Ezetimibe
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| Pronunciation | /ɛˈzɛtᵻmɪb, -maɪb/ |
| Trade names | Zetia, Ezetrol |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a603015 |
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| Routes of administration |
By mouth (tablets) |
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| Pharmacokinetic data | |
| Bioavailability | 35–65% |
| Protein binding | >90% |
| Metabolism | Intestinal wall, liver |
| Biological half-life | 19–30 hours |
| Excretion | Renal 11%, faecal 78% |
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| ECHA InfoCard | 100.207.996 |
| Chemical and physical data | |
| Formula | C24H21F2NO3 |
| Molar mass | 409.4 g·mol−1 |
| 3D model (Jmol) | |
| Melting point | 164 to 166 °C (327 to 331 °F) |
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Ezetimibe is a drug that lowers plasma cholesterol levels. It acts by decreasing cholesterol absorption in the small intestine. It may be used alone (marketed as Zetia or Ezetrol), when other cholesterol-lowering medications are not tolerated, or together with statins (e.g., ezetimibe/simvastatin, marketed as Vytorin or Inegy) when statins alone do not control cholesterol.
Ezetimibe is recommended as second line therapy for those intolerant of statins or unable to achieve target LDL cholesterol levels on statins alone by several major medical group practice guidelines, but not by those of the American Heart Association and American College of Cardiology. In the United States as of 2015 the 10 mg pill costs between 4.84 and 7.88 USD.
As of mid-2014, treatment guidelines of the American Heart Association/American College of Cardiology recommend that people with dyslipidemia be treated with a statin. These guidelines recommend increasing the statin dose in certain populations, but do not recognize target serum cholesterol levels or recommend the use of non-statin cholesterol lowering drugs. Guidelines issued by the European Society of Cardiology/European Atherosclerosis Society, the Japan Atherosclerosis Society, the National Institute for Health and Clinical Excellence, and the International Atherosclerosis Society recommend ezetimibe as one of several second line treatment options for people who are intolerant of statins or who are unable to reach serum LDL goals using statins alone.
While ezetimibe reduces LDL cholesterol, it has not been shown to affect outcomes such as risk of death or major cardiovascular event like heart attack or stroke. Its effectiveness in reducing atherosclerosis in clinical trials has been inconsistent. The question of whether ezetimibe could make a difference in major outcomes was examined in the IMPROVE-IT trial, which compared treatment with ezetimibe vs. placebo on top of a background regimen of statin therapy in people who have had recent episodes of acute coronary syndrome over a six-year period. The trial results showing that ezetimibe treatment lowered the risk of experiencing a vascular event by 2%.
Ezetimibe is indicated in the United States as an add-on to dietary measures to:
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