[Effect of histamine H2-receptor antagonists on the hepatic elimination of drugs]

Klin Wochenschr. 1983 Jul 1;61(13):625-32. doi: 10.1007/BF01487578.
[Article in German]


H2-blocking agents, such as cimetidine or ranitidine are used in numerous patients. This treatment is often associated with the co-administration of a variety of other drugs. From clinical observations and pharmacokinetic studies it is obvious that even short-term treatment with therapeutic doses of cimetidine inhibits the hepatic elimination of antipyrine, warfarin, diazepam, desmethyldiazepam, chlordiazepoxide, propranolol, labetalol, metoprolol, phenytoin, carbamazepine, chlormethiazole, theophylline and caffeine. All these drugs are metabolized by cytochrome-dependent so-called phase I reactions. Cimetidine can interact with drug binding to the cytochrome P450 system leading to impaired drug metabolism. On the other hand drugs which are eliminated by glucuronidation (cytochrome independent phase II reaction), such as oxazepam and lorazepam are not affected by cimetidine. Other H2-blocking agents (ranitidine, oxmetidine) did not impair the elimination of antipyrine, warfarin, diazepam or propranolol. Furthermore, cimetidine and ranitidine might slightly reduce hepatic blood flow which could reduce the elimination of drugs with high hepatic clearance.

Publication types

  • English Abstract
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Cimetidine / pharmacology
  • Cytochrome P-450 Enzyme System / metabolism
  • Drug Interactions
  • Furans / pharmacology
  • Half-Life
  • Histamine H2 Antagonists / pharmacology*
  • Humans
  • Imidazoles / pharmacology
  • Kinetics
  • Liver / drug effects*
  • Liver / metabolism
  • Liver Circulation / drug effects
  • Pharmaceutical Preparations / metabolism*
  • Ranitidine
  • Time Factors


  • Furans
  • Histamine H2 Antagonists
  • Imidazoles
  • Pharmaceutical Preparations
  • Cimetidine
  • Ranitidine
  • Cytochrome P-450 Enzyme System
  • oxmetidine