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Medications> Dyslipidemia>
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Ezetimibe

Simeon Margolis, M.D.and Paul A. Pham, Pharm.D.
01-08-2010

INDICATIONS

FDA

  • Reduce total and LDL cholesterol to prevent cardiovascular disease or events

MECHANISM

  • Ezetimibe selectively inhibits absorption of cholesterol and related phytosterols in the small intestine.

USUAL ADULT DOSING

  • 10 mg daily with or without food 
  • Can be used as monotherapy, but is usually added to a statin.

FORMS

brand 
name
 
generic 
Mfg 
brand 
forms
 
cost* 
Zetia Ezetamibe Merck & Co Inc. oral
tab
10 mg
$4.03

*Prices represent cost per unit specified and are representative of "Average Wholesale Price" (AWP). AWP Prices were obtained and gathered by Lakshmi Vasist Pharm D using the Red Book, manufacturer's information, and the McKesson database.

^Dosage is indicated in mg unless otherwise noted.

DOSING IN SPECIAL POPULATIONS

HEPATIC

  • Not recommended in patients with moderate to severe hepatic impairment.
PREGNANCY

  • Category C.
BREASTFEEDING

  • Not recommended unless the potential benefit justifies the possible risk to the fetus.

ADVERSE DRUG REACTIONS

GENERAL

  • No significant adverse drug reactions unless ezetimibe is taken with a statin.
  • Generally well tolerated with ADR comparable to placebo.
RARE

  • Arthalgias
  • Dizziness

DRUG INTERACTIONS

  • Cyclosporine: cyclosporine and ezetamibe concentration may be increased. Cyclosporine AUC was increased by 15%. Monitor cyclosporine concentrations closely with co-administration.
  • Fibrates: fenofibrate and gemfibrozil increased total ezetimibe concentrations by approx. 50% or 70%, respectively. Limited data on the co-administration; use with close monitoring for potential increased risk of cholelithiasis.
  • Cholestyramine and other bile acid sequestrants: ezetamibe serum concentrations (AUC) decreased by 55%. Administered ezetamibe at least 2 hours before or 4 hours after bile acid sequestrant.
  • Coumarin anticoagulants: case report of increased INR. Monitor INR closely with ezetamibe co-administration.
  • When combined with a statin, adverse effects and contraindications are the same as for the statin.

PHARMACOKINETIC

COMMENTS

  • The addition of ezetamibe to a statin can decrease LDL cholesterol by an additional ~15%; however, regression of carotid artery intima/media thickness in patients with type 2 diabetes is not affected. (Fleg)
  • Since ezetamibe is very well tolerated, it is reasonable to add ezetimibe in patients who fail to meet their LDL cholesterol targets despite maximal use of statins. (Brown)
  • Ezetimibe does not inhibit absorption of triglycerides, fat soluble vitamins, ethinyestradiol or progesterone. (van Heek)
  • Ezetimibe inhibits the absorption of plant sterols like sitosterol and campesterol and is useful in treatment of sitosterolemia.

REFERENCES


 
 
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