MISOPROSTOL—A LOGICAL THERAPEUTIC APPROACH TO GASTRODUODENAL MUCOSAL INJURY INDUCED BY NON‐STEROIDAL ANTI‐INFLAMMATORY DRUGS?

Abstract

Misoprostol is a synthetic analogue of naturally occurring prostaglandin E1. The basis of the damaging actions of non‐steroidal anti‐inflammatory drugs (NSAIDs) on the gastrointestinal (GI) tract is believed to be a consequence of two events: a direct damaging action on mucosal integrity and depletion of endogenous mucosal prostaglandins (PGs). Due to the latter effect, and because current evidence indicates that PGs play an important role in maintaining the integrity of the GI tract, misoprostol has been developed as a logical therapy to prevent and heal gastric and duodenal damage caused by NSAIDs. The purpose of this review is to consider the need for such a therapy, to describe its pharmaceutical development, to review its pharmacology and to review its efficacy compared with other available agents. Misoprostol is a synthetic analogue of PGE1 and the first prostaglandin to be licensed for the treatment of peptic ulcer disease. Misoprostol is a safe and well‐tolerated drug that exerts potent gastric antisecretory effects and mucosal protective actions on the gastric and duodenal mucosa. In a dosage of 800 μg daily in two or four divided doses, misoprostol produced rates of complete ulcer healing in both gastric and duodenal ulcer patients significantly superior to placebo and comparable to H2‐receptor antagonists. Misoprostol has been shown in a large number of controlled clinical trials to effectively heal and prevent NSAID‐induced gastropathy, a therapeutic need previously unserved. The therapeutic data indicate that misoprostol is superior to other agents in the prevention and treatment of NSAID‐induced gastric and duodenal damage. These data indicate that there are distinct differences in the pathogenesis of NSAID gastropathy and idiopathic peptic ulcer disease, and suggest that prostaglandin replacement is currently the most logical therapy available for NSAID gastropathy. Copyright © 1991, Wiley Blackwell. All rights reserved