atorvastatin + ezetimibe: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
atorvastatin + ezetimibe: clinical details
Prescribing considerations
- Use as substitution therapy only after adequate control on corresponding separate atorvastatin and ezetimibe products; it is not intended for initial titration.
- Review alcohol intake, liver history, hypothyroidism, renal impairment, previous statin or fibrate muscle toxicity, hereditary muscle disorders and interacting medicines.
- Use caution after previous haemorrhagic stroke or lacunar infarct and when myopathy risk is increased.
- Safety and efficacy of the fixed combination have not been established in children.
Contraindications and cautions
- Hypersensitivity to either active ingredient or an excipient
- Pregnancy, breastfeeding, or child-bearing potential without appropriate contraception
- Active liver disease or unexplained persistent transaminase elevation above the product threshold
- Concurrent glecaprevir with pibrentasvir
Monitoring
- Check liver function before treatment and periodically thereafter; repeat promptly if symptoms suggest liver injury.
- Consider baseline creatine kinase when rhabdomyolysis risk factors are present; investigate new muscle symptoms.
- Monitor INR when starting or changing treatment in a patient taking warfarin or another coumarin anticoagulant.
- Monitor ciclosporin concentrations if concurrent use is necessary.
- Monitor glycaemia clinically and biochemically in patients at increased diabetes risk.
Clinical pharmacology
Ezetimibe inhibits intestinal NPC1L1-mediated sterol uptake and undergoes extensive glucuronidation with enterohepatic recycling. Atorvastatin competitively inhibits HMG-CoA reductase and is metabolised mainly through CYP3A4. The fixed product is bioequivalent to the corresponding separate tablets.
Formulation and product differences
- The film-coated fixed combination is intended to replace the corresponding separate components.
- The tablet contains lactose and is essentially sodium-free.
- The tablet is oval, biconvex and should be protected from light in its original packaging.
atorvastatin + ezetimibe preparations and strengths
Tablet
Route: Oral
Strengths: 10 mg + 10 mg, 10 mg + 20 mg, 10 mg + 40 mg, 10 mg + 80 mg
atorvastatin + ezetimibe interactions
Check new prescriptions, over-the-counter medicines and supplements with a pharmacist or prescriber because several interactions can increase muscle toxicity or reduce cholesterol lowering.
Systemic fusidic acid
The combination substantially increases the risk of myopathy and rhabdomyolysis and requires medical management.
Strong CYP3A4 or transporter inhibitors
Clarithromycin, itraconazole, some HIV or hepatitis C antivirals, ciclosporin and letermovir can increase atorvastatin exposure and muscle toxicity.
Glecaprevir with pibrentasvir
Use with the fixed combination is contraindicated because atorvastatin exposure may rise substantially.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.