Clinical pharmacology of etintidine in patients with duodenal ulcer.
The gastric antisecretory activity of etintidine, a new histamine H2-receptor antagonist, was evaluated in 5 patients with quiescent duodenal ulcer disease. Meal-stimulated acid secretion was measured after 100 and 300 mg oral doses of etintidine, 100 and 300 mg oral doses of cimetidine, and placebo. Reductions from placebo in four-hour gastric acid secretion were 49, 65, 80, and 94%, with 100 mg cimetidine, 100 mg etintidine, 300 mg cimetidine, and 300 mg etintidine, respectively. Drug concentrations in plasma were determined by HPLC. The pharmacokinetics of the 2 drugs were similar. We analyzed sigmoid-shaped concentration-response curves to both agents; the concentrations causing 50% inhibition of meal-stimulated gastric acid secretion were 0.44 +/- 0.04 and 0.15 +/- 0.04 micrograms/ml for cimetidine and etintidine, respectively. However, characteristics of these curves were such that the potency difference diminished at higher concentrations.
D002927:Cimetidine / Q000097:blood / Q000627:therapeutic use; D004381:Duodenal Ulcer / Q000188:drug therapy*; D005260:Female; D005744:Gastric Acid / Q000378:metabolism; D005745:Gastric Acidity Determination; D005755:Gastrins / Q000097:blood; D006635:Histamine H2 Antagonists / Q000378:metabolism / Q000627:therapeutic use*; D006801:Humans; D007093:Imidazoles / Q000097:blood / Q000627:therapeutic use*; D007700:Kinetics; D008297:Male; D008875:Middle Aged
D005755:Gastrins; D006635:Histamine H2 Antagonists; D007093:Imidazoles; D002927:Cimetidine; C036616:etintidine