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

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

Heart failure

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

References

  1. Anonymous (2015), 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.