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
| 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
- Ascites
- Chronic kidney disease[3]
- Hirsutism[4]
- Hypertension
- Prevention of hypokalemia caused by thiazide diuretic therapy
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
- ↑ Anonymous (2023), Aldosterone antagonist (English). Medical Subject Headings. U.S. National Library of Medicine.
- ↑ 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
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.