Ranitidine--a new H2-receptor antagonist.

The pharmacokinetics and gastric antisecretory effects of a new histamine H2-receptor antagonist, ranitidine hydrochloride, have been investigated in healthy subjects. In the pharmacokinetic study six subjects received 20 mg, 40 mg, and 80 mg ranitidine, both orally and intravenously. Plasma levels of ranitidine were dose-related and in most subjects after oral drug the concentration time curve was bimodal. The estimated elimination half-life was 140 minutes and the bioavailability of the oral drug was about 50%. Five subjects received bolus intravenous injections of ranitidine 20 mg, 40 mg, and 80 mg during continuous gastric stimulation with pentagastrin. There was a dose-related reduction in acid output (P less than 0.05).