Role of H2-receptor blockers in the prevention of gastric injury resulting from nonsteroidal anti-inflammatory agents.

Nonsteroidal anti-inflammatory drugs (NSAIDs) can produce injury to the gastric and duodenal mucosa. The histamine (H2)-receptor blocker cimetidine was studied to determine whether protection of the gastric mucosa of normal volunteers could be provided against a single dose of aspirin, 1,300 mg. Gastric mucosal injury was assessed with gastroscopy performed two hours after aspirin intake. Three liquid cimetidine doses were administered over 24 hours prior to the aspirin dose, the last dose one hour before the aspirin. The 200-mg and 400-mg doses of cimetidine protected a sufficient number of subjects to warrant further study. In the second study, these two doses were further examined to determine whether three doses were necessary and whether the final dose could be coadministered with the aspirin instead of one hour before. Concomitant administration of a single dose of cimetidine with aspirin was found to protect the gastric mucosa from aspirin damage as effectively as the other cimetidine regimens employed. A final, double-blind comparison of cimetidine, 200 mg, with placebo administered with the aspirin, 1,300 mg, confirmed that cimetidine protected the gastric mucosa from the hemorrhagic effects of aspirin.