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HandWiki. H2 Antagonist. Encyclopedia. Available online: https://encyclopedia.pub/entry/31955 (accessed on 20 September 2026).
HandWiki. H2 Antagonist. Encyclopedia. Available at: https://encyclopedia.pub/entry/31955. Accessed September 20, 2026.
HandWiki. "H2 Antagonist" Encyclopedia, https://encyclopedia.pub/entry/31955 (accessed September 20, 2026).
HandWiki. (2022, October 31). H2 Antagonist. In Encyclopedia. https://encyclopedia.pub/entry/31955
HandWiki. "H2 Antagonist." Encyclopedia. Web. 31 October, 2022.
H2 Antagonist
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H2 antagonists, sometimes referred to as H2RAs and also called H2 blockers, are a class of medications that block the action of histamine at the histamine H2 receptors of the parietal cells in the stomach. This decreases the production of stomach acid. H2 antagonists can be used in the treatment of dyspepsia, peptic ulcers and gastroesophageal reflux disease. They have been surpassed by proton pump inhibitors (PPIs); the PPI omeprazole was found to be more effective at both healing and alleviating symptoms of ulcers and reflux oesophagitis than the H2 blockers ranitidine and cimetidine. H2 antagonists are a type of antihistamine, although in common use the term "antihistamine" is often reserved for H1 antagonists, which relieve allergic reactions. Like the H1 antagonists, some H2 antagonists function as inverse agonists rather than receptor antagonists, due to the constitutive activity of these receptors. The prototypical H2 antagonist, called cimetidine, was developed by Sir James Black at Smith, Kline & French – now GlaxoSmithKline – in the mid-to-late 1960s. It was first marketed in 1976 and sold under the trade name Tagamet, which became the first blockbuster drug. The use of quantitative structure-activity relationships (QSAR) led to the development of other agents – starting with ranitidine, first sold as Zantac, which has fewer adverse effects and drug interactions and is more potent. H2 blockers, which all end in "-tidine," are not the same as H1 receptor antagonists, which relieve allergy symptoms.

gastroesophageal reflux glaxosmithkline parietal cells

References

  1. Rossi S (Ed.) (2005). Australian Medicines Handbook 2005. Adelaide: Australian Medicines Handbook. ISBN:0-9578521-9-3.
  2. Miller, Ronal D; Eriksson, Lars; Fleisher, Lee A; Wiener-Kronish, Jeanine P (25 November 2014). Miller's Anesthesia Airway management in the Adult (8th ed.). Elsevier. pp. 1647–1681. 
  3. Drugs.com "Cimetidine Side Effects" https://www.drugs.com/sfx/cimetidine-side-effects.html
  4. "Use of acid-suppressive drugs and risk of pneumonia: a systematic review and meta-analysis". CMAJ 183 (3): 310–9. 2011. doi:10.1503/cmaj.092129. PMID 21173070.  (adjusted odds ratio [OR] 1.22) http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=3042441
  5. "Review article: drug interactions with agents used to treat acid-related diseases". Alimentary Pharmacology & Therapeutics 13 Suppl 3: 18–26. August 1999. doi:10.1046/j.1365-2036.1999.00021.x. PMID 10491725.  https://dx.doi.org/10.1046%2Fj.1365-2036.1999.00021.x
  6. "Interactions and non-interactions with ranitidine". Clinical Pharmacokinetics 9 (6): 493–510. 1984. doi:10.2165/00003088-198409060-00002. PMID 6096071.  https://dx.doi.org/10.2165%2F00003088-198409060-00002
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