Recommended Dose of Ezetimibe

The recommended dose of ezetimibe is 10 mg orally once daily, with or without food. 1, 2

Dosing Information

Ezetimibe is administered at a fixed dose of 10 mg orally once daily, regardless of patient characteristics 1
The medication can be taken with or without food, as concomitant food administration does not significantly affect the extent of absorption 2, 3
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, 3
The 10 mg daily dose is effective as a single daily dose due to ezetimibe's long half-life of approximately 22 hours 2, 4

Ezetimibe inhibits the Niemann-Pick C1-like 1 (NPC1L1) protein in the small intestine, reducing cholesterol absorption 1
As monotherapy, ezetimibe reduces LDL-C by approximately 18% 1, 4
When combined with statin therapy, ezetimibe provides an additional 25% incremental reduction in LDL-C beyond statin therapy alone 1, 5
The maximum effect of ezetimibe is typically observed within 2 weeks of initiating therapy 6

No dose adjustment is necessary based on age, sex, or race 2, 3
No dose adjustment is required in patients with mild hepatic impairment or mild-to-severe renal insufficiency 2, 3
Ezetimibe is not recommended in patients with moderate or severe hepatic impairment due to unknown effects of increased exposure 2

Ezetimibe is generally well tolerated with a safety profile similar to placebo 1, 6
Common adverse effects include upper respiratory tract infection, diarrhea, arthralgia, sinusitis, and pain in extremities 1, 5
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

Higher doses of ezetimibe (20 mg daily) have been studied and may provide additional LDL-C lowering in patients on concomitant statin therapy (approximately 10% further reduction), but this is not an FDA-approved dosage 7
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 1, 5
Ezetimibe has a favorable drug-drug interaction profile, with minimal interactions with commonly used medications 3
Avoid use during pregnancy as no safety data exists in humans 1

Monitor for interactions with cyclosporine, fibrates, and bile acid sequestrants 1, 5
Ezetimibe does not significantly affect drugs metabolized by cytochrome P450 enzymes 2, 3
Colestyramine significantly decreases ezetimibe bioavailability, so these medications should be administered several hours apart 3