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Aldosterone antagonist

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In pharmacology, aldosterone antagonists are "compounds which inhibit or antagonize the biosynthesis or actions of aldosterone."[1] Their actions affect the larger renin-angiotensin system.

Availability[edit]

Costs of (prices from Drugstore.com 2/2011)
Drug Size Cost per 90 pills
Eplerenone (Inspra brand) 50 mg $405.09
Eplerenone (generic) 50 mg $275.99
Spironolactone (Aldactone brand) 25 mg $96.97
Spironolactone (generic) 25 mg $29.97
  • Canrenone
  • Drospirenone
  • Eplerenone. Compared to spironolactone, eplerenone is eplerenone is more selective the mineralocorticoid receptor than than androgen and progesterone receptors.[2]
  • Spironolactone

Uses[edit]

Heart failure[edit]

Randomized controlled trials of aldosterone antagonist for heart failure.
Trial Patients Intervention Comparison Outcome Results Drug toxicity
Intervention Control
EMPHASIS-HF[5]
2010		 2737 patients
• EF≤35%
• NYHA Class II		 eplerenone up to 50 mg/day Placebo mortality at 21 months 12.5% 15.5% HR=0.76 (95% CI: 0.62 - 0.93) (P=0.008)
(stopped early)		 • > 5.5 meq/dl = 11.8%
• Mean potassium increase = 0.16 mmol/L
EPHESUS[2]
2003		 6642 patients
• Clinical CHF
• ≤ 2 weeks after myocardial infarction
• ≤ 40 percent ejection fraction		 eplerenone up to 50 mg/day Placebo mortality at 24 months 14% 17% RR=0.85 (P=0.008) • "Serious hyperkalemia" (≥6.0)= 5.5%
• Median potassium increase = 0.30 mmol/L
RALES[6]
1999		 1663 patients
• EF≤35%
• NYHA Class III/IV		 spironolactone 25 mg/day Placebo mortality at 24 months 35% 46% RR=0.70 (95% CI: 0.60 to 0.82) P<0.001
(stopped early)		 • "Serious hyperkalemia" = 2%
• Median potassium increase = 0.30 mmol/L
• Gynecomastia or breast pain = 10%

Side effects[edit]

References[edit]

  1. ↑ Anonymous (2023), Aldosterone antagonist (English). Medical Subject Headings. U.S. National Library of Medicine.
  2. ↑ 2.0 2.1 Pitt B, Remme W, Zannad F, Neaton J, Martinez F, Roniker B et al. (2003). "Eplerenone, a selective aldosterone blocker, in patients with left ventricular dysfunction after myocardial infarction.". N Engl J Med 348 (14): 1309-21. DOI:10.1056/NEJMoa030207. PMID 12668699. Research Blogging. Review in: J Fam Pract. 2003 Aug;52(8):598-9 Review in: ACP J Club. 2003 Sep-Oct;139(2):32
  3. ↑ Navaneethan SD, Nigwekar SU, Sehgal AR, Strippoli GF (2009). "Aldosterone antagonists for preventing the progression of chronic kidney disease.". Cochrane Database Syst Rev (3): CD007004. DOI:10.1002/14651858.CD007004.pub2. PMID 19588415. Research Blogging.
  4. ↑ Brown J, Farquhar C, Lee O, Toomath R, Jepson RG (2009). "Spironolactone versus placebo or in combination with steroids for hirsutism and/or acne.". Cochrane Database Syst Rev (2): CD000194. DOI:10.1002/14651858.CD000194.pub2. PMID 19370553. Research Blogging.
  5. ↑ Zannad F, McMurray JJ, Krum H, van Veldhuisen DJ, Swedberg K, Shi H et al. (2011). "Eplerenone in patients with systolic heart failure and mild symptoms.". N Engl J Med 364 (1): 11-21. DOI:10.1056/NEJMoa1009492. PMID 21073363. Research Blogging.
  6. ↑ Pitt B, Zannad F, Remme WJ, Cody R, Castaigne A, Perez A et al. (1999). "The effect of spironolactone on morbidity and mortality in patients with severe heart failure. Randomized Aldactone Evaluation Study Investigators.". N Engl J Med 341 (10): 709-17. DOI:10.1056/NEJM199909023411001. PMID 10471456. Research Blogging.
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