etintidine and Duodenal-Ulcer

Greatly improved understanding of the cellular basis for gastric acid secretion and gastroduodenal mucosal defense has led to a dramatic improvement in the pharmacologic treatment of peptic ulcer disease. The advances produced by cimetidine and ranitidine are being continued by a new generation of histamine receptor antagonists, as well as by other anti-ulcer agents. These new drugs, when used appropriately, will greatly expand the surgeon's ability to treat patients with peptic ulcer disease. A knowledge of the pathophysiologic characteristics of peptic ulceration and of the inherent limitations of each agent will become increasingly important for surgeons who treat these patients.

Topics: Acetylcholine; Benzimidazoles; Chemical Phenomena; Chemistry; Cimetidine; Disease Susceptibility; Dose-Response Relationship, Drug; Duodenal Ulcer; Gastric Acid; Gastric Mucosa; Gastrins; Histamine; Histamine H2 Antagonists; Humans; Imidazoles; Intestinal Mucosa; Peptic Ulcer; Ranitidine; Receptors, Muscarinic; Stimulation, Chemical; Stomach Ulcer

Topics: Adult; Clinical Trials as Topic; Dose-Response Relationship, Drug; Duodenal Ulcer; Gastric Acid; Gastric Mucosa; Humans; Imidazoles; Male; Placebos; Smoking

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.

Topics: Cimetidine; Duodenal Ulcer; Female; Gastric Acid; Gastric Acidity Determination; Gastrins; Histamine H2 Antagonists; Humans; Imidazoles; Kinetics; Male; Middle Aged

Topics: Adult; Aged; Drug Administration Schedule; Duodenal Ulcer; Female; Humans; Imidazoles; Male; Middle Aged; Ranitidine