L), penicillin (1,000,000 U/L), and methylprednisolone (250 mg/L) were given slowly through the portal vein . A fat emulsion 2 ml, methylprednisolone 30 mg, and heparin sodium 20 mg were given through the portal vein every 2 hours . No inotropic drugs were used . Aortic systolic pressures ranged from 79 to 97 mm Hg; the aortic diastolic pressures ranged from 44 to 61 mm Hg . Central venous pressures ranged from 0.4 to 2.0 mm Hg, and the heart rate was 69 to 81 beats/min . Left ventricular maximum dp/dt ranged from 1405 to 1836 mm Hg/sec, and maximum dp/dt/p ranged from 17.0 to 26.2 (sec-1) . Aortic blood flow ranged from 1.2 to 1.6 L/min, and systemic resistance ranged from 33 to 53 U . Lactic acid decreased from 8.15 to 2.80 mmol/L . Myocardium wet/dry weight ratio after preservation averaged 5.13 (vs 5.09 for control) . These results suggest that the heart may be preserved up to 24 hours with minimal change in function with this new autoperfusion preparation.(ABSTRACT TRUNCATED AT 250 WORDS) Antimicrob Agents Chemother, 1991 May, 35(5), 886 - 91 Characterization of a beta-lactamase found in Eikenella corrodens; Lacroix JM et al.; Eleven strains of Eikenella corrodens with beta-lactamase activity were isolated from a patient with refractory periodontitis who had previously been treated with penicillin antibiotics . These strains were relatively resistant to benzylpenicillin, amoxicillin, and ampicillin (MICs, greater than or equal to 64 micrograms/ml); susceptible to amoxicillin-clavulanate (2:1) (MICs, less than or equal to 4 micrograms/ml); and moderately susceptible to cephalothin and cephaloridine (MICs, 0.12 to 16 micrograms/ml) . The addition of 1 microgram of potassium clavulanate, a beta-lactamase inhibitor, per ml resulted in a significant increase in the susceptibilities of these strains to penicillins but not to cephalosporins . Potassium clavulanate had no effect on non-beta-lactamase-producing strains . Enzyme production was constitutive since activity was not increased when cells were cultivated in the presence of benzylpenicillin . Enzyme activity was strongly inhibited by potassium clavulanate, sulbactam, and iodine; weakly inhibited by cloxacillin, imipenem, and moxalactam; but not inhibited by aztreonam, EDTA, or p-chloromercuribenzoate . By gel infiltration, the enzyme had an estimated molecular mass of 29 kDa . Isoelectric focusing of the partially purified enzyme gave a major beta-lactamase band at pH 5.50 and a minor band at pH 5.60 . Plasmids were not detected in any of the 11 beta-lactamase-positive strains . This enzyme is considered to belong to class 2a of the Bush classification scheme. Neuropediatrics, 1991 May, 22(2), 107 - 9 Infective acute transverse myelopathy . Report of two cases; Linssen WH et al.; Two children with acute transverse myelopathy following adenovirus and Borrelia Burgdorferi infections are presented . The diagnosis stems from the clinical presentation, the determination of specific antibodies in serum and the favorable response to penicillin treatment in the case of neuroborreliosis . Both children made a good recovery . The cerebrospinal fluid examination showed a highly increased myelin basic protein concentration, indicating demyelination. Trends Biochem Sci, 1991 May, 16(5), 195 - 7 Early discoveries in the penicillin series; Nayler JH; It is now 50 years since the therapeutic potential of penicillin was first demonstrated . This first antibiotic and the series of compounds derived from it have been of immense importance in modern medicine . This article describes the early search for more potent penicillin derivatives, culminating with the discovery of an intermediate of penicillin biosynthesis, 6-beta-amino penicillanic acid (6-APA) . A companion article in next month's TIBS will chart the subsequent exploitation of 6-APA and the preparation of a range of clinically important semi-synthetic penicillins. Hinyokika Kiyo, 1991 May, 37(5), 507 - 14 {Clinical analysis of male urethritis}; Nakata S et al.; We reviewed 497 patients with male urethritis diagnosed between January, 1986 and March, 1989 at the Asama General Hospital . The incidence of gonococcal urethritis (GU) was 47.7%, and that of non-gonococcal urethritis (NGU) 52.3% . There was no difference in the age distribution between GU and NGU . Prostitutes were the most common source of the infection in both GU and NGU . Incubation periods were longer in NGU than in GU, statistically . Urethral discharge was the most common symptom . Purulent urethral discharge was seen more commonly than serous urethral discharge in GU . On the contrary, serous urethral discharge was more common in NGU . Penicillin-resistant gonococcus comprised 29.4% and mixed infection of the C . trachomatis existed 25.6% in GU . C . trachomatis was detected in 71.8% in NGU . In GU, new quinolones and penicillins were administered frequently . The effective rates 1 week after the administration were 80.6% and 83.3%, respectively . In NGU, new quinolones and minocycline were administered frequently . The effective rates were 70.4% and 85.3%, respectively . Ofloxacin (OFLX) showed the highest effective rate to NGU among the four new quinolones . The relapse rate for the two-week administration group was lower than that for the one-week-administration group, but the difference was not statistically significant. Eur J Biochem, 1991 Apr 10, 197(1), 75 - 80 Site-directed chemical conversion of serine to cysteine in penicillin acylase from Escherichia coli ATCC 11105 . Effect on conformation and catalytic activity; Slade A et al.; Penicillin acylase (EC 3.5.1.11) was completely inactivated with equimolar phenylmethane {35S}sulphonyl fluoride (PhMe35SO2F); the stability of the sulphonyl group in the modified protein was determined by measurement of the radioactivity in ultrafiltrates . In 8 M urea, the rate of loss of the sulphonyl group was similar to that observed in PhMeSO2F-inactivated chymotrypsin {Gold, A.M . & Fahrney, D . (1964) Biochemistry 3, 783-791} . Incubation of the PhMeSO2F-inactivated acylase with 0.7 M potassium thioacetate yielded an acetylthiol enzyme which was subsequently converted to a thiol-enzyme during incubation with 10 mM 6-aminopenicillanic acid . 4-Pyridyl-ethylcysteine was released by acid hydrolysis after reaction of the thiol-protein with 4-vinylpyridine . The rates of reaction of thiol-penicillin acylase with iodoacetic acid and 2,2'-dipyridyl disulphide were consistent with the presence of an incompletely accessible cysteinyl sidechain . After carboxymethylating the thiol-enzyme with iodo{2-3H}acetic acid, the label was shown by SDS/PAGE and sequencing analysis to be associated exclusively with the beta-chain NH2-terminal residue, indicating conversion of Ser290 to S-carboxymethyl-cysteine . Near-ultraviolet CD spectra showed the conformation of thiol-penicillin acylase to be indistinguishable from that of the native protein but the catalytic activity was less than 0.02% of that of the normal enzyme . The possibility that Ser290 acts as a nucleophile in catalysis is discussed. J Pediatr Gastroenterol Nutr, 1991 Apr, 12(3), 310 - 4 Liver function in early congenital syphilis: does penicillin cause a deterioration? Venter A, Pettifor JM, Duursma J, Pudifin DJ, Smyth A, Becker PJ. In this prospective study, neonates with clinical congenital syphilis were investigated to determine if penicillin therapy caused a deterioration in liver function . The relationship between circulating immune complexes and liver involvement was monitored, and the efficacy of steroid therapy as an adjunct in the treatment of congenital syphilis was investigated . Thirty neonates with clinical congenital syphilis were randomly assigned into two groups: one group received penicillin therapy only, and the other group penicillin and prednisone as an adjunct . Twenty-one infants who did not have clinical or serological syphilis, born to seropositive mothers, served as a "control" group . Liver function tests, full blood counts, and immunological studies were performed at various intervals up to 3 months of age . Although the symptomatic groups differed significantly from the asymptomatic group in most of the parameters measured, there were no significant differences noted between the two symptomatic groups at any time point . No direct relationship between penicillin therapy and either deteriorating liver function or the presence of circulating immune complexes could be demonstrated . Also, prednisone therapy did not modify any of the parameters studied. Clin Orthop, 1991 Apr, (265), 178 - 82 Infections of the clavicle in children; Rasool MN et al.; Of 23 children with infections of the clavicle, 11 had pyogenic osteomyelitis, four had tuberculosis, and eight (infants) had congenital syphilis . Acute pyogenic infections were treated by drainage . Resection of the clavicle was performed in chronic cases . Curettage and antituberculosis drugs were effective for children with tuberculous infection of the clavicle . Procaine penicillin was used for the treatment of congenital syphilis . Biopsy is generally necessary to differentiate chronic infection from neoplasm. Farmaco, 1991 Apr, 46(4), 565 - 77 Enzymatic synthesis of ampicillin: a chemometric optimization; Boccu E et al.; Statistical methods of optimization were applied to the enzymatic semisynthesis of ampicillin catalyzed by penicillin acylase . Since the traditional approach fails in determining both the presence of interactions between the variables and their magnitude, the reaction was reconsidered by means of chemometric techniques . In this work we determined the interaction between temperature and pH for the first time. Int J Pediatr Otorhinolaryngol, 1991 Apr, 21(2), 155 - 61 Beta-lactamase production and bacterial tolerance in recurrent acute otitis media; Roos K et al.; Different reasons for treatment failure or relapse of acute otitis media (AOM) have been suggested . In this study 38 children (8 treatment failures, 13 relapses of AOM within one month and 17 with a new AOM) were compared to 25 matching healthy children, regarding beta-lactamase producing bacteria and tolerance to penicillin V and ampicillin . Branhamella catarrhalis was the most common bacteria found in the nasopharynx and was isolated in 60% of children with AOM and in 48% of the control group . Fifty-two percent of the children classified as treatment failure or relapse of AOM had aerobic beta-lactamase producing bacteria in NPH . No bacteria tolerant to penicillin or ampicillin were found . Thus, beta-lactamase-producing bacteria seem to play a decisive role in treatment failure and relapse of AOM . On the other hand, tolerance to penicillin V or ampicillin does not seem to have any impact on healing of AOM. Analyst, 1991 Apr, 116(4), 387 - 90 Utility of certain pi-acceptors for the spectrophotometric determination of some penicillins; Askal HF et al.; Two simple and sensitive spectrophotometric methods are described for the determination of six penicillin derivatives . The methods are based on the reaction of these drugs as n-electron donors with either 2,3-dichloro-5,6-dicyano-p-benzoquinone (DDQ) or 7,7,8,8-tetracyanoquinodimethane (TCNQ) as pi-acceptors, to give a highly coloured radical anion . The coloured products are quantified spectrophotometrically at 460 and 842 nm for DDQ and TCNQ, respectively . The optimization of the different experimental conditions is described . The interference from streptomycin sulphate and common degradation products was also studied . The proposed methods were applied successfully to the determination of the different penicillins investigated, either in pure or dosage forms, with good accuracy and precision . The results were compared with those given by the official United States Pharmacopeial XXI method. Sex Transm Dis, 1991 Apr-Jun, 18(2), 102 - 6 Failure of recommended maternal therapy to prevent congenital syphilis; Rawstron SA et al.; A pregnant women with secondary syphilis received appropriate therapy with penicillin in the last trimester of pregnancy . At delivery, her titre had fallen fourfold, and the baby had a non-reactive cord blood titre at birth . However, the treatment failed to prevent infection in the infant, and the baby had developed signs of congenital syphilis at 10 weeks of age . The definition of "adequate therapy" of pregnant women is unclear, and recent guidelines are contradictory . Therefore, literature that pertains to penicillin therapy in pregnancy is reviewed, and new guidelines for therapy proposed. Biull Eksp Biol Med, 1991 Apr, 111(4), 351 - 3 {Effects of PN 200-110 on penicillin-induced epileptic activity in the cerebral cortex of rats}; Kryzhanovskii GN et al.; In experiments on freely moving Wistar rats it was shown that an intraperitoneal administration of PN 200-110 in a