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Concept
H2 receptor antagonist
Summary
DISPLAYTITLE:H2 receptor antagonist
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.
cimetidine
ranitidine (withdrawn in USA, suspended in EU and Australia for carcinogen contamination in manufacturing process)
famotidine
nizatidine
roxatidine
lafutidine
lavoltidine (discontinued as carcinogen)
niperotidine (withdrawn as causing liver damage)
sufotidine
Cimetidine was the prototypical histamine H2-receptor antagonist from which later drugs were developed. Cimetidine was the culmination of a project at Smith, Kline & French (SK&F; now GlaxoSmithKline) by James W.
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