II. Indications
- Hyperlipidemia monotherapy
-
Hyperlipidemia combination therapy
- Adjunct to Statin agents in multi-drug regimen
- Homozygous Sitosterolemia
III. 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
IV. Adverse effects
- Minimal adverse effects due to minimal absorption
- Provokes Statin-related myalgias and Arthralgias
V. 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
VI. Preparations
- Ezetimibe (Zetia)
- Vytorin: Simvastatin (Zocor) combined with Ezetimibe (Zetia)
- Liptruzet: Atorvastatin (Lipitor) combined with Ezetimibe (Zetia)
VII. Dosing: Adults and Children over age 10 years
- Ezetimibe 10 mg PO qd
VIII. Contraindications
- Active liver disease (when used in combination with a Statin)
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| 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 |
