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Influence of liver disease on metabolism and pharmacokinetics of cephalothin (CET) was studied. CET was given 1g bolus intravenously to 7 patients with liver cirrhosis, 7 patients with hepatitis (3 cases of acute hepatitis and 4 of chronic active hepatitis) and 7 patients with normal liver function. Serum consentration of CET and deacetyl CET was measured by High Performance Liquid Chromatography.<BR>Ratio of deacetyl CET to CET was less in cirrhosis compared to that in hepatitis or control group, demonstrating impaired metabolism of CET to deacetyl CET in cirrhosis. Deacetyl CET/CET ratio was correlated to such liver function test as BSP retention rate, prothrombin time or serum γ -globulin level which were characteristic in chronic liver disease, while not correlated to GP T, GOT, γ -GTP, total bilirubin which are characteristic in acute hepatic parenchymal disorders.<BR>Pharmacokinetic parameters calculated as two compartment open model were not statistically different among three groups.<BR>These results show that severe chronic liver disease impairs the biotransformation of CET to deacetyl CET, but does not affect pharmacokinetics of CET.