Statins · Cardiovascular
Ezetimibe
Ezetrol® · Zetia®(brand names vary by market)
The add-on that blocks absorption rather than synthesis.
Mechanism
Inhibits the NPC1L1 sterol transporter in the small intestine, cutting cholesterol absorption. Because statins increase absorption as they cut synthesis, the two are genuinely complementary.
Indications
- Hypercholesterolemia, usually added to a statin
- Statin intolerance, as monotherapy
Formulations
Dosing concepts
Add-on
Adds roughly a further 15 to 25 percent LDL reduction on top of a statin, which is usually more than doubling the statin dose would achieve.
Monotherapy
A reasonable option in genuine statin intolerance, though the outcome evidence is weaker than for statins.
Concepts, not prescribing instructions. Practice numbers live in current references and local protocols.
Pharmacokinetics
- Bioavailability
- Variable; extensively glucuronidated in the intestinal wall
- Half-life
- ~22 h
- Elimination
- hepatic: Enterohepatic recirculation keeps it at the site of action
- Protein binding
- >90%
Adverse effects
- Diarrhoeacommon
- MyalgiacommonLess than with statins, and it does not seem to add much when combined.
- Transaminase elevation, mainly in combinationserious
Contraindications & precautions
Contraindications
- Active liver disease when combined with a statin
- Pregnancy in combination
Precautions
- Moderate to severe hepatic impairment
- Concurrent fibrates, which raise gallstone risk
Interactions
Monitoring
Lipid panel
Response · 6 to 12 weeks after adding
Liver enzymes if combined with a statin
Combination raises the rate of elevation
Counselling points
- Once daily, any time.
- Separate it from bile acid sequestrants by several hours.
- It works alongside your statin rather than replacing it.
Clinical pearls
- It is the cleanest demonstration in lipid therapy that lowering LDL by any mechanism lowers events: the outcome trial adding it to a statin is the reason 'lower is better' survived.
References & review
- Ezetimibe product monograph (consult the current version for your market) (monograph)
- Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed. (reference-work)
Last reviewed 2026-08-16 · jurisdiction: global · drug information changes; verify against current references before practice use.