Ranolazine (3 brand names, 2 dosage forms, 1 route)
Available dosage forms: TABLET, EXTENDED RELEASE, GRANULE, EXTENDED RELEASE.
Routes of administration: ORAL.
Brand Names
- ASPRUZYO SPRINKLE
- RANEXA
- RANOLAZINE
Indications and Usage
Ranolazine extended-release tablets are indicated for the treatment of chronic angina. Ranolazine extended-release tablets may be used with beta-blockers, nitrates, calcium channel blockers, anti- platelet therapy, lipid-lowering therapy, ACE inhibitors, and angiotensin receptor blockers.
Contraindications
Ranolazine is contraindicated in patients: • Taking strong inhibitors of CYP3A [see Drug Interactions (7.1)] • Taking inducers of CYP3A [see Drug Interactions (7.1)] • With liver cirrhosis [see Use in Specific Populations (8.6)]
Mechanism of Action
The mechanism of action of ranolazine’s antianginal effects has not been determined. Ranolazine has anti-ischemic and antianginal effects that do not depend upon reductions in heart rate or blood pressure. It does not affect the rate-pressure product, a measure of myocardial work, at maximal exercise. Ranolazine at therapeutic levels can inhibit the cardiac late sodium current (INa). However, the relationship of this inhibition to angina symptoms is uncertain. The QT prolongation effect of ranolazine on the surface electrocardiogram is the result of inhibition of IKr, which prolongs the ventricular action potential.
Overdosage
Hypotension, QT prolongation, bradycardia, myoclonic activity, severe tremor, unsteady gait/incoordination, dizziness, nausea, vomiting, dysphasia, and hallucinations have been seen in cases of oral overdose of ranolazine. In cases of extreme overdose of ranolazine fatal outcomes have been reported. In clinical studies, high intravenous exposure resulted in diplopia, paresthesia, confusion, and syncope. In addition to general supportive measures, continuous ECG monitoring may be warranted in the event of overdose. Since ranolazine is about 62% bound to plasma proteins, hemodialysis is unlikely to be effective in clearing ranolazine.