Disposition of fleroxacin, a new trifluoroquinolone, and its metabolites. Pharmacokinetics in elderly patients

Clinical Pharmacokinetics
A M TaburetE Singlas

Abstract

The pharmacokinetics of fleroxacin and its main metabolites, N-demethyl-fleroxacin and N-oxide-fleroxacin, were studied in 12 elderly patients aged 63 to 88 years. Plasma and urine samples collected at different times after drug administration were analysed by a specific reverse phase high performance liquid chromatography (HPLC) method. The peak plasma concentration (Cmax) of fleroxacin was 15.6 +/- 1.6 mg/L, time to Cmax (tmax) was about 3h, elimination half-life (t1/2) was 16 +/- 1h and the percentage of unchanged fleroxacin excreted in urine was 39 +/- 3% of the dose. The plasma concentrations of metabolites were very low and accounted for no more than 4% of the concentration of unchanged fleroxacin. Plasma parameters were mainly correlated with age and weight; urinary parameters were correlated with creatinine clearance. Compared with results in younger normal patients, no significant change in the t1/2 of fleroxacin or metabolites was observed. Assuming that the bioavailability (f) is complete, the apparent volume of distribution (Vd/f) was lower in elderly (0.9 +/- 0.1 L/kg) than in younger patients (1.3 +/- 0.1 L/kg) and a 2-fold decrease in apparent total clearance (CL/f) was noted (2.58 +/- 0.42 vs 4.86 +/- 0.72 L/h);...Continue Reading

Citations

Jun 1, 1994·Antimicrobial Agents and Chemotherapy·J SchrenzelD P Lew
Jul 1, 1993·International Journal of Antimicrobial Agents·E Ludwig
Jan 1, 1993·International Journal of Antimicrobial Agents·W CullmannA Braunsteiner
Aug 23, 2006·Expert Opinion on Drug Metabolism & Toxicology·Klaus Turnheim
Aug 1, 1996·Antimicrobial Agents and Chemotherapy·D E UehlingerF J Frey

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