摘要:

The absorption and tissue distribution of a new rifamycin, L/105, which chemically is 4-deoxy-4’-methylpyrido [l’,2’-l,2] imidazo [5,4 C] rifamycin SV, were studied in rats after oral administration of 100 mg/kg. This study showed that L/105, contrary to what was observed for rifampicin, was practically not absorbed: neither serum nor significant tissue levels were evidenced. Also in dogs, after oral administration of L/105 in a single dose (25 mg/kg) and a multiple dosage (10 mg/kg/day, for 8 days), no traces of the compound were detected in the serum. The elimination was investigated in the rat: the highest recovery of L/105 (more than 50% of the administered dose) was in feces after 72 h, hardly any traces were found in

ISSN:0009-3157    

DOI:10.1159/000238165

出版商:S. Karger AG    

年代:1983

数据来源: Karger

摘要:

The pharmacokinetics of cefotaxime, a new semi-synthetic cephalosporin for injection, was studied in 30 subjects with various degrees of renal function after a single 1-gram intramuscular injection. Serum and urinary concentrations of cefotaxime and desacetyl cefotaxime were determined by high pressure liquid chromatography. The pharmacokinetic parameters of cefotaxime were obtained using a one-compartment open model. The mean serum half-life of the parent compound (cefotaxime), 0.87 h in normal subjects, was prolonged to 2.35 h in hemodialysis patients. There was a significant lineal correlation between the elimination rate constant of cefotaxime and creatinine clearance. The mean cumulative urinary recovery of the administered dose in the 24-hour urine was 51.7% as cefotaxime and 25 6% as desacetyl cefotaxime in normal subjects.

ISSN:0009-3157    

DOI:10.1159/000238166

出版商:S. Karger AG    

年代:1983

数据来源: Karger

摘要:

Before appendectomy 36 adult patients were given an intravenous infusion of 500 mg of tinidazole. In the operation tissue samples were taken (blood, base of appendix vermiformis, muscle, fat) either 10, 20, 30, 60, or 120 min after cessation of infusion. The tinidazole concentrations were determined by liquid chromatography. The weight-standardized tinidazole concentrations in the serum, muscle tissue and appendix in all specimens were higher than the minimal inhibitory concentration (2 μg/g) of Bac-teroides fragilis. The tinidazole concentrations of adipose tissue exceeded the limit of 1 μg/g in all samples. The concentrations were high already in the 10-min patient group. The authors consider a tinidazole infusion started half an hour before the operation at a dose of 10 mg/kg of the patient’s body weight to be a reliable procedure if the objective is to acquire a sufficient tissue concentration of tinidazole (2 μg/g) to prevent infection complications caused by anaerobic bact

ISSN:0009-3157    

DOI:10.1159/000238167

出版商:S. Karger AG    

年代:1983

数据来源: Karger

摘要:

Beta-lactamase produced by Bacteroides fragilis could protect from antibiotics group A beta-hemolytic streptococci (GABHS), penicillin-susceptible pathogens frequently isolated from acute tonsillitis in children. To test this hypothesis we determined the minimal bactericidal concentration (MBC) to penicillin and cephalothin of GABHS alone and in mixed culture with eleven beta-lactamase-producing strains of B. fragilis. B. fragilis strains with MBC values ≤ 32 μg/mlto penicillin and ≤64 μg/ml to cephalothin did not provide any protection for GABHS. However, strains with MBC ≥ 128 μg/ml to penicillin and ≥ 256 μg/ml to cephalothin provided protection by increasing the MBC of GABHS at least 8,534 times for penicillin and 2,048 times for cephalothin. This phenomenon was most marked in 5% CO2. B. fragilis provided no protection against clindamycin. These results may explain the inability of penicillin therapy to completely eradicate GABHS from cases of recurrently infec

ISSN:0009-3157    

DOI:10.1159/000238168

出版商:S. Karger AG    

年代:1983

数据来源: Karger

摘要:

The synergistic bactericidal effect of the oxolinic acid-trimethoprim combination has been confirmed on an exponentially growing strain of Escherichia coli, and is paralleled by a synergistic inhibition of 14C-uracil incorporation into the bacterial DNA. These data provide experimental support for the postulate that the synergistic effect of quinolone-trimethoprim combinations, observed both in vitro and in vivo, is due to a complementary blockade of bacterial DNA synthesis.

ISSN:0009-3157    

DOI:10.1159/000238169

出版商:S. Karger AG    

年代:1983

数据来源: Karger

摘要:

The antibiotic resistance of Staphylococcus aureus and coagulase-negative staphylococci has been followed over 4 years (1977–1980). 90% of the strains produced β-lactamase. Coagulase-negative staphylococci were more resistant than S. aureus, although β-lactamase production occurred more rarely. Strains from the sputum of children with cystic fibrosis (CF) were more multiresistant than isolates from other sources. The strains from hospitalized patients (HP) were more resistant than isolates from outpatients. A higher frequency of β-Lactamase production occurred among strains from CF and HP patients compared to out-patients. This occurred in samples from pus and wounds in 66% of the strains derived from non-hospitalized patients compared with 93 % from surgical pati

ISSN:0009-3157    

DOI:10.1159/000238170

出版商:S. Karger AG    

年代:1983

数据来源: Karger

摘要:

843 isolates from clinical specimens were tested against moxalactam by disc agar diffusion. The bacteria used in this study consisted of Escherichia coli, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae, Klebsiella pneumoniae, Proteus mirabilis, Providencia rettgeri, Pseudomonas aeruginosa, Serratia marcescens, Staphylococcus aureus, Staphylococcus epidermidis and group B and group D Streptococci. In vitro activity of moxalactam was compared with the following antibiotics: ampicillin, amikacin, carbenicillin, cefamandole, cefoxitin, cephalothin, chloramphenicol, clindamycin, colistin, erythromycin, gentamicin, oxacillin, penicillin, tetracycline, tobramycin, trimethoprim-sulfamethoxazole and vancomycin. Of the 471 strains of Enterobacteriaceae tested, 466 (98.9%) were susceptible to moxalactam. Except for penicillin G, the gram-positive cocci were generally more resistant to moxalactam than the other beta-lactam antibiotics. Moxalactam was comparable to gentamicin, as far as its activity against P. aeruginosa was concerned, but was less effective than amikacin, tobramycin, carbenicillin or colistin.

ISSN:0009-3157    

DOI:10.1159/000238171

出版商:S. Karger AG    

年代:1983

数据来源: Karger

摘要:

The IgG immunoglobulin preparation Polyglobin® failed to enhance the combined phagocytic and serum bactericidal activity of 65 vol% of fresh defibrinated human blood from healthy adults against representative test strains of Serratia marcescens, despite documented O-agglutinin activity of Polyglobin against every test strain employed. It was concluded that pooled human IgG immunoglobulin, i.e. ‘natural’ IgG antibodies, would not be expected to exert a beneficial effect against S. marcescens in patients with sufficient residual, functional ‘natural’ antibodies and co

ISSN:0009-3157    

DOI:10.1159/000238172

出版商:S. Karger AG    

年代:1983

数据来源: Karger

摘要:

Neither cefoperazone, cefotaxime, mezlocillin nor piperacillin significantly killed intraphagocytic bacteria of representative assay strains of Serratia marcescens, as determined with 55 vol% of fresh defibrinated human blood treated with 2 mg/ml of phenylbutazone, which permitted phagocytic ingestion of bacteria, but selectively inhibited the microbicidal activity of peripheral blood leukocytes. Extraphagocytic bacteria were killed with group A (phage tail) bacteriocins of S. marcescens. However, minimal bactericidal concentrations of fosfomycin displayed intraphagolysosomal bactericidal activity which approximated that of rifampin. Inhibitory and subinhibitory concentrations of cefoperazone, cefotaxime, fosfomycin, mezlocillin, and piperacillin combined with 55 vol% of defibrinated human blood, respectively, yielded additive effects against all test strains of S. marcescens utilized and Escherichia coli control strain ATCC 25922.

ISSN:0009-3157    

DOI:10.1159/000238173

出版商:S. Karger AG    

年代:1983

数据来源: Karger

摘要:

Cell-free folate synthesizing extracts have been isolated from Escherichia coli, Mycobacterium lufu, Mycobacterium smegmatis (ATCC 607) and Mycobacterium leprae, and the inhibitory power of diaminodiphenylsulfone (DDS) in such cell-free systems on the synthesis of dihydropteroic acid has been determined. M. lufu and M. leprae extracts show very similar high sensitivities against DDS. Mode of action studies seem to indicate that the observed high sensitivity of M. lufu and M. leprae as compared to E. coli can be solely attributed to a high affinity for the dihydropteroic acid synthetase. A dihydropteroic acid analog formation where DDS is incorporated instead of p-aminobenzoic acid – as has been observed in E. coli – could not be detec

ISSN:0009-3157    

DOI:10.1159/000238174

出版商:S. Karger AG    

年代:1983

数据来源: Karger