Clinical pharmacology of famotidine.
The results of the initial clinical pharmacology studies of famotidine, a new H2 receptor antagonist, are summarized. These studies indicate that: single oral doses of famotidine (5-80 mg) were well tolerated; famotidine effectively suppressed basal, nocturnal, pentagastrin- and meal-stimulated acid secretion; the duration of the antisecretory action of famotidine was dose related: up to 12 h for the 20-mg dosages, and 18-24 h for the 80-mg dose; the elimination half-life was 3.8 h; 5 mg of famotidine gave acid suppression similar to that of 300 mg of cimetidine; a dose response was identified: 2 h after oral dosing, 5 mg famotidine suppressed stimulated acid secretion to 60% of control and was comparable to 300 mg cimetidine (55% suppression), whereas higher doses of famotidine yielded significantly more suppression of acid secretion (10 mg yielding 70% and 20 mg 90%), significantly greater than 300 mg cimetidine; plasma famotidine concentration and urinary recovery were dose related, and famotidine (10-40 mg) had no effect on serum prolactin. Thus, famotidine is a safe and potent H2 blocker of acid secretion with a long duration of action.
Smith
J L
JL
D000818:Animals; D002927:Cimetidine / Q000494:pharmacology; D002940:Circadian Rhythm / Q000187:drug effects; D004285:Dogs; D004305:Dose-Response Relationship, Drug; D004381:Duodenal Ulcer / Q000188:drug therapy; D015738:Famotidine; D005502:Food; D005744:Gastric Acid / Q000378:metabolism; D006207:Half-Life; D006632:Histamine / Q000494:pharmacology; D006635:Histamine H2 Antagonists / Q000378:metabolism* / Q000494:pharmacology; D006801:Humans; D007700:Kinetics; D010418:Pentagastrin / Q000494:pharmacology; D010434:Pepsin A / Q000378:metabolism; D011388:Prolactin / Q000097:blood; D051381:Rats; D013758:Tetragastrin / Q000494:pharmacology; D013844:Thiazoles / Q000378:metabolism* / Q000494:pharmacology; D013997:Time Factors
D006635:Histamine H2 Antagonists; D013844:Thiazoles; D013758:Tetragastrin; D015738:Famotidine; D002927:Cimetidine; D006632:Histamine; D011388:Prolactin; D010434:Pepsin A; D010418:Pentagastrin