Ranexa

Ranolazine

Add-on therapy for symptomatic treatment of patients w/ stable angina pectoris who are inadequately controlled or intolerant to 1st-line antianginal therapies (eg, β-blockers &/or Ca antagonists).

Adult Initially 375 mg bd, titrated to 500 mg bd after 2-4 wk, further titrated to max: 750 mg bd.

May be taken with or without food: Swallow whole, do not break/chew/crush.

Hypersensitivity. Concomitant administration of potent CYP3A4 inhibitors (eg, itraconazole, ketoconazole, voriconazole, posaconazole, HIV PIs, clarithromycin, telithromycin, nefazodone) & class IA (eg, quinidine) or III (eg, dofetilide, sotalol) antiarrhythmics other than amiodarone. Severe renal (CrCl <30 mL/min) & moderate or severe hepatic impairment.

Patients w/ low wt (≤60 kg); moderate to severe CHF (NYHA class III-IV); lacking CYP2D6 activity; history of congenital or family history of long QT syndrome, known acquired QT interval prolongation & treatment w/ drugs affecting QTc interval. Not to be used in patients treated w/ CYP3A4 inducers eg, rifampicin, phenytoin, phenobarb, carbamazepine, St. John's wort. Check renal function regularly during treatment. Allergic reactions due to azo colouring agents E102. Concomitant use of moderate CYP3A4 or P-gp inhibitors. Mild hepatic or mild to moderate renal impairment (CrCl 30-80 mL/min). May affect ability to drive & use machines. Not to be used during pregnancy & lactation. Childn <18 yr. Elderly. 750 mg: Galactose intolerance, Lapp lactase deficiency, glucose-galactose malabasorption.

Dizziness, headache; constipation, vomiting, nausea; asthenia.

Increased plasma conc w/ CYP3A4 inhibitors (eg, itraconazole, ketoconazole, voriconazole, posaconazole, HIV PIs, clarithromycin, telithromycin, nefazodone, grapefruit juice; diltiazem, erythromycin, fluconazole), P-gp inhibitors (eg, ciclosporin, verapamil) & CYP2D6 inhibitors (eg, paroxetine). Decreased steady-state conc w/ CYP3A4 inducers (eg, rifampicin, phenytoin, phenobarb, carbamazepine, St. John's wort). Increased plasma conc of P-gp or CYP3A4 substrates (eg, simvastatin, lovastatin, atorvastatin; ciclosporin, tacrolimus, sirolimus, everolimus), other CYP2D6 substrates (eg, propafenone & flecainide, TCAs & antipsychotics), metoprolol, digoxin. Increased plasma exposure of metformin & other OCT2 substrates (eg, pindolol & varenicline). Theoretical risk of increased possible risk of ventricular arrhythmias w/ other drugs prolonging QTc interval eg, certain antihistamines (eg, terfenadine, astemizole, mizolastine), antiarrhythmics (eg, quinidine, disopyramide, procainamide), erythromycin & TCAs (eg, imipramine, doxepin, amitriptyline).

Anti-Anginal Drugs

C01EB18 - ranolazine ; Belongs to the class of other cardiac preparations.

B