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Selective Aldosterone Receptor Antagonist

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

  • Mechanism
  1. Selective Aldosterone Receptor Antagonist
  2. More selective for aldosterone than Spironolactone
  3. These agents are also Potassium-Sparing Diuretics
  • Pharmacokinetics
  1. Liver metabolism to active metabolite (canrenone)
  2. Half-Life: 4-6 hours
  • 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
  • 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)
    1. Significantly increases Eplerenone levels
  • 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]