Ranolazine

Drug #2226

Ranolazine is used as an adjunctive anti-anginal treatment for patient with symptomatic stable angina pectoris who are inadequately controlled or intolerant to first-line anti-anginal tharapies. Ranolazine is a racemic mixture, chemically described as 1-piperazineacetamide, N-(2,6dimethylphenyl)-4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]-, (±)-. It has an empirical formula of C24H33N3O4. 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. Ranolazine at therapeutic levels can inhibit the cardiac late sodium current (INa). However, the relationship of this inhibition to angina symptoms is uncertain.

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Primary Characteristics

Ranolazine is also known as Ranolazine Dihydrochloride.

It is classified in Anti anginal pharmacological group.

Molecular Weight: 427.54 · pK_a: 14.25 · Solubility in Water: very slightly soluble. · Solubility in Alcohol: slightly · Non-proprietary name: Ranolazine.

Pharmacokinetics

Absorption: Ranolazine has an oral bioavailability is 76%.

Distribution: Ranolazine has a plasma protein binding is 62%.

Elimination: it is metabolised via CYP3A and to a lesser extent by CYP2D6., plasma half-life is 7 hours, renal excretion is 75%.

Indications

Ranolazine is primarily indicated in conditions like Angina, Stable angina.

Contraindications

Ranolazine is contraindicated in conditions like Hypokalaemia, Hypomagnesaemia, Hepatic impairment, Ventricular tachycardia, Acute myocardial infarction, Severe renal impairment.

Dosage

Ranolazine's dosage details are as follows:

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
750 mg	750 mg	Every 12h	oral	May be taken with or without food. Dose adjustments may be needed when taken with other drugs.
Paediatric Dosage (20kg)
No data.
Neonatal Dosage (3kg)
No data.

Drug Interactions

7 interactions

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

Ranolazine in overdosage may give rise to further complications which include Hematuria, Blurred vision , Tremors , QT prolongation, Pulmonary fibrosis .

The signs and symptoms that are produced after acute overdosage of Ranolazine are Dizziness, Paresthesia, Nausea, Confusion , Vomiting, Syncope .

Ranolazine is known to cause more or less tolerable side effects which are usually transient. These include Abdominal pain, Asthenia , Dizziness, Dry mouth, Headache, Nausea, Tinnitus, Vertigo, Vomiting .

Warnings / Precautions

Safety not established in pediatric patients. Ranolazine concentration increases 30% and 60% in in patients with mild and moderate hepatic impairment. Take with caution in patients with renal impairment as its concentration increases upto 50% in patients with varying degree of renal impairment. There are no adequate well-controlled studies in pregnant women. Ranolazine should be used during pregnancy only when the potential benefit to the patient justifies the potential risk to the fetus.

Available Brands

Click on a strength to view available brands.

Single Ingredient

Tabs

1 g 1000 mg 500 mg

Tabs SR

500 mg

Storage Conditions

Ranolazine should be stored tablet.

Drug Classification

1.12.1 — Antianginal drugs

Manufacturers

Manufacturers of Ranolazine in Pakistan:

Getz Highnoon Maple Searle