Mineralocorticoid receptor antagonists · Cardiovascular
Eplerenone
Inspra®(brand names vary by market)
Spironolactone without the gynecomastia, at a price.
Mechanism
Selective mineralocorticoid receptor antagonist: the aldosterone blockade without meaningful androgen or progesterone receptor binding.
Open the interactive pathwayIndications
- Heart failure with reduced ejection fraction
- Post myocardial infarction with left ventricular dysfunction
- Resistant hypertension
Formulations
Dosing concepts
Switching
The usual reason to be on it is spironolactone-induced breast symptoms; the potassium risk transfers unchanged and so does the monitoring schedule.
Interactions
A CYP3A4 substrate, so strong inhibitors raise exposure considerably and change the safe dose.
Concepts, not prescribing instructions. Practice numbers live in current references and local protocols.
Pharmacokinetics
- Bioavailability
- ~70%
- Half-life
- 4 to 6 h
- Elimination
- hepatic: CYP3A4; no active metabolites, unlike spironolactone
- Protein binding
- ~50%
Adverse effects
- Hyperkalemiacommon & serious
- Dizzinesscommon
- Acute kidney injury when volume-depleteserious
Contraindications & precautions
Contraindications
- Hyperkalemia
- Severe renal impairment
- Strong CYP3A4 inhibitors
Precautions
- RAAS blockade
- Diarrhoeal illness
- Moderate CYP3A4 inhibitors
Interactions
Monitoring
Potassium and creatinine
Identical schedule to spironolactone · Baseline, 1 week, 4 weeks, then periodically
Blood pressure
Effect
Counselling points
- Blood tests soon after starting and after any change.
- Hold it and seek advice if you have vomiting or diarrhoea.
- Avoid potassium salt substitutes.
- Avoid grapefruit juice and tell us before starting any new antifungal or antibiotic.
Clinical pearls
- Being selective buys freedom from gynecomastia and nothing else. Every potassium precaution that applies to spironolactone applies here in full.
References & review
- Eplerenone product monograph (consult the current version for your market) (monograph)
- Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed. (reference-work)
Last reviewed 2026-08-16 · jurisdiction: global · drug information changes; verify against current references before practice use.