Eplerenone

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Eplerenone, an aldosterone receptor agonist.

Eplerenone (e pler' en one) is an aldosterone receptor agonist, similar to spironolactone. Because it inhibits the negative regulatory feedback of aldosterone on renin secretion, increased plasma renin, and serum aldosterone, occur with its use. Eplerenone selectively binds to mineralocorticoid receptors relative to its binding to glucocorticoid, progesterone and androgen receptors.

History

Inspra brand of eplerenone, submitted by GD Searle, was approved by the Food and Drug Administration in the United States with a New Drug Application (NDA) on September 27, 2002.[1] Generic versions with a AB Therapeutic Equivalence Code was approved with a Abbreviated New Drug Application (ANDA) on July 30, 2008 (Apotex)[2] and August 1, 2008 (Sandoz)[3].

Uses

Eplerenone may help patients with mild[4] or moderate-to-severe[5] symptoms of heart failure.

However, eplerenone may not help ventricular remodeling among patients with heart failure due to systolic dysfunction.[6]

External links

The most up-to-date information about Eplerenone and other drugs can be found at the following sites.


References

  1. Anonymous. Drugs@FDA for FDA Application No. 021437. U S Food and Drug Administration
  2. Anonymous. Drugs@FDA for FDA Application No. 078482. U S Food and Drug Administration
  3. Anonymous. Drugs@FDA for FDA Application No. 078510. U S Food and Drug Administration
  4. 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.
  5. 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
  6. Udelson JE, Feldman AM, Greenberg B, Pitt B, Mukherjee R, Solomon HA et al. (2010). "Randomized, double-blind, multicenter, placebo-controlled study evaluating the effect of aldosterone antagonism with eplerenone on ventricular remodeling in patients with mild-to-moderate heart failure and left ventricular systolic dysfunction.". Circ Heart Fail 3 (3): 347-53. DOI:10.1161/CIRCHEARTFAILURE.109.906909. PMID 20299607. Research Blogging.