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The H 2 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. H 2 antagonists are used in the treatment of dyspepsia, although they have been surpassed in popularity by the more effective [1] proton pump inhibitors.
Famotidine, sold under the brand name Pepcid among others, is a histamine H 2 receptor antagonist medication that decreases stomach acid production. [4] It is used to treat peptic ulcer disease , gastroesophageal reflux disease , and Zollinger-Ellison syndrome . [ 4 ]
In general, proton pump inhibitors are well tolerated, and the incidence of short-term adverse effects is relatively low. The range and occurrence of adverse effects are similar for all of the PPIs, though they have been reported more frequently with omeprazole. This may be due to its longer availability and, hence, clinical experience.
Ranitidine was introduced in 1981 and was the world's biggest-selling prescription drug by 1988. The H 2 receptor antagonists have since largely been superseded by the even more effective proton pump inhibitors (PPIs), with omeprazole becoming the biggest-selling drug for many years.
The pharmacologic treatment of acid peptic disorders centers on redressing this imbalance by either improving mucosal defenses with drugs like sucralfate, bismuth, and prostaglandin analogs, neutralizing acid with antacids, or decreasing acid secretion with histamine 2 receptor antagonists or, more recently, proton pump inhibitors. [2]
A derivative of timoprazole, omeprazole, was discovered in 1979, and was the first of a new class of drug that control acid secretion in the stomach, a proton pump inhibitor (PPI). [11] [12] Addition of 5-methoxy-substitution to the benzimidazole moiety of omeprazole was also made and gave the compound much more stability at neutral pH. [6]
A 14-day course of "quadruple therapy" with a proton pump inhibitor, bismuth, tetracycline, and metronidazole or tinidazole is a more complicated but also more effective regimen. In a 2011 randomized, controlled trial, the per protocol eradication rates were 93% with quadruple therapy and 70% with triple therapy.
With the development of proton pump inhibitors, such as omeprazole, approved for the same indications, cimetidine is available as an over-the-counter formulation to prevent heartburn or acid indigestion, along with the other H2-receptor antagonists. [12] Cimetidine was developed in 1971 and came into commercial use in 1977.