• Chronic angina pectoris.

Contraindicated in:

• Hypersensitivity
• Concurrent use of potent CYP3A inhibitors
• Concurrent use of CYP3A inducers
• Hepatic impairment
• Lactation: Lactation.

Use Cautiously in:

• Renal impairment
• OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk
• Pedi: Safety and effectiveness not established in children
• Geri: ↑ risk of adverse reactions in patients >75 yr.

CV: QT interval prolongation, palpitations, TORSADES DE POINTES.

EENT: tinnitus.

GI: abdominal pain, constipation, dry mouth, nausea, vomiting.

GU: acute renal failure.

Neuro: dizziness, headache.

Drug-Drug:

• Ketoconazole, itraconazole, clarithromycin, nefazodone, nelfinavir, and ritonavir significantly ↑ levels; concurrent use contraindicated.
• Rifampin, rifabutin, rifapentin, phenobarbital, phenytoin, and carbamazepine significantly ↓ levels; concurrent use contraindicated.
• Verapamil, diltiazem, aprepitant, erythromycin, and fluconazole ↑ levels (do not exceed ranolazine dose of 500 mg twice daily).
• Cyclosporine may ↑ levels.
• Paroxetine may ↑ levels.
• May ↑ levels of simvastatin.
• May ↓ metabolism and ↑ effects of metoprolol, tricyclic antidepressants, and antipsychotics; dosage adjustments may be necessary.
• May ↑ digoxin levels; dose adjustment may be required.

Drug-Natural Products:

• St. John's wort significantly ↓ levels (contraindicated).

Drug-Food:

• Grapefruit juice↑ levels (do not exceed ranolazine dose of 500 mg twice daily).

(Generic available)

• Extended-release tablets: 500 mg; 1000 mg;
• Extended-release granules: 500 mg/pkt; 1000 mg/pkt;

• PO (Adults): 500 mg twice daily initially, may be ↑ to 1000 mg twice daily.

Aspruzyo Sprinkle, Ranexa

• Does not ↓ BP or heart rate; remainder of mechanism is not known.

• Decreased frequency of angina.

Therapeutic Classification: antianginals

Absorption: Highly variable.

Distribution: Unknown.

Metabolism/Excretion: Metabolized by the liver primarily by the CYP3A isoenzyme and to a lesser extent by the CYP2D6 isoenzyme; <5% excreted unchanged in urine and feces.

Half-life: 7 hr.

Corzyna

(plasma concentrations)

• Instruct patient to take ranolazine as directed. If a dose is missed, take the usual dose at the next scheduled time; do not double doses. Explain to patient that ranolazine is used for chronic therapy and will not help an acute angina episode.
• Advise patient to avoid grapefruit juice and grapefruit products when taking ranolazine.
• May cause dizziness and light-headedness. Caution patient to avoid driving and other activities requiring alertness until response to medication is known.
• Advise patient to notify health care professional if fainting occurs.
• Inform patient that ranolazine may cause changes in the ECG. Patient should inform health care professional if they have a personal or family history of QTc prolongation, congenital long QT syndrome, or proarrhythmic conditions such as hypokalemia.
• Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
• Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected, or if breastfeeding.

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