Home Drug Guide Ranolazine

Drug Guide

Generic Name

Ranolazine

Brand Names Ranexa, Aspruzyo Sprinkle

Classification

Therapeutic: Antianginal agent

Pharmacological: Late sodium current inhibitor

FDA Approved Indications

Chronic angina pectoris

Mechanism of Action

Ranolazine selectively inhibits the late phase of the sodium current in myocardial cells, which reduces intracellular calcium overload, thereby improving myocardial relaxation and reducing ischemia.

Dosage and Administration

Adult: Initially 500 mg twice daily; may be increased to 1000 mg twice daily based on response and tolerability.

Pediatric: Not established for pediatric use.

Geriatric: Use with caution; start at lower dose due to potential with reduced renal or hepatic function.

Renal Impairment: Adjust dose based on renal function; contraindicated in severe renal impairment (CrCl <30 mL/min).

Hepatic Impairment: Use caution; dose adjustment recommended in hepatic impairment.

Pharmacokinetics

Absorption: Well absorbed, with oral bioavailability of approximately 37%.

Distribution: Extensive tissue distribution; plasma protein binding approximately 62%.

Metabolism: Metabolized primarily via CYP3A4 and CYP2D6 enzymes.

Excretion: Excreted mainly via urine (about 75%), with some fecal excretion.

Half Life: Approximately 7 hours.

Contraindications

Concurrent use with strong CYP3A inhibitors or inducers.
Severe hepatic impairment.

Precautions

Use with caution in hepatic impairment, renal impairment, or electrolyte imbalance. Monitor for QT prolongation.
Pregnancy Category C; benefits must outweigh risks.

Adverse Reactions - Common

Dizziness (Common)
Headache (Common)
Constipation (Common)
Nausea (Common)

Adverse Reactions - Serious

QT prolongation (Less common)
Serious arrhythmias (Rare)

Drug-Drug Interactions

CYP3A4 inhibitors (e.g., ketoconazole, erythromycin) may increase ranolazine levels.
CYP3A4 inducers (e.g., rifampin) may decrease efficacy.
Other QT prolonging agents.

Drug-Food Interactions

N/A

Drug-Herb Interactions

N/A

Nursing Implications

Assessment: Monitor for signs of angina, arrhythmias, and adverse effects such as dizziness or QT prolongation.

Diagnoses:

Risk for decreased cardiac perfusion
Risk for arrhythmias

Implementation: Administer as prescribed, monitor ECG, blood pressure, and symptom relief.

Evaluation: Assess for reduction in anginal episodes, adverse effects, and laboratory abnormalities.

Patient/Family Teaching

Take medication exactly as prescribed.
Report symptoms like dizziness, chest pain, or irregular heartbeat.
Avoid alcohol and CYP3A4 inhibitors or inducers unless directed by healthcare provider.

Special Considerations

Black Box Warnings:

QT interval prolongation leading to torsades de pointes.

Genetic Factors: Consider individual variability in CYP2D6 metabolizer status.

Lab Test Interference: May cause falsely elevated serum digoxin or other drug levels.

Overdose Management

Signs/Symptoms: Dizziness, hypotension, bradycardia, signs of arrhythmia.

Treatment: Supportive care, electrolyte correction, ECG monitoring, and in case of severe overdose, consider activated charcoal or hospitalization for advanced care.

Storage and Handling

Storage: Store at room temperature away from moisture, heat, and light.

Stability: Stable for 24 months when stored properly.