Ranexa (Menarini)
New Product
HKPharm J Volume 30 (2), May-Aug-2023 (2023-12-21): P.60
Ranolazine inhibits sodium and potassium ion channel currents. It has been shown to exert weak activity on L-type calcium channels making it a weak direct vasodilator and exerts minimal direct effects on atrioventricular nodal conduction. Some additional mechanisms have been elucidated. Ranolazine exerts antagonistic activity towards the alpha 1 and beta 1 adrenergic receptors and inhibition of fatty acid oxidation.
Ranexa
(Menarini)
edited by Lucilla Leung
Active Ingredients
Ranolazine
Pharmacological Properties
Ranolazine inhibits sodium and potassium ion channel currents. It has been shown to exert weak activity on L-type calcium channels making it a weak direct vasodilator and exerts minimal direct effects on atrioventricular nodal conduction. Some additional mechanisms have been elucidated. Ranolazine exerts antagonistic activity towards the alpha 1 and beta 1 adrenergic receptors and inhibition of fatty acid oxidation.
Indications
Add-on therapy for the symptomatic treatment of adult patients w/ stable angina pectoris who are inadequately controlled or intolerant to 1st-line antianginal therapies (e.g. β-blockers &/or Ca antagonists).
Dosage Forms and Strengths
Each tablets contains 375 mg ranolazine in a prolong release tablet.
Each tablets contains 500 mg ranolazine in a prolong release tablet.
Each tablets contains 750 mg ranolazine in a prolong release tablet.
Administration
Adult
Initially 375 mg twice daily. After 2-4 week, the dose should be titrated to 500 mg bd, and according to patient's response, further titrated to a maximum 750 mg twice daily.
Contraindications
Hypersensitivity.
Severe renal impairment (CrCl <30 mL/min).
Moderate or severe hepatic impairment.
Concomitant administration of potent CYP3A4 inhibitors (e.g. itraconazole, ketoconazole, voriconazole, posaconazole, HIV PIs, clarithromycin, telithromycin, nefazodone).
Concomitant administration of class Ia (e.g. quinidine) or class III (e.g. dofetilide, sotalol) antiarrhythmics other than amiodarone.
Interactions
Increased plasma conc w/ CYP3A4 inhibitors (e.g. itraconazole, ketoconazole, voriconazole, posaconazole, HIV PIs, clarithromycin, telithromycin, nefazodone, grapefruit, diltiazem, erythromycin, fluconazole); P-gp inhibitors (e.g. ciclosporin, verapamil); CYP2D6 inhibitors (e.g. paroxetine). Decreased steady-state conc w/ CYP3A4 inducers (e.g. rifampicin, phenytoin, phenobarb, carbamazepine, St. John's wort). Increased plasma conc of P-gp substrates; sensitive CYP3A4 substrates (e.g. simvastatin, lovastatin) & CYP3A4 substrates w/ a narrow therapeutic range (e.g. ciclosporin, tacrolimus, sirolimus, everolimus); metoprolol or other CYP2D6 substrates (e.g. propafenone & flecainide or, to a lesser extent, TCAs & antipsychotics); digoxin; atorvastatin. Increased plasma exposure of metformin (OCT2 substrate). Caution during co-administration w/ CYP2B6 substrates (e.g. bupropion, efavirenz, cyclophosphamide). Increased possible risk of ventricular arrhythmias w/ other drugs known to prolong the QTc interval e.g. certain antihistamines (e.g. terfenadine, astemizole, mizolastine), certain antiarrhythmics (e.g. quinidine, disopyramide, procainamide), erythromycin, & TCAs (e.g. imipramine, doxepin, amitriptyline).
Adverse Reactions
Dizziness, headache; constipation, vomiting, nausea; asthenia.
Dosage Available
Ranexa Prolonged-Release Tablets 375 mg in the pack of 60’s.
Ranexa Prolonged-Release Tablets 500 mg in the pack of 60’s.
Ranexa Prolonged-Release Tablets 750 mg in the pack of 60’s.
Forensic classification
P1S1S3