Which medications in the drug class H2-Receptor Antagonists are used in the treatment of Gastroesophageal Reflux Disease?

Updated: May 23, 2019
  • Author: Marco G Patti, MD; Chief Editor: BS Anand, MD  more...
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Answer

H2-Receptor Antagonists

H2 receptor antagonists are the first-line agents for patients with mild to moderate symptoms and grades I-II esophagitis. Options include ranitidine (Zantac), cimetidine (Tagamet), famotidine (Pepcid), and nizatidine (Axid).

The H2 receptor antagonists are reversible competitive blockers of histamine at the H2 receptors, particularly those in the gastric parietal cells, where they inhibit acid secretion. They are highly selective, do not affect the H1 receptors, and are not anticholinergic agents. Although IV administration of H2 blockers may be used to treat acute complications (eg, gastrointestinal bleeding), the benefits are not yet proven.

These agents are effective for healing only mild esophagitis in 70%-80% of patients with GERD and for providing maintenance therapy to prevent relapse. Tachyphylaxis has been observed, suggesting that pharmacologic tolerance can reduce the long-term efficacy of these drugs.

Additional H2 blocker therapy has been reported to be useful in patients with severe disease (particularly those with Barrett esophagus) who have nocturnal acid breakthrough.

Ranitidine (Zantac)

Ranitidine inhibits histamine stimulation of the H2 receptor in the gastric parietal cells, which, in turn, reduces gastric acid secretion, gastric volume, and hydrogen concentrations.

Cimetidine (Tagamet)

Cimetidine inhibits histamine at H2 receptors of the gastric parietal cells, which results in reduced gastric acid secretion, gastric volume, and hydrogen concentrations.

Famotidine (Pepcid)

Famotidine competitively inhibits histamine at H2 receptor of the gastric parietal cells, resulting in reduced gastric acid secretion, gastric volume, and hydrogen concentrations.

Nizatidine (Axid)

Nizatidine competitively inhibits histamine at the H2 receptor of the gastric parietal cells, resulting in reduced gastric acid secretion, gastric volume, and hydrogen concentrations.


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