Inhibition of Tolbutamide Elimination by Cimetidine but not Ranitidine

This study was designed to compare the effects of equivalent therapeutic doses of two H2 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...

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Veröffentlicht in:Journal of clinical pharmacology 1986-05, Vol.26 (5), p.372-377
Hauptverfasser: Cate, Emily W., Rogers, John F., Powell, J. Robert
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container_title Journal of clinical pharmacology
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creator Cate, Emily W.
Rogers, John F.
Powell, J. Robert
description This study was designed to compare the effects of equivalent therapeutic doses of two H2 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.
doi_str_mv 10.1002/j.1552-4604.1986.tb03540.x
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Robert</creatorcontrib><title>Inhibition of Tolbutamide Elimination by Cimetidine but not Ranitidine</title><title>Journal of clinical pharmacology</title><addtitle>J Clin Pharmacol</addtitle><description>This study was designed to compare the effects of equivalent therapeutic doses of two H2 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. 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Robert</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4380-381b2a260bf426f7db46eccdcbd7a1e650d0b74e153b930e9daf16018f2073fb3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1986</creationdate><topic>Adult</topic><topic>Biological and medical sciences</topic><topic>Blood Glucose - analysis</topic><topic>Chromatography, High Pressure Liquid</topic><topic>Cimetidine - pharmacology</topic><topic>Double-Blind Method</topic><topic>Half-Life</topic><topic>Histamine and antagonists. Allergy</topic><topic>Humans</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Pharmacology. 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source MEDLINE; Wiley Online Library Journals Frontfile Complete
subjects Adult
Biological and medical sciences
Blood Glucose - analysis
Chromatography, High Pressure Liquid
Cimetidine - pharmacology
Double-Blind Method
Half-Life
Histamine and antagonists. Allergy
Humans
Male
Medical sciences
Pharmacology. Drug treatments
Ranitidine - pharmacology
Tolbutamide - analogs & derivatives
Tolbutamide - blood
Tolbutamide - metabolism
title Inhibition of Tolbutamide Elimination by Cimetidine but not Ranitidine
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