Ranolazine

Ranolazine is an anti-anginal medicine. Ranolazine was licensed by the US FDA and became available for medicinal use in the United States in 2006. It is primarily used to treat persistent angina, which is heart-related chest pain. It is also beneficial for avoiding atrial fibrillation. It reduces the heart's oxygen need by relaxing the cardiac muscle. It won't help with acute chest discomfort. Ranolazine is typically used in combination with other medications.

BRAND NAMES:

Aspruzyo sprinkle - It contains ranolazine as the active ingredient available as Aspruzyo sprinkle 1000mg granules extended release in a packet used in the treatment of chest pain.

Ranexa – Ranolazine is the major active ingredient present in Ranexa that is available for oral usage in the form of tablets.

MECHANISM OF ACTION:

Ranolazine is known to inhibit the phase of inward sodium channels in cardiac myocytes, reducing the intracellular sodium concentration and reducing intracellular calcium influx through the Na-Ca channel. The decreasing of intracellular calcium reduces ventricular wall tension and reduces oxygen consumption, and it doesn’t affect heart rate and blood pressure. It significantly increased exercise duration compared to placebo and had negligible effects on heart rate and blood pressure.

PHARMACOKINETICS:

Absorption: The time to reach peak concentration of ranolazine varies within 2 to 6 hours, with steady state within 3 days.

Distribution: The volume of distribution of Ranolazine ranges from 85 to 180 L.

Metabolism: The drug is metabolized hepatically mainly through the CYP3A4 enzyme, and minor metabolism occurs through CYP2D6.

Excretion: 75% of the ranolazine dose that is administered is excreted really, and the remaining is excreted through the feces.

PHARMACODYNAMICS:

Ranolazine at higher concentrations inhibits rapid delayed rectifier potassium, delaying the action potential and prolonging the QT interval. It also inhibits fatty acid oxidation, which enhances glucose oxidation, reduces lactic acid production, and improves heart function.

DOSAGE AND ADMINISTRATION:

Ranolazine is available in extended-release tablets and extended-release granules, which are taken orally. The dose of medicine administration depends on the patient's condition. The amount of medicine that is prescribed depends on the strength of the medicine.

In adults suffering from chronic angina, the recommended dose of extended-release tablets and granules is 500 mg, two times a day. Depending on the patient's tolerability and condition, the dose may be titrated to 1000 mg twice daily. The dose should not exceed more than 1000 mg twice a day.

CONTRAINDICATIONS:

Ranolazine is contraindicated in patients with sensitivity to the drug or any ingredient in the formulation.

DRUG INTERACTIONS:

When taking ranolazine certain medications should be avoided to control adverse effects and also to increase the functioning of the drug properly.