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Inhibition of Tolbutamide Elimination by Cimetidine but not Ranitidine
Author(s) -
Cate Emily W.,
Rogers John F.,
Powell J. Robert
Publication year - 1986
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1002/j.1552-4604.1986.tb03540.x
Subject(s) - tolbutamide , cimetidine , ranitidine , pharmacokinetics , histamine h2 receptor , pharmacology , placebo , crossover study , drug interaction , medicine , chemistry , endocrinology , antagonist , diabetes mellitus , receptor , alternative medicine , pathology
This study was designed to compare the effects of equivalent therapeutic doses of two H 2 antagonists, cimetidine and ranitidine, on tolbutamide pharmacokinetics. Twelve healthy men were given a 1‐g oral dose of tolbutamide on three occasions. Subjects were randomly assigned to three treatments in a crossover fashion: cimetidine 1,200 mg/d, ranitidine 300 mg/d, and placebo. Cimetidine significantly increased the tolbutamide area under the plasma concentration‐time curve by 20% (range, −5% to 42%), increased the elimination half‐life by 17%, and decreased the carboxytolbutamide:tolbutamide plasma ratio from 0.042 to 0.036. Ranitidine did not significantly alter tolbutamide pharmacokinetics.