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Ezetimibe

Statinprescriptionoral · inferred

Selective inhibitor of intestinal cholesterol absorption via NPC1L1, lowering LDL-C ~15-20% as monotherapy and additively with statins. Undergoes enterohepatic recirculation producing a long effective half-life of ~22 hours. Standard dose 10 mg once daily. IMPROVE-IT established CV event reduction when added to statin therapy post-ACS.

Projected serum levels — 10 mg, once daily

Ezetimibe
Ezetimibe modeled serum levels, 10 mg once daily over 15 days Population-based pharmacokinetic estimate. Steady state reached after approximately 2 days. 0 2.5 5 7.5 10 Day 0 Day 4 Day 8 Day 11 Day 15 Time on a regular schedule ≈ steady state · day 2
Ezetimibe modeled serum levels with a loading dose of 18.5 mg, then 10 mg once daily The first dose is larger so levels approach steady state faster. 0 2.5 5 7.5 10 Day 0 Day 4 Day 8 Day 11 Day 15 Time on a regular schedule

Maintenance schedule: 10 mg once daily (oral).

Loading schedule: 18.5 mg on day 1, then 10 mg once daily — reaching therapeutic levels sooner.

Modeled steady state after ~2 days: peak ≈ 6.2 mg, trough ≈ 3.0 mg body load. Population-based estimate over 15 days for a 10 mg dose at a 70 kg reference body mass — the interactive app scales curves to your doses, timing, and body mass.

Key facts

Category
Statin
Route modeled
Oral
Model confidence
inferred
Half-life
22 h
Common dose
10 mg
Suggested maximum
10 mg/day
Reference dose range
5–10 mg (single dose)
Suggested cadence
once daily
Validated against
10 mg oral — Cmax 0.004 mg/L at 1.5 h

Documented interactions

  • moderate
    Efavirenz (Sustiva) + Ezetimibe CYP induction

    Efavirenz (Sustiva) inducer of UGT1A1 predicted to change Ezetimibe AUC by ~0.68x

  • moderate
    Entacapone (Comtan) + Ezetimibe Transporter inhibition

    Entacapone (Comtan) inhibitor of OATP1B1 may alter Ezetimibe absorption / distribution

  • moderate
    Glecaprevir + Ezetimibe CYP inhibition

    Glecaprevir reversible_inhibitor of UGT1A1 predicted to change Ezetimibe AUC by ~1.50x

  • moderate
    Green Tea Extract (Camellia sinensis) + Ezetimibe Transporter inhibition

    Green Tea Extract (Camellia sinensis) inhibitor of OATP1B1 may alter Ezetimibe absorption / distribution

  • moderate
    Phenobarbital + Ezetimibe CYP induction

    Phenobarbital inducer of UGT1A1 predicted to change Ezetimibe AUC by ~0.58x

  • moderate
    Pibrentasvir + Ezetimibe Transporter inhibition

    Pibrentasvir inhibitor of OATP1B1 may alter Ezetimibe absorption / distribution

Serum checks 12 modeled interaction pairings for ezetimibe across your whole stack — absorption conflicts, enzyme inhibition, and nutrient depletion included.

Research behind this entry

  1. Ezetimibe Added to Statin Therapy after Acute Coronary Syndromes Cannon CP et al. (IMPROVE-IT Investigators) · New England Journal of Medicine, 2015 DOI

    IMPROVE-IT RCT of 18144 post-ACS patients showed simvastatin plus ezetimibe reduced composite CV events by 6.4% vs simvastatin alone over 6 years, validating the LDL-C hypothesis below 70 mg/dL.

  2. Intensive lipid lowering with simvastatin and ezetimibe in aortic stenosis (SEAS) Rossebo AB et al. · New England Journal of Medicine, 2008 DOI

    SEAS RCT in 1873 patients with mild-moderate aortic stenosis found simvastatin+ezetimibe did not slow stenosis progression but reduced ischemic CV events by 22%.

  3. Clinical pharmacokinetics of ezetimibe Kosoglou T et al. · Clinical Pharmacokinetics, 2005 DOI

    PK review characterizing ezetimibe's rapid glucuronidation to the active ezetimibe-glucuronide, enterohepatic recirculation, and 22-hour effective half-life supporting once-daily dosing.

3 published studies referenced in the app, each with a plain-language summary.