Comparative pharmacokinetics of ciprofloxacin, gatifloxacin, grepafloxacin, levofloxacin, trovafloxacin, and moxifloxacin after single oral administration in healthy volunteers

In an open, randomized, six-period crossover study, the pharmacokinetics of ciprofloxacin, gatifloxacin, grepafloxacin, levofloxacin, moxifloxacin, an d trovafloxacin were compared after a single oral dose in 12 healthy volunt eers (6 men and 6 women). The volunteers received 250 mg of ciprofloxacin, 400 mg of gatifloxacin, 600 mg of grepafloxacin, 500 mg of levofloxacin, 40 0 mg of moxifloxacin, and 200 mg of trovafloxacin. The concentrations of th e six fluoroquinolones in serum and urine were measured by a validated high -performance liquid chromatography method. Blood and urine samples were col lected before and at different time points up to 48 h after medication. Lev ofloxacin had the highest peak concentration (C-max, in micrograms per mill iliter) (6.21 +/- 1.34), followed by moxifloxacin (4.34 +/- 1.61) and gatif loxacin (3.42 +/- 0.74). Elimination half-lives ranged from 12.12 +/- 3.93 h (grepafloxacin) to 5.37 +/- 0.82 h (ciprofloxacin). The total areas under the curve (AUC(tot), in microgram-hours per milliliter) for levofloxacin ( 44.8 +/- 4.4), moxifloxacin (39.3 +/- 5.35), and gatifloxacin (30 +/- 3.8) were significantly higher than that for ciprafloxacin (5.75 +/- 1.25). Calc ulated from a normalized dose of 200 mg, the highest C(max)s (in micrograms per milliliter) were observed for levofloxacin (2.48 +/- 0.53), followed b y moxifloxacin (2.17 +/- 0.81) and trovafloxacin (2.09 +/- 0.58). The highe st AUC(tot) (in microgram-hours per milliliter) for a 200-mg dose were obse rved for moxifloxacin (19.7 +/- 2.67) and trovafloxacin (19.5 +/- 3.1); the lowest was observed for ciprofloxacin (4.6 +/- 1.0). No serious adverse ev ent was observed during the study period. The five recently developed fluor oquinolones (gatifloxacin, grepafloxacin, levofloxacin, moxifloxacin, and t rovafloxacin) showed greater bioavailability, longer half-lives, and higher C(max)s than ciprofloxacin.