Inhibits intestinal absorption of cholesterol without affecting the absorption of triglycerides or fat-soluble vitamins.
The most effective and frequently used alternative to statins.
Trade name Zetia.
Not approved to prevent cardiovascular events, and the number of patients needed to treat per year to prevent a cardiovascular event is approximately 350.
A cholesterol absorption inhibitor that reduces LDL-C levels by 18%, which when used alone is unlikely to achieve LDL-C goals and is more commonly used in combination with statins.
Selectively inhibits cholesterol absorption by binding to the Niemann-Pick C1-like 1 (NPC-1L1) protein.
For patient to have LDL-C levels of 70 mg/dL or higher despite maximally tolerated statins should be considered for ezetimibe, which prevents the intestines from absorbing cholesterol.
Niemann-Pick C1-like1 protein is located at the brush border membrane of the enterocyte where it contributes to the uptake and cellular transfer of cholesterols and non cholesterols.
Polymorphisms that effect NPC1L1 are associated with lower LDL cholesterol level and low risk of cardiovascular disease.
Reduces LDL-C by 17% compared to placebo.
It reduces LDL cholesterol absorption in the small intestine, typically decreasing the level by 15 to 20%.
Co-administration with statins increases the effectiveness of either agent alone in reducing LDL-C levels.
When added to statins lowers LDL-cholesterol by an additional 23-24%.
Co-administration with statins improves HDL-C and total cholesterol:HDL-C ratios and improves reduction in CRP levels more than the use of single agents.
Co-administration with statins has the same safety profile as statins alone.
In combination with simvastatin (Vytorin) highly effective in reducing LDL-C through dual inhibition of cholesterol absorption and biosynthesis.
In a double blind randomized trial involving 18,144 patients acute coronary syndrome when added to statin therapy ezetimibe resulted in incremental lowering the LDL cholesterols and improved cardiovascular outcomes (Cannon CP et al).
In combination with simvastatin (Vytorin) in the Simvastatin and Ezetimibe in Aortic Stenosis (SEAS) trial indicated a larger percentage of patients treated with combination of drugs were diagnosed with or died from cancer compared to placebo, during a 5 year study.
In combination with simvastatin (Vytorin) have not shown increased risk of cancer in other large cardiovascular trials.
In combination with simvastatin (Vytorin) better than atorvastatin alone in modifying lipid abnormalities in type 2 diabetes.
Its addition to the highest recommended doses of simvastatin does not reduce the intimal-media thickness of the carotid artery inpatients with familial hypercholesterolemia despite significant reductions in levels of both LDL cholesterol and C-reactive protein.
With simvastatin (Vytorin)-in the ENHANCE trial, a double blinded 24 month trial involving 724 patients with familial hypercholesterolemia randomized to receive daily 80 mg of simvastatin with placebo or 10 mg of Ezetimibe : intima-media thickness of the walls of the carotid and femoral arteries were assessed with ultrasound: no significant changes were noted in the media-intima thickness but the baseline reduction in low-density lipoprotein cholesterol was 56% in the combination group vs. 39% in the simvastatin/placebo group
Mean intimal-media thickness between groups of patients receiving simvastatin alone and simvastatin with ezetimibe did not differ.
The Arterial Biology for the Investigation of the Treatment Effects Reducing Cholesterol 6-HDL and LDL (ARBITER 6-HALTS) study compared either niacin or ezetimibe added to a long-term statin therapy on carotid intima-media thickness over a 14 month period:the use of extended release niacin causes significant regression in the carotid intima-media thickness when combined with a statin and that niacin is superior to ezetimibe.
Combined treatment with this agent and statin provides an incremental reduction in LDL cholesterol levels of 12-19%.
GAUSS-3 trial-year-enrolled patients with elevated LDL levels unable to tolerate effective doses of statins: evolocumab compared with ezetimbe resulted in a significantly greater reduction in LDL-C levels at 24 weeks.