Biliary excretion Cefoperazone (CPZ) in a dose of 1 g was intravenously injected to each of 13 cases with obstructive jaundice. Entire bile was collected through percutaneous transhepatic cholangiodrainage (PTCD) catheter in every 1 hour for 6 hours. The mean concentration of CPZ in serum was 112.1 +/- 17.8 micrograms/ml (mean +/- S.E.) at 1 hour and 55.1 +/- 19.2 micrograms/ml at 6 hours after injection. The mean recovery of CPZ in bile within 6 hours was 1.13 +/- 0.60%. Average CPZ concentrations in bile were 64.0 +/- 45.8 micrograms/ml in the 1 hour fraction, 142.7 +/- 78.4 micrograms/ml in the 2 hours fraction and 72.2 +/- 34.0 micrograms/ml in the 6 hours fraction. Biliary excretion of CPZ was low in cases where the serum concentration of total bilirubin was high, but maximum CPZ level in bile in patients with higher serum bilirubin concentrations than 30 mg/dl was still more than 3 micrograms/ml. Clinical evaluation. CPZ was administered to 43 patients with biliary tract infections. The efficacy ratio was 88.4% (excellent and good cases) in all cases, and especially high in cases with cholecystolithiasis. But no difference in efficacy ratio was observed among cases with cholecystolithiasis, choledocholithiasis without gallstone and cases subjected to PTCD. In 10 patients examined by ultrasonography, 8 cases showed reduced diameters of gallbladder. No adverse effect of CPZ was noted in any cases. These results suggest that a fairly large portion of CPZ was excreted through bile and that CPZ is a very useful drug for the treatment of biliary tract infections.