It is an antianginal indicated for the treatment of chronic angina.
Ranolazine has anti-ischemlc and antlanginal effects that do not depend upon reductions in heart rate or blood pressure.The exact mechanism of action of ranolazine is unknown. 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.
Absorption: Cmax: 2-5 h
Half-life: 6-22 h
Distribution: Over the concentration range of 0.25 to 10 µg/ml, Ranolazine is approximately 62% bound to human plasma proteins.
Metabolism and Excretion: Ranolazine is metabolized mainly by CYP3A and, to a lesser extent, by CYP2D6. Ranolazine is metabolized rapidly and extensively in the liver and intestine; less than 5% is excreted unchanged in urine and feces. Following a single oral dose of Ranolazine solution, approximately 75% of the dose is excreted in urine and 25% in feces.
500 mg twice daily and increase to 1000 mg twice daily, based on clinical symptoms
CYP 3A Inhibitors: Do not use Ranolazine with strong CYP 3A inhibitors. With moderate CYP 3A inhibitors (e.g., diltiazem, verapamil, erythromycin) limit maximum dose of ranolazine to 500 mg twice daily.
CYP 3A Inducers: Do not use Ranolazine with inducers.
P-gp Inhibitors (e.g., Cyclosporin): May need to lower the Ranolazine dose based on clinical dose.
Drugs transported by P-gp or metabolized by CYP2D6 (eg., digoxin, TCA): May need reduced doses of these drugs when used with ranolazine.
Can occur with ranolazine. Little data available on high doses, long exposure, use with QT intervalprolonging drugs, potassium channel variants causing prolonged QT interval, in patients with a family history of (or congenital) long QT syndrome, or in patients with known acquired QT interval prolongation.
Most common adverse reactions (>4% and more common than with placebo) are dizziness, headache, constipation, nausea.
This drug should not be used during pregnancy unless clearly needed. Use should be avoided during breastfeeding.
High oral doses of Ranolazine produce dose-related increases in dizziness, nausea, and vomiting. High intravenous exposure also produces 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.
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
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