Selective Aldosterone Receptor Antagonist

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

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II. Indications

  1. Congestive Heart Failure
  2. Hypertension

III. Mechanism

  1. Selective Aldosterone Receptor Antagonist
  2. More selective for aldosterone than Spironolactone
  3. These agents are also Potassium-Sparing Diuretics

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
    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)
    1. Significantly increases Eplerenone levels

IX. 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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Related Studies

Cost: Medications

eplerenone (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
EPLERENONE 25 MG TABLET Generic $1.88 each
EPLERENONE 50 MG TABLET Generic $2.07 each
inspra (on 6/1/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
INSPRA 25 MG TABLET Generic $1.88 each
INSPRA 50 MG TABLET Generic $2.07 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.

Ontology: Aldosterone Antagonists (C0002007)

Definition (CSP) agent that counteracts or opposes the action of aldosterone.
Concepts Pharmacologic Substance (T121)
MSH D000451
SnomedCT 346312000, 372603003
English Antagonists, Aldosterone, aldosterone inhibitor, ALDOSTERONE ANTAG, Aldosterone Antagonists, aldosterone inhibitors, aldosterone antagonists, aldosterone antagonist, antagonist aldosterone, Aldosterone antagonists, Aldosterone antagonists (product), Aldosterone antagonists (substance), Aldosterone antagonist (substance), Aldosterone antagonist
Spanish antagonista de la aldosterona (sustancia), antagonista de la aldosterona, antagonistas de la aldosterona (sustancia), antagonistas de la aldosterona, Antagonistas de Aldosterona, antagonista de aldosterona (producto), antagonista de aldosterona, antagonistas de aldosterona (producto), antagonistas de aldosterona (sustancia), antagonistas de aldosterona
French Antagonistes de l'aldostérone, Anti-aldostérones, Antialdostérones
Swedish Aldosteronblockerare
Finnish Aldosteroniantagonistit
Czech antagonisté aldosteronu, aldosteron - antagonisté
German Aldosteronantagonisten, Aldosteron-Antagonisten
Italian Antagonisti dell'aldosterone
Croatian ALDOSTERONSKI ANTAGONISTI
Norwegian Aldosteronantagonister
Portuguese Antagonistas da Aldosterona
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: eplerenone (C0961485)

Definition (NCI) A selective aldosterone receptor antagonist. Eplerenone binds to the mineralocorticoid receptor and blocks the binding of aldosterone, thereby decreasing sodium resorption and subsequently increasing water outflow. This leads to a decrease in blood pressure. Eplerenone is used in the treatment of hypertension and congestive heart failure.
Concepts Pharmacologic Substance (T121) , Steroid (T110)
MSH C414690
SnomedCT 398699008, 407010008
English 9,11alpha-Epoxy-17-hydroxy-3-oxo-17alpha-pregn-4-ene-7alpha,21-dicarboxylic acid, gamma-lactone, Methyl Ester, eplerenone (medication), eplerenon, EPLERENONE, eplerenone [Chemical/Ingredient], eplerenone, 9,11-epoxy-7-(methoxycarbonyl)-3-oxo-17-pregn-4-ene-21,17-carbolactone, Eplerenone (product), Eplerenone (substance), Eplerenone
Spanish eplerenona (producto), eplerenona (sustancia), eplerenona
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: Inspra (C1144054)

Concepts Pharmacologic Substance (T121) , Steroid (T110)
MSH C414690
English Inspra, Pfizer brand of eplerenone, inspra
Derived from the NIH UMLS (Unified Medical Language System)

Related Topics in Pharmacology

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