Ranexa (ranolazine) is a prescription medication specifically indicated for the treatment of chronic angina. It is used in combination with other antianginal agents, such as amlodipine, beta-blockers, or nitrates, in patients who have not achieved an adequate response with conventional therapy alone. Unlike traditional antianginal medications, Ranexa works through a unique mechanism, inhibiting the late sodium current in cardiac cells, which reduces calcium overload and improves myocardial oxygen supply-demand balance without significantly affecting heart rate or blood pressure. This makes it a valuable option for a broad range of patients, including those who may not tolerate hemodynamic changes associated with other therapies. It is available in extended-release tablet form, designed to provide sustained symptom control.

Features

• Active ingredient: Ranolazine
• Available as extended-release tablets (500 mg and 1000 mg)
• Unique mechanism of action: selective inhibitor of the late sodium current
• Does not cause clinically significant changes in heart rate or blood pressure
• Twice-daily dosing regimen for consistent 24-hour coverage
• Can be used concomitantly with other antianginal medications

Benefits

• Reduces frequency of angina attacks and nitroglycerin use
• Improves exercise tolerance and functional capacity in patients with chronic angina
• Offers a hemodynamically neutral profile, making it suitable for patients with hypotension or bradycardia
• Provides an additional therapeutic option when first-line agents are insufficient or poorly tolerated
• May improve quality of life by enabling greater physical activity with less chest pain
• Extended-release formulation supports adherence and consistent therapeutic effect

Common use

Ranexa is indicated for the treatment of chronic angina in patients who remain symptomatic despite standard antianginal therapy. It is typically prescribed as part of a comprehensive management plan that may include lifestyle modifications (e.g., smoking cessation, dietary changes, exercise) and other pharmacologic agents. It is not intended for use in the acute termination of angina attacks, and sublingual nitroglycerin should remain accessible for breakthrough symptoms. Clinical studies have demonstrated its efficacy in reducing both angina frequency and nitroglycerin consumption, with benefits observed across various patient subgroups, including the elderly and those with comorbid conditions such as diabetes.

Dosage and direction

The recommended starting dose of Ranexa is 500 mg taken orally twice daily. Based on clinical response and tolerability, the dose may be increased to a maximum of 1000 mg twice daily. Tablets should be swallowed whole and must not be crushed, chewed, or split, as this may alter the extended-release properties and increase the risk of adverse effects. Ranexa may be taken with or without food, though consistency in administration relative to meals is advised to minimize variability in absorption. Dose adjustments are recommended in patients with moderate to severe renal impairment (e.g., creatinine clearance <60 mL/min), with a maximum dose of 500 mg twice daily in such cases. Hepatic impairment is a contraindication to use.

Precautions

Patients should be advised that Ranexa may cause QT interval prolongation, although the clinical significance of this effect at therapeutic doses is not fully established. ECG monitoring may be considered in patients with known congenital long QT syndrome, or those taking other drugs that prolong the QT interval. Renal function should be assessed before initiation and periodically during treatment, as ranolazine is excreted renally. Use with caution in patients with moderate renal impairment; it is contraindicated in severe impairment. Patients should be informed that dizziness or syncope may occur, particularly when standing up quickly, and should avoid activities requiring mental alertness until they know how the medication affects them. Grapefruit juice should be avoided due to inhibition of CYP3A metabolism and potential increases in ranolazine exposure.

Contraindications

Ranexa is contraindicated in patients with:

• Severe renal impairment (creatinine clearance <30 mL/min)
• Hepatic impairment (Child-Pugh Class B or C)
• Concomitant use with strong CYP3A inhibitors (e.g., ketoconazole, clarithromycin, ritonavir)
• Concomitant use with CYP3A inducers (e.g., rifampin, phenobarbital)
• Known hypersensitivity to ranolazine or any component of the formulation

Possible side effect

Common adverse reactions (≥2% and more frequent than placebo) include:

• Dizziness
• Headache
• Constipation
• Nausea

Less common but potentially serious side effects may include:

• QT prolongation
• Syncope
• Acute renal failure (in susceptible individuals)
• Hypoesthesia or paresthesia

Patients should report any persistent or severe symptoms to their healthcare provider. In clinical trials, discontinuation due to adverse events was comparable to placebo.

Drug interaction

Ranexa is primarily metabolized by CYP3A and to a lesser extent by CYP2D6. Significant interactions may occur with:

• Strong CYP3A inhibitors (e.g., ketoconazole, itraconazole, clarithromycin): Contraindicated due to大幅 increased ranolazine exposure.
• Moderate CYP3A inhibitors (e.g., diltiazem, verapamil, erythromycin): Limit Ranexa to 500 mg twice daily.
• CYP3A inducers (e.g., rifampin, carbamazepine): Contraindicated due to reduced efficacy.
• P-gp inhibitors (e.g., cyclosporine): May increase ranolazine levels.
• Drugs that prolong QT interval (e.g., sotalol, quinidine): additive effect possible; monitor ECG.
• Digoxin: Ranexa may increase digoxin levels; monitor concentrations.
• Simvastatin: Ranexa may increase simvastatin exposure; limit simvastatin to 20 mg daily.

Missed dose

If a dose is missed, it should be taken as soon as possible unless it is nearly time for the next dose. In that case, the missed dose should be skipped and the regular dosing schedule resumed. Doubling the dose to make up for a missed dose is not recommended.

Overdose

Symptoms of overdose may include severe nausea, vomiting, drowsiness, paresthesia, and syncope. QT prolongation and hypotension are also possible. There is no specific antidote; treatment should be supportive and symptomatic. Hemodialysis is unlikely to be effective due to high protein binding. In case of suspected overdose, contact a poison control center or seek emergency medical attention.

Storage

Store Ranexa tablets at room temperature (20–25°C or 68–77°F), with excursions permitted between 15–30°C (59–86°F). Keep in the original container, tightly closed, and protect from moisture and light. Keep out of reach of children and pets. Do not use after the expiration date printed on the packaging.

Disclaimer

This information is intended for educational purposes and does not replace professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before starting or changing any medication regimen. Individual patient needs and responses may vary. Only a licensed healthcare professional can determine the appropriate use of Ranexa based on a comprehensive medical evaluation.

Reviews

Clinical trials and post-marketing experience have demonstrated that Ranexa is generally well-tolerated and effective in reducing angina symptoms in appropriate patient populations. Many patients report decreased frequency of angina attacks and improved exercise capacity. Some note the convenience of twice-daily dosing and the lack of significant hemodynamic effects. Criticisms occasionally include gastrointestinal side effects or cost considerations. Overall, it is regarded as a valuable addition to antianginal therapy, particularly for patients not adequately controlled on first-line agents.