THE TOLERANCE AND PHARMACOKINETICS OF CLINAFLOXACIN (CI-960) IN HEALTHY-SUBJECTS

The single-dose tolerance and pharmacokinetics of clinafloxacin, a new fluoroquinolone antibacterial agent, were evaluated in healthy volunt eers. Single oral doses of 25, 50, 100, and 200 mg were well tolerated . Adverse events after placebo and clinafloxacin were similar, with mi ld drowsiness, dizziness, headache, and rash being reported most frequ ently. The frequency and intensity of side-effects did not increase wi th dose. Clinafloxacin was rapidly absorbed, with C-max occurring at a pproximately 40 min postdose. Plasma concentrations increased proporti onately and, following 100 or 200 mg doses, remained above MIC(90)s re quired for most nosocomial pathogens for at least 12 h. Clinafloxacin elimination half-life averaged 5.2 h and renal clearance was approxima tely 200 mL/min. About 50% of the administered dose was excreted uncha nged in the urine.