Plasma and urine levels of flumequine and 7-hydroxyflumequine following single and multiple oral dosing

Plasma and urine concentrations of flumequine and its microbiologically active metabolite, 7-hydroxyflumequine, were determined in healthy subjects following single oral doses of 400, 800, and 1200 mg of flumequine, and following multiple oral doses of 800 mg given four-times daily. After administra...

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Bibliographic Details
Published inJournal of antimicrobial chemotherapy Vol. 15; no. 3; p. 337
Main Authors Schuppan, D, Harrison, L I, Rohlfing, S R, Miller, H L, Funk, M L, Hansen, C S, Ober, R E
Format Journal Article
LanguageEnglish
Published England 01.03.1985
Subjects
Administration, Oral
Adult
Biotransformation
Fluoroquinolones
Humans
Male
Metabolic Clearance Rate
Middle Aged
Quinolizines - administration & dosage
Quinolizines - blood
Quinolizines - metabolism
Quinolizines - urine
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Summary:Plasma and urine concentrations of flumequine and its microbiologically active metabolite, 7-hydroxyflumequine, were determined in healthy subjects following single oral doses of 400, 800, and 1200 mg of flumequine, and following multiple oral doses of 800 mg given four-times daily. After administration of the single oral doses, antimicrobial levels in plasma and urine were rapidly attained, were proportional to the dose given, and were maintained for 12 to 24 h. The multiple dosage regimen yielded antimicrobial levels in both plasma and urine that were several-fold higher than the levels required to inhibit the growth of susceptible bacteria. Following both the single and multiple dose regimens, the plasma elimination half-life of flumequine was about 7h. The excretion of 7-hydroxyflumequine in the urine contributed significantly to the antimicrobial activity.
ISSN:0305-7453
DOI:10.1093/jac/15.3.337