H₂ Antagonist

H₂ Antagonist

The H₂ receptor antagonists are a class of drugs used to block the action of histamine on parietal cells in the stomach, decreasing the production of acid by these cells. H₂ antagonists are used in the treatment of dyspepsia, although they have been surpassed in popularity by the more effective proton pump inhibitors. In the United States, all four FDA-approved members of the group—cimetidine, ranitidine, famotidine, and nizatidine—are available over the counter in relatively low doses.

The prototypical H₂ antagonist was cimetidine, developed by Smith, Kline & French (now GlaxoSmithKline) in the mid-to-late 1960s and first marketed in 1976; sold under the trade name Tagamet, cimetidine would later become the first ever 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.