Eplerenone

Aka: Eplerenone, Inspra, Selective Aldosterone Receptor Antagonist, Selective Aldosterone Blocker, Aldosterone Antagonist

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II. Indications

  1. Congestive Heart Failure
  2. Hypertension

III. Mechanism

  1. Eplerenone and Spironolactone are Potassium-Sparing Diuretics (as are Triamterene and Amiloride)
  2. Eplerenone and Spironolactone are also both Selective Aldosterone Receptor Antagonists
    1. Eplerenone is more selective for Aldosterone than Spironolactone

IV. Pharmacokinetics

  1. Liver metabolism to active metabolite (canrenone)
  2. Half-Life: 4-6 hours

V. Contraindications

  1. Serum Potassium >5.0 mEq/L
  2. Type II Diabetes Mellitus with Microalbuminuria
  3. Renal Insufficiency
    1. Serum Creatinine >2.5 (GFR <30 ml/min)
    2. Anuria

VI. Dosing

  1. Hypertension
    1. Start: 50 mg orally daily
      1. Decrease starting dose to 25 mg orally daily if using strong Cytochrome P450 3A4 inhibitor
    2. May increase to 50 mg orally twice daily after 4 weeks
  2. Congestive Heart Failure
    1. Start: 25 mg orally daily for 4 weeks (then increase to target dose if tolerated)
    2. Target: 50 mg orally daily

VII. Adverse Effects

  1. Hyperkalemia
  2. Hypertriglyceridemia
  3. Hyponatremia
  4. Dizziness
  5. Fatigue
  6. Diarrhea
  7. Cough
  8. Less Gynecomastia and Erectile Dysfunction than Spironolactone

VIII. Drug Interactions

  1. Increased Serum Potassium (Hyperkalemia risk)
    1. Potassium Supplementation
    2. NSAIDs
    3. ACE Inhibitor
    4. Trimethoprim-Sulfamethoxazole
  2. Digoxin
    1. Increased Digoxin Toxicity risk via increased Digoxin half life
  3. Norepinephrine
    1. Decreases NorepinephrineVasopressor activity
  4. Cytochrome P450 3A4 inhibitors (e.g. Ketoconazole, Itraconazole)
    1. Significantly increases Eplerenone levels
    2. Limit max Eplerenone dose to 25 mg daily or twice daily if used with a strong CYP 3A4 inhibitor

IX. Safety

  1. Pregnancy Category B
  2. Unknown Safety in Lactation

X. Resources

  1. Eplerenone (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=e2a51c12-bdc2-4b3b-8e9e-bf363c2817ed

XI. References

  1. Olson (2020) Clinical Pharmacology, Medmaster, Miami, p. 62-3
  2. Hamilton (2010) Tarason Pocket Pharmacopeia, p. 74
  3. (2003) Lexi-Comp Drug Database
  4. (2003) Med Lett Drugs Ther 45(1156):39-40 [PubMed]
  5. Stier (2003) Heart Dis 5(2):102-18 [PubMed]

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Cost: Medications

eplerenone (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
EPLERENONE 25 MG TABLET Generic $0.65 each
EPLERENONE 50 MG TABLET Generic $0.77 each
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information. GoodRx is another tool for finding lower drug prices.

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