ra-NOLE-a-zeen

Therapeutic Classification: antianginals

• Chronic angina pectoris.

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

• Decreased frequency of angina.

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.

(plasma concentrations)

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: palpitations, QT interval prolongation, 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).

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

(Generic available)

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

• Assess location, duration, intensity, and precipitating factors of anginal pain.
• Monitor ECG at baseline and periodically during therapy to evaluate effects on QT interval.

• Monitor renal function after starting and periodically during therapy in patients with moderate to severe renal impairment (CCr <60 mL/min) for ↑ serum creatinine accompanied by ↑ BUN. Usually has a rapid onset, but does not progress during therapy and is reversible with discontinuation of ranolazine. If acute renal failure develops, discontinue ranolazine.
  • May cause transient eosinophilia.
  • May cause small mean ↓ in hematocrit.

• Ranolazine should be used in combination with calcium channel blockers, beta blockers, or nitrates.
  • Do not administer with grapefruit juice or grapefruit products.
• PO: May be administered without regard to food. DNC: Tablets should be swallowed whole; do not break, crush, or chew.
  • Sprinkle granules on one tablespoonful of soft food (applesauce or yogurt) and consume immediately. Do not crush or chew granules.
  • Nasogastric (NG) tube: Add content of a sachet to a plastic catheter tip syringe and add 50 mL of water. Gently shake syringe for approximately 15 seconds. Promptly deliver through a 12 French or larger NG tube. Ensure no granules are left in the syringe. Rinse with additional water (about 15 mL) if needed.
  • Gastrostomy/Gastric (G) tube: Add content of a sachet to a plastic catheter tip syringe and add 30 mL of water. Gently shake syringe for approximately 15 seconds. Promptly deliver through a 12 French or larger G-tube. Rinse with 20 mL of water in the syringe. Ensure no granules are left in the syringe. Rinse with additional water (about 15 mL) if needed.

• 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.

• Decrease in frequency of angina attacks.

Aspruzyo Sprinkle, Ranexa

Corzyna