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Lack of effect of colesevelam HCl on the single-dose pharmacokinetics of aspirin, atenolol, enalapril, phenytoin, rosiglitazone, and sitagliptin.
MedLine Citation:
PMID:  24721587     Owner:  NLM     Status:  Publisher    
AIMS: Drug interactions with bile acid sequestrants are primarily due to the potential of these agents to bind to concomitant drugs. Six clinical studies were performed to determine the effects of colesevelam on the pharmacokinetics of aspirin, atenolol, enalapril, phenytoin, rosiglitazone, and sitagliptin.
METHODS: All six studies enrolled healthy subjects aged 18-45 years. The phenytoin study used a single-dose, three-period crossover design (phenytoin alone, phenytoin simultaneously with colesevelam, and phenytoin 4h before colesevelam). The other studies used a two-period crossover design (test drug alone and test drug simultaneously with colesevelam). Colesevelam (3750mg once daily) was dosed throughout the pharmacokinetic sampling period. After each single dose of the test drug, serial blood samples were collected for determination of plasma drug concentrations and calculation of pharmacokinetic parameters.
RESULTS: For all six test drugs, 90% CIs for geometric least-squares mean ratios of AUC and Cmax for the measured analytes were within specified limits, indicating no interaction between the test drug and colesevelam.
CONCLUSIONS: Aspirin, atenolol, enalapril, rosiglitazone, and sitagliptin may be taken with colesevelam. Although the phenytoin study indicated no pharmacokinetic interaction, phenytoin should continue to be taken ≥4h before colesevelam in accordance with current prescribing information.
Ling He; Prachi Wickremasingha; James Lee; Ben Tao; Jeanne Mendell-Harary; Joseph Walker; Douglas Wight
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2014-1-14
Journal Detail:
Title:  Diabetes research and clinical practice     Volume:  -     ISSN:  1872-8227     ISO Abbreviation:  Diabetes Res. Clin. Pract.     Publication Date:  2014 Jan 
Date Detail:
Created Date:  2014-4-11     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8508335     Medline TA:  Diabetes Res Clin Pract     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2014 Elsevier Ireland Ltd. All rights reserved.
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