A CLINICAL STUDY ON CEFOTIAM WITH SPECIAL REFERENCE TO EXCRETION IN BILE AND CONCENTRATION IN GALLBLADDER TISSUE

Following 1 hour intraveous drip infusion of 1.0 g of cefotiam (CTM), 38 patients with cholelithiasis were operated at scheduled intervals. The CTM concentrations in serum, common duct bile, gallbladder bile and gallbladder tissue were measured.1. The mean level of CTM concentration in serum showed a peak of 53.1 μg/ml at 1 hour, and decreased in the level of 1.0 μg/ml at 5 hours after administration.2. CTM concentrations in common duct bile revealed a mean level of 162 μg/ml at 1 hour and similarly high concentrations from 1 to 5 times of the peak level in serum were maintained for 3.5 hours. In patients with impaired liver function, the levels of CTM concentration were lower than those without them.3. CTM concentrations in gallbladder bile showed a high value at 2-3.5 hours after administration.In many cases the levels were relatively lower than those in common duct bile, particularly in patients with cystic duct obstruction and/or with marked chronic cholecystitis.4. As for gallbladder tissue levels, CTM concentrations showed low levels less than 50 μg/g in patients with pathological changes of gallbladder, as well as in gallbladder bile. While, favorable concentrations of 50-100 μg/g were obtained in patients without them.5. There was a positive correlation between CTM concentrations in common duct bile and gallbladder bile, and also between the concentrations in gallbladder bile and those in gallbladder tissue in patients without cystic duct obstruction or marked chronic cholecystitis.Then, in the situation, CTM transfer into gallbladder bile or gallbladder tissue might be mainly dependent on biliary excretion of CTM. Moreover, according to the condition of the pathological changes of inflam-mation, another factors such as blood supply to the gallbladder, direct transfer through the liver to the wall and/or mucosal excretion from gallbladder wall are thought to affect on the CTM concentration in gall-bladder tissue or bile.