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EzetimibeAka: Zetia, Vytorin

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  1. Indications
    1. Hyperlipidemia monotherapy
    2. Hyperlipidemia combination therapy
      1. Adjunct to Statin agents in multi-drug regimen
    3. Homozygous Sitosterolemia
  2. 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
  3. Adverse effects
    1. Minimal adverse effects due to minimal absorption
  4. Efficacy
    1. 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
    2. 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
  5. Preparations
    1. Ezetimibe (Zetia)
    2. Vytorin: Simvastatin (Zocor) combined with ezetimibe (Zetia)
  6. Dosing: Adults and Children over age 10 years
    1. Ezetimibe 10 mg PO qd

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.
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC108606
Englishezetimib, ezetimibe, EZETIMIBE PREPARATION
Spanishezetemibe
Parent ConceptsAntilipidemic Agent (C1516000), Antilipemic Agents (C0003367), Unclassified Ingredients (C1372954), Drug allergen (C1320237), Azetidine derivative (C1562360), Lipid Absorption Inhibitors (C1579266)
SourcesMSH, MTHSPL, NCI, NDFRT, RXNORM, SCTSPA, SNOMEDCT, USPMG, VANDF
Derived from the NIH UMLS (Unified Medical Language System)


Zetia (C1170736)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC108606
EnglishMerck brand of ezetimibe, Schering-Plough brand of ezetimibe, Zetia
SourcesMSH, NCI, RXNORM
Derived from the NIH UMLS (Unified Medical Language System)



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