Which of the following is not metabolized by acetylation:
Ans. B: Phenytoin Phenytoin is extensively metabolised in the liver to 5-(4-hydroxypheny1)-5 phenyl-hydantoin, which is inactive. This para hydroxylation of phenytoin is carried out by cytochrome P450 2C9. This enzyme also hydroxylates tolbutamide and warfarin. This explains the interaction with these substances. The p-hydroxylated phenytoin is in turn conjugated to its glucuronide. Phenytoin hydroxylation is capacity-limited because of the saturable enzyme systems in the liver. At therapeutic doses, metabolism is nonlinear (first-order kinetics), while at toxic doses the metabolism is linear zero-order kinetics). Phenytoin undergoes entero-hepatic recycling.
Hydralazine
Phenytoin
Isoniazid
Procainamide