Selectively inhibits the intestinal absorption of cholesterol and related phytosterols
Form:
Free Base
REVIEW A drug that lowers plasma cholesterol levels. Ezetimibe localizes at the brush border of the small intestine, where it inhibits the absorption of cholesterol from the intestine. Specifically, it appears to bind to a critical mediator of cholesterol absorption, the Niemann-Pick C1-Like 1 (NPC1L1) protein on the gastrointestinal tract epithelial cells as well as in hepatocytes. In addition to this direct effect, decreased cholesterol absorption leads to an upregulation of LDL-receptors on the surface of cells and an increased LDL-cholesterol uptake into cells, thus decreasing levels of LDL in the blood plasma which contribute to atherosclerosis and cardiovascular events.
REFERENCES
[1]
Sasaki J, Otonari T, Sawayama Y, Hata S, Oshima Y, Saikawa T, Biro S, Kono S; PEAS study investigators (2012). Double-dose pravastatin versus add-on ezetimibe with low-dose pravastatin - effects on LDL cholesterol, cholesterol absorption, and cholesterol synthesis in Japanese patients with hypercholesterolemia (PEAS study). J Atheroscler Thromb. 19(5):485-93. PMID 22659533.
[2]
Patel A, Macwana C, Parmar V, Patel S (2012). Simultaneous determination of atorvastatin calcium, ezetimibe, and fenofibrate in a tablet formulation by HPLC. J AOAC Int. 95(2):419-23. PMID 22649929.
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