Ranexa

Ranolazine

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

Adult Initially 375 mg bid, titrated to 500 mg after 2-4 wk. Max: 750 mg bid.

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

Hypersensitivity. Severe renal (CrCl <30 mL/min). Moderate or severe hepatic impairment. 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.

Concomitant use w/ moderate CYP3A4 & P-gp inhibitors. Mild hepatic impairment. Mild to moderate renal impairment (CrCl 30-80 mL/min). Patients w/ low wt (≤60 kg); moderate to severe CHF (NYHA class III-IV); w/ lacking CYP2D6 activity (poor metabolizers); history of congenital or family history of long QT syndrome, known acquired QT interval prolongation & those treated w/ drugs affecting the QTc interval. Renal impairment. Co-administration w/ CYP3A4 inducers (eg, rifampicin, phenytoin, phenobarb, carbamazepine, St. John's wort). May affect ability to drive or operate machinery. Pregnancy & lactation. Childn <18 yr. Elderly.

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

Increased plasma conc w/ inhibitors of CYP3A4 (eg, itraconazole, ketoconazole, voriconazole, posaconazole, HIV PIs, clarithromycin, telithromycin, nefazodone, grapefruit juice; diltiazem, erythromycin, fluconazole), P-gp (eg, ciclosporin, verapamil) & CYP2D6 (eg, paroxetine) inhibitors. 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); digoxin. Increased exposure to metoprolol or other CYP2D6 substrates (eg, propafenone & flecainide or to a lesser extent, TCAs & antipsychotics); metformin & other OCT2 substrates (eg, pindolol & varenicline). CYP2B6 substrates (eg, bupropion, efavirenz, cyclophosphamide). Increased possible risk of ventricular arrhythmias w/ 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.

Rx