Ezetimibe Dosage and Efficacy

Dosing Information

The American College of Cardiology recommends a fixed dose of 10 mg of ezetimibe orally once daily, regardless of patient characteristics 1, 2
When used in combination with bile acid sequestrants, ezetimibe should be taken either ≥2 hours before or ≥4 hours after the bile acid sequestrant to avoid reducing ezetimibe's efficacy 1

Ezetimibe inhibits the Niemann-Pick C1-like 1 (NPC1L1) protein in the small intestine, reducing cholesterol absorption 1, 2
As monotherapy, ezetimibe reduces LDL-C by approximately 18% 1
When combined with statin therapy, ezetimibe provides an additional 25% incremental reduction in LDL-C beyond statin therapy alone 1, 3

The American College of Cardiology states that ezetimibe is generally well tolerated with a safety profile similar to placebo 1
Common adverse effects of ezetimibe include upper respiratory tract infection, diarrhea, arthralgia, sinusitis, and pain in extremities 1, 3
Persistent elevations in hepatic transaminases may occur with concomitant statin therapy; monitoring of liver enzymes is recommended based on statin monitoring guidelines 1
Cases of myopathy and rhabdomyolysis have been reported when ezetimibe was used alone or in combination with statin therapy 1

Ezetimibe is preferred as the initial non-statin agent for most patients requiring additional LDL-C lowering beyond statin therapy due to its tolerability, convenience, and single-tablet daily dose 4, 3
Avoid use of ezetimibe during pregnancy as no safety data exists in humans 1

The American College of Cardiology recommends monitoring for interactions with cyclosporine, fibrates, and bile acid sequestrants 1, 3