Aldosterone antagonist

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This editable Main Article is under development and subject to a disclaimer.

[edit intro]

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.

## Contents

* 1 Availability
* 2 Uses
* 2.1 Heart failure
* 3 Side effects
* 4 References

## Availability[edit]

Costs of (prices from Drugstore.com 2/2011)  Drug | Size | Cost per 90 pills

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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]

* Ascites
* Chronic kidney disease[3]
* Hirsutism[4]
* Hypertension
* Prevention of hypokalemia caused by thiazide diuretic therapy

### Heart failure[edit]

* Heart failure

Randomized controlled trials of aldosterone antagonist for heart failure.  Trial | Patients | Intervention | Comparison | Outcome | Results | Drug toxicity

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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]

* Hyperkalemia
* Gynecomastia

## References[edit]

1. ↑ Anonymous (2025), 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.