Aldosterone antagonist: Difference between revisions
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In [[pharmacology]], '''aldosterone antagonists''' are "compounds which inhibit or antagonize the biosynthesis or actions of [[aldosterone]]."<ref>{{MeSH}}</ref> Their actions affect the larger [[renin-angiotensin system]]. | In [[pharmacology]], '''aldosterone antagonists''' are "compounds which inhibit or antagonize the biosynthesis or actions of [[aldosterone]]."<ref>{{MeSH}}</ref> Their actions affect the larger [[renin-angiotensin system]]. | ||
==Availability== | |||
{| class="wikitable" align="right" | |||
|+ 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 | * Canrenone | ||
* Drospirenone | * Drospirenone | ||
* [[Eplerenone]] | * [[Eplerenone]]. Compared to spironolactone, eplerenone is eplerenone is more selective the mineralocorticoid receptor than than androgen and progesterone receptors.<ref name="pmid12668699">{{cite journal| author=Pitt B, Remme W, Zannad F, Neaton J, Martinez F, Roniker B et al.| title=Eplerenone, a selective aldosterone blocker, in patients with left ventricular dysfunction after myocardial infarction. | journal=N Engl J Med | year= 2003 | volume= 348 | issue= 14 | pages= 1309-21 | pmid=12668699 | doi=10.1056/NEJMoa030207 | pmc= | url=http://www.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&tool=sumsearch.org/cite&retmode=ref&cmd=prlinks&id=12668699 }} [http://www.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&tool=sumsearch.org/cite&retmode=ref&cmd=prlinks&id=12899810 Review in: J Fam Pract. 2003 Aug;52(8):598-9] [http://www.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&tool=sumsearch.org/cite&retmode=ref&cmd=prlinks&id=12954024 Review in: ACP J Club. 2003 Sep-Oct;139(2):32] </ref> | ||
* [[Spironolactone]] | * [[Spironolactone]] | ||
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* [[Ascites]] | * [[Ascites]] | ||
* [[Chronic kidney disease]]<ref name="pmid19588415">{{cite journal| author=Navaneethan SD, Nigwekar SU, Sehgal AR, Strippoli GF| title=Aldosterone antagonists for preventing the progression of chronic kidney disease. | journal=Cochrane Database Syst Rev | year= 2009 | volume= | issue= 3 | pages= CD007004 | pmid=19588415 | * [[Chronic kidney disease]]<ref name="pmid19588415">{{cite journal| author=Navaneethan SD, Nigwekar SU, Sehgal AR, Strippoli GF| title=Aldosterone antagonists for preventing the progression of chronic kidney disease. | journal=Cochrane Database Syst Rev | year= 2009 | volume= | issue= 3 | pages= CD007004 | pmid=19588415 | ||
| url=http://www.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&tool=clinical.uthscsa.edu/cite&email=badgett@uthscdsa.edu&retmode=ref&cmd=prlinks&id=19588415 | doi=10.1002/14651858.CD007004.pub2 }} | | url=http://www.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&tool=clinical.uthscsa.edu/cite&email=badgett@uthscdsa.edu&retmode=ref&cmd=prlinks&id=19588415 | doi=10.1002/14651858.CD007004.pub2 }}</ref> | ||
* [[Hirsutism]]<ref name="pmid19370553">{{cite journal| author=Brown J, Farquhar C, Lee O, Toomath R, Jepson RG| title=Spironolactone versus placebo or in combination with steroids for hirsutism and/or acne. | journal=Cochrane Database Syst Rev | year= 2009 | volume= | issue= 2 | pages= CD000194 | pmid=19370553 | * [[Hirsutism]]<ref name="pmid19370553">{{cite journal| author=Brown J, Farquhar C, Lee O, Toomath R, Jepson RG| title=Spironolactone versus placebo or in combination with steroids for hirsutism and/or acne. | journal=Cochrane Database Syst Rev | year= 2009 | volume= | issue= 2 | pages= CD000194 | pmid=19370553 | ||
| url=http://www.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&tool=clinical.uthscsa.edu/cite&email=badgett@uthscdsa.edu&retmode=ref&cmd=prlinks&id=19370553 | doi=10.1002/14651858.CD000194.pub2 }} | | url=http://www.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&tool=clinical.uthscsa.edu/cite&email=badgett@uthscdsa.edu&retmode=ref&cmd=prlinks&id=19370553 | doi=10.1002/14651858.CD000194.pub2 }}</ref> | ||
* [[Hypertension]] | * [[Hypertension]] | ||
** Prevention of [[hypokalemia]] caused by [[diuretic#thiazides|thiazide]] [[diuretic]] therapy | ** Prevention of [[hypokalemia]] caused by [[diuretic#thiazides|thiazide]] [[diuretic]] therapy | ||
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{| class="wikitable" | {| class="wikitable" | ||
|+ [[Randomized controlled trial]]s of aldosterone antagonist for [[heart failure]]. | |+ [[Randomized controlled trial]]s of aldosterone antagonist for [[heart failure]]. | ||
! rowspan="2"|Trial!!rowspan="2"| Patients!!rowspan="2"| Intervention!!rowspan="2"|Comparison !!rowspan="2"|Outcome!!colspan="3"|Results | ! rowspan="2"|Trial!!rowspan="2"| Patients!!rowspan="2"| Intervention!!rowspan="2"|Comparison !!rowspan="2"|Outcome!!colspan="3"|Results!!rowspan="2"|[[Drug toxicity]] | ||
|-<br/> | |-<br/> | ||
! Intervention!!Control!! | ! Intervention!!Control!! | ||
|- | |- | ||
| EMPHASIS-HF<ref name="pmid21073363">{{cite journal| author=Zannad F, McMurray JJ, Krum H, van Veldhuisen DJ, Swedberg K, Shi H et al.| title=Eplerenone in patients with systolic heart failure and mild symptoms. | journal=N Engl J Med | year= 2011 | volume= 364 | issue= 1 | pages= 11-21 | pmid=21073363 | doi=10.1056/NEJMoa1009492 | pmc= | url= }} </ref><br/>2010|| | | EMPHASIS-HF<ref name="pmid21073363">{{cite journal| author=Zannad F, McMurray JJ, Krum H, van Veldhuisen DJ, Swedberg K, Shi H et al.| title=Eplerenone in patients with systolic heart failure and mild symptoms. | journal=N Engl J Med | year= 2011 | volume= 364 | issue= 1 | pages= 11-21 | pmid=21073363 | doi=10.1056/NEJMoa1009492 | pmc= | url= }} </ref><br/>2010||2737 patients<br/>• EF≤35%<br/>• [[New York Heart Association Functional Classification|NYHA Class II]]|| [[eplerenone]] up to 50 mg/day||Placebo|| mortality at 21 months|| 12.5%|| 15.5%||HR=0.76 ([[confidence interval|95% CI]]: 0.62 - 0.93) (P=0.008)<br/>(stopped early)|| • > 5.5 meq/dl = 11.8%<br/>• Mean potassium increase = 0.16 mmol/L | ||
|- | |- | ||
| EPHESUS<ref name="pmid12668699">{{cite journal| author=Pitt B, Remme W, Zannad F, Neaton J, Martinez F, Roniker B et al.| title=Eplerenone, a selective aldosterone blocker, in patients with left ventricular dysfunction after myocardial infarction. | journal=N Engl J Med | year= 2003 | volume= 348 | issue= 14 | pages= 1309-21 | pmid=12668699 | doi=10.1056/NEJMoa030207 | pmc= | url=http://www.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&tool=sumsearch.org/cite&retmode=ref&cmd=prlinks&id=12668699 }} [http://www.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&tool=sumsearch.org/cite&retmode=ref&cmd=prlinks&id=12899810 Review in: J Fam Pract. 2003 Aug;52(8):598-9] [http://www.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&tool=sumsearch.org/cite&retmode=ref&cmd=prlinks&id=12954024 Review in: ACP J Club. 2003 Sep-Oct;139(2):32] </ref><br/>2003|| 6642 patients<br/>• < 2 weeks after [[myocardial infarction]]• | | EPHESUS<ref name="pmid12668699">{{cite journal| author=Pitt B, Remme W, Zannad F, Neaton J, Martinez F, Roniker B et al.| title=Eplerenone, a selective aldosterone blocker, in patients with left ventricular dysfunction after myocardial infarction. | journal=N Engl J Med | year= 2003 | volume= 348 | issue= 14 | pages= 1309-21 | pmid=12668699 | doi=10.1056/NEJMoa030207 | pmc= | url=http://www.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&tool=sumsearch.org/cite&retmode=ref&cmd=prlinks&id=12668699 }} [http://www.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&tool=sumsearch.org/cite&retmode=ref&cmd=prlinks&id=12899810 Review in: J Fam Pract. 2003 Aug;52(8):598-9] [http://www.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&tool=sumsearch.org/cite&retmode=ref&cmd=prlinks&id=12954024 Review in: ACP J Club. 2003 Sep-Oct;139(2):32] </ref><br/>2003|| 6642 patients<br/>• Clinical CHF<br/>• ≤ 2 weeks after [[myocardial infarction]]<br/>• ≤ 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%<br/>• Median potassium increase = 0.30 mmol/L | ||
|- | |- | ||
| RALES<ref name="pmid10471456">{{cite journal| author=Pitt B, Zannad F, Remme WJ, Cody R, Castaigne A, Perez A et al.| title=The effect of spironolactone on morbidity and mortality in patients with severe heart failure. Randomized Aldactone Evaluation Study Investigators. | journal=N Engl J Med | year= 1999 | volume= 341 | issue= 10 | pages= 709-17 | pmid=10471456 | doi=10.1056/NEJM199909023411001 | pmc= | url= }} </ref><br/>1999|| | | RALES<ref name="pmid10471456">{{cite journal| author=Pitt B, Zannad F, Remme WJ, Cody R, Castaigne A, Perez A et al.| title=The effect of spironolactone on morbidity and mortality in patients with severe heart failure. Randomized Aldactone Evaluation Study Investigators. | journal=N Engl J Med | year= 1999 | volume= 341 | issue= 10 | pages= 709-17 | pmid=10471456 | doi=10.1056/NEJM199909023411001 | pmc= | url= }} </ref><br/>1999||1663 patients<br/>• EF≤35%<br/>• [[New York Heart Association Functional Classification|NYHA Class III/IV]]|| [[spironolactone]] 25 mg/day||Placebo|| mortality at 24 months|| 35%||46%||RR=0.70 ([[confidence interval|95% CI]]: 0.60 to 0.82) P<0.001<br/>(stopped early)||• "Serious hyperkalemia" = 2%<br/>• Median potassium increase = 0.30 mmol/L<br/>• Gynecomastia or breast pain = 10% | ||
|} | |} | ||
Latest revision as of 00:07, 21 February 2011
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 (2024), 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.