Effects of cimetidine and ranitidine on hepatic drug metabolism

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Abstract
Cimetidine impairs elimination of a number of drugs metabolized by the human hepatic mixed-function oxidase enzymes. It is uncertain whether this is related to its histamine H2-receptor antagonism or to its intrinsic structure. Ranitidine is a more potent H2-receptor antagonist and has a completely different structure. Cimetidine (1 g/day for 7 days) induced a 23 and 35% fall in mean systemic clearance of antipyrine and theophylline, respectively, whereas ranitidine (300 mg/day for 7 days) had no significant effect on the clearance of either drug. Evidently, the inhibition of drug metabolism by cimetidine is not related to histamine H2-receptor antagonism.

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