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Ezetimibe

Cholesterol absorption inhibitor · Lipid-lowering therapy

START
10 mg PO once daily (add to statin or as statin-intolerant option)
TYPICAL MAX
10 mg/day (fixed)
STOP IF
Persistent unexplained transaminase elevation (with statin), myopathy, hypersensitivity
WATCH
Lipid response, LFTs if combined with statin, muscle symptoms
CDSCO approvedSchedule HATC C10AX09
Renal dose adjustmenteGFR mL/min/1.73m²
FULLNo dose adjustment at any eGFR90

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours
1.5hONSET1.5hPEAK22h1dDURATION
ONSET
1.5h · absorption (enterohepatic)
PEAK
1.5h · Cmax
22h · plasma t½
DURATION
1d · once-daily
EXCRETION
Glucuronidation; ~78% faecal, ~11% renal
route + CYP
INTERACTIONS
11 major
SEVERE in our sources
PREGNANCY
Avoid (especially with a statin) — discontinue if pregnancy planned/confirmed
FDA category + note
Top interactionssee all 12
  • AmiodaroneSevereTextbookG&G 14e · p736
  • Azole AntifungalsSevereTextbookG&G 14e · p736
  • ErythromycinSevereTextbookKDT 7e · p637
  • Hiv Protease InhibitorSevereTextbookKDT 7e · p637
Available in India

22 branded formulations and 14 fixed-dose combinations. Look up specific brands in the Drugs workspace.

Mechanism

Selectively inhibits intestinal NPC1L1 transporter, blocking absorption of dietary and biliary cholesterol → reduced hepatic cholesterol stores, upregulated LDL receptors and lowered LDL-C; complementary to statins.

Indications

Primary hypercholesterolaemia (with statin or alone if statin-intolerant)Homozygous familial hypercholesterolaemia (adjunct)Homozygous sitosterolaemiaASCVD risk reduction adjunct (with statin, per IMPROVE-IT)

Dosing

Adult
10 mg PO once daily, with or without food (± statin).
Pediatric
≥10 years: 10 mg once daily.
Renal adjustment
No adjustment.
Hepatic adjustment
Mild: no adjustment. Moderate–severe: not recommended (increased exposure).
Geriatric
No adjustment.
Max dose
10 mg/day (fixed)

Pharmacokinetics

Onset
LDL reduction over ~2 weeks
Peak effect
Cmax (ezetimibe-glucuronide) ~1–2 h; multiple peaks (enterohepatic)
Duration
Once daily
Half-life
~22 h (ezetimibe + active glucuronide)
Bioavailability
Variable; acts at gut lumen
Protein binding
>90%
Metabolism
Intestinal/hepatic glucuronidation (active glucuronide); enterohepatic recirculation
Excretion
Faecal (~78%) and renal (~11%)

Contraindications

  • Active liver disease / unexplained persistent transaminase elevation (when combined with a statin)
  • Hypersensitivity to ezetimibe
  • Pregnancy/breastfeeding when combined with a statin

Side effects

Common
DiarrhoeaArthralgiaUpper respiratory infectionFatigue
Serious
  • Myopathy/rhabdomyolysis (mainly with statin)
  • Hepatotoxicity (with statin — transaminase rise)
  • Pancreatitis; cholelithiasis
  • Hypersensitivity (angioedema, rash)

Pregnancy & lactation

Pregnancy

Avoid (especially with a statin) — discontinue if pregnancy planned/confirmed

Lactation

Avoid (excreted in animal milk)

Drug interactions

Amiodarone
Severe
Textbook

Increased plasma concentrations of statins and their active metabolites, leading to an increased risk of myopathy and rhabdomyolysis.

Consider using pravastatin, fluvastatin, or rosuvastatin, as they are not extensively metabolized by CYP3A4. Carefully weigh the benefits against the risk of myopathy.

Source: G&G 14e · p736

Azole Antifungals
Severe
Textbook

Increased plasma concentrations of statins and their active metabolites, leading to an increased risk of myopathy and rhabdomyolysis.

Consider using pravastatin, fluvastatin, or rosuvastatin, as they are not extensively metabolized by CYP3A4. Carefully weigh the benefits against the risk of myopathy.

Source: G&G 14e · p736

Erythromycin
Severe
Textbook

Increased risk of myopathy and rhabdomyolysis.

Concomitant use should be avoided or used with extreme caution, especially for statins metabolized by CYP3A4. Dose reduction of the statin and vigilant monitoring for muscle symptoms are necessary.

Source: KDT 7e · p637

Hiv Protease Inhibitor
Severe
Textbook

Increased risk of myopathy and rhabdomyolysis.

Concomitant use should be avoided or used with extreme caution, especially for statins metabolized by CYP3A4. Dose reduction of the statin and vigilant monitoring for muscle symptoms are necessary.

Source: KDT 7e · p637

Hiv Protease Inhibitors
Severe
Textbook

Increased plasma concentrations of statins and their active metabolites, leading to an increased risk of myopathy and rhabdomyolysis.

Consider using pravastatin, fluvastatin, or rosuvastatin, as they are not extensively metabolized by CYP3A4. Carefully weigh the benefits against the risk of myopathy. For simvastatin, coadministration is contraindicated.

Source: G&G 14e · p736

Ketoconazole
Severe
Textbook

Increased risk of myopathy and rhabdomyolysis.

Concomitant use should be avoided or used with extreme caution, especially for statins metabolized by CYP3A4. Dose reduction of the statin and vigilant monitoring for muscle symptoms are necessary.

Source: KDT 7e · p637

Macrolide Antibiotics
Severe
Textbook

Increased plasma concentrations of statins and their active metabolites, leading to an increased risk of myopathy and rhabdomyolysis.

Consider using pravastatin, fluvastatin, or rosuvastatin, as they are not extensively metabolized by CYP3A4. Carefully weigh the benefits against the risk of myopathy. For simvastatin, coadministration is contraindicated.

Source: G&G 14e · p736

Nefazodone
Severe
Textbook

Increased plasma concentrations of statins and their active metabolites, leading to an increased risk of myopathy and rhabdomyolysis.

Consider using pravastatin, fluvastatin, or rosuvastatin, as they are not extensively metabolized by CYP3A4. Carefully weigh the benefits against the risk of myopathy.

Source: G&G 14e · p736

Niacin
Severe
Textbook

Increased risk of myopathy.

Avoid coadministration. The FDA withdrew approval for statin drug combinations containing niacin in 2016.

Source: G&G 14e · p736

Nicotinic Acid
Severe
Textbook

Increased risk of myopathy and rhabdomyolysis.

A lower dose of statin is advisable when nicotinic acid is given concurrently. Close monitoring for muscle symptoms is essential.

Source: KDT 7e · p637, p640

Ciclosporin
Severe
Database

Markedly increased ezetimibe (and ciclosporin) exposure

Monitor ciclosporin levels; use lowest ezetimibe dose, caution

Source: Kimi deep-research + Cla

Bezafibrate
Moderate
Textbook

Reduced risk of rhabdomyolysis compared to other fibrate-statin combinations, but vigilance for myopathy is still advised due to class effect.

This combination is generally considered safer than statin-gemfibrozil, but practitioners should still exercise caution and monitor for muscle symptoms.

Source: KDT 7e · p639

Related guidelines

Ask House about Ezetimibe

Continue into a citation-backed clinical answer with the drug context already attached.

Sources: KD Tripathi 7e, Goodman & Gilman 14e, Harrison 22e, BNF·Verified: 2026-05-19 · House clinical team·Cockpit curated: 2026-05-19