Pharmacology · Potassium-sparing diuretics
Eplerenone !
A selective aldosterone blocker that improves survival in heart failure after a heart attack, with fewer hormonal effects than spironolactone.
Updated 2026-11-01
The figure shows eplerenone in the ligand-binding domain of the human mineralocorticoid receptor.
Mechanism of action
Eplerenone binds the mineralocorticoid receptor and blocks aldosterone, with little binding to glucocorticoid, progesterone and androgen receptors. In the collecting duct less sodium is reabsorbed and less potassium is secreted; in the heart and vessels it reduces aldosterone-driven remodelling.
- Eplerenone selectively blocks the aldosterone receptor
- Less sodium reabsorbed, less potassium secreted
- Less aldosterone-driven heart remodelling
- Few hormonal effects: little gynecomastia
Pharmacokinetics
- Absorption
- Absorbed by mouth; food does not change absorption
- Metabolism
- By CYP3A4, with no active metabolites
- Half-life
- 3 to 6 hours
- Onset and duration
- Steady state within about 2 days
Indications
- Heart failure with reduced ejection fraction after myocardial infarction, to improve survival Heart failure →
- High blood pressure Arterial hypertension →
Adverse effects
Common
- Hyperkalaemia
- Dizziness
- Raised creatinine
- Cough and diarrhoea
Contraindications
- High serum potassium at the start
- Severe kidney impairment
- Strong CYP3A inhibitors (e.g. ketoconazole, itraconazole, clarithromycin, ritonavir)
- In hypertension: type 2 diabetes with microalbuminuria, reduced kidney function, potassium supplements or potassium-sparing diuretics
Key interactions
- Strong CYP3A inhibitors
- Much higher eplerenone levels; contraindicated
- Moderate CYP3A inhibitors (e.g. verapamil, erythromycin, fluconazole)
- Higher levels; a lower exposure is used
- ACE inhibitors, ARBs or potassium supplements
- More hyperkalaemia
- Lithium
- Risk of lithium toxicity
What is monitored
- Serum potassium before starting, in the first week, at one month and then regularly
- Kidney function
- Blood pressure
Nursing care
- Before giving: potassium and kidney function; hold and report if potassium is high.
- Review all medicines for CYP3A inhibitors and potassium-raising drugs.
- Watch for signs of hyperkalaemia: weakness, slow pulse, palpitations.
- Teach: avoid potassium salt substitutes, tell the team about any new medicine, report weakness.
Pregnancy and breastfeeding
Human data are limited; used only if the benefit justifies the risk.
Test yourself
Think of the answer, then tap the question to see it.
How does eplerenone differ from spironolactone?
It is more selective for the mineralocorticoid receptor, so it causes fewer hormonal effects such as gynecomastia.
Why are strong CYP3A inhibitors contraindicated with eplerenone?
Eplerenone is cleared mainly by CYP3A4; strong inhibitors raise its levels sharply and the risk of hyperkalaemia.
In which heart failure setting does eplerenone improve survival?
Symptomatic heart failure with reduced ejection fraction after a myocardial infarction.
Related drugs
Related conditions
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Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: DailyMed - EPLERENONE tablet, film coated (DailyMed (U.S. National Library of Medicine), 2026); Eplerenone: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026); RCSB PDB - 5MWY: The structure of MR in complex with eplerenone. (RCSB Protein Data Bank, 2026).
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Representative model, for educational purposes only.