摘要:

Sulfonamide-sensitive cells of Escherichia coli were incubated under standardized conditions with various sulfonamides and the quantity of sulfonamide uptake into the bacteria measured. The test substances reached a higher concentration inside the bacteria than in the incubation medium, the degree of accumulation varying for the individual substances despite uniformly applied incubation conditions. In all cases a pH dependency was detected which varied with the pKa values of the substances tested. On the basis of the pKa dependency of the pH effect, the sulfonamide uptake can be interpreted as being a passive diffusion process. Knowing the intracellular pH value, which was determined by the DMO method, it was then possible to calculate the theoretically expected value for the accumulation as a concentration coefficient. Since the calculated and experimentally determined values differ approximately by a factor of 2, an intracellular binding of the sulfonamides is assumed. The same results were obtained in cells of sulfonamide-resistant E. coli strains.

ISSN:0009-3157    

DOI:10.1159/000237899

出版商:S. Karger AG    

年代:1980

数据来源: Karger

摘要:

The administration of phenobarbitone to the rat (8 mg/100 g BW) once daily for 3 days significantly decreased the serum and tissue levels of erythromycin administered intraperitoneally (5 mg/l00 g BW). Furthermore, phenobarbitone stimulated the hepatic microsomal N-demethylation of erythromycin and increased the biliary concentration and the biliary excretion rate of the unmetabolized antibiotic. These effects were accompanied by augmented liver mass and bile flow. The possibility is discussed that erythromycin concentrates in the bile through a specialized hepatic drug transport system, activated by phenobarbitone.

ISSN:0009-3157    

DOI:10.1159/000237900

出版商:S. Karger AG    

年代:1980

数据来源: Karger

摘要:

The pharmacokinetics of the acylureido-penicillin, azlocillin, were studied after intravenous or intramuscular injections in 53 premature and full-term infants with infections. Effective concentrations were achieved in premature babies after doses of 50 mg/kg every 12 h and in full-term infants with 100 mg/kg every 12 h. No untoward effects of azlocillin were observed. On the basis of these studies, a dosage schedule for azlocillin has been established.

ISSN:0009-3157    

DOI:10.1159/000237901

出版商:S. Karger AG    

年代:1980

数据来源: Karger

摘要:

The in vitro activity of cefotaxime (HR 756) was tested in comparison with cefuroxime, cefamandole, cefoxitin, cefazolin, ampicillin, mezlocillin, gentamicin and amicacin. MIC values were investigated on 168 freshly isolated gram-positive and gram-negative bacteria from clinical sources. Enterococci and Pseudomonas aeruginosa behaved cefotaxime-resistant. All the other species examined showed a very good sensitivity range against cefotaxime. Cefotaxime was the most active antibiotic of our study.

ISSN:0009-3157    

DOI:10.1159/000237902

出版商:S. Karger AG    

年代:1980

数据来源: Karger

摘要:

Combination of 9-(S)-(2,3-dihydroxypropyl)adenine [(S)-DHPA] and 6-azauridine (AzUrd) is highly active in the selective inhibition of vaccinia virus in chick embryo cell culture. Synergic effect of this combination of compounds was not encountered in HeLa cell culture. Of the 17 analogues related to DHPA studied in this paper, 3 showed medium activity against vaccinia virus, but none of them was as effective as (S)-DHPA in combination with AzUrd.

ISSN:0009-3157    

DOI:10.1159/000237903

出版商:S. Karger AG    

年代:1980

数据来源: Karger

摘要:

The in vitro activity of various tetracyclines and antimalarials alone and in combinations against 20 clinical isolates of Escherichia coli was investigated. The minimum inhibition concentration of the tetracyclines ranged from 1.2 to 160 μg/ml. Demeclocycline was the highest in activity. The antimalarials were ineffective. Variable percentage of strains responded to the synergistic effect of the various antibiotics-drugs combinations. Strains which are relatively insensitive to the tetracyclines did not respond to the synergistic effect of the combinations. The bactericidal effect of the combinations was shown by the enhanced rate of killing that occurred at 6 h. Synergism was reversed by divalent cations

ISSN:0009-3157    

DOI:10.1159/000237904

出版商:S. Karger AG    

年代:1980

数据来源: Karger

摘要:

Meningitis and meningoencephalomyelitis caused by Listeria monocytogenes were experimentally established in mice. The pathological changes in brain and spinal cord resulting from the infection resemble those observed in man and domestic animals. The efficacy of 24 antibiotics in treating this experimental infection was determined. Minocycline and chlortetracycline were the most efficacious antibiotics followed by amoxicillin, which was 2- to 4-fold less active than the former. However, the acute toxicity of amoxicillin to the murine central nervous system was at least 10-fold lower than that of the tetracyclines. Since parenteral amoxicillin may be of value in the management of listerial meningitis and meningoencephalomyelitis in man and domestic animals, clinical trials seem warranted.

ISSN:0009-3157    

DOI:10.1159/000237905

出版商:S. Karger AG    

年代:1980

数据来源: Karger

摘要:

The in vitro study of the amoxicillin-clavulanate association has been carried out using a triple layer technique by means of paper strips which show a T configuration. Synergy observation proves to be most favorable with the following reservoir load: (a) when the latter is sufficiently low so that the inhibiting effect of the clavulanate and amoxicillin, taken in isolation, becomes weak or nil; (b) when the ratio between the two substances is amoxicillin 5, clavulanate 1. Under such conditions, the inhibition of the bacterial growth occurs solely in the confluence area of the substances. The neutralization of amoxicillin through penicillinase respectively after 4, 6 and 24 h of incubation makes possible an appraisal of the bactericidal action of the association.

ISSN:0009-3157    

DOI:10.1159/000237906

出版商:S. Karger AG    

年代:1980

数据来源: Karger

摘要:

Cefuroxime is a very effective agent for the treatment of severe purulent respiratory infections. 190 patients with purulent exacerbations of bronchitis or bronchiectasis, pneumonia or secondarily infected lung cancer received 2.25–3.0 g cefuroxime daily for an average of 9 days. A good clinical response was seen in 91% of 184 assessable patients. A remarkable improvement in sputum purulence was observed and side-effects to cefuroxime were minima

ISSN:0009-3157    

DOI:10.1159/000237907

出版商:S. Karger AG    

年代:1980

数据来源: Karger

摘要:

Analogies with dose-dependent transient prophylaxis and with delayed take of reinfection in drug-cleared Trypanosoma evansi (T. venezuelense) infected animals indicate that relapse following chemotherapy is induced by the same underlying mechanism, i.e., termination of the trypanostatic effect of residual drug concentrations. Correspondingly, both the complete (‘true’) prophylaxis and the radical cure without relapse require trypanocidal drug concentrati

ISSN:0009-3157    

DOI:10.1159/000237908

出版商:S. Karger AG    

年代:1980

数据来源: Karger