PHASE I STUDY OF FLEROXACIN (II) MULTIPLE ADMINISTRATION OF 200mg AND 300mg

• Published in: CHEMOTHERAPY Vol. 38; no. Supplement2; pp. 312 - 327
• Main Authors: NAKASHIMA, MITSUYOSHI, UEMATSU, TOSHIHIKO, TAKIGUCHI, YOSHIHARU, MIZUNO, ATSUHIRO, KANAMARU, MITSUTAKA, OOIE, TSUYOSHI, MACHIDA, MASAAKI, KUSAJIMA, HISAO, ISHIDA, RYOZO, UCHIDA, HIROSHI
• Format: Journal Article
• Language: Japanese
• Published: Japanese Society of Chemotherapy 30-11-1990
• Subjects: Fleroxacin
• ISSN: 0009-3165; 1884-5894
• DOI: 10.11250/chemotherapy1953.38.Supplement2_312

We studied the pharmacokinetics and tolerance of fleroxacin in healthy male volunteers given 200mg and 300mg of the drug once daily for 7 days. Serum and urinary concentrations of unchanged drug reached a steady-state after 2-3 days with both doses. During the steady-state, mean serum concentrations of unchanged drug at 2 h after administration of 200 and 300 mg were 1.9-2.8 (n=4) and 3.7-4.2μg/ml (n= 5), and those at 24 h after administration were 0.4-0.5 and 0.7-0.9μg/ml. Serum half-life was 8.3-8.7h, independent of the dose and multiple administration. Fleroxacin concentrations in urine for 24h at steady-state were about 120 and 170μg/ml on average at 200 and 300mg. Mean urinary fleroxacin concentrations at 24 h after the first administration of 200 and 300 mg were 54 and 87μg/ml. The amounts of the drug excreted in urine up to 72 h after the last administration were 77-78% of the total dose on average, independent of the dose. Total urinary excretion, including metabolites, amounted to 87-88% of the total dose. No side-effects related to the drug were observed during the study.