Ranexa: Advanced Angina Relief for Chronic Chest Pain
Ranexa
| Product dosage: 500mg | |||
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Ranexa (ranolazine) is an FDA-approved antianginal medication specifically designed for the treatment of chronic angina pectoris. It represents a distinct class of therapeutic agents that work via inhibition of the late sodium current in cardiac cells, leading to a reduction in intracellular calcium overload—a key mechanism in myocardial ischemia. Unlike traditional antianginal drugs such as beta-blockers or calcium channel blockers, Ranexa does not significantly affect heart rate or blood pressure, making it a suitable option for a broader patient population, including those with contraindications to conventional therapies. Its unique mechanism offers an effective adjunct or alternative for patients who remain symptomatic despite standard treatment regimens.
Features
- Active ingredient: Ranolazine
- Available in extended-release tablets: 500 mg and 1000 mg
- Mechanism: Late sodium current inhibitor
- Formulation: Designed for twice-daily dosing
- Prescription-only medication
- Not associated with hemodynamic effects such as bradycardia or hypotension
Benefits
- Reduces frequency of angina episodes and nitroglycerin use
- Improves exercise tolerance and functional capacity in patients with chronic angina
- Does not cause clinically significant changes in heart rate or blood pressure
- Suitable for use in combination with other antianginal agents
- May be used in patients with comorbidities where beta-blockers or calcium channel blockers are contraindicated
- Provides an alternative mechanism of action for patients unresponsive to traditional therapies
Common use
Ranexa is indicated for the treatment of chronic angina pectoris in patients who have not achieved an adequate response with other antianginal drugs, or as part of a combination regimen. It is typically prescribed for adults with stable angina who continue to experience symptoms despite optimal management with beta-blockers, calcium channel blockers, and/or nitrates. The medication is not intended for the treatment of acute anginal episodes and should not be used as a rescue medication.
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 may alter the extended-release properties. Ranexa may be taken with or without food, but consistency in administration with regard to meals is advised. Dose adjustments are necessary in patients with moderate to severe renal impairment or hepatic impairment, as detailed in prescribing information.
Precautions
Patients should be advised that Ranexa may cause QT interval prolongation, although the clinical significance of this effect remains under evaluation. Renal function should be assessed prior to initiation and periodically during treatment, as ranolazine and its metabolites are 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 cirrhosis. Patients should be monitored for potential drug interactions, particularly with CYP3A inhibitors and P-gp inhibitors. Dizziness or syncope may occur; patients should avoid driving or operating machinery until they know how Ranexa affects them.
Contraindications
Ranexa is contraindicated in patients with:
- Known hypersensitivity to ranolazine or any component of the formulation
- Cirrhosis of the liver (any degree)
- Concomitant use with strong CYP3A inhibitors (e.g., ketoconazole, clarithromycin, nelfinavir)
- Concomitant use with CYP3A inducers (e.g., rifampin, phenobarbital, St. John’s wort)
- Severe renal impairment (CrCl <30 mL/min)
Possible side effect
Common adverse reactions (≥4% and more frequent than placebo) include:
- Dizziness
- Headache
- Constipation
- Nausea
Other reported side effects:
- QT interval prolongation
- Syncope
- Tinnitus
- Vertigo
- Blurred vision
- Dry mouth
- Abdominal pain
- Palpitations
Serious but rare adverse effects include acute renal failure, thrombocytopenia, and hallucinations. Patients should report any unusual symptoms to their healthcare provider promptly.
Drug interaction
Ranexa is primarily metabolized by CYP3A and is a substrate of P-glycoprotein. Significant interactions include:
- Strong CYP3A inhibitors (e.g., ketoconazole, itraconazole, clarithromycin): Contraindicated—increase ranolazine exposure
- Moderate CYP3A inhibitors (e.g., diltiazem, verapamil, erythromycin): Limit Ranexa to 500 mg twice daily
- CYP3A inducers (e.g., rifampin, carbamazepine, phenytoin): Contraindicated—reduce ranolazine efficacy
- Digoxin: May increase digoxin levels—monitor concentrations
- Simvastatin: May increase simvastatin exposure—limit simvastatin to 20 mg daily
- Metformin: May require dose adjustment—monitor glycemic control
Missed dose
If a dose is missed, it should be taken as soon as remembered, unless it is nearly time for the next scheduled dose. In that case, the missed dose should be skipped and the regular dosing schedule resumed. Patients should not take a double dose to make up for a missed one.
Overdose
Cases of Ranexa overdose have been reported, with symptoms including nausea, vomiting, drowsiness, paresthesia, and syncope. QT prolongation may occur. There is no specific antidote for ranolazine overdose. Management should include supportive care, ECG monitoring, and treatment of symptoms. 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, tightly closed, and protect from moisture and light. Keep out of reach of children and pets.
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 medication. Do not disregard professional medical advice or delay in seeking it because of something you have read here.
Reviews
Clinical trials and post-marketing surveillance have demonstrated Ranexa’s efficacy in reducing angina frequency and improving exercise tolerance. In the CARISA trial, Ranexa significantly increased exercise duration and time to angina onset compared to placebo. The ERICA trial showed a reduction in nitroglycerin use and angina attacks. Patient-reported outcomes often highlight improved quality of life and reduced symptom burden. However, individual responses may vary, and some patients report side effects such as dizziness or constipation. Overall, Ranexa is considered a valuable option in the antianginal armamentarium, particularly for patients with contraindications or inadequate response to conventional therapies.