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Pathway Description
Cimetidine Action Pathway
Homo sapiens
Drug Action Pathway
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
Gastric Acid Production References
Wolfe MM, Soll AH: The physiology of gastric acid secretion. N Engl J Med. 1988 Dec 29;319(26):1707-15. doi: 10.1056/NEJM198812293192605.
Pubmed: 3060722
Schubert ML: Gastric acid secretion. Curr Opin Gastroenterol. 2016 Nov;32(6):452-460. doi: 10.1097/MOG.0000000000000308.
Pubmed: 27607343
Schubert ML: Functional anatomy and physiology of gastric secretion. Curr Opin Gastroenterol. 2015 Nov;31(6):479-85. doi: 10.1097/MOG.0000000000000213.
Pubmed: 26376477
Heitzmann D, Warth R: No potassium, no acid: K+ channels and gastric acid secretion. Physiology (Bethesda). 2007 Oct;22:335-41. doi: 10.1152/physiol.00016.2007.
Pubmed: 17928547
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