Limeitong Eplerenone Tablets

1. Indications and Usage
Heart Failure Post-Myocardial Infarction: Improves survival in adult patients with left ventricular ejection fraction (LVEF) ≤40% and symptomatic stable heart failure following acute myocardial infarction.
Hypertension: Treatment of essential hypertension in adults to lower blood pressure and reduce cardiovascular risks.
2. Dosage and Administration
Route of Administration: Oral administration ONLY.
Recommended Dosage:
Heart Failure: Initial dose of 25 mg once daily. Titrate to 50 mg once daily within 4 weeks based on tolerance.
Hypertension: Initial dose of 50 mg once daily. May increase to 50 mg twice daily if response is inadequate. Maximum daily dose is 100 mg.
Critical Administration Instructions:
Dosing Consistency: Administer at the same time each day, with or without food.
Renal Impairment: Contraindicated if creatinine clearance ≤30 mL/min. Use with caution and monitor electrolytes closely if CrCl is >30 mL/min.
Monitoring: Monitor serum potassium and creatinine before initiation, at 1 week and 1 month after starting, then periodically thereafter.
3. Mechanism of Action
Selective Antagonism: Eplerenone is a selective aldosterone receptor antagonist.
Pathway Inhibition: It competitively inhibits the binding of aldosterone to mineralocorticoid receptors in the heart, kidneys, and blood vessels.
Physiological Effects: This blockade reduces sodium reabsorption and potassium excretion, attenuates myocardial fibrosis, and lowers blood pressure.
4. Safety and Warnings
Hypersensitivity: Contraindicated in patients with known hypersensitivity to eplerenone or its excipients.
Hypokalemia: Use with caution in patients with a history of hypokalemia.
Hyperkalemia Risk: The risk of hyperkalemia increases significantly when co-administered with ACE inhibitors, ARBs, potassium-sparing diuretics, or in patients with diabetes and renal impairment.
Pregnancy and Lactation: Contraindicated during pregnancy. Safety during breastfeeding has not been established.
5. Adverse Reactions and Clinical Research
Most Common Adverse Reactions:
Heart Failure: Hyperkalemia and increased creatinine.
Hypertension: Headache, dizziness, palpitations, and abdominal pain.
Clinical Research Highlights:
EMPHASIS-HF: Demonstrated significant reduction in cardiovascular death and heart failure hospitalization in patients with chronic heart failure.
EALOR-HF: Confirmed significant blood pressure reduction compared to placebo in hypertensive patients.
6. Drug Interactions
CYP3A4 Inhibitors: Strong inhibitors (e.g., ketoconazole, ritonavir, clarithromycin) increase eplerenone exposure and are contraindicated. Moderate inhibitors (e.g., verapamil, erythromycin) require dose reduction and close monitoring.
Potassium-Sparing Agents: Concomitant use with potassium supplements, salt substitutes, or other aldosterone antagonists increases the risk of hyperkalemia.
NSAIDs: May impair the antihypertensive effect and increase the risk of hyperkalemia and renal impairment.
7. Pharmaceutical Information
Chemical Composition: Active Ingredient: Eplerenone. Excipients: Lactose monohydrate, microcrystalline cellulose, magnesium stearate, etc.
Appearance: Film-coated tablets (e.g., yellow diamond-shaped tablets).
Packaging: Blister packaging (e.g., 30 or 100 tablets per box).
Storage: Store at 25°C (77°F); protect from moisture.