CHEMOTHERAPY OF BILIARY TRACT INFECTIONS (XXXVII): EXCRETION INTO BILE AND GALLBLADDER TISSUE LEVELS OF LEVOFLOXACIN AND ITS CLINICAL EFFECT IN BILIARY TRACT INFECTIONS

Evaluations were made on biliary excretion and penetration into the gallbladder tissue of levofloxacin (LVFX, DR-3355), a new quinolone antibacterial agent, and its clinical efficacy in biliary tract infections. 1.Gallbladder tissue concentrations and biliary concentrations of LVFX at 2-6 hours after oral administration of 100 mg were 0.58-1.99μg/g and 0. 49-5. 63μg/ml, respectively. These tissue and biliary levels are almost equal or somewhat higher than the serum levels (0. 55-1. 63μg/ml) of the compound. 2. The concentrations of LVFX and optical isomer DR-3354 in the serum, gallbladder tissue, and bile were determined after a single or a concomitant administration of LVFX 100 mg and/or ofloxacin (OFLX) 100 to 200 mg. The concentration ratio of LVFX to DR-3354 paralleled with the ratio of the 2 compounds administrated. 3. At a dose of 100 mg, the glucuronide of LVFX in the commom duct bile was detected at proportions between 0. 9 and 36. 0%. 4. A total of 11 patients with biliary tract infections, including 6 cholecystitis 3 cholangitis, and 1 each of cholecystocholangitis and liver abscess was treated with LVFX at 100-200 mg t. i. d. for 3-14 days. Clinical results were excellent or good in 8 cases and fair in 3 cases, resulting in an efficacy rate of 72. 7%. 5. A side effect and an abnormal change in laboratory findings were observed in both 1 case each and they were both mild. It was concluded that LVFX showed good penetration to the biliary tract as does OFLX, and that it would be a useful oral agent for the treatment of biliary tract infections.