ezetimibe: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
ezetimibe: clinical details
Prescribing considerations
- Continue appropriate dietary measures.
- Review the accompanying statin's product information during combination therapy.
- Paediatric initiation should be under specialist review; evidence is limited.
- Ezetimibe is not recommended in moderate or severe hepatic impairment.
- Consider gallbladder risk when co-prescribing fenofibrate.
Contraindications and cautions
- Hypersensitivity to ezetimibe or a formulation excipient.
- When combined with a statin: pregnancy or breastfeeding.
- When combined with a statin: active liver disease or unexplained persistent serum-transaminase elevation.
- The selected lactose-containing product should not be used in specified rare hereditary disorders of galactose handling.
Monitoring
- Assess lipid response and adherence to treatment and dietary measures.
- With a statin, check liver function at initiation and subsequently as required by the statin's product information.
- Investigate unexplained muscle symptoms and measure creatine kinase when myopathy is suspected.
- Monitor INR with warfarin, another coumarin or fluindione.
- Monitor ciclosporin concentrations during combined treatment.
- Investigate possible gallstones or gallbladder disease with fenofibrate.
Clinical pharmacology
Ezetimibe and its active glucuronide inhibit intestinal NPC1L1-mediated sterol uptake. Ezetimibe undergoes glucuronidation and enterohepatic recycling, with minimal oxidative cytochrome P450 metabolism.
Formulation and product differences
- The selected product is a white to off-white, capsule-shaped, uncoated tablet.
- It contains lactose monohydrate and is essentially sodium-free.
- Keep it protected from moisture in its original blister or tightly closed bottle.
- Appearance and excipients can differ between manufacturers; check the supplied product information when relevant.
ezetimibe preparations and strengths
Tablet
Route: Oral
Strengths: 10 mg
ezetimibe interactions
Tell your prescriber or pharmacist about all medicines and supplements. Important interactions include:
Bile-acid sequestrants, such as colestyramine
They reduce ezetimibe exposure and may lessen its effect, so administration must be separated.
Ciclosporin
Ezetimibe exposure may rise and ciclosporin concentrations can change; caution and monitoring are required.
Warfarin, other coumarin anticoagulants or fluindione
The INR can increase after ezetimibe is added, so anticoagulation monitoring is required.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.