2. Composition and Physical and Chemical Properties (3.1/19.)
1 tablet of Eprelenone (China National Pharmaceutical Group) 25.00/50.00/100.00 mg.
C24H30O6 Molecular weight: 414.49. A white crystalline powder with multiple crystalline forms.
3. Mechanism of Action (18.)
Selectively binds to the mineralocorticoid receptor to block aldosterone. Its affinity for glucocorticoid, androgen, and progesterone receptors is less than 1/20 that for the mineralocorticoid receptor. It lowers blood pressure by blocking the effects of aldosterone in non-epithelial tissues such as the kidneys, heart, blood vessels, and brain; it also improves cardiac function and inhibits remodeling in animal models of heart failure. It may cause a sustained increase in plasma renin activity and serum aldosterone levels, but this does not diminish the drug’s efficacy.
4. Indications and Usage
Hypertension:Approved in China: 50–100 mg once daily.
Chronic heart failure (systolic dysfunction, NYHA Class II–IV):Added to standard therapy. Treatment is typically initiated at 25 mg once daily (25 mg every other day for eGFR 30–<50), adjusted according to serum potassium levels; for eGFR ≥50, the dose should not exceed 50 mg/day, and for eGFR 30–<50, it should not exceed 25 mg/day.
5. Contraindications and Precautions (2.)
"Adaptation (General)"
Allergy to any ingredient in this product
Hyperkalemia, or an initial serum potassium level > 5.0 mEq/L
Severe renal impairment (Ccr < 30 mL/min)
Severe hepatic impairment (Child-Pugh Class C)
Currently taking a potassium-sparing diuretic or a mineralocorticoid receptor antagonist
Currently taking itraconazole, voriconazole, posaconazole, ritonavir-containing formulations, cobicistat-containing formulations, ceritinib, ensitrelvir fumarate, or lonafarnib
"Hypertension"
Patients with diabetes who have microalbuminuria or proteinuria
Moderate or severe renal impairment (Ccr < 50 mL/min)
Currently taking potassium supplements (except for potassium iodide used for thyroid protection or to reduce radioactive iodine)
Major side effects include hyperkalemia, headache, dizziness, and nausea. Serum potassium levels must be monitored. For detailed contraindications regarding drug interactions and dosage adjustments, refer to the original Japanese version.
6. Clinical Summary
Chronic Heart Failure EMPHASIS-HF:Cardiovascular death or hospitalization for heart failure: HR 0.63 [0.54–0.74] (p < 0.0001). In the domestic J-EMPHASIS-HF study: HR 0.85 [0.53–1.36].
Hypertension can be treated with this medication alone or in combination with ACE inhibitors, ARBs, CCBs, or beta-blockers; the approved dosage in China is 50–100 mg per day.
The information regarding medications, treatments, or health management contained in this article is compiled from international authoritative medical journals and official clinical literature, and is intended for general science and educational reference only.
The indications, side effects, and contraindications of related medications may vary depending on national regulations and individual physical conditions. Do not blindly take medication on your own or change your treatment plan.
The author and publishing platform assume no legal liability for any medical delays, adverse reactions, or direct or indirect losses caused by the use of the information in this article. All medical decisions should be discussed with your attending physician before being made.
Both blood pressure and heart rate have stabilized completely, my heart doesn't feel as tired, and I feel much more energetic after taking it. Truly a high-quality blood pressure medication!
dicedice Lai –
Both blood pressure and heart rate have stabilized completely, my heart doesn't feel as tired, and I feel much more energetic after taking it. Truly a high-quality blood pressure medication!