Generic
Ranolazine
13 brands available in the market
At a glance
Ranolazine is an anti-anginal medication used for the treatment of chronic angina. It helps prevent new attacks of angina by decreasing the oxygen requirement of the heart through relaxation of heart muscle, but does not stop an acute attack once it has started.
Description
Ranolazine exerts its antianginal and anti-ischaemic effects through concentration-, voltage-, and frequency-dependent inhibition of the late Na current and other cardiac ion channels and transporters. It decreases the late Na current, resulting in reduced intracellular Na concentrations, reversal of Ca overload, restoration of ventricular pump function, and prevention of ischaemia-induced arrhythmias. Its antianginal effects are not dependent upon reductions in heart rate or BP.
Indications
- Chronic angina
Therapeutic class
Other Anti-anginal & Anti-ischaemic drugs
Pharmacological class
Late Sodium Channel Inhibitor (Antianginal)
Pharmacology
Ranolazine inhibits the late Na current, reducing intracellular Na concentrations and reversing Ca overload, which restores ventricular pump function and prevents ischaemia-induced arrhythmias. Its antianginal effects are not dependent on heart rate or blood pressure reduction. QT prolongation is caused by IKr inhibition.
Mechanism of action
Relieves angina by reducing intracellular calcium overload through late sodium current inhibition.
Dosage
Adult Dose (Oral):
- Initial dose: 500 mg twice daily
- May increase to 1000 mg twice daily if needed
- Maximum daily dose: 1000 mg twice daily
- With moderate CYP3A4 inhibitors: Max 500 mg twice daily
- Mild hepatic impairment: Dose titration needed; Moderate-severe: Contraindicated
- Renal impairment (CrCl 30-80 mL/min): Dose titration needed; CrCl <30 mL/min: Contraindicated
Administration
- May be taken with or without food
- Swallow tablet whole; do not crush, break or chew
- If a dose is missed, take the prescribed dose at the next scheduled time; do not double the next dose
Missed dose
If you miss a dose, take it as soon as possible; if almost time for next dose, skip it; do not double the dose.
Side effects
Side Effects:
- Nausea
- Vomiting
- Headache
- Dizziness
- Constipation
- Weakness
- Bradycardia
- Palpitations
- Tinnitus
- Vertigo
- Abdominal pain
- Dry mouth
- Peripheral edema
- Dyspnea
- Hypotension
Precautions & warnings
- May affect driving ability; do not drive if dizzy or drowsy
- Take with food to avoid stomach upset
- ECG should be performed (QTc interval may be prolonged)
- May improve HbA1c and blood sugar in diabetics
- Avoid alcohol
Contraindications
- Pre-existing QT prolongation
- Hepatic impairment
- Taking QT prolonging drugs
- Taking strong CYP3A4 inhibitors (ketoconazole, clarithromycin, nelfinavir, itraconazole, ritonavir)
Drug interactions
- Strong CYP3A4 inhibitors: Do not use concomitantly
- Moderate CYP3A4 inhibitors (diltiazem, fluconazole, erythromycin): Limit dose to 500 mg twice daily
- P-gp inhibitors (verapamil, cyclosporine): May need to lower dose
- CYP3A4 inducers (rifampicin, phenytoin, phenobarbital, carbamazepine): Do not use
- Digoxin, TCAs: May need reduced doses
- Simvastatin: Increased risk of rhabdomyolysis
- QT prolonging drugs (terfenadine, astemizole, class 1A/III antiarrhythmics): Increased risk of ventricular arrhythmias
Food interactions
It is not known whether it is safe to consume alcohol with Ranolazine.
Use in pregnancy
Use in Pregnancy: May be unsafe during pregnancy; animal studies have shown harmful effects; consult your doctor.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Probably unsafe; limited human data suggests drug may pass into breast milk; consult your doctor.
Pediatric use
Safety and efficacy not established in pediatric patients.
Geriatric use
Caution required in elderly patients; dose adjustment may be needed.
Renal / hepatic impairment
Renal Impairment: Mild-moderate (CrCl 30-80 mL/min): Dose titration needed; Severe (CrCl <30 mL/min): Contraindicated; consult your doctor.
Hepatic Impairment: Mild: Dose titration needed; Moderate-severe: Contraindicated; consult your doctor.
Overdose effects
Overdose: Dizziness, nausea, vomiting (dose-related); high IV doses: diplopia, paresthesia, confusion, syncope; treatment: supportive measures, continuous ECG monitoring; hemodialysis is unlikely to be effective (62% protein-bound).
Storage conditions
Store below 30°C, away from light and moisture; keep out of reach of children.
Chemical structure
Ranolazine