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.
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Authors | A S Lees, J M Andrews, R Wise |
Journal | The Journal of antimicrobial chemotherapy
(J Antimicrob Chemother)
Vol. 32
Issue 6
Pg. 853-9
(Dec 1993)
ISSN: 0305-7453 [Print] England |
PMID | 8144425
(Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Cephalosporins
- Clavulanic Acids
- loracarbef
- Cefaclor
- Amoxicillin-Potassium Clavulanate Combination
- Amoxicillin
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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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