EXCRETION INTO BILE AND GALLBLADDER TISSUE LEVEL OF A NEW QUINOLONE, SPARFLOXACIN, AND ITS CLINICAL EFFICACY ON SURGICAL INFECTIONS

• Published in: CHEMOTHERAPY Vol. 39; no. Supplement4; pp. 620 - 632
• Main Authors: Tanimura, Hiroshi, Ishimoto, Kiwao, Yukawa, Hirofumi, Sakamoto, Yukitomo, Ohnishi, Hironobu, Kitamura, Tsuguo, Yamamoto, Shinji, Shimada, Kohsuke, Kobayashi, Yasuto, Aoki, Yozo, Oka, Sumikazu, Nagahama, Miho, Tabuse, Yohji, Kashiwagi, Hideo
• Format: Journal Article
• Language: Japanese
• Published: Japanese Society of Chemotherapy 28.08.1991
• Subjects: Sparfloxacin
• ISSN: 0009-3165; 1884-5894
• DOI: 10.11250/chemotherapy1953.39.Supplement4_620

We evaluated the excretion into bile and gallbladder tissue level of a new quinolone, sparfloxacin (SPFX), and its clinical efficacy on surgical infections. 1) In 13 patients with biliary tract infections, SPFX was evaluated for its biliary excretion in 3 groups of patients; Group I: 4 cases with an indwelling T-tube after choledochotomy, Group II: 3 cases with percutaneous transhepatic cholangio-drainage (PTCD) before the operation on cholangioma or tumor of the head of the pancreas, Group III: 6 cases with concomitant biliary and pancreatic drainage after pancreatoduodenectomy, and Group IV: 3 cases before cholecystectomy. Groups I, II and ifi received orally 300mg of SPFX once. Blood, bile and urine levels of SPFX and its glucuronide (SPFX-G) were measured by HPLC. The average Cmax values of SPFX in plasma, and bile, in groups I to III were 0.65 to 1.0μg/ml, and 2.5 to 8.6μg/ml, respectively. Biliary level of SPFX was still 1.43μg/ml at 72 hr after administration. 2) Three cases before cholecystectomy received the same dose daily as above for 2 days. The average SPFX level was 1.32μg/ml in plasma, the markedly high value of 108.5μg/ml in bile, and 9.2μg/g in gallbladder tissue. 3) 17 cases with cholecystitis and 9 cases with cholangitis were treated orally at a daily dose of 300mg of SPFX for 3-14 days. The clinical results were excellent in 4 cases and good in 17, the efficacy rate being 80.8%. Eight cases of other surgical infections including periproctal abscess were also treated with 300mg of SPFX, and an efficacy rate of 62.5% was obtained. A 76.5% efficacy rate was obtained in the total 34 cases with surgical infections. Bacteriologically, 25 of 36 strains clinically isolated before administration were eradicated by treatment with SPFX. Mild or moderate gastrointestinal symptoms were noticed in three cases. From theses results, we conclude that SPFX is a useful drug for the treatment of surgical infections, especially biliary tract infections.