[Clinical studies on the transference of cephem-type antibiotics into bile and gallbladder tissues with special reference to cefotiam and cefmenoxime].

Cefotiam (CTM) and cefmenoxime (CMX) were studied for their serum concentrations and transference into bile in patients with PTCD or T-tube. One gram of CTM or either 1 g or 2 g of CMX was administered by an intravenous drip infusion for over 30 minutes. These drugs were also studied for their serum concentrations, bile concentrations, and tissue concentrations in the walls of the gallbladder of patients operated on for cholelithiasis. Intravenous drip infusion (over 30 minutes) was used to administer 1 g of CTM or 1 g or 2 g CMX immediately before surgery. Both CTM and CMX were readily transferred into bile. Their bile concentrations, however, varied greatly among patients, and extremely low levels were detected in some patients. A crossover analysis of concentrations of CMX in bile of patients given doses of 1 g and 2 g revealed a dose-response relationship. The crossover analysis of drug concentrations in bile of patients given CTM and CMX showed that CMX is transferred more readily to bile. The relationship between liver functions and drug transfer to bile was examined by plotting the total bilirubin level against drug concentrations in bile. The plots formed an exponential curve with a correlation coefficient (r) being -0.52 in cases when each subjects received 1 g of CTM and -0.72 in cases when each subjects received 1 g of CMX. A study of 3 patients given CMX at a dose of 1 g suggested that bile levels of CMX may be correlated to ICG. Concentrations of CTM and CMX in tissues of the gallbladder wall were fairly high, with unexpectedly small variance among patients. Even in patients with low bile concentrations of these drugs, drug levels in the tissues of the gallbladder wall were high. Drug levels in the noninflammatory tissues were higher than those in inflammatory lesions. The above findings suggest that CTM should be the antibiotic of choice for patients with ordinary biliary tract infections and after the surgery of the liver and biliary tract system, while CMX should be the antibiotic of choice for patients with severe biliary tract infections, and for compromised hosts after the surgery of the liver and biliary tract system.