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Ranolazine

Angina Pectoris

DRUG STATUS

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Approvals

US(FDA), UK(BNF)

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Essential Medicine

NO

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Teratogenicity

Unlisted

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Pharmaceutical Class

Anti-anginal

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Drug Ingredient

Ranolazine

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Summary

  • Ranolazine is primarily used to treat chronic angina, which is chest pain that occurs due to heart disease. It helps improve blood flow to the heart muscle, reducing the strain on the heart and making it function more efficiently.

  • Ranolazine works by inhibiting certain sodium and calcium channels in heart cells. This helps reduce stress on the heart cells and improves the usage of oxygen, which in turn reduces symptoms of angina, such as chest pain.

  • The usual starting dose of Ranolazine for adults is 500 mg taken twice daily. This can be increased to 1000 mg twice daily based on individual response. The tablets should be swallowed whole, with or without food.

  • Common side effects of Ranolazine include dizziness, headache, constipation, nausea, and fatigue. More serious side effects, although rare, can include an abnormal heart rhythm known as QT prolongation, low blood pressure, or liver enzyme abnormalities.

  • Ranolazine should be used with caution in patients with liver disease or severe kidney impairment. It is not recommended for patients with preexisting QT prolongation or those taking certain other medications that affect the QT interval. It can interact with other drugs that affect CYP3A enzymes, so it's important to consult a healthcare provider before starting or combining treatments.

Indications and Purpose

What is Ranolazine used for?

Ranolazine is primarily indicated for the treatment of chronic angina (chest pain) in patients with stable coronary artery disease. It helps to manage angina symptoms by improving blood flow to the heart and reducing the heart's oxygen demand. Ranolazine may be used in combination with other medications to control symptoms of angina and improve overall heart function.

How does Ranolazine work?

Ranolazine works by inhibiting certain sodium and calcium channels in the heart cells. This reduces the sodium overload in the heart muscle, helping to prevent an increase in intracellular calcium levels, which in turn reduces the heart's oxygen demand. By improving the heart's efficiency in using oxygen, Ranolazine helps to reduce symptoms of angina (chest pain) and improve exercise tolerance, without significantly affecting heart rate or blood pressure.

Is Ranolazine effective?

Clinical studies have shown that Ranolazine is effective in reducing angina symptoms and improving exercise tolerance in patients with chronic angina. Trials demonstrated that Ranolazine can significantly reduce the frequency of chest pain episodes and improve the overall quality of life without causing major side effects. It has also been shown to be beneficial when used in combination with other angina medications, providing enhanced symptom control and reducing the need for additional treatments.

How does one know if Ranolazine is working?

The benefit of Ranolazine is evaluated by monitoring improvements in angina symptoms, such as reduced chest pain, increased exercise tolerance, and better overall quality of life. Doctors may use exercise stress tests or patient-reported outcomes to assess the medication’s effectiveness. Regular follow-up appointments allow healthcare providers to track symptom changes and adjust treatment if needed.

Directions for Use

What is the usual dose of Ranolazine?

For adults, the usual dose of ranolazine for chronic angina is:

  • Initial Dose: 500 mg taken orally twice daily.
  • Titration: May increase to 1000 mg taken orally twice daily based on clinical response.
  • Maximum Dose: 1000 mg twice daily.

For children, the use of ranolazine has not been established, and dosing should be determined by a healthcare provider.

How do I take Ranolazine?

Ranolazine can be taken with or without food. There are no specific food restrictions while taking this medication. However, it should be swallowed whole, and the tablets should not be crushed or chewed. If you are taking other medications or have any concerns, consult your doctor to avoid any potential interactions or issues. Always follow your healthcare provider’s specific instructions regarding dosage and administration.

For how long do I take Ranolazine?

The typical duration of ranolazine use for chronic angina is generally long-term, as it is intended for ongoing management rather than a short-term treatment. Clinical trials have administered ranolazine for up to 12 weeks, but many patients may continue using it for months or years under a healthcare provider's supervision to maintain control over their symptoms. Regular follow-ups are essential to assess efficacy and adjust dosing as needed.

How long does it take for Ranolazine to start working?

Ranolazine typically starts to show its effects in 1 to 2 weeks, with some patients experiencing noticeable improvements in their angina symptoms, such as reduced chest pain or improved exercise tolerance. However, the full therapeutic benefit may take up to 4 weeks to become evident. It’s important to continue taking the medication as prescribed and follow up with your doctor to monitor progress.

How should I store Ranolazine?

Ranolazine should be stored at room temperature (20°C to 25°C or 68°F to 77°F) in a tightly closed container. Keep it away from moisture, heat, and direct sunlight. Do not store it in the bathroom or places with high humidity. Keep the medication out of reach of children, and dispose of expired or unused tablets properly. Always check the expiration date before use.

Warnings and Precautions

Who should avoid taking Ranolazine?

Ranolazine should be used with caution in patients with liver disease, as it may affect liver function. It is contraindicated in patients with pre-existing QT prolongation or those who are taking medications that significantly affect the QT interval, such as certain antiarrhythmic drugs. It should also be avoided in patients with severe kidney impairment. Additionally, Ranolazine can interact with other drugs that affect CYP3A enzymes and should be used with caution when combined with drugs like antifungals or antibiotics. Always consult a healthcare provider before starting or combining treatments.

Can I take Ranolazine with other prescription drugs?

Ranolazine has several significant prescription drug interactions:

  1. CYP3A inhibitors (e.g., ketoconazole, clarithromycin) can increase Ranolazine levels, increasing the risk of side effects such as QT prolongation.
  2. CYP3A inducers (e.g., rifampin, St. John’s Wort) can lower Ranolazine levels, reducing its effectiveness.
  3. Antiarrhythmic drugs like amiodarone or dofetilide can increase the risk of QT prolongation when taken with Ranolazine.
  4. Grapefruit and grapefruit juice should be avoided as they can increase Ranolazine blood levels.

Can I take Ranolazine with vitamins or supplements?

Ranolazine has minimal interactions with vitamins or supplements. However, it may interact with supplements that affect CYP3A enzymes, such as grapefruit or grapefruit juice, which can increase Ranolazine levels in the blood, raising the risk of side effects. While St. John’s Wort may reduce the effectiveness of Ranolazine by affecting liver enzymes, most vitamins and mineral supplements do not pose significant interactions. Always consult a healthcare provider before adding new supplements.

Can Ranolazine be taken safely while pregnant?

Ranolazine is classified as a Category C drug during pregnancy, meaning that animal studies have shown potential risks to the fetus, but human studies are limited. While there is no conclusive evidence of harm, it should only be used during pregnancy if the potential benefits outweigh the risks. Pregnant women should consult their doctor before using Ranolazine, especially if they are at risk for heart disease or angina.

Can Ranolazine be taken safely while breastfeeding?

Ranolazine is excreted in breast milk in small amounts, but there is limited data on its safety during lactation. Due to the potential for adverse effects on a breastfeeding infant, it's recommended to either avoid breastfeeding while using Ranolazine or discontinue the medication if the infant is nursing. Mothers should consult their healthcare provider to weigh the risks and benefits of using Ranolazine while breastfeeding.

Is Ranolazine safe for the elderly?

When prescribing ranolazine to elderly patients, consider the following recommendations and warnings for safe use:

  • Cautious Dose Titration: Start at the lowest effective dose due to increased sensitivity and potential for adverse effects, particularly in those over 75 years old.
  • Increased Adverse Events: Elderly patients may experience a higher incidence of side effects, including constipation, nausea, hypotension, and vomiting.
  • Monitor Renal Function: Regularly assess renal function, as age-related decline may increase ranolazine exposure and risk of adverse effects.
  • Drug Interactions: Be cautious of potential interactions with other medications, especially CYP3A4 inhibitors.

Is it safe to exercise while taking Ranolazine?

Exercise is safe while on Ranolazine, but avoid overexertion, as dizziness may occur. If you feel lightheaded during exercise, stop and consult your doctor for guidance.

Is it safe to drink alcohol while taking Ranolazine?

Drinking alcohol may worsen Ranolazine's side effects like dizziness. It's advisable to limit alcohol while on this medication.