摘要:

Mecillinam is a new amidinopenicillin which is taken orally as its ester pivmecillinam. 10 healthy volunteers were each given 200 mg of pivmecillinam hydrochloride four times daily and all urine was collected and cooled to -20°C to minimize antibiotic degradation. 43% of the ingested antibiotic was recovered from the urine in its micro-biologically active form, during the first 12 h and 34% during the subsequent 24 h. The corresponding figures for 10 volunteers receiving double this dose of antibiotic was 30 and 34%. The mean half life of mecillinam in urine due to spontaneous breakdown at 37 °C was 17 h. There was evidence that stearate-film-coated pivmecillinam hydrochloride tablets may be less likely to cause dyspepsia than gelatine capsule

ISSN:0009-3157    

DOI:10.1159/000237814

出版商:S. Karger AG    

年代:1979

数据来源: Karger

摘要:

A significant correlation has been found between the in vitro activity of 16 commonly employed sulphonamides and their molar refractivity. The molar refractivity has been shown to be a superior parameter for the description of the activity of sulphonamides than the sum of electronegativities of atoms making up a heterocyclic substituent in the sulphonamide molecule and molecular weight of the substituent.

ISSN:0009-3157    

DOI:10.1159/000237815

出版商:S. Karger AG    

年代:1979

数据来源: Karger

摘要:

BL-S 578 (Cefadroxil) is a new orally active semisynthetic cephalosporin antibiotic with broad-spectrum antibacterial activity. The new compound was evaluated in vitro in comparison with cephalexin. Some properties studies such as, antibacterial activity, binding with serum proteins and stability in acid and neutral solution at 37 °C for both cephalosporins were similar. In experimental infections of mice, the protective action of BL-S 578 was more effective than cephalexin against Staphylococcus aureus and Streptococcuspneumoniae. BL-S 578 was more resistant than cephalexin to the β-lactamases produced by Klebsiella pneumoniae and Escherichia coli

ISSN:0009-3157    

DOI:10.1159/000237816

出版商:S. Karger AG    

年代:1979

数据来源: Karger

摘要:

Experiments with Staphylococcus aureus and Streptococcus pyogenes have shown that when cells are exposed to a bactericidal concentration of benzylpenicillin or am-picillin and the antibiotic then inactivated with β-lactamase the count of the surviving viable cells (colony-forming units) remains essentially constant for a period of approximately 1.5–3 h before increasing at a normal rate. No such recovery period was observed, however, when Escherichia coli or Proteus mirabilis was exposed to a bactericidal concentration of ampicillin and the antibiotic then inactivated. Microscopic observation of individual surviving cells of S. aureus following exposure to benzylpenicillin showed that in some cases resumption of cell division was delayed as long as 4 h. However, other cells in the same population showed no recovery period and resumed division within 30 min of inactivation of the antibiotic. In the latter case, the recovery period which is observed in terms of viable count may represent the period of time required for individual surviving cells to divide and give rise to normal aggregates before these fragment to produce new colony-forming uni

ISSN:0009-3157    

DOI:10.1159/000237817

出版商:S. Karger AG    

年代:1979

数据来源: Karger

摘要:

69 clinical isolates of gentamicin-resistant Pseudomonas aeruginosa, regarded as causal agents, have been investigated. Various complex spectra of multiple drug resistance to newer aminoglycoside derivatives could be established in these strains which we call ‘resistotypes’. Among them, 20 have been found with high-level resistance to gentamicin (64 ng/ml and more, by a tube dilution method): these strains were highly co-resistant to one or more drugs of the group: tobramycin, sisomicin, amikacin and netilmicin. High-level netilmicin resistance was demonstrated in 5 such strains: 2 of them transferred netilmicin resistance to recipient strain ML-4561. High-level amikacin resistance was demonstrated in one strain, it transferred this determinant to the same recipient. Netilmicin, sisomicin and gentamicin resistance was also transferred, and co-transfer of amikacin resistance determinant was demonstrated with netilmicin. This strain is susceptible to tobramycin. Other netilmicin- (plus gentamicin) resistant strains were fully susceptible to amikacin. It is suggested that a variety of drug-modifying enzymes is responsible for this extended multiresistance to specific aminoglycoside derivatives. Genes, coding for these enzymes may be exchanged by means of plasmid transfers. While Sisomicin resistance could not be, by genetic analysis of exconjugants, separated from that of gentamicin, it was separated from netilmicin resistance determinants, indicating that enzymatic mechanisms responsible for netilmicin and sisomicin resistance may be differ

ISSN:0009-3157    

DOI:10.1159/000237818

出版商:S. Karger AG    

年代:1979

数据来源: Karger

摘要:

The antibacterial activity of a combination of equal parts of amoxycillin and flucloxacillin was compared in vitro and in vivo with that of amoxycillin and flucloxacillin against a range of gram-positive and gram-negative bacteria. The combination generally showed additive effects against bacteria sensitive to the individual penicillins and there was no evidence of antagonism, but synergistic effects were observed between amoxycillin and flucloxacillin against certain amoxycillin-resistant gram-negative bacilli. The extent of synergism varied according to the particular bacterial species under test and synergy was observed only against bacteria with chromosomally-mediated β-lactamases and not against bacteria with R-factor-mediated β-lactamases. In general, amoxycillin+flucloxacillin demonstrated activity against experimental mouse infections in good agreement with its in vitro activity, and synergy was produced against a range of gram-negative bacilli in vivo. The data suggest that clinical trial with amoxycillin+flucloxacillin in the treatment of selected infections including those due to some amoxycillin-resistant bacteria may well be justifie

ISSN:0009-3157    

DOI:10.1159/000237819

出版商:S. Karger AG    

年代:1979

数据来源: Karger

摘要:

The effect of tinidazole on several ciliates (Stylonychia muscorum, Stylonychia mytilus, Tetrahymena pyriformis, Vorticella campanula) has been studied. There is a very pronounced difference in sensitivity against this drug between the free-living ciliates here investigated and certain parasitic protozoa. A high resistance of the free-living ciliates against tinidazole, probably due to their aerobic condition, has been found. Nonetheless, tinidazole at high doses (1–3 mg/ml) caused severe alterations in 3 of the 4 aerobic ciliate species here studie

ISSN:0009-3157    

DOI:10.1159/000237820

出版商:S. Karger AG    

年代:1979

数据来源: Karger

摘要:

Of 97 well-defined strains of Pseudomonas, isolated from sputum of patients with cystic fibrosis (CF), the minimum inhibitory concentration (MIC) of several antibiotics was determined with a broth dilution method. The majority of the strains were resistant to ampicillin and cephalothin, moderately susceptible to carbenicillin (70% to 100 μg/ml) and highly susceptible to piperacillin (100% to 25 μg/ml, 88% to 6.25 μg/ml and 60% to 3.12 μg/ml). If the pharmacological properties of piperacillin are comparable with those of carbenicillin, it can be expected that the sputum level of this drug will be adequate to treat Pseudomonas pulmonary infections. At the lowest concentration tested (0.78 μg/ml) 3% of the strains were susceptible to kanamycin, 85,5% to amikacin, 95% to gentamicin, 98% of tobramycin, and 80% to colimycin. With regard to clinically attainable concentrations, 98.9% of the strains were susceptible to gentamicin and tobramycin, 97.9% to amikacin, 96.9% to colimycin, 88.6% to piperacillin, 38% to carbenicillin, 25.7% to kanamycin, 12.3% to ampicillin, and 1% to cephalo

ISSN:0009-3157    

DOI:10.1159/000237821

出版商:S. Karger AG    

年代:1979

数据来源: Karger

摘要:

5-Fluorocytosine (5-FC) is weakly immunosuppressive when given in lethal doses to mice, and inhibits the responses of mouse and human lymphoid cells to plant lectins at concentrations of 1 mg/ml or more. 5-FC has about 1% of the immunosuppressive activity of 5-fluorouracil in vivo and 0.1% in vitro. Deamination of small amounts of 5-FC to 5-FU or conversion to other toxic metabolites may account for its immunosuppressive effects. The in vitro effects of 5-FC could also be accounted for by the presence of traces (0.1%) of 5-FU as a contaminant.

ISSN:0009-3157    

DOI:10.1159/000237822

出版商:S. Karger AG    

年代:1979

数据来源: Karger

ISSN:0009-3157    

DOI:10.1159/000237823

出版商:S. Karger AG    

年代:1979

数据来源: Karger