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Inhibition of pentagastrin-stimulated gastric acid secretion and plasma levels of the new histamine H2-receptor antagonist ramixotidine dihydrochloride (CM 57755) in human volunteers.

Abstract：

:The new competitive histamine H2-receptor antagonist, ramixotidine 2 HCl (CM 57755), has been tested in healthy male volunteers for its ability to inhibit pentagastrin-stimulated gastric acid secretion. In the first study, in 8 subjects, pentagastrin 6 micrograms.kg-1 was injected s.c., 90 min after the following 4 oral treatments given in random order at weekly intervals: placebo, 100, 200 and 400 mg CM 57755. Gastric contents were collected over 15-min periods during the 2 h after pentagastrin stimulation. In a second, similar study, 8 subjects received placebo, 0.5 and 1.0 g CM 57755 and 800 mg cimetidine, 120 min before a 2 h i.v. infusion of 6 micrograms.kg-1.h-1 pentagastrin. Cumulative gastric secretion in placebo-treated subjects was 46 +/- 14 and 62 +/- 11 mmol H+.2 h-1 (mean +/- SD), respectively, in the first and second studies. It was significantly reduced only after 400 mg CM 57755 in the first study. In the second study either dose of CM 57755 and cimetidine caused a significant reduction in gastric acid secretion. Average plasma levels of ramixotidine were dose-related after 0.2 and 1.0 g and ranged from 0.3 and 1.6 micrograms/ml, respectively, at 60 min to 0.5 and 3.7 micrograms/ml at 180 min. The peak cimetidine level averaged 3.6 micrograms/ml at 150 min. Individual CM 57755 plasma levels throughout the test period were fairly consistent with the inhibition of cumulative gastric acid secretion scored concurrently in each subject. No subjective side-effects attributable to the treatments were reported, and no abnormal findings were seen in the ECG or in laboratory tests.

journal_name

Eur J Clin Pharmacol

journal_title

European journal of clinical pharmacology

authors

Brassinne A,Dresse A,Basilisco G,Manara L

doi

10.1007/BF00637671

subject

Has Abstract

pub_date

1987-01-01 00:00:00

pages

467-70

issue

eissn

0031-6970

issn

1432-1041

journal_volume

pub_type

临床试验,杂志文章,随机对照试验

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Inhibition of pentagastrin-stimulated gastric acid secretion and plasma levels of the new histamine H2-receptor antagonist ramixotidine dihydrochloride (CM 57755) in human volunteers.