A review of the pharmacokinetic profile of temafloxacin.

Temafloxacin is a new fluoroquinolone with potent activity against several important bacteria. Studies in healthy volunteers indicate that the average bioavailability of temafloxacin exceeds 90%, with little intersubject variability. Steady-state peak serum levels are approximately 1 mg/L per 100 mg oral dose administered; thus, the steady-state peak serum level after 600 mg bd oral dosing is approximately 6 mg/L. The long serum elimination half-life (approximately 8 h in patients with normal renal function) allows for single or twice-daily dosing. Approximately 60% of a dose is recovered unchanged in the urine in normal volunteers. Non-renal clearance is approximately 60-80 mL per minute and consists of metabolism (5% of dose), biliary secretion of unchanged drug, and presumptive transintestinal elimination. A doubling of the dosing interval (e.g. from 12 to 24 h) is indicated in patients with a creatinine clearance less than 40 mL/min. No special adjustment of dose is required in those with hepatic dysfunction or the elderly. Studies with temafloxacin show no significant effects on the metabolism of theophylline. Integration of drug pharmacokinetic and pharmacodynamic properties support use of single or twice-daily dosing of temafloxacin.