eplerenone
Brand: Inspra
Prototype: spironolactone
Drug Class: mineralocorticoid receptor antagonist
Drug Family: diuretic
Subclass: selective steroidal MRA
Organ Systems: cardiovascularrenal
Mechanism of Action
Selective MRA with no affinity for androgen or progesterone receptors; reduces sodium retention and ventricular remodeling post-MI.
mineralocorticoid receptor (aldosterone receptor)
Indications
- HFrEF post-MI (EPHESUS)
- hypertension (adjunct)
Contraindications
- hyperkalemia
- severe renal impairment
- strong CYP3A4 inhibitors
- DM with microalbuminuria + HCTZ/ACEi/ARB combination
Adverse Effects
Common
- hyperkalemia
- dizziness
- diarrhea
- fatigue
Serious
- life-threatening hyperkalemia
Pharmacokinetics (ADME)
| Absorption | 69% oral, not affected by food |
| Distribution | moderate |
| Metabolism | extensive hepatic CYP3A4 |
| Excretion | renal 67%, fecal 32% |
| Half-life | 4-6 hours |
| Onset | 4 hours |
| Peak | 1.5 hours |
| Duration | 24 hours |
| Protein Binding | 49% |
| Vd | moderate |
Drug Interactions
| Drug / Agent | Mechanism | Severity |
|---|---|---|
| strong CYP3A4 inhibitors (ketoconazole, clarithromycin) | significantly increases eplerenone exposure — contraindicated | major |
| ACE inhibitors/ARBs | additive hyperkalemia | major |
| potassium supplements | additive hyperkalemia | major |
Nursing Considerations
- K+ monitoring same as spironolactone
- No gynecomastia — preferred when antiandrogen effects intolerable
- Avoid strong CYP3A4 inhibitors (contraindicated)
- EPHESUS: reduced mortality post-MI with LV dysfunction
Clinical Pearls
- Selective for aldosterone receptor: no gynecomastia or menstrual side effects
- EPHESUS trial: reduced CV mortality in post-MI LV dysfunction
Safety Profile
Pregnancy avoid
Lactation avoid
Renal Adjustment Required
Hepatic Adjustment Required
TDM Not required
Concordance Terms
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