Ezetimibe: A Selective Cholesterol Absorption Inhibitor

Medication Overview

The American College of Cardiology recommends ezetimibe as a selective cholesterol absorption inhibitor that works by blocking the Niemann-Pick C1-Like 1 (NPC1L1) protein in the small intestine, thereby reducing intestinal cholesterol absorption 1
The standard dosing of ezetimibe is 10 mg orally once daily, with or without food, as recommended by the American College of Cardiology 1

The American College of Cardiology recommends ezetimibe for the treatment of primary hyperlipidemia, mixed hyperlipidemia, and homozygous familial hypercholesterolemia (HoFH) when combined with atorvastatin or simvastatin 1, 2, 3
The American College of Cardiology also recommends ezetimibe for the treatment of homozygous sitosterolemia (phytosterolemia) 2

The IMPROVE-IT trial demonstrated that ezetimibe, when added to moderate-intensity statin therapy in post-acute coronary syndrome patients, reduced the composite endpoint of cardiovascular death, nonfatal MI, unstable angina requiring hospitalization, coronary revascularization, or nonfatal stroke over 6 years median follow-up, as reported by the American College of Cardiology 1
The SHARP trial showed that simvastatin plus ezetimibe reduced major atherosclerotic cardiovascular disease events in patients with chronic kidney disease over 4.9 years median follow-up, as reported by the American College of Cardiology 4

The American College of Cardiology reports that ezetimibe is generally well tolerated, with common adverse effects including upper respiratory tract infection, diarrhea, arthralgia, sinusitis, and pain in extremities 1, 2
The American College of Cardiology also reports that ezetimibe is contraindicated in patients with hypersensitivity to ezetimibe and recommends monitoring hepatic transaminases when used with statins 1

The American College of Cardiology notes that ezetimibe is available as a generic medication, making it a cost-effective option for LDL-cholesterol lowering 1, 4, 5
The Trends in Cardiovascular Medicine journal reports that the generic availability of ezetimibe is a reason to favor it as the first-line nonstatin agent before considering more expensive PCSK9 inhibitors in very high-risk patients 4