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Pharmacology of antiulcer medications

INTRODUCTION

The treatment of peptic ulcers has changed dramatically in the past two decades, mirroring the revolution in understanding of the etiologies of peptic ulcers. Principles of treatment include:

  • Antibiotic therapy is indicated for ulcer disease associated with Helicobacter pylori (H. pylori) infection.
  • Anti-secretory drugs (H2 receptor antagonists [H2RAs] and proton pump inhibitors [PPIs]) are the mainstays of treatment for ulcer healing.
  • Maintenance therapy, once a mainstay of treatment for peptic ulcer disease, is no longer indicated after successful eradication of H. pylori [1].
  • Antacids, bismuth, and protective agents (eg, sucralfate) were shown to heal peptic ulcers in an era before the role of H. pylori was recognized, and, in retrospect, studies were performed on largely H. pylori-positive peptic ulcer patients. The efficacy of these agents for nonsteroidal antiinflammatory drug (NSAID) ulcers or for non-NSAID, non-H. pylori ulcers has not been established, and, thus, they have no role in the current treatment of peptic ulcers. The only exception is the use of bismuth as part of antibiotic regimens to cure H. pylori infection.
  • Prostaglandin analogues (eg, misoprostol) are effective for preventing NSAID-induced ulcers, but they have no established role for healing ulcers.

The pharmacology of antiulcer drugs, excluding the antibiotics used to treat H. pylori, will be reviewed here. The treatment of H. pylori as well as an overview of the natural history and treatment of peptic ulcer disease are discussed elsewhere. (See "Treatment regimens for Helicobacter pylori" and "Overview of the natural history and treatment of peptic ulcer disease".)

H2 RECEPTOR ANTAGONISTS

H2 receptor antagonists (H2RAs) inhibit acid secretion by blocking histamine H2 receptors on the parietal cell (figure 1). H2RAs (eg, cimetidine, ranitidine, famotidine, and nizatidine) are still used for treatment and maintenance therapy of peptic ulcer disease, treatment of gastroesophageal reflux disease, and management of dyspepsia. However, they achieve less acid suppression than proton pump inhibitors.

H2RAs have efficacy for inhibiting acid secretion, preventing NSAID-induced ulcers, and in healing peptic ulcers when used at appropriate doses [2]. However, proton pump inhibitors have been shown to have superior healing rates for both duodenal and gastric ulcers [3]. In patients with NSAID-induced ulcers who require continued NSAID therapy while receiving treatment for ulcer disease, proton pump inhibitors are also superior to H2RAs [4].

                       

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Literature review current through: Aug 2014. | This topic last updated: May 11, 2013.
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