Ranexa: Advanced Angina Relief with Ranolazine
| Product dosage: 500mg | |||
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Ranexa (ranolazine) is a prescription medication specifically indicated for the treatment of chronic angina. It represents a distinct therapeutic class, functioning as a late sodium current inhibitor to address the underlying ionic imbalances in cardiac cells during ischemia. Unlike traditional antianginal agents such as beta-blockers or calcium channel blockers, Ranexa does not significantly lower heart rate or blood pressure, making it a suitable option for a broader patient population, including those with contraindications to first-line therapies. It is used as part of a comprehensive management plan that includes lifestyle modifications and other cardiovascular medications to reduce angina frequency and improve exercise tolerance.
Features
- Active Ingredient: Ranolazine
- Available Strengths: 500 mg and 1000 mg extended-release tablets
- Pharmacologic Class: Late sodium current inhibitor
- Dosage Form: Oral, extended-release tablet
- Mechanism of Action: Modulates cardiac late sodium influx, reducing intracellular sodium and calcium overload during ischemia
- Prescription Status: Rx-only, requires healthcare provider authorization
Benefits
- Reduces the frequency of angina attacks and the need for sublingual nitroglycerin
- Improves exercise tolerance and time to onset of angina in patients with chronic stable angina
- Exhibits a hemodynamically neutral profile, with no significant effects on heart rate or blood pressure in most patients
- Provides an additive anti-ischemic effect when combined with other antianginal agents like beta-blockers, calcium channel blockers, or nitrates
- May be used in patients with contraindications or intolerance to traditional antianginal therapies
- Offers a twice-daily dosing regimen for patient convenience and adherence
Common use
Ranexa is indicated for the treatment of chronic angina in patients who have not achieved an adequate response with other antianginal drugs. It is typically prescribed as part of a combination regimen. It is not indicated for the treatment of acute anginal episodes, for which sublingual nitrates remain the standard of care. Its use is supported in various patient subgroups, including those with comorbid conditions like diabetes or hypertension, where its neutral hemodynamic effects are particularly advantageous.
Dosage and direction
The recommended initial 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 broken, as this alters the extended-release properties and may increase the risk of adverse effects. Ranexa may be taken with or without food, but consistency in administration with respect to meals is advised to maintain stable plasma concentrations. Dose adjustments are necessary in patients with hepatic impairment, moderate to severe renal impairment, or when co-administered with certain CYP3A inhibitors.
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. Renal function should be assessed before initiation and periodically during treatment, as ranolazine is excreted renally. Use with caution in patients with pre-existing renal impairment. Hepatic impairment can significantly increase ranolazine exposure; it is contraindicated in patients with hepatic cirrhosis. Patients should be monitored for signs of dizziness, constipation, or nausea, which are among the more common side effects. Ranexa is not recommended as first-line therapy for angina.
Contraindications
Ranexa is contraindicated in patients with clinically significant hepatic impairment (Child-Pugh Class B and C). It is also contraindicated in patients taking strong inhibitors of CYP3A4 (e.g., ketoconazole, clarithromycin, nelfinavir) or inducers of CYP3A (e.g., rifampin, phenobarbital, St. John’s Wort), due to the risk of altered plasma levels and potential toxicity or reduced efficacy. Concomitant use with other drugs that prolong the QT interval should be avoided unless the benefit clearly outweighs the risk.
Possible side effect
Common adverse reactions (≥2% and more frequent than placebo) include dizziness, headache, constipation, and nausea. QT interval prolongation (dose-dependent) has been observed. Other reported side effects include dry mouth, vomiting, asthenia, and peripheral edema. Serious but rare adverse effects include syncope, torsades de pointes (in susceptible individuals), and acute renal failure. Patients should report any persistent or severe symptoms to their healthcare provider.
Drug interaction
Ranexa is primarily metabolized by CYP3A and to a lesser extent by CYP2D6. It is a moderate inhibitor of CYP3A and CYP2D6, and a substrate of P-glycoprotein. Co-administration with strong CYP3A inhibitors (e.g., ketoconazole, itraconazole, clarithromycin) is contraindicated. Moderate CYP3A inhibitors (e.g., diltiazem, verapamil, erythromycin) may increase ranolazine levels—dose reduction may be necessary. CYP3A inducers (e.g., rifampin, carbamazepine) may decrease efficacy. Ranexa can increase levels of digoxin, simvastatin, and other CYP3A or 2D6 substrates; monitoring and dose adjustments may be required.
Missed dose
If a dose of Ranexa is missed, the patient should take it as soon as remembered, unless it is almost time for the next scheduled 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 one is not recommended.
Overdose
In case of suspected overdose, supportive measures should be instituted, including ECG monitoring for QT prolongation and arrhythmias. There is no specific antidote for ranolazine overdose. Hemodialysis is unlikely to be effective due to high protein binding and extensive tissue distribution. Management should focus on symptomatic treatment and maintaining vital functions. Contact a poison control center for latest guidance.
Storage
Store Ranexa tablets at room temperature, between 20°C to 25°C (68°F to 77°F), in a tightly closed container. Protect from moisture and light. Keep out of reach of children and pets. Do not use beyond the expiration date printed on the packaging.
Disclaimer
This information is intended for educational purposes and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or before starting any new treatment. Never disregard professional medical advice or delay in seeking it because of something you have read in this document.
Reviews
Clinical trials and post-marketing surveillance have demonstrated that Ranexa is effective in reducing angina frequency and improving exercise tolerance in a significant proportion of patients with chronic stable angina. It is particularly valued for its hemodynamically neutral profile, allowing use in patients with hypotension or bradycardia who cannot tolerate conventional therapies. Some patients report gastrointestinal side effects, but these are often manageable with dose adjustment. Overall, it is considered a valuable addition to the antianginal armamentarium for appropriate patient populations.