Document Detail

Mexiletine kinetics in healthy subjects taking cimetidine.
MedLine Citation:
PMID:  4006366     Owner:  NLM     Status:  MEDLINE    
Cimetidine, a commonly used H2-receptor antagonist, was found to interact adversely with many drugs, including class I antiarrhythmics such as lidocaine and quinidine. To test the effect of cimetidine on the kinetics of mexiletine, a class I antiarrhythmic similar to lidocaine, the absorption and disposition of mexiletine were followed in six healthy subjects before and after 1 week of cimetidine, 300 mg by mouth four times a day. Cimetidine did not alter the distribution and elimination of mexiletine, as shown by similar mean kinetics including total body clearance, AUC, and the elimination t1/2 before and after cimetidine treatment. Cimetidine did have a significant effect on mexiletine absorption, as demonstrated by a longer mean absorption t1/2 (from 0.20 +/- 0.14 to 0.61 +/- 0.35 hours), a longer mean time to peak mexiletine concentration (from 1.13 +/- 0.31 to 1.88 +/- 0.83 hours), and decreased mexiletine plasma concentration (from 0.74 +/- 0.19 to 0.59 +/- 0.15 mg/ml). We conclude that cimetidine does not alter the disposition of oral mexiletine in normal subjects.
A Klein; M Sami; K Selinger
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Clinical pharmacology and therapeutics     Volume:  37     ISSN:  0009-9236     ISO Abbreviation:  Clin. Pharmacol. Ther.     Publication Date:  1985 Jun 
Date Detail:
Created Date:  1985-07-31     Completed Date:  1985-07-31     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0372741     Medline TA:  Clin Pharmacol Ther     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  669-73     Citation Subset:  AIM; IM    
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MeSH Terms
Cimetidine / pharmacology*
Drug Interactions
Mexiletine / metabolism*
Propylamines / metabolism*
Time Factors
Reg. No./Substance:
0/Propylamines; 31828-71-4/Mexiletine; 51481-61-9/Cimetidine

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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