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L-656,575 (OCP-9-176): a novel oxacephem. Pharmacokinetics and experimental chemotherapy.

Abstract
L-656,575 is a new oxacephem that, based on studies in rhesus monkeys, is expected to have a moderately long half-life in humans. After administration of a 10-mg/kg dose by the intramuscular route to rhesus monkeys, peak serum concentrations of 32-54 micrograms/ml were seen at about 30 minutes, and the half-life was estimated to be 63 minutes. Urinary recovery of administered dose was greater than 94% in 6 hours. In mice given a 20-mg/kg dose by the subcutaneous route, a peak serum concentration of 22.9 microgram/ml was observed at 15 minutes after dosing, and the half-life in serum was about 18 minutes. Urinary recovery of the dose was 59% in 6 hours. In another study in mice, administration of probenecid did not extend the half-life of L-656,575, suggesting that the antibiotic is excreted primarily by glomerular filtration in this species. Binding to human plasma proteins was 30% at drug concentrations from 25-100 micrograms/ml. L-656,575 also was shown to be efficacious in experimental bacteremias due to Gram-positive and Gram-negative pathogens in mice, thus confirming the broad spectrum of activity demonstrated for L-656,575 in vitro.
AuthorsE C Gilfillan, B A Pelak, R A Fromtling, J Bland, S Hadley, H H Gadebusch
JournalThe Journal of antibiotics (J Antibiot (Tokyo)) Vol. 41 Issue 8 Pg. 1137-41 (Aug 1988) ISSN: 0021-8820 [Print] England
PMID3049491 (Publication Type: Comparative Study, Journal Article)
Chemical References
  • Anti-Bacterial Agents
  • Blood Proteins
  • Cephalosporins
  • L 656575
  • Ceftazidime
Topics
  • Animals
  • Anti-Bacterial Agents (analysis, pharmacokinetics, therapeutic use)
  • Bacterial Infections (drug therapy)
  • Blood Proteins (metabolism)
  • Ceftazidime (pharmacokinetics)
  • Cephalosporins
  • Dose-Response Relationship, Drug
  • Female
  • Glomerular Filtration Rate
  • Humans
  • Macaca mulatta
  • Metabolic Clearance Rate
  • Mice
  • Protein Binding

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