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CARDIOVASCULAR SYSTEM › CARDIAC THERAPY › OTHER CARDIAC PREPARATIONS › Other cardiac preparations
ranolazine
C01EB18
Forms & Strengths
- Extended-release tablets: 500 mg, 1000 mg
Adult Dosing
- Initial: 500 mg orally twice daily
- Maintenance: Increase to 1000 mg orally twice daily based on clinical response
- Maximum dose: 1000 mg twice daily
Pediatric Dosing
- Safety and efficacy not established in pediatric patients (< 18 years)
Indications
- Treatment of chronic angina
Mechanism of Action
- Inhibits late sodium current (INa) in cardiac myocytes, reducing intracellular sodium and subsequent calcium overload
- Improves myocardial relaxation and decreases oxygen consumption during ischemia
Contraindications
- Pre-existing QT prolongation or concurrent use of QT-prolonging drugs
- Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin, ritonavir)
- CYP3A4 inducers (e.g., rifampin, carbamazepine, St. John's wort)
- Hepatic impairment
Adverse Reactions
- Dizziness
- Headache
- Constipation
- Nausea
- QT interval prolongation
Drug Interactions
- Strong CYP3A4 inhibitors significantly increase ranolazine exposure and risk of QT prolongation
- Strong CYP3A4 inducers significantly decrease ranolazine efficacy
- Moderate CYP3A4 inhibitors (e.g., diltiazem, verapamil, erythromycin) require dose limitation to 500 mg twice daily
- P-glycoprotein inhibitors (e.g., cyclosporine) increase ranolazine concentrations
- Substrates of CYP3A4 (e.g., simvastatin) or CYP2D6 (e.g., metoprolol, tricyclic antidepressants) may have increased plasma levels
Curated Content: Needs Vetting Before Put to Clinical Use