Vol.56 No.S-1 April 2008

Pharmacokinetic profiles of sitafloxacin in patients with renal dysfunction

Mitsuyoshi Nakashima¹⁾ and Yukimichi Kawada²⁾

¹⁾Hamamatsu Institute of Clinical Pharmacology and Therapeutics, 40-3 Sukenobu, Naka-ku, Hamamatsu, Shizuoka, Japan
²⁾Gifu University School of Medicine

Abstract

We compared pharmacokinetic profiles of sitafloxacin(STFX) in patients with renal dysfunction divided into 3 creatinine clearance (C_cr) based groups: mild dysfunction (Group I), moderate dysfunction (Group II), and severe dysfunction (Group III). The area under the blood concentration-time curve (AUC) was 4.66 μg·h/mL in Group I, 8.04 μg·h/mL in Group II, and 9.95 μg·h/mL in Group III after STFX administration (50 mg). These results indicate that AUC increased with renal dysfunction severity. The half-life was 7.5 h in Group I, 11.5 h in Group II, and 16.3 h in Group III, and prolonged depending on renal dysfunction severity. Urinary excretion (0-48 h) was 48.9% in Group I, 44.7% in Group II, and 20.1% in Group III, and decreased depending on renal dysfunction severity. The incidence of adverse reactions was 25% (3/12).
Our results suggest that the STFX dosage and dosing interval be determined with care in patients with renal dysfunction.

Key word

sitafloxacin, renal dysfunction, pharmacokinetics, clinical trial

Received

October 5, 2007

Accepted

December 28, 2007

Jpn. J. Chemother. 56 (S-1): 21-24, 2008