摘要:

The determination of the serum and urine concentrations of cephaloridine permitted calculation of the pharmacokinetic constants of this antibiotic: after administration of a 1-gram intravenous dose in five normal subjects; after administration of a 1-gram intramuscular dose in five normal subjects, five patients with renal impairment and five patients on maintenance hemodialysis. In normal subjects, serum half-life averaged 1.56 h (Ke = 0.4445) after intravenous administration and 1.63 h (Ke = 0.4254) after intramuscular administration of a 1-gram dose of the antibiotic. The urinary excretion of cephaloridine over the 6 h following its intramuscular administration in normal subjects amounted to 56.4% of the administered dose. The renal clearance of cephaloridine was 194 ml/min. A linear correlation (Ke=0.0670+ 0.0028 CrCl) was established between overall elimination rate-constant values and the creatinine clearances of the patients under investigation. These data were used to calculate the maintenance and loading doses and intervals adjusted to creatinine clearance values. Accurate dosage regimens adjusted to the renal status of each individual patient were derived from the calculated values.

ISSN:0009-3157    

DOI:10.1159/000221904

出版商:S. Karger AG    

年代:1976

数据来源: Karger

摘要:

The hypothesis that defective cell wall synthesis seems to represent a final common pathway of drug-induced injury either within the bacterial cell or on its surface was supported by two different findings: (1) sulfamethoxazole and trimethoprim, either alone or in combination, induced morphological findings in various Escherichia coli and Proteus mirabilis strains identical to those found after incubation with so-called cell-wall-active antibiotics (e.g., penicillin) and (2) cell-wall-defective bacteria (L forms, spheroblasts) were resistant to sulfonamides and/or trimethoprim as compared to their normal bacterial cells.

ISSN:0009-3157    

DOI:10.1159/000221905

出版商:S. Karger AG    

年代:1976

数据来源: Karger

摘要:

Pharmacokinetic characteristics of ornidazole and metronidazole were compared in man. Both drugs were labelled with 14C in the imidazole ring at position 2. Four healthy volunteers were given an oral dose of 750 mg of one of the drugs, followed 2–4 weeks later by the same dose of the other. The same technique for determining the unchanged compound was used for both drugs. Results may be summarized as follows: mean peak concentrations in the plasma of 10.9 μg/ml for ornidazole and of 12.3 μg/ml for metronidazole were reached 2–4 h and 30–60 min after administration, respectively; both drugs showed the same volume of distribution. Their binding to human plasma proteins was less than 15%; the mean half-life of elimination from the plasma was 14.4 h for ornidazole and 8.4 h for metronidazole; the mean radioactivity recovered from the urine and faeces during the first 5 days was 85% of the dose for ornidazole and 91% for metronidazole, the major proportion in each case being excreted in the urine; the radioactivity found in the faeces was 22.1% of the dose for ornidazole and 13.9% for metron

ISSN:0009-3157    

DOI:10.1159/000221906

出版商:S. Karger AG    

年代:1976

数据来源: Karger

摘要:

The biliary excretion of cefazolin was compared with that of cephalothin and cephaloridine in rats and man. In rats, the biliary levels were dose-related with cefazolin and cephalothin but not with cephaloridine. Biliary levels were higher than serum levels after injection of 10–80 mg/kg of cefazolin and cephalothin, whereas serum levels of cephaloridine after injection were higher than biliary levels. The highest biliary levels of cefazolin were obtained by intravenous injection, followed by intramuscular injection and drip infusion. In man, a crossover study was made to compare biliary levels of cefazolin with those of cephaloridine and cephalothin. After a single 1-gram intravenous injection, the peak levels of cefazolin ranged from 0.85 to 21 μg/ml and those of cephaloridine varied from 0.55 to 3.9 μg/ml. After a 3-gram intravenous injection, the peak biliary levels of cefazolin ranged from 35.5 to 270 μg/ml and those of cephalothin from 0.3 to 64 μg/ml. The chemotherapeutic biliary levels of cefazolin able to inhibit susceptible organisms were obtained by 3-gram intravenous injec

ISSN:0009-3157    

DOI:10.1159/000221907

出版商:S. Karger AG    

年代:1976

数据来源: Karger

ISSN:0009-3157    

DOI:10.1159/000221958

出版商:S. Karger AG    

年代:1976

数据来源: Karger

摘要:

The possible immunosuppressive properties of the combination sulphamethoxazole-trimethoprim or either of the agents alone were studied in healthy human volunteers. The effect of the 4-day drug treatment on the antibody synthesis after vaccination was measured by titrating tetanus antitoxin, mumps antibody and Salmonella Hb antibody levels 4 and 5 weeks after vaccination. No significant differences were found in mumps or Salmonella antibody titres in the drug-treated group compared to controls. Tetanus antitoxin levels, however, were significantly lower than in controls after the combined drug. When a fourfold or greater increase in tetanus antitoxin titre was obtained in 75% of controls, the respective figures were 38% in the sulphamethoxazole-trimethoprim-treated group (p 0.05). The implications of these findings are discussed.

ISSN:0009-3157    

DOI:10.1159/000221908

出版商:S. Karger AG    

年代:1976

数据来源: Karger

摘要:

The susceptibility of 83 non-pigmented Serratia marcescens strains was determined by an agar dilution technique. They originated from miscellaneous pathological specimens submitted to the diagnostic laboratory during a nosocomial infection outbreak in 1974. All strains were completely resistant to 128 μg/ml of cephalothin, colistin sulphomethate, lincomycin and penicillin G. They were also resistant to clinically attainable concentrations of ampicillin, chloramphenicol, erythromycin, novobiocin and tetracycline. With regard to drugs with some activity, 84% of the strains were susceptible to nalidixic acid, 48% to sulphamethoxazole, 57% to streptomycin, 60% to kanamycin, 61% to gentamicin, 85% to co-trimoxazole and 100% to amikacin. Environmental strains isolated from the infected units were strikingly more sensitive than the patient strains

ISSN:0009-3157    

DOI:10.1159/000221909

出版商:S. Karger AG    

年代:1976

数据来源: Karger

ISSN:0009-3157    

DOI:10.1159/000221959

出版商:S. Karger AG    

年代:1976

数据来源: Karger

摘要:

Body lice (Pediculus humanus corporis L) and ticks (Ornithodoros moubata) that had been infected with Rickettsia prowazekii received varying doses of erythromycin. The anti-rickettsial activity of this drug was evaluated with regard to the determination of the numbers of surviving microorganism (LID100) and the in vivo concentration of erythromycin in both arthropod hosts. Erythromycin was found to exert a rickettsiostatic effect in lice, whereas in ticks the drug at concentrations of 0.3–0.04 μg/mg body weight completely eliminated R. prowazekii

ISSN:0009-3157    

DOI:10.1159/000221910

出版商:S. Karger AG    

年代:1976

数据来源: Karger

ISSN:0009-3157    

DOI:10.1159/000221911

出版商:S. Karger AG    

年代:1976

数据来源: Karger