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Selective Aldosterone Receptor Antagonist
Aka: Selective Aldosterone Receptor Antagonist, Selective Aldosterone Blocker, Aldosterone Antagonist, Eplerenone, Inspra
- Indications
- Congestive Heart Failure
- Hypertension
- Mechanism
- Selective Aldosterone Receptor Antagonist
- More selective for aldosterone than Spironolactone
- These agents are also Potassium-Sparing Diuretics
- Pharmacokinetics
- Liver metabolism to active metabolite (canrenone)
- Half-Life: 4-6 hours
- Contraindications
- Serum Potassium >5.0 mEq/L
- Type II Diabetes Mellitus with Microalbuminuria
- Renal Insufficiency
- Serum Creatinine >2.5
- Anuria
- Dosing
- Hypertension
- Start: 50 mg orally daily
- Decrease starting dose to 25 mg orally daily if using strong Cytochrome P450 3A4 inhibitor
- May increase to 50 mg orally twice daily after 4 weeks
- Congestive Heart Failure
- Start: 25 mg orally daily for 4 weeks (then increase to target dose if tolerated)
- Target: 50 mg orally daily
- Adverse Effects
- Hyperkalemia
- Hypertriglyceridemia
- Hyponatremia
- Dizziness
- Fatigue
- Diarrhea
- Cough
- Less Gynecomastia and Erectile Dysfunction than Spironolactone
-
Drug Interactions
- Increased Serum Potassium (Hyperkalemia risk)
- Potassium Supplementation
- NSAIDs
- ACE Inhibitor
- Trimethoprim-Sulfamethoxazole
- Digoxin
- Increased Digoxin Toxicity risk via increased Digoxin half life
- Norepinephrine
- Decreases NorepinephrineVasopressor activity
- Cytochrome P450 3A4 inhibitors (e.g. Ketoconazole)
- Significantly increases Eplerenone levels
- References
- Olson (2020) Clinical Pharmacology, Medmaster, Miami, p. 62-3
- Hamilton (2010) Tarason Pocket Pharmacopeia, p. 74
- (2003) Lexi-Comp Drug Database
- (2003) Med Lett Drugs Ther 45(1156):39-40 [PubMed]
- Stier (2003) Heart Dis 5(2):102-18 [PubMed]