II. Indications

  1. Hyperlipidemia monotherapy
  2. Hyperlipidemia combination therapy
    1. Adjunct to Statin agents in multi-drug regimen
  3. Homozygous Sitosterolemia

III. Mechanism: Cholesterol absorption inhibitor

  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

IV. Adverse effects

  1. Minimal adverse effects due to minimal absorption
  2. Provokes Statin-related myalgias and Arthralgias

V. 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

VI. Preparations

  1. Ezetimibe (Zetia)
  2. Vytorin: Simvastatin (Zocor) combined with Ezetimibe (Zetia)
  3. Liptruzet: Atorvastatin (Lipitor) combined with Ezetimibe (Zetia)

VII. Dosing: Adults and Children over age 10 years

  1. Ezetimibe 10 mg PO qd

VIII. Contraindications

  1. Active liver disease (when used in combination with a Statin)

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Related Studies

Cost: Medications

ezetimibe (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
EZETIMIBE 10 MG TABLET Generic $6.84 each
zetia (on 3/22/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
ZETIA 10 MG TABLET Generic $6.84 each
vytorin (on 2/22/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
VYTORIN 10-10 MG TABLET $9.98 each
VYTORIN 10-20 MG TABLET $9.97 each
VYTORIN 10-40 MG TABLET $9.96 each
VYTORIN 10-80 MG TABLET $9.91 each

Ontology: ezetimibe (C1142985)

Definition (NCI) An azetidinone derivative and a cholesterol absorption inhibitor with lipid-lowering activity. Ezetimibe appears to interact physically with cholesterol transporters at the brush border of the small intestine and inhibits the intestinal absorption of cholesterol and related phytosterols. As a result, ezetimibe causes a decrease in the level of blood cholesterol or an increase in the clearance of cholesterol from the bloodstream. Overall, the following effects observed are a reduction of hepatic cholesterol stores and a reduction of total cholesterol, LDL cholesterol, and other triglycerides in the blood.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C108606
SnomedCT 408041006, 409149001
LNC LP171397-5
English 1-(4-fluorophenyl)-3(R)-[3-(4-fluorophenyl)-3(S)-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone, ezetimibe (medication), EZETIMIBE, ezetimibe [Chemical/Ingredient], (1-(4-fluorophenyl)-(3R)-(3-(4-fluorophenyl)-(3S)-hydroxypropyl)-(4S)-(4-hydroxyphenyl)-2-azetidinone), ezetimibe, ezetimib, Ezetimibe, Ezetimibe (product), Ezetimibe (substance)
Spanish ezetemibe (producto), ezetimibe (producto), ezetimibe (sustancia), ezetemibe, ezetemibe (sustancia), ezetimibe

Ontology: Zetia (C1170736)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C108606
English Zetia, zetia, Merck brand of ezetimibe, Schering-Plough brand of ezetimibe