Effects of Rate of Infusion and Probenecid on Serum Levels, Renal Excretion, and Tolerance of Intravenous Doses of Cefoxitin in Humans: Comparison with Cephalothin
- 1 September 1974
- journal article
- clinical trial
- Published by American Society for Microbiology in Antimicrobial Agents and Chemotherapy
- Vol. 6 (3), 338-346
- https://doi.org/10.1128/aac.6.3.338
Abstract
Using a randomized crossover design, 1-g intravenous doses of cephalothin and cefoxitin, a cephalosporinase-resistant cephamycin, were infused into 12 normal adult males over periods of 120, 30, and 3 min, the last with and without prior intravenous infusions of probenecid (1 g). Mean peak serum concentrations of antibiotic activity after cephalothin infusions were 23, 56, 103, and 102 μg/ml, respectively, and after cefoxitin infusions they were 27, 74, 115, and 125 μg/ml, respectively. Probenecid treatment prolonged the terminal serum half-life of cephalothin-like activity from 0.52 to 1.0 h, and of cefoxitin from 0.68 to 1.4 h. In contrast to cephalothin, which was found to be metabolized about 25% to the less active desacetyl form, cefoxitin was metabolized less than 2% to the virtually inactive descarbamyl form, as judged from urinary recoveries. Neither antibiotic displayed detectable organ toxicity. Of 300 recent clinical isolates of gram-negative bacilli other than Pseudomonas spp., 83% were susceptible to cephalothin but 95% were susceptible to cefoxitin. Organisms resistant to cephalothin but susceptible to cefoxitin included strains of Escherichia coli, Proteus vulgaris, Klebsiella spp., Serratia marcescens, Enterobacter spp., and Bacteroides spp.Keywords
This publication has 15 references indexed in Scilit:
- Cefoxitin, a Semisynthetic Cephamycin Antibiotic: Resistance to Beta-Lactamase InactivationAntimicrobial Agents and Chemotherapy, 1974
- Cephalosporinase Activity in Bacteroides fragilisAntimicrobial Agents and Chemotherapy, 1973
- Cephamycins, a New Family of β-Lactam Antibiotics: Antibacterial Activity and Resistance to β-Lactamase DegradationAntimicrobial Agents and Chemotherapy, 1973
- Cephamycins, a New Family of β-Lactam Antibiotics. IV. In Vivo StudiesAntimicrobial Agents and Chemotherapy, 1972
- Cephamycins, a New Family of β-Lactam Antibiotics. III. In Vitro StudiesAntimicrobial Agents and Chemotherapy, 1972
- Cephamycins, a New Family of β-Lactam Antibiotics I. Production by Actinomycetes, Including Streptomyces lactamdurans sp. nAntimicrobial Agents and Chemotherapy, 1972
- Resistance of Haemophilus influenzae to TrimethoprimBMJ, 1972
- Predictive Value of the Probenecid Test for the Effect of L-Dopa Therapy in Parkinson's DiseaseNature New Biology, 1972
- In vitro and in vivo laboratory comparison of cephalothin and desacetylcephalothin.1965
- PHYSIOLOGICAL DISPOSITION OF PROBENECID, INCLUDING RENAL CLEARANCE, IN MAN, STUDIED BY AN IMPROVED METHOD FOR ITS ESTIMATION IN BIOLOGICAL MATERIAL1963