Ezetimibe, Zetia, Vytorin, Liptruzet

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