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Simeon Margolis, M.D.and Paul A. Pham, Pharm.D.
01-08-2010
- Reduce total and LDL cholesterol to prevent cardiovascular disease or events
- Ezetimibe selectively inhibits absorption of cholesterol and related phytosterols in the small intestine.
- 10 mg daily with or without food
- Can be used as monotherapy, but is usually added to a statin.
brand name
| generic
| Mfg
| brand forms
| cost*
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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.
- Not recommended in patients with moderate to severe hepatic impairment.
- Not recommended unless the potential benefit justifies the possible risk to the fetus.
- No significant adverse drug reactions unless ezetimibe is taken with a statin.
- Generally well tolerated with ADR comparable to placebo.
- 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.
- 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.
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