Pharmacokinetic interaction between ezetimibe and lovastatin in healthy volunteers

Current Medical Research and Opinion
Larisa ReydermanPaul Statkevich

Abstract

Ezetimibe (Zetia) is a novel inhibitor of intestinal absorption of cholesterol that is approved for the treatment of primary hypercholesterolemia. In a separate pilot study, co-administration of ezetimibe and lovastatin resulted in a significant pharmacodynamic interaction, leading to an additive reduction in LDL-C. The current study was designed to further investigate the potential for pharmacokinetic interaction between ezetimibe and lovastatin. This was a randomized, open-label, 3-way crossover study in 18 healthy adult volunteers. All subjects received the following treatments orally once daily for 7 days: ezetimibe 10 mg, lovastatin 20 mg, or ezetimibe 10 mg plus lovastatin 20 mg. Plasma samples obtained on day 7 were evaluated for steady-state pharmacokinetics of ezetimibe (unconjugated), total ezetimibe (ezetimibe and ezetimibe-glucuronide conjugate), lovastatin, and beta-hydroxylovastatin. Co-administration of ezetimibe with lovastatin did not affect the pharmacokinetics of ezetimibe. There were no significant differences in the exposure to total ezetimibe, ezetimibe-glucuronide and ezetimibe after co-administration with lovastatin vs. ezetimibe given alone. Co-administration of ezetimibe with lovastatin had no signific...Continue Reading

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Citations

Aug 9, 2005·Current Medical Research and Opinion·Larisa ReydermanPaul Statkevich
Feb 24, 2012·Pharmacological Reports : PR·Dariusz SuchyBogusław Okopień
Jan 12, 2010·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Chih-Chieh ChenJia-You Fang
Nov 16, 2006·Expert Opinion on Therapeutic Targets·Irene F Gazi, Dimitri P Mikhailidis
May 6, 2005·Clinical Pharmacokinetics·Teddy KosoglouKevin B Alton

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