This drug is indicated for hyperlipidemia, which refers to abnormally high levels of lipids or lipoproteins in the blood.
Ezetimibe is a cholesterol absorption blocker that targets Niemann-Pick C1-Like 1 (NPC1L1), a sterol transporter, resulting in decreased uptake of cholesterol at the brush border of the small intestine. They are especially effective when combined with statins, another class of drugs used to treat hyperlipidemia.
Ezetimibe decreases cholesterol absorption, which leads to LDL receptor upregulation. This results in increased uptake of LDL into cells and decreased levels in the blood.
A side effect of ezetimibe is diarrhea, as inhibition of cholesterol absorption keeps cholesterol in the intestinal lumen to be excreted.
Patients taking ezetimibe are cautioned to monitor liver function tests (LFT), although increased LFT values is a very rare side effect.
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