Ranexa: Advanced Chronic Angina Management with Ranolazine
| Product dosage: 500mg | |||
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Ranexa (ranolazine) is an FDA-approved antianginal medication specifically indicated for the treatment of chronic angina pectoris. Unlike traditional antianginal agents, Ranexa operates through a unique late sodium current inhibition mechanism, which reduces myocardial ischemia without significantly affecting heart rate or blood pressure. It is typically prescribed when symptoms persist despite therapy with other antianginal drugs like beta-blockers, calcium channel blockers, or nitrates. This makes it a valuable option for patients requiring adjunctive therapy to achieve better symptom control and improve exercise tolerance.
Features
- Active ingredient: Ranolazine
- Available in extended-release tablets: 500 mg and 1000 mg
- Unique mechanism of action: selective inhibitor of the late sodium current
- Does not cause clinically significant hemodynamic changes (e.g., hypotension or bradycardia)
- Twice-daily dosing regimen for sustained 24-hour coverage
- Can be used concomitantly with beta-blockers, calcium channel blockers, nitrates, aspirin, statins, and ACE inhibitors
Benefits
- Reduces frequency of angina attacks and nitroglycerin use
- Improves exercise tolerance and time to onset of angina during physical activity
- Provides symptomatic relief without negatively impacting heart rate or blood pressure
- Suitable for long-term management of chronic angina
- May be used in a broad patient population, including those with comorbidities like diabetes
- Offers an alternative mechanism when first-line therapies are insufficient or contraindicated
Common use
Ranexa is indicated for the treatment of chronic angina in patients who have not achieved an adequate response with other antianginal agents. It is used as part of a comprehensive management plan that includes lifestyle modifications and risk factor reduction. It is not intended for use during acute anginal episodes and does not replace sublingual nitroglycerin for immediate symptom relief.
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. Ranexa may be taken with or without food. Dose adjustments are recommended in patients with moderate to severe renal impairment (creatinine clearance <60 mL/min) or in those taking certain CYP3A inhibitors.
Precautions
- Renal impairment: Use with caution and dose adjustment in patients with moderate to severe renal impairment.
- Hepatic impairment: Contraindicated in patients with hepatic cirrhosis.
- QT interval prolongation: Although small increases in QT interval have been observed, Ranexa should be used cautiously in patients with known congenital long QT syndrome or who are taking other QT-prolonging drugs.
- CYP3A inhibitors: Concomitant use with strong CYP3A inhibitors (e.g., ketoconazole, clarithromycin) is contraindicated; moderate inhibitors (e.g., diltiazem) require dose limitation.
- Elderly patients: No specific dose adjustment is required based on age, but greater sensitivity may occur.
Contraindications
- Patients with clinically significant hepatic impairment (Child-Pugh Class B or C)
- Concomitant use with strong CYP3A inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, nefazodone, nelfinavir, ritonavir, indinavir, saquinavir)
- Concomitant use with CYP3A inducers (e.g., rifampin, phenobarbital, phenytoin, carbamazepine, St. John’s wort)
- History of hypersensitivity to ranolazine or any component of the formulation
Possible side effects
Common adverse reactions (≥4% and more frequent than placebo) include:
- Dizziness
- Headache
- Constipation
- Nausea
Less common but serious side effects may include:
- QT prolongation
- Syncope
- Acute renal failure (rare)
- Hallucinations, confusion, or dizziness (particularly in the elderly)
Drug interaction
Ranexa is primarily metabolized by CYP3A and to a lesser extent by CYP2D6. Significant interactions include:
- Strong CYP3A inhibitors: Contraindicated (e.g., ketoconazole, clarithromycin)
- Moderate CYP3A inhibitors: Limit maximum dose to 500 mg twice daily (e.g., diltiazem, verapamil, erythromycin)
- CYP3A inducers: Avoid coadministration (e.g., rifampin, carbamazepine)
- CYP2D6 substrates: May increase levels of drugs metabolized by CYP2D6 (e.g., tricyclic antidepressants, antipsychotics, beta-blockers like metoprolol)
- Digoxin: May increase digoxin levels; monitor concentrations
- Simvastatin: May increase simvastatin exposure; limit simvastatin dose to 20 mg daily
Missed dose
If a dose is missed, it should be taken as soon as remembered unless it is almost time for the next dose. In that case, skip the missed dose and resume the usual dosing schedule. Do not double the dose to make up for a missed one.
Overdose
Cases of overdose have been reported with symptoms including dizziness, nausea, vomiting, diplopia, paresthesia, confusion, and syncope. QT prolongation may also occur. There is no specific antidote for ranolazine overdose. Treatment should be supportive and symptomatic, including ECG monitoring. Hemodialysis is unlikely to be effective due to high protein binding.
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 and protect from moisture. Keep out of reach of children and pets.
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 responses may vary.
Reviews
Clinical studies and post-marketing experience support the efficacy and safety of Ranexa in reducing angina frequency and improving exercise tolerance. Many patients report meaningful symptomatic improvement, particularly those who have not responded adequately to conventional antianginal therapies. However, side effects such as dizziness and constipation may limit use in some individuals. Always discuss benefits and risks with a cardiologist or prescribing physician.