:Receptor Antagonist

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Pharmacokinetic and Pharmacological effects of injected ranitidine, a new histamine H2-receptor antagonist, were studied on six male healthy volunteers. Inhibition of tetragastrin-induced gastric acid secretion and changes of various hormones in plasma were also studied after ranitidine administrations by double-blind cross-over comparison with placebo. Plasma ranitidine concentration-time curve was well fitted to the two compartment open model. Following intravenous administration of 50mg ranitidine, the apparent volume of distribution (Vd) was 81. 4±4.81 and total body clearance (Clp) and renal clearance (Clr) were 38.0±2.9 and 32.2±2.4 l/hr, respectively, and elimination half-life (t1/2β) was 1.9±0.09hr. The fraction of drug excreted unchanged in urine expressed as a percentage of administered dose, was 85%within 24 hours after administration. Tetragastrin-induced gastric acid secretion was significantly inhibted until two hours after administration of ranitidine. Plasma prolactin and parathormone concentrations were not influenced by ranitidine.Plasma gastrin and secretin were not influenced by ranitidine except for slight changes at three hours and one hour, respectively, after administration of ranitidine.
一般社団法人日本臨床薬理学会の論文