Oxamniquine inhibits metabolism of caffeine, hexobarbitone and antipyrine in vivo in mice

Abstract

Inhibition of hepatic metabolism of caffeine (as assessed from expiration of (14)CO(2) resulting from N-demethylation of (14)C-labelled caffeine), hexobarbitone (as assessed from sleeping times) and antipyrine (as assessed from expiration of I4CO2 resulting from the oxidation of "C-labelled antipyrine) was studied in male GB-1 mice administered a single SO mg kg-1 oral dose of the schistosomicidal drug oxamniquine. Metabolism of caffeine, catalysed by cytochrome P-4S0 1A2(CYP1A2), was inhibited most, while hexobarbitone and antipyrine metabolism were inhibited to a lesser, though significant, degree. These results indicate a need for further studies to investigate possible clinically relevant inhibition of hepatic drug metabolism by oxamniquine