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 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.