Ezetimibe

Cholesterol absorption inhibitor, Lipid-lowering agent

Ezetimibe

Zetia

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Summary

Classes

Cholesterol absorption inhibitor, Lipid-lowering agent

Pharmacy

Starting dose

10 mg PO once daily, with or without food

Preparations

10 mg tablet; also as fixed-dose combinations with simvastatin (Vytorin) and atorvastatin (Liptruzet, withdrawn US 2015 but generics exist)

US FDA Max

10 mg/d

Pharmacology

Routes

Oral

Onset

LDL lowering within 2 weeks

Duration

24 hours

Half-life

~22 hours (parent + active glucuronide)

Bioavailability

Variable (oral; rapidly conjugated to active glucuronide; food does not affect)

Pregnancy

Limited data; generally avoided particularly in combination with statin.^{[citation needed]}

Legal status

Rx-only in US

Purported mechanism

Ezetimibe binds the Niemann-Pick C1-like 1 (NPC1L1) transporter on the apical brush border of small-intestinal enterocytes, blocking the absorption of cholesterol (both dietary and biliary) without inhibiting absorption of triglycerides, fatty acids, bile acids, or fat-soluble vitamins.▲0▼ Reduced enterohepatic cholesterol delivery raises LDL receptor expression and lowers circulating LDL ~15-20% on top of statin. The IMPROVE-IT trial (2015) established that ezetimibe added to simvastatin improves post-ACS cardiovascular outcomes, validating the "lower LDL = better" hypothesis with a non-statin agent.