Gastric acid inhibition and oxmetidine kinetics in duodenal ulcer

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Abstract
Gastric acid inhibitory effects and kinetics of oxmetidine, a new histamine H2-receptor antagonist, were examined in 5 patients with duodenal ulcer disease. A constant i.v. infusion of impromidine was used to stimulate gastric acid secretion for 6 h. Oxmetidine was then given in a 28-mg i.v. infusion and a 200-mg oral solution. The maximum inhibition of gastric acid output was, on average, 77% after infusion and 92% after oral doses, with similar values for volume inhibition. Mean overall percent inhibition of acid output, volume and H+ concentration was 22, 8 and 15% for the i.v. dose and 51, 33 and 29% for the oral dose. The effect lasted for 3 h after the i.v. dose and for 5 h after the oral dose. Mean values for systemic clearance and half-life were 161 ml/min and 2.3 h. An average of 4.3% of the dose was recovered in urine as unchanged drug and 27% was recovered as a glucuronide metabolite. Mean bioavailability was 36%. Plasma concentration for 50% inhibition of acid output was 0.50 .mu.g/ml, indicating that oxmetidine is 2.5 times as potent as cimetidine. No adverse effects were noted.

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