Ranolazine

Introduction

Ranolazine is a medication used primarily for the management of chronic angina (chest pain) in patients with coronary artery disease. It is often used in combination with other medications to improve exercise tolerance and reduce the frequency of angina attacks.

Uses

Ranolazine is used to:

Manage chronic angina in patients with coronary artery disease.
Improve exercise tolerance and reduce the frequency of angina attacks.
Be used in combination with other anti-anginal agents when additional control of symptoms is needed.

Brand Name	Ranolazine
Type
Weight
Generic	Ranolazine
Manufacturer
Available in	English বাংলা

Mechanism of Action

Ranolazine works by inhibiting late sodium current in cardiac myocytes. This action reduces intracellular sodium and calcium overload, which helps to decrease myocardial oxygen demand and improve the heart's efficiency. Unlike many other anti-anginal agents, ranolazine does not significantly affect heart rate or blood pressure.

How Long Does It Take to Work?

Ranolazine may start to provide symptomatic relief within 1-2 weeks of starting therapy, but it often takes up to 4-6 weeks to achieve its full therapeutic effect. Consistent use as prescribed is important for optimal results.

Absorption

Ranolazine is well absorbed after oral administration, with peak plasma concentrations typically occurring within 2-4 hours. Its absorption can be influenced by food, and taking the drug with a high-fat meal may increase its absorption.

Route of Elimination

Ranolazine is primarily metabolized in the liver by the cytochrome P450 enzyme system, mainly CYP3A4. Its metabolites are excreted through the urine, with a small amount being eliminated via feces.

Dosage

Initiate Ranolazine dosing at 500 mg twice daily and increase to 1000 mg twice daily, if needed, based on clinical symptoms. Take Ranolazine with or without meals. Swallow Ranolazine tablets whole; do not crush, break or chew. The maximum recommended daily dose of Ranolazine is 1000 mg twice daily. If a dose of Ranolazine is missed, take the prescribed dose at the next scheduled time; do not double the next dose.

Pediatric use: Safety and effectiveness in pediatric patients have not been established.

The usual dosage of Ranolazine is:

Initial dose: 500 mg taken orally twice daily.
Maintenance dose: Can be increased to 1000 mg twice daily based on patient response and tolerance.
Adjustments may be necessary in patients with hepatic impairment or those taking interacting medications.

Administration

Ranolazine is administered orally in the form of extended-release tablets. It should be taken with or without food, but it is recommended to take it consistently with respect to meals to ensure stable blood levels.

Side Effects

Common side effects include:

Dizziness or lightheadedness.
Headache.
Nausea and constipation.

Less common but serious side effects may include:

Prolonged QT interval leading to abnormal heart rhythms.
Severe gastrointestinal issues.

Toxicity

Toxicity from Ranolazine is rare but can occur with overdose or excessive use. Symptoms may include severe dizziness, confusion, or abnormal heart rhythms. Seek immediate medical attention if an overdose is suspected.

Precautions

Precautions include:

Monitoring for signs of prolonged QT interval, especially in patients with preexisting heart conditions.
Use with caution in patients with liver impairment, as the drug is extensively metabolized by the liver.
Regular monitoring of blood pressure and heart rate is recommended, especially when used with other anti-anginal medications.

Interaction

Ranolazine may interact with:

CYP3A4 inhibitors (e.g., ketoconazole, ritonavir), which can increase Ranolazine levels and enhance the risk of side effects.
CYP3A4 inducers (e.g., rifampin, phenytoin), which can decrease Ranolazine levels and reduce its efficacy.
Drugs that prolong the QT interval.

Disease Interaction

Use Ranolazine with caution in patients with:

Severe hepatic impairment due to altered metabolism.
Heart conditions that may predispose to prolonged QT interval.

Drug Interaction

Drug interactions can occur with:

Antiarrhythmic agents that may enhance the risk of QT prolongation.
Other medications metabolized by CYP3A4.

Food Interactions

There are no significant food interactions with Ranolazine , but taking the medication consistently with respect to food intake is recommended to maintain stable drug levels.

Pregnancy Use

Ranolazine is classified as a Category C drug during pregnancy. This means that risk to the fetus cannot be ruled out. Use during pregnancy should be considered only if the potential benefits outweigh the risks, and only under the guidance of a healthcare provider.

Lactation Use

The safety of Ranolazine during lactation is not well established. It is recommended to consult a healthcare provider before using Ranolazine while breastfeeding, as the drug may be excreted in breast milk.

Acute Overdose

In the event of acute overdose, symptoms may include severe dizziness, confusion, and potential cardiac arrhythmias. Immediate medical attention is required for appropriate treatment and management of overdose symptoms.

Contraindication

Ranolazine is contraindicated in:

Patients with a known hypersensitivity to the drug or its components.
Severe hepatic impairment due to risk of increased drug levels and potential toxicity.
Patients on strong CYP3A4 inhibitors or inducers that may interact significantly with Ranolazine .

Use Direction

Follow the prescribed dosage and administration instructions carefully. Take Ranolazine orally, twice daily, with or without food. Do not exceed the recommended dose and consult a healthcare provider for any dose adjustments or concerns.

Storage Conditions

Store Ranolazine tablets at room temperature, away from direct light and moisture. Keep out of reach of children and do not use past the expiration date.

Volume of Distribution

The volume of distribution for Ranolazine is approximately 2-4 L/kg, indicating that it is distributed widely in body tissues.

Half Life

The half-life of Ranolazine is approximately 7 hours, which supports its dosing schedule of twice daily administration.

Clearance

Ranolazine is primarily cleared through hepatic metabolism, with renal excretion of its metabolites. The clearance rate can be influenced by liver function and the presence of interacting drugs.

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