Ranexa

Ranolazine

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 (eg, β-blockers &/or Ca antagonists).

Adult Initially 375 mg bd. After 2-4 wk, the dose should be titrated to 500 mg bd, & according to patient's response, further titrated to a max 750 mg bd.

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

Hypersensitivity. Severe renal impairment (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). Concomitant administration of class Ia (eg, quinidine) or class III (eg, dofetilide, sotalol) antiarrhythmics other than amiodarone.

Patients w/ low body wt (≤60 kg); moderate to severe CHF (NYHA Class III-IV); mild hepatic impairment; mild to moderate renal impairment (CrCl 30-80 mL/min); elderly; poor CYP2D6 metabolisers. Risk of QT prolongation. Regularly check renal function at regular intervals during treatment. Concomitant administration of moderate CYP3A4 inhibitors; P-gp inhibitors; CYP3A4 inducers. May affect ability to drive & operate machinery. Pregnancy. Should not be used during breast-feeding. 750 mg tab: Rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption. Contains azo colouring agent E102 which may cause allergic reactions.

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

Increased plasma conc w/ CYP3A4 inhibitors (eg, itraconazole, ketoconazole, voriconazole, posaconazole, HIV PIs, clarithromycin, telithromycin, nefazodone, grapefruit, 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 substrates; sensitive CYP3A4 substrates (eg, simvastatin, lovastatin) & CYP3A4 substrates w/ a narrow therapeutic range (eg, ciclosporin, tacrolimus, sirolimus, everolimus); metoprolol or other CYP2D6 substrates (eg, 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 (eg, bupropion, efavirenz, cyclophosphamide). Increased possible risk of ventricular arrhythmias w/ other drugs known to prolong the QTc interval eg, certain antihistamines (eg, terfenadine, astemizole, mizolastine), certain antiarrhythmics (eg, quinidine, disopyramide, procainamide), erythromycin, & TCAs (eg, imipramine, doxepin, amitriptyline).

Anti-Anginal Drugs

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

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