Ezetimibe
ZETIA
What it isNPC1L1 cholesterol-transporter inhibitor; hyperlipidemia.
Why this oneIt is the usual first add-on to a statin: oral, well tolerated and free of the burden of another statin dose increase.
What limits itLDL lowering is modest alone. Check liver enzymes when combined with a statin; myopathy remains possible but uncommon.
FDA-approved for
- hyperlipidemia (2002)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Primary hyperlipidemia (adjunct to diet; alone or with statin) | Adults | 10 mg QD | 10 mg QD (fixed dose) | 10 mg QD |
| HeFH, in combination with a statin | ≥10 yr | 10 mg QD | 10 mg QD | 10 mg QD |
| HoFH, with a statin/other LDL-C-lowering therapies | Adults & peds ≥10 yr | 10 mg QD | 10 mg QD | 10 mg QD |
| Homozygous familial sitosterolemia (adjunct to diet) | Adults & peds ≥9 yr | 10 mg QD | 10 mg QD | 10 mg QD |
Renal No adjustment needed
Hepatic Not recommended in moderate–severe impairment (Child-Pugh B or C) — unknown effects of increased exposure
Instructions
- With or without food
- Give ≥2 h before or ≥4 h after a bile acid sequestrant
- Missed dose: take ASAP; do not double the next dose
- Assess LDL-C as early as 4 wk after initiation
Contraindications
- When combined with a statin, fenofibrate, or other LDL-C-lowering therapy: contraindicated in patients for whom that partner drug is contraindicated (see its labeling)
Cautions
- Liver enzyme elevations — test as clinically indicated; consider withdrawal if ALT/AST ≥3× ULN persist (transaminase elevations 1.3% with statin vs 0.4% statin alone)
- Myopathy/rhabdomyolysis — most postmarketing cases on concomitant statin or fibrate; discontinue if myopathy suspected
- Combination therapy carries the partner drug's risks — refer to statin/fenofibrate labeling
Adverse reactions
- Monotherapy (≥2%, > placebo): URI, diarrhea, arthralgia, sinusitis, pain in extremity, fatigue, influenza
- With statin: nasopharyngitis, myalgia, URI, arthralgia, diarrhea, back pain
- Postmarketing: hypersensitivity (anaphylaxis, angioedema, rash, urticaria), thrombocytopenia, pancreatitis, hepatitis, cholelithiasis/cholecystitis, elevated CPK, myopathy/rhabdomyolysis, dizziness, paresthesia, depression, headache, erythema multiforme
Pregnancy Insufficient human data; no adverse developmental effects in rats/rabbits at up to 10–150× human exposure; use only if potential benefit justifies fetal risk (with a statin, follow statin labeling)
Lactation No human milk data (present in rat milk); do not use unless potential benefit justifies risk to the infant
NO BOXED WARNINGS
Principal riskMyopathy when combined with a statin
Cost, est. cash$4–$80/month
Generic entry2015
Classes and tags
Clinical profile
Legacy pregnancy categoryC
Defining liabilityMyopathy/rhabdomyolysis and hepatotoxicity; interaction burden varies by agent.
Mechanism of action: Ezetimibe ballicule
Open Ezetimibe in the interactive console ↗
Memory aids: mascots and interaction avatars
LDL ball being dribbled = lowers “bad cholesterol”
