[Clinical investigation of the biliary excretion of cefoperazone in obstructive jaundice]

In the present study, we investigated the biliary excretion of cefoperazone (CPZ) in patients with complete obstruction in the lower bile duct governing PTC drainage, i.e., patients with completely blocked enterohepatic circulation. The blockage was observed to cause a delay in the excretion of CPZ due to hepatic dysfunction and the half-life of CPZ levels in serum was as long as 4.9 hours on the average. This is approximately the same as the half-life of 4.8 hours in hepatic dysfunction reported by Belaieff. Biliary concentration of CPZ reached their peak levels within the first 2 to 6 hours. The time to peak in cases with hepatic dysfunction was similar to that reported by observed in patients without hepatic dysfunction Yura et al. In our cases, however, peak biliary concentrations of CPZ were observed to be between 28 to 954 micrograms/ml with a mean of 320.5 micrograms/ml. These peak levels were lower than those reported by several investigators, but sufficiently effective concentrations seem to have been achieved in the bile even in jaundice because MIC80 values of CPZ are reported to be 6 to 10 micrograms/ml against E. coli, Klebsiella, and Enterobacter and 50 micrograms/ml against the most resistant Serratia. As mentioned above, the lowest peak biliary concentration was found to be 28 micrograms/ml and peak levels reached at least 50 micrograms/ml in 8 out of the 10 patients. Urinary concentrations of CPZ reached their peak levels within the first 30 minutes to 2 hours and CPZ urinary recovery ratio in 24 hours was 24.2 to 93.1% with a mean of 64.1%.(ABSTRACT TRUNCATED AT 250 WORDS)