Comparison of the in vivo and in vitro rates of formation of the three main oxidative metabolites of antipyrine in man.

1 The metabolism of antipyrine to its three main oxidative metabolites, 4-hydroxyantipyrine, 3-hydroxymethylantipyrine and norphenazone was investigated in vivo and in vitro in separate groups of subjects with normal hepatic function and in the same group of patients with suspected liver disease. 2 The rank order for the rate of formation of the three metabolites of antipyrine was similar in vivo and in vitro. 3 There was no significant correlation between the rates of formation of any pair of antipyrine metabolites either in vivo or in vitro. 4 Despite this there was a significant correlation between the in vivo and in vitro rates for formation of each of the three metabolites in the same group of patients. 5 It is concluded that determination of rates of formation of antipyrine metabolites from their excretion in urine provides an indication of the activity of the enzymes involved in their formation.