Eplerenone CAS NO.107724-20-9
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Category：Active Pharmaceutical Ingredients Own Brand：MT /MOQ:100KG /From China/ B2B only.
Introduction
Catalog ID80017761
CAS NO.107724-20-9
Purity 95%
MDL NumberMFCD07783647
Molecular FormulaC24H30O6
Molecular Weight414.4914
Melting point: 238~243°C
| Aspect | Details |
|---|---|
| Mechanism of Action | Eplerenone is an aldosterone receptor antagonist that selectively binds to mineralocorticoid receptors, blocking aldosterone binding. This inhibits aldosterone-mediated effects such as sodium reabsorption and potassium excretion, reducing blood pressure and myocardial fibrosis. |
| Indications | – Approved for heart failure with reduced ejection fraction (EF ≤ 40%) following acute myocardial infarction (MI) and for hypertension, either alone or in combination with other agents.<br>- Used off-label for general heart failure patients with EF ≤ 35% and primary aldosteronism. |
| Pharmacokinetics | – Absorption: Oral administration with peak plasma concentrations reached in 1.5 hours.<br>- Distribution: Volume of distribution is 43 to 90 L.<br>- Metabolism: Primarily metabolized by CYP3A4; no active metabolites identified.<br>- Elimination: Half-life is 4 to 6 hours.<br>- Excretion: Renal (67%) and fecal (32%). |
| Administration | – Heart Failure: Start at 25 mg once daily, titrate to 50 mg once daily after 4 weeks if potassium ≤ 5 mEq/L and eGFR ≥ 50 mL/min/1.73 m².<br>- Hypertension: May require twice-daily dosing for optimal effect.<br>- Renal Impairment: Use with caution in CrCl 31 to 50 mL/min; contraindicated in CrCl < 30 mL/min. |
| Storage Conditions | Store at room temperature (15° to 30°C; 59° to 86°F). Protect from moisture. |
| Special Considerations | – Increased risk of hyperkalemia, especially with CYP3A4 inhibitors.<br>- Monitor potassium levels and renal function regularly.<br>- Use with caution in patients with renal or hepatic impairment.<br>- Hemodialysis does not remove eplerenone |
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