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The pharmacokinetics, tissue penetration and in-vitro activity of loracarbef, a beta-lactam antibiotic of the carbacephem class.

Abstract
The pharmacokinetics of loracarbef in plasma and a mild inflammatory exudate were studied in human volunteers. After a single oral dose of 400 mg, a mean maximum drug concentration (Cmax) of 17.8 mg/L was achieved in the plasma at 1.2 h (mean Tmax). The mean plasma elimination half-life (T1/2) was 1.3 h. In the inflammatory exudate the mean Cmax was 8.9 mg/L at a mean Tmax of 2.0 h and with a mean T1/2 of 1.7 h. The mean penetration into the inflammatory exudate was 90.1%. The in-vitro activity of loracarbef was determined against Haemophilus influenzae and Moraxella catarrhalis (MIC90s of 4 mg/L and 1 mg/L respectively, regardless of beta-lactamase production), as well as Streptococcus pneumoniae (MIC90 of 2 mg/L). Loracarbef was also active against Escherichia coli, Proteus mirabilis and Klebsiella pneumoniae (MIC90s of < or = 2 mg/L). The in-vitro activity and pharmacokinetics of loracarbef suggest that it would be efficative therapy for patients with community-acquired respiratory and urinary tract infections caused by the most frequently-encountered bacterial pathogens.
AuthorsA S Lees, J M Andrews, R Wise
JournalThe Journal of antimicrobial chemotherapy (J Antimicrob Chemother) Vol. 32 Issue 6 Pg. 853-9 (Dec 1993) ISSN: 0305-7453 [Print] England
PMID8144425 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Cephalosporins
  • Clavulanic Acids
  • loracarbef
  • Cefaclor
  • Amoxicillin-Potassium Clavulanate Combination
  • Amoxicillin
Topics
  • Adult
  • Amoxicillin (pharmacology)
  • Amoxicillin-Potassium Clavulanate Combination
  • Cefaclor (pharmacology)
  • Cephalosporins (blood, pharmacokinetics, pharmacology)
  • Clavulanic Acids (pharmacology)
  • Drug Therapy, Combination (pharmacology)
  • Enterobacteriaceae (drug effects)
  • Exudates and Transudates (metabolism)
  • Haemophilus influenzae (drug effects)
  • Half-Life
  • Humans
  • Male
  • Microbial Sensitivity Tests
  • Moraxella catarrhalis (drug effects)
  • Staphylococcus aureus (drug effects)
  • Streptococcus pneumoniae (drug effects)

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