Introduction

RANEXA is a prescription medication used to treat chronic Angina. It relieves chest pain by enhancing the way the heart uses oxygen without a large effect on heart rate or blood pressure. Unlike other angina drugs, Ranexa has a distinct mechanism that works on the cellular processes within the heart.

Composition

Active Ingredient: Ranolazine

Formulation: Extended release (ER) tablets

500 mg

1,000 mg

Other ingredients: Lactose monohydrate, microcrystalline cellulose, magnesium stearate, titanium dioxide, hypromellose, polyethylene glycol, etc.

Mechanism of Action

The mechanism of action of Ranolazine is at the

cellular level – it acts by:

Sodium Current Inhibition (INa):

In typical ischemia (lessened blood perfusion), sodium floods into cardiac cells. This leads to calcium overload, which inhibits the heart from relaxing. Ranexa decreases this sodium influx, and results in normal calcium levels.

As a result, the heart needs less oxygen, making blood flow more efficient and decreasing chest pain.

No Significant Impact on Heart Rate or Blood Pressure:

This makes Ranexa appropriate for patients who cannot tolerate conventional therapies for angina, such as the beta-blockers.

Indications and Usage

Ranexa is approved for:

Chronic Stable Angina:

As monotherapy or in association with other antianginal agents (e.g., beta-blockers, calcium channel blockers, nitrates).

Off-Label Uses (Growing Evidence):

Arrhythmias (eg, atrial fibrillation): Ranexa may assist with decreasing certain patients’ irregular heartbeats.

Currently under investigation for enhancing diastolic

 function in heart failure;

Heart failure (diastolic dysfunction): Dosage and Administration

Dosage and Administration

Adult Dosage

Recommended Starting Dose: 500 mg twice daily.

Maintenance Dosage: Titrate up to 1,000 mg twice daily as tolerated and according to symptom control.

Maximum Dose: 1,000 mg × 2/day.

Administration Guidelines

Tablets should be swallowed whole (do not break, crush or chew).

Can be taken with food or without food

Do not eat grapefruit or drink grapefruit juice, which can raise blood levels of the drug.

Warnings and Precautions

Key Risks

QT Prolongation:

Having found that “Ranexa can prolong the QT interval (a measure of electrical activity in the heart), increasing the risk of arrhythmias (torsades de pointes),”” If you have heart failure (a condition in which the heart cannot pump enough blood to meet the body’s needs).

Use with caution for patients with a history of QT prolongation or receiving other QT prolonging medications.

Liver Impairment:

Avoided in patients with significant liver dysfunction, as drug will accumulate and become toxic.

Kidney Impairment:

Care of patients with moderate to severe renal impairment

Ranexa is also known to lower blood pressure, especially in patients with moderate to severe impairment of renal function.

Hypersensitivity:

Stop if you notice any signs of an allergic reaction (rash, swelling, difficulty breathing).

Contraindications

Ranexa should not be used in:

[8] De-compensated liver disease patients.

CYP3A inhibitors (strong) (eg, ketoconazole, ritonavir) or CYP3A inducers (strong) (eg, rifampin, phenytoin)

Side Effects

Common Side Effects:

Dizziness

Nausea

Constipation

Headache

Fatigue

Less Common Side Effects That Are More Concerning:

QT interval prolongation and arrhythmias.

Syncope (fainting).

Palpitations.

Allergic reactions (such as itchy skin, rash, swelling).

What To Do if You Have Side Effects:

For mild side effects, stay on the medication but alert your doctor if they don’t go away.

Severe side effects (such as fainting and irregular heartbeats) merit immediate medical attention.

Drug Interactions

Major Interactions:

CYP3A Inhibitors:

Increased levels of ranolazine, resulting in toxicity

 Strong inhibitors: Ketoconazole, clarithromycin, ritonavir.

Moderate inibitors: Diltiazem, verapamil.

CYP3A Inducers:

Cut levels of ranolazine, which reduces its efficacy. Examples include: rifampin phenytoin carbamazepine

QT Interval-Prolonging Drugs:

Use in combination may lead to a higher risk of arrhythmias. Such as Sotalol, amiodarone.

P-Glycoprotein Inhibitors:

Cyclosporine or verapamil can increase ranolazine levels.

Digoxin:

Ranolazine increases serum digoxin levels, which may require up-titrating or down-titrating the digoxin dose.

Use in Special Populations

Pregnancy and Breastfeeding:

Pregnancy:

Ranexa should be used only when clearly needed and if the benefits outweigh risks (see your doctor).

Breastfeeding:

Ranolazine passes into breast milk and should be used with caution.

Pediatrics:

The safety and efficacy of Ranexa have not been established in the pediatric population.

Elderly:

No specific dose adjustment is necessary, but older patients may be more sensitive to dizziness or other adverse effects.

Overdose Management

Symptoms of Overdose:

Severe dizziness.

Nausea or vomiting.

Abnormal heart rhythms (arrhythmias).

Treatment:

Offer supportive care (e.g., ECG monitoring, treatments for symptoms).

Ranolazine is highly protein bound, so hemodialysis is unlikely to be effective.

Monitoring During Therapy

ECG: Periodically monitor QT interval, particularly in at-risk patients.

Liver Function Tests: Assess for hepatotoxicity.

Kidney:Routine monitoring of renal function in patients with renal insufficiency.

Storage Instructions

Keep in a dry place at 20–25°C (68–77°F).

Avoid excess heat and moistness or direct sunlight.

Read information on how to keep children safe.

FAQs

Does Ranexa terminate an acute angina attack?

No, Ranexa is not meant to relieve chest pain immediately. For acute episodes, use fast-acting nitroglycerin.

Does Ranexa decrease blood pressure?

Ranexa has minimal impact on blood pressure, but small increases can occur in some patients, especially those with kidney issues.

Question: Can you take Ranexa daily for the long term?

Yes, You can takeranexa long term as long as it is done under proper medical supervision. Follow ups are done at regular intervals to monitor any side effects.

Can I drive when taking Ranexa?

If you experience dizziness, lightheadedness or blurred vision, do not drive or operate heavy machinery.

Do not take Ranexa if you take specific other medications.

Summary

Ranexa is an effective treatment for chronic angina when other therapies are inadequate. Its distinct mechanism offers relief without greatly affecting heart rate or blood pressure. Patients must follow their health care provider’s instructions and promptly report any side effects or concerns.