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Ezetimibe

Aka: Ezetimibe, Zetia, Vytorin
  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
    2. Provokes Statin-related myalgias and arthralgias
  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 358:1431-43
    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 90:1092-7
    3. 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
  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
  7. Contraindications
    1. Active liver disease (when used in combination with a Statin)

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 Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C108606
SnomedCT 408041006, 409149001
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
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Zetia (C1170736)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C108606
English Zetia, zetia, Merck brand of ezetimibe, Schering-Plough brand of ezetimibe
Sources
Derived from the NIH UMLS (Unified Medical Language System)


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