Comparative Pharmacokinetics of Ciprofloxacin, Gatifloxacin, Grepafloxacin, Levofloxacin, Trovafloxacin, and Moxifloxacin after Single Oral Administration in Healthy Volunteers

Abstract

In an open, randomized, six-period crossover study, the pharmacokinetics of ciprofloxacin, gatifloxacin, grepafloxacin, levofloxacin, moxifloxacin, and trovafloxacin were compared after a single oral dose in 12 healthy volunteers (6 men and 6 women). The volunteers received 250 mg of ciprofloxacin, 400 mg of gatifloxacin, 600 mg of grepafloxacin, 500 mg of levofloxacin, 400 mg of moxifloxacin, and 200 mg of trovafloxacin. The concentrations of the six fluoroquinolones in serum and urine were measured by a validated high-performance liquid chromatography method. Blood and urine samples were collected before and at different time points up to 48 h after medication. Levofloxacin had the highest peak concentration (C max , in micrograms per milliliter) (6.21 ؎ 1.34), followed by moxifloxacin (4.34 ؎ 1.61) and gatifloxacin (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 ciprofloxacin (5.75 ؎ 1.25). Calculated 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 by moxifloxacin (2.17 ؎ 0.81) and trovafloxacin (2.09 ؎ 0.58). The highest AUC tot (in microgram-hours per milliliter) for a 200-mg dose were observed 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 event was observed during the study period. The five recently developed fluoroquinolones (gatifloxacin, grepafloxacin, levofloxacin, moxifloxacin, and trovafloxacin) showed greater bioavailability, longer half-lives, and higher C max s than ciprofloxacin.Fluoroquinolones are widely used alternatives to ␤-lactam agents in the treatment of many bacterial infections. Their antimicrobial activity results from a selective antagonism between host DNA and bacterial DNA without interfering with eucaryotic topoisomerases. The early fluoroquinolones, from the early 1960s, had a limited spectrum of antibacterial activity, mainly against gram-negative pathogens. Further observations of structure-related increases in activity, changes in pharmacokinetic characteristics, and reduced toxicity were followed by numerous chemical modifications of the quinolone molecule. The resulting new fluoroquinolone antimicrobial agents have enhanced activity against gram-positive organisms and anaerobes (1, 2) and improved pharmacokinetic parameters in comparison to previous derivatives. However, only reports on single-drug kinetics have been published so far, and there have been no direct comparisons between the new drugs and the standard drug, ciprofloxacin (1-3).We therefore evaluated and compared the pharmacokinetics of six fluoroquinolones after a single oral dose in the same volunteers.( (mean, 28.4 Ϯ 4.3 years) and with an average weight of 67.4 ...

Efficacy of Levofloxacin in the Treatment of BK Viremia

“…Levofloxacin has greater bioavailability than ciprofloxacin, and a 500-mg/d dosage of levofloxacin is probably similar to the slightly higher doses of ciprofloxacin used in other studies (15,16,28,29). Furthermore, a higher dose or longer course of levofloxacin would have increased potential for microbacterial resistance and rates of adverse events in an immunologically vulnerable population.…”

Moxifloxacina: profilo farmacologico, terapeutico e farmacoeconomico

“…I principali parametri farmacocinetici della moxifloxacina dopo somministrazione orale sono riassunti e confrontati con quelli della ciprofloxacina e della levofloxacina nelle Tabelle 6 e 7 [59,81].…”

“…La moxifloxacina, nel volontario sano, presenta un'emivita di eliminazione di 10-14 ore, nettamente più lunga di quella della ciprofloxacina e della levofloxacina [59,81].…”

“…La clearance renale della moxifloxacina è nettamente inferiore a quella della ciprofloxacina e della levofloxacina [75,81].…”

Pharmacokinetic Parameters of Ciprofloxacin in Bangladeshi Volunteers: A Preliminary Evaluation

“…14 There are different methods to estimate ciprofloxacin in plasma, especially by HPLC 9,[15][16] , however, the initial challenge was to establish a suitable method to estimate plasma ciprofloxacin in laboratories of Bangladesh. Therefore, the aim of this study was to establish a method of estimation of ciprofloxacin in plasma as well as to get preliminary idea about the pharmacokinetic behaviour of Bangladeshi healthy volunteers of two different ethnic groups.…”