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Ezetimibe
Aka: Ezetimibe, Zetia, Vytorin, Liptruzet
- Indications
- Hyperlipidemia monotherapy
- Hyperlipidemia combination therapy
- Adjunct to Statin agents in multi-drug regimen
- Homozygous Sitosterolemia
- Mechanism: Cholesterol absorption inhibitor
- Class: 2-Azetidinone
- Blocks Cholesterol absorption from diet and bile acids
- Selective Cholesterol absorption inhibitor
- Inhibits absorption at Small Intestine brush border
- Adverse effects
- Minimal adverse effects due to minimal absorption
- Provokes Statin-related myalgias and Arthralgias
- Efficacy
- IMPROVE-IT Trial
- NNT 50 for one less CV event in high risk patients taking Vytorin (10/40) instead of Simvastatin alone for 7 years
- (2015) Presc Lett 22(1): 2
- Enhance Study
- Found that Vytorin is not more effective than Simvastatin alone
- Despite LDL lowering, did not further slow atherosclerosis
- Casts doubt on Ezetimibe (Zetia) benefit, but further trials are needed
- Kastelein (2008) N Engl J Med 358:1431-43 [PubMed]
- Initial Data
- Triglyceride levels did not change significantly
- LDL Cholesterol reduced 17%
- HDL Cholesterol increased 1.3%
- Dujovne (2002) Am J Cardiol 90:1092-7 [PubMed]
- Postulated reason for lack of effect in coronary event prevention despite LDL lowering
- Scavenger Receptor B1 inhibition appears to be the mechanism for this lack of effect
- This inhibition results in HDL inhibition
- Preparations
- Ezetimibe (Zetia)
- Vytorin: Simvastatin (Zocor) combined with Ezetimibe (Zetia)
- Liptruzet: Atorvastatin (Lipitor) combined with Ezetimibe (Zetia)
- Dosing: Adults and Children over age 10 years
- Ezetimibe 10 mg PO qd
- Contraindications
- Active liver disease (when used in combination with a Statin)