Excretion into bile and gallbladder tissue levels of a new quinolone, temafloxacin, and its clinical efficacy in biliary tract infections

• Published in: CHEMOTHERAPY Vol. 41; no. Supplement5; pp. 662 - 676
• Main Authors: Tanimura, Hiroshi, Yukawa, Hirofumi, Masaki, Kazuto, Arii, Kazuo, Kitamura, Tuguo, Aoki, Yozo, Nakatsuka, Hirohisa, Yamamoto, Shinji, Ichimiya, Genta, Kobayashi, Yasuto, Michiura, Jun, Tabuse, Katsuyoshi, Nagahama, Miho, Tabuse, Yohji, Minami, Mitsuaki, Iwahashi, Hideyuki, Mishima, Hideo
• Format: Journal Article
• Language: Japanese
• Published: Japanese Society of Chemotherapy 25.12.1993
• Subjects: temafloxacin
• ISSN: 0009-3165; 1884-5894
• DOI: 10.11250/chemotherapy1953.41.Supplement5_662

We evaluated the excretion into bile and gallbladder tissue levels of a new quinolone, temafloxacin (TMFX), and its clinical efficacy in 47 patients with biliary tract infections. 1) When TMFX was administered to 20 patients for 3 days at doses of 150 or 300 mg b.i.d., the concentrations of TMFX in the gallbladder tissue were 0.69-9.86 μg/g and the serum levels were 0.35-5.76 μg/ml 3-6 hours after the final dose. 2) In 5 patients with an indwelling T-tube, TMFX and ofloxacin (OFLX)(300 mg) were administered in a crossover design to compare their patterns of transfer to bile over 12 hours. The mean peak level of TMFX in bile was 21.7 μg/ml, higher than that of OFLX. 3) Twelve cases of cholecystitis and 7 cases of cholangitis were treated orally at daily doses of 300 or 600 mg of TMFX for 4-8 days. The clinical results were excellent in 5 cases and good in 9, the efficacy rate being 87.5%. Bacteriologically, 10 of the 12 strains isolated clinically before administration were eradicated by treatment with TMFX. No drug-related side effects were observed in any of the 47 patients. Based on these results, we conclude that TMFX is a useful drug for the treatment of biliary tract infections.