Eplerenone

ATC code

C03DA04

Therapeutic class

Aldosterone antagonist and potassium-sparing agent · Aldosterone antagonist

Forms

film-coated tablet

Brand names

Elecor (ES) · Inspra (US)

Overall confidence

medium

Regulatory sources consulted

Approved indications

Add-on to standard therapy (including beta-blockers) to reduce the risk of cardiovascular morbidity and mortality in stable patients with left ventricular dysfunction (LVEF ≤ 40%) and clinical evidence of heart failure after a recent myocardial infarction.
Add-on to standard optimal therapy to reduce the risk of cardiovascular morbidity and mortality in adult patients with (chronic) heart failure of NYHA Class II and left ventricular systolic dysfunction (LVEF ≤ 30%).
Treatment of primary aldosteronism, especially in bilateral forms not suitable for surgery. · off-label

Contraindications

Absolute

Serum potassium > 5.0 mmol/L at initiation.
Severe renal impairment (eGFR < 30 mL/min/1.73 m²).
Severe hepatic impairment (Child-Pugh Class C).
Concomitant use of potent CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, ritonavir).
Concomitant use of potassium-sparing diuretics.

Clinical warnings

Major warning · Hyperkalemia: Significant risk, especially in patients with renal impairment, diabetes with proteinuria, or on concomitant ACEi/ARB therapy. Monitor serum potassium regularly. — EMA SPC

Drug interactions

HighKetoconazoleJ02AB02
Mechanism: Potent inhibition of eplerenone metabolism via CYP3A4, resulting in a ~5-fold increase in exposure (AUC).
Recommendation: Concomitant use is contraindicated.
EMA SPC
ModerateACE Inhibitors and Angiotensin Receptor Blockers (ARBs)C09
Mechanism: Additive pharmacodynamic effect increasing the risk of hyperkalemia, especially in patients with renal dysfunction.
Recommendation: Monitor serum potassium closely, especially at initiation and upon dose changes. The triple combination of ACEi + ARB + eplerenone is contraindicated.
EMA SPC

Adverse events

Common (≥1%)

hyperkalemia · hypotension · dizziness · diarrhea · increased creatinine

Rare but serious

acute renal failure · angioedema · gynecomastia

Pregnancy and lactation

FDA category: Not assigned

No adequate data in pregnancy. Use only if the potential benefit justifies the potential risk to the fetus. It is unknown if excreted in human milk; a decision should be made whether to discontinue nursing or the drug.

Recent literature (PubMed)

Executive summary of the Spanish consensus for the diagnosis, management, and follow-up of primary hyperaldosteronism.
Araujo-Castro M, et al. · Endocrinol Diabetes Nutr (Engl Ed) · 2024 · Relevance 5/5
Resumen ejecutivo del consenso español multidisciplinar sobre el hiperaldosteronismo primario (HP). Subraya que el HP es la causa más común de hipertensión secundaria y está infradiagnosticado. Recomienda un diagnóstico precoz y un tratamiento adecuado, incluyendo antagonistas del receptor mineralocorticoide como la eplerenona, para reducir la morbimortalidad cardiometabólica.
Primary aldosteronism: Practical recommendations for treatment and follow-up.
Araujo-Castro M, et al. · Hipertens Riesgo Vasc · 2023 · Relevance 4/5
Revisión que proporciona recomendaciones prácticas para el manejo del hiperaldosteronismo primario (HP). Destaca el uso de antagonistas del receptor mineralocorticoide (ARM), como la eplerenona, como tratamiento principal para las formas bilaterales de HP, con el objetivo de revertir los efectos cardiovasculares adversos y normalizar la presión arterial y el potasio.