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.
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| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Hypertension | adult | 50 mg QD | 50 mg BID if inadequate response | 50 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.
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
Legacy pregnancy categoryB
Defining liabilityHyperkalemia and kidney dysfunction, especially with RAAS blockers or CYP3A inhibitors.

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