PHARMACOKINETICS AND CLINICAL STUDIES ON SPARFLOXACIN

• Published in: CHEMOTHERAPY Vol. 39; no. Supplement4; pp. 234 - 244
• Main Authors: Saito, Atsushi, Hojo, Toshio, Shimada, Jingoro, Kaji, Masanobu, Hori, Seiji, Imai, Takeo, Sakai, Osamu, Shiba, Kohya, Yoshida, Masaki, Matsumoto, Fumio
• Format: Journal Article
• Language: English; Japanese
• Published: Japanese Society of Chemotherapy 1991; 公益社団法人 日本化学療法学会
• Subjects: Probenecid; Sparfloxacin; 制酸剤; 吸収; 臨床
• ISSN: 0009-3165; 1884-5894
• DOI: 10.11250/chemotherapy1953.39.Supplement4_234

We performed basic and clinical studies on sparfloxacin (SPFX), a newly synthesized quinolone, and obtained the following results. 1. Effects of antacid (dried aluminium hydroxide gel, AL) and probenecid on the gastrointestinal absorption and renal excretion of SPFX were investigated by a cross-over design in six healthy male volunteers. The subjects received orally 200mg of SPFX with and without 1g of AL or 1.5g of probenecid, and the time course of blood levels, urinary concentrations and urinary recovery of SPFX and its pharmacokinetic parameters were determined. SPFX concentrations in the samples were measured by the HPLC method. The obtained pharmacokinetic parameters for SPFX after each of the treatment were as follows: the Cmax, Tmax, T1/2 and AUC0→∞ for SPFX alone were 0.865μg/ml, 5.3h, 14.7h and 21.1μg·h/ml, respectively; those for co-administration with AL were 0.683μg/ml, 4.0h, 14.0h and 13.7μg·h/ml; and those for co-administration with probenecid were 0.810μg/ml, 3.5h, 15.7h and 20.1μg·h/ml. Gastrointestinal absorption of SPFX was inhibited by interaction with AL, but SPFX was the least inhibited among the new quinolones. 2. Twenty-three patients with respiratory infections, 5 with urinary tract infections and one with mastitis were treated orally at a daily dose of 100-300mg of SPFX for 3-4 days. The clinical results were excellent in 8 cases, good in 16 and poor in 5, giving the efficacy rate of 82.8%. We encountered adverse reactions to SPFX in two cases: vertigo, nausea and epigastric pain in one case, and fever and eosinophilia in another case. These adverse reactions disappeared shortly after completion of the treatment. There were no cases in which the administration of SPFX was discontinued due to adverse effects.