ranolazine

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.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	2–5 hr	12 hr

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Concurrent use of strong 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.

Adv. Reactions/Side Effects ⬆ ⬇

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

Interactions ⬆ ⬇

Drug-drug:

Ketoconazole, itraconazole, clarithromycin, nefazodone, nelfinavir, and ritonavir significantly ↑ levels and risk of toxicity; concurrent use contraindicated.
Rifampin, rifabutin, rifapentin, phenobarbital, phenytoin, and carbamazepine significantly ↓ levels and effectiveness; concurrent use contraindicated.
Verapamil, diltiazem, aprepitant, erythromycin, and fluconazole may ↑ levels and risk of toxicity; do not exceed ranolazine dose of 500 mg twice daily.
Cyclosporine and paroxetine may ↑ levels and risk of toxicity.
May ↑ levels and risk of toxicity of simvastatin, metoprolol, tricyclic antidepressants, and antipsychotics.
May ↑ digoxin levels and risk of toxicity; dose adjustment may be required.

Drug-Natural Products:

St. John's wort significantly ↓ levels and effectiveness; concurrent use contraindicated.

Drug-Food:

Grapefruit juice↑ levels and risk of toxicity; do not exceed ranolazine dose of 500 mg twice daily.

Route/Dosage ⬆ ⬇

PO (Adults ): 500 mg twice daily initially; may ↑ to 1000 mg twice daily.

Availability ⬆ ⬇

(Generic available)

Extended-release tablets: 500 mg; 1000 mg

Assessment ⬆ ⬇

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

Lab Test Considerations:

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 rapid onset, but does not progress and is reversible with discontinuation of ranolazine. If acute renal failure occurs, discontinue ranolazine.
- May cause transient eosinophilia.
- May ↓ hematocrit.

Implementation ⬆ ⬇

Ranolazine should be used in combination with calcium channel blockers, beta blockers, or nitrates.
PO: May be administered without regard to food. DNC: Tablets should be swallowed whole; do not break, crush, or chew.

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication to patient. Advise to read Patient Information before starting therapy.
If dose is missed, instruct patient to take the usual dose at the next scheduled time; do not double doses. Explain 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 interval 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.
Rep: Advise women of reproductive potential to notify health care professional if pregnancy is planned or suspected, or if breastfeeding.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇