Effect of the bile acid sequestrant colesevelam on the pharmacokinetics of pioglitazone, repaglinide, estrogen estradiol, norethindrone, levothyroxine, and glyburide.


Journal Article

The purpose of this study was to assess effects of colesevelam on the pharmacokinetics of glyburide, levothyroxine, estrogen estradiol (EE), norethindrone (NET), pioglitazone, and repaglinide in healthy volunteers. Six drugs with a potential to interact with colesevelam were studied in open-label, randomized clinical studies. The presence of a drug interaction was concluded if the 90% confidence intervals for the geometric least squares mean ratios of AUC(0-t) (AUC(0-48) for levothyroxine) and C(max) fell outside the no-effect limits of (80.0%, 125.0%). Concomitant administration of colesevelam had no effect on the AUC(0-t) or C(max) of pioglitazone but significantly decreased the AUC(0-t) and C(max) of glyburide, levothyroxine, and EE and the C(max) of repaglinide and NET. AUC(0-t) and C(max) of glyburide and EE, but not repaglinide or NET, were significantly decreased when the drug was given 1 hour before colesevelam. When glyburide, EE, or levothyroxine was given 4 hours before colesevelam, no drug interaction was observed. Although colesevelam has a cleaner drug interaction profile than other bile acid sequestrants, it does interfere with absorption of some drugs. A 4-hour window appears sufficient to eliminate these interactions.

Full Text

Cited Authors

  • Brown, KS; Armstrong, IC; Wang, A; Walker, JR; Noveck, RJ; Swearingen, D; Allison, M; Kissling, JC; Kisicki, J; Salazar, DE

Published Date

  • May 2010

Published In

Volume / Issue

  • 50 / 5

Start / End Page

  • 554 - 565

PubMed ID

  • 19789374

Pubmed Central ID

  • 19789374

Electronic International Standard Serial Number (EISSN)

  • 1552-4604

International Standard Serial Number (ISSN)

  • 0091-2700

Digital Object Identifier (DOI)

  • 10.1177/0091270009349378


  • eng