摘要:

The biliary excretion of tetroxoprim (TXP) was studied in 10 patients with T-tube drainage. A mean biliary peak of 32.56 ± 7.69 μg/ml was observed 2–3 h after a single oral dose of 200 mg. The biliary elimination rate constant (kb) of TXP was found to be 0.056 (h-1), indicating a longer elimination from the bile than from the central blood compartment. Taking into account the TXP serum levels, following the same oral dose as reported in the literature, concentration factors of 6–8 can be calculated in the

ISSN:0009-3157    

DOI:10.1159/000238097

出版商:S. Karger AG    

年代:1982

数据来源: Karger

摘要:

The pharmacokinetics of Mezlocillin were determined after the intramuscular injection of a single 1-gram dose in 10 subjects with normal renal function, in 10 patients with stabilized renal impairment and in 5 patients with end-stage renal disease submitted to repeated hemodialysis. In normal subjects, biological half-life, Tb ½„ was equal to 0.9 h; total clearance (Ct) to 449 ml/min/1.73 m2; renal clearance (Cr) to 263 ml/min/1.73 m2.72.2% of the administered dose was excreted in the urine within 12 h. In patients with renal insufficiency and in patients undergoing long-term hemodialysis, the serum concentration decrease was markedly slower. During a 6-hour dialysis session, 62% of the Mezlocillin present in the central compartment at the start of hemodialysis was removed. In the 25 subjects under study, a significant correlation was found between the values of Ke and those of creatinine clearance, Ccr (Ke=0.1973+ 0.0046 Ccr). This relation was used to calculate the loading doses, the maintenance doses and the dosage intervals adjusted to the degree of renal impairment, allowing assessment of useful dosage recommendatio

ISSN:0009-3157    

DOI:10.1159/000238098

出版商:S. Karger AG    

年代:1982

数据来源: Karger

摘要:

The objective of this study was to evaluate the concentration in the bronchial secretions of a new injectable cephalosporin, cefotiam, which is characterized by an excellent antibacterial activity, stability against β-lactamases and interesting pharmacokinetic properties, 30 patients suffering from acute exacerbation of a chronic bronchitis or bronchiectasis with expectoration, received either 1 g i. v. of cefotiam in a single dose or four doses of 1 g each over a period of 3 days. The bronchial secretion samples were obtained by fibroscopy, 1, 2, or 4 h after the last dose, in order to evaluate the kinetics of the bronchial concentration of cefotiam. Blood samples were taken simultaneously in order to establish a possible correlation between the bronchial and serum levels of the drug. The results of the study show a rapid and significant transfer of the drug through the bronchoalveolar capillaries, elevated bronchial concentrations starting from the 2nd h, reaching 10 μg/ml (or more) in certain cases, slow elimination with bronchial concentrations persisting at high levels for up to 4 h and a ratio between bronchial and serum concentrations of 25–60% at the 2nd h and more than 100% at the 3rd and 4th h. These results confirm the excellent diffusion of cefotiam, especially in the respiratory tract, allowing bronchial levels largely superior to the minimum inhibitory concentrations required to kill the bacteria usually responsible for lower respiratory tract infecti

ISSN:0009-3157    

DOI:10.1159/000238099

出版商:S. Karger AG    

年代:1982

数据来源: Karger

摘要:

The serum profiles of ceftriaxone (CEF) and netilmicin (NET) were produced in a liquid culture of Pseudomonas aeruginosa, and the change in viable count recorded. Synergism was detectable between CEF and NET despite of the widely disparate serum halflife times of NET and CEF.

ISSN:0009-3157    

DOI:10.1159/000238100

出版商:S. Karger AG    

年代:1982

数据来源: Karger

摘要:

Experiments were designed to determine the nature of amphotericin B (AMB)– 5-fluorocytosine (5-FC) synergism against strains of Candida albicans susceptible to either drug alone. AMB strongly inhibited cell uptake of 14C-labeled 5-FC during incubation in a synthetic liquid medium. After several hours, however, this inhibition was dramatically released. Onset of 14C-5-FC uptake correlated with the known kinetics of AMB decay. These findings support the concept of sequential drug action proposed earlier. AMB apparently acts first and essentially alone until it approaches depletion. Experiments with a 5-FC-resistant mutant indicated that AMB interferes with transport of 5-FC to the cell interio

ISSN:0009-3157    

DOI:10.1159/000238101

出版商:S. Karger AG    

年代:1982

数据来源: Karger

摘要:

The influence of glucose-6-phosphate (G6P) on the fosfomycin minimum inhibitory concentration (MIC) of six Serratia marcescens strains was determined using two standard media (Müller-Hinton and nutrient agar) and three synthetic media. G6P did not affect fosfomycin MIC when S. marcescens was grown on standard media, but on synthetic media the presence of 5–100 mg/1 G6P lowered the MIC by 1–7 log2. Five fosfomycin-resistant mutants were grown on synthetic media. In the presence of G6P, four of five mutant strains became more sensitive (MICs were 128 mg/1 or less). The fifth mutant strain remained resistant under all culture conditions. The implications of these results are discussed with regard to the mechanism of action of fosfomycin, and the practical determination of the MIC in the cl

ISSN:0009-3157    

DOI:10.1159/000238102

出版商:S. Karger AG    

年代:1982

数据来源: Karger

摘要:

The in vitro activity of cefotetan against Staphylococcus aureus and gram-negative bacterial strains including nonfermenting species has been compared with that of cefoxitin, cefotaxim, moxalactam, cefoperazone and ceftazidime by use of an agar dilution method. Cefotetan was found to be inactive against Pseudomonas aeruginosa and Acineto-bacter species and only moderately active against Staphylococcus aureus, Pseudomonas maltophilia, Pseudomonas cepacia, and Enterobacter cloacae. It was more active than cefoxitin and cefoperazone against Escherichia coli, Klebsiella pneumoniae, and indole-positive Proteus strains.

ISSN:0009-3157    

DOI:10.1159/000238104

出版商:S. Karger AG    

年代:1982

数据来源: Karger

摘要:

Fresh, defibrinated human blood (65 vol%) from normal adults reduced cell inocula of Serratia marcescens, comprising ‘delayed serum-sensitive’, ‘pseudo-serum-resistant’, and ‘non-serum-sensitive’ human serum susceptibility categories, by up to approximately 3 log10 units, provided cell inocula did not significantly exceed 105 colony-forming units/ml at 0 time. Phenylbutazone (2 mg/ml) antagonized neither serum bactericidal activity nor the biological activity of group A (phage tail) bacteriocins bA+ 16 and bA+ 18. These bacteriocins were suitable for killing extraphagocytic S. marcescens cells, since they were not internalized by peripheral blood leukocytes. Phenylbutazone at 2 mg/ml failed to interfere with ingestion of S. marcescens by leukocytes; however, this drug inhibited intraphagocytic killing of ingested S. marcescens bacteria. Pilot experiments, utilizing this latter system, disclosed that rifampin effectively killed intraphagolysosom

ISSN:0009-3157    

DOI:10.1159/000238123

出版商:S. Karger AG    

年代:1982

数据来源: Karger

摘要:

14 of 74 test strains of Serratia marcescens yielded reproducible cocarde-like growths (coc+) around 30-μg disks of polymyxin B (PB) on Müller-Hinton, brain heart infusion and tryptic soy agar. The coc+ phenomenon was not due to nutrient effects of growth medium nor did it correlate with either group A (phage tail) bacteriocinogeny or colicinogeny as determined with 32 selected test strains; mitomycin C failed to give rise to coc+ growths. The anionic bile salts of MacConkey agar as well as aqueous sodium deoxy-cholate neutralized the coc+ activity of PB. Benzalkonium chloride, chlorhexidine diglu-conate, and cetyltrimethylammonium bromide by themselves did not produce cocardes. Rather, these cationic detergents enhanced PB activity somewhat against selected coc+ and coc–– strains of 5. marcescens. It was concluded that the PB-induced growth phenomenon of S. marcescens was due to the cationic detergent-like activity of this polypeptide antib

ISSN:0009-3157    

DOI:10.1159/000238124

出版商:S. Karger AG    

年代:1982

数据来源: Karger

摘要:

Minimal bactericidal concentrations of trimethoprim, nalidixic acid, and nitrofurantoin revealed effective intraphagolysosomal bactericidal activity against several assay strains of Serratia marcescens as determined with phenylbutazone-treated (2 mg/ml) fresh defibrinated human blood (55 vol%), following killing of extraphagocytic test bacteria with group A (phage tail) bacteriocins of S. marcescens. The degree of intraphagocytic killing activity of trimethoprim, nalidixic acid, and nitrofurantoin approximated that of rifampin. Inhibitory and subinhibitory concentrations of cotrimoxazole or trimethoprim combined with 55 vol% of defibrinated blood, respectively, yielded additive effects against all test strains of S. marcescens. However, combinations of nalidixic acid and nitrofurantoin with blood, respectively, resulted in essentially indifferent effects against S. marcescens.

ISSN:0009-3157    

DOI:10.1159/000238125

出版商:S. Karger AG    

年代:1982

数据来源: Karger