Inhibition of gastric secretion by a new H2-antagonist, YM-11170 in healthy subjects.
Oral administration of YM-11170 (5-20 mg) inhibited both basal and tetragastrin-induced gastric secretion of acid and pepsin in healthy volunteers. YM-11170 was at least 20 times more potent than cimetidine in inhibiting stimulated acid secretion. The area under the plasma concentration of YM-11170 vs time curve correlated positively to both dose and percent inhibition of acid output in response to tetragastrin. YM-11170 significantly inhibited basal and stimulated acid secretion even 10 h after a 20-mg dose. A plasma level of YM-11170 required for 50% inhibition of stimulated acid secretion was found to be 13 ng/ml. These results indicate that YM-11170 is a very potent inhibitor of gastric acid secretion and that twice daily medication of 20 mg YM-11170 is recommendable for further antisecretory studies with ulcer patients.
D000284:Administration, Oral; D000328:Adult; D002927:Cimetidine / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D015738:Famotidine; D005744:Gastric Acid / Q000378:metabolism*; D005750:Gastric Juice / Q000032:analysis / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D008297:Male; D010434:Pepsin A / Q000378:metabolism*; D011899:Ranitidine / Q000494:pharmacology; D013844:Thiazoles / Q000008:administration & dosage / Q000032:analysis / Q000097:blood / Q000494:pharmacology*; D013997:Time Factors
D013844:Thiazoles; D015738:Famotidine; D002927:Cimetidine; D011899:Ranitidine; D010434:Pepsin A