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Pathway Description
Cimetidine Metabolism Pathway
Homo sapiens
Drug Metabolism Pathway
Created: 2013-09-11
Last Updated: 2019-09-12
Cimetidine, sold as Tagamet, is a compound related to histamine. It is a H2 antagonist drug, also called H2RAs or H2 blockers, and was the first of this class to be discovered. H2 antagonist drugs compete with histamine to bind to the histamine H2-receptors found on the basolateral membrane of gastric parietal cells. This blocks histamine effects, resulting in reduced gastric acid secretion and a reduction in gastric volume and acidity. Cimetidine also helps to block pepsin and gastrin output, and due to the inhibition of gastric acid secretion, it is typically used to treat heartburn and ulcers. Cimetidine also blocks the activity of cytochrome P-450 enzymes CYP1A2, 2C9, 2C19, 2D6, 2E1 and 3A4, which may affect the metabolism of other drugs.
References
Cimetidine Pathway References
Bertaccini G, Coruzzi G: Control of gastric acid secretion by histamine H2 receptor antagonists and anticholinergics. Pharmacol Res. 1989 Jul-Aug;21(4):339-52.
Pubmed: 2570417
Cimetidine. (2009). e-CPS (online version of Compendium of Pharmaceuticals and Specialties). Retrieved July 2, 2009.
Pounder RE: Histamine H2-receptor antagonists and gastric acid secretion. Pharmacol Ther. 1984;26(2):221-34.
Pubmed: 6152495
Gantz I, Munzert G, Tashiro T, Schaffer M, Wang L, DelValle J, Yamada T: Molecular cloning of the human histamine H2 receptor. Biochem Biophys Res Commun. 1991 Aug 15;178(3):1386-92. doi: 10.1016/0006-291x(91)91047-g.
Pubmed: 1714721
Nishi T, Koike T, Oka T, Maeda M, Futai M: Identification of the promoter region of the human histamine H2-receptor gene. Biochem Biophys Res Commun. 1995 May 16;210(2):616-23. doi: 10.1006/bbrc.1995.1703.
Pubmed: 7755641
Murakami H, Sun-Wada GH, Matsumoto M, Nishi T, Wada Y, Futai M: Human histamine H2 receptor gene: multiple transcription initiation and tissue-specific expression. FEBS Lett. 1999 May 28;451(3):327-31. doi: 10.1016/s0014-5793(99)00618-3.
Pubmed: 10371214
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