ranolazine: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
ranolazine: clinical details
Prescribing considerations
- Reserve for add-on symptomatic treatment of stable angina within the selected licence.
- Review renal and hepatic function, QT risk, interacting medicines and grapefruit consumption before initiation.
- Use additional caution where exposure may be increased, including older age, low body weight, mild hepatic impairment, mild-to-moderate renal impairment or advanced heart failure.
- Safety and efficacy are not established in people under 18 years.
- The selected tablets contain lactose.
Contraindications and cautions
- Hypersensitivity to ranolazine or an excipient
- Severe renal impairment
- Moderate or severe hepatic impairment
- Concurrent potent CYP3A4 inhibitors
- Concurrent Class Ia or Class III antiarrhythmics other than amiodarone
Monitoring
- Check renal function regularly, particularly in older adults or when renal function may change.
- Assess dizziness, nausea, vomiting, constipation, hypotension and other exposure-related adverse effects.
- Consider ECG assessment when QT risk factors, interacting medicines, syncope or palpitations are present.
- Monitor digoxin or transplant-immunosuppressant concentrations when clinically indicated.
Clinical pharmacology
Ranolazine inhibits late cardiac sodium current and also blocks IKr, producing concentration-related QTc prolongation. It is a CYP3A4 and CYP2D6 substrate and a P-glycoprotein substrate; metabolism is extensive and the steady-state terminal half-life is approximately seven hours.
Formulation and product differences
- The selected Aspire products are prolonged-release tablets and must not be crushed, divided or chewed.
- Available strengths differ in tablet colour and size; all selected Aspire tablets contain lactose.
- The prolonged-release tablets can be taken with or without food.
ranolazine preparations and strengths
Modified-release tablet
Route: Oral
Strengths: 375 mg, 500 mg, 750 mg
ranolazine interactions
A full prescription, non-prescription and herbal-medicine review is important because ranolazine has several clinically significant interactions.
Potent CYP3A4 inhibitors, including clarithromycin, azole antifungals and HIV protease inhibitors
Can markedly raise ranolazine exposure and are contraindicated with the selected product.
Diltiazem, verapamil, erythromycin, fluconazole or ciclosporin
Can increase ranolazine levels and adverse effects, requiring careful clinical review.
Rifampicin, carbamazepine, phenytoin, phenobarbital or St John’s wort
Can substantially reduce ranolazine exposure and effectiveness; concurrent use should be avoided.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.