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Eplerenone

INSPRA

What it isSelective aldosterone receptor antagonist; heart failure and resistant hypertension.

Why this oneMortality benefit in HFrEF without the gynecomastia spironolactone causes, because it does not bind androgen receptors.

What limits itHyperkalemia is the limiting toxicity. CYP3A4-dependent, so strong inhibitors are contraindicated; weaker than spironolactone per milligram.

FDA-approved for

Off-label

FDA label

FDA dosingPopulationStartTargetMax
Hypertensionadult50 mg QD50 mg BID if inadequate response50 mg BID (100 mg/day)

Titration Allow ~4 weeks for full effect before increasing 50 mg QD to 50 mg BID.

Renal Contraindicated at CrCl <=30 mL/min (all patients); for hypertension also contraindicated at CrCl <50 mL/min or serum Cr >2.0 mg/dL (M) / >1.8 mg/dL (F).

Hepatic Undefined

With a concomitant moderate CYP3A inhibitor (hypertension): initiate 25 mg QD; for inadequate BP response may increase to max 25 mg BID.

Instructions

Contraindications

Cautions

Adverse reactions

Pregnancy Insufficient human data; animal studies show no adverse developmental effects at 31–32× human exposure.

Lactation Undefined

NO BOXED WARNINGS

Principal riskHyperkalemia

Cost, est. cash$5–$150/month

Generic entry2008

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4
Overdose danger3 / 4
Weight-gain liability0 / 4
Sedation liability0 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk2 / 4

Legacy pregnancy categoryB

Defining liabilityHyperkalemia and kidney dysfunction, especially with RAAS blockers or CYP3A inhibitors.

Mechanism of action: Eplerenone ballicule

Eplerenone ballicule: receptor binding, kinetics and half-life diagram

Open Eplerenone in the interactive console ↗

Memory aids: mascots and interaction avatars

Eplerenone INSPRA mascot mnemonic cartoon
“E pluribus unum Inspirer”
“INSPRA”ational background
Bananas in bunches → ↑ serum potassium
Eplerenone CYP3A4 substrate avatar
CYP3A4 substrate

Open Eplerenone in the interactive console ↗