About: Eplerenone     Goto   Sponge   Distinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

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  • Eplerenone, an aldosterone receptor antagonist similar to spironolactone, has been shown to produce sustained increases in plasma renin and serum aldosterone, consistent with inhibition of the negative regulatory feedback of aldosterone on renin secretion. The resulting increased plasma renin activity and aldosterone circulating levels do not overcome the effects of eplerenone. Eplerenone selectively binds to recombinant human mineralocorticoid receptors relative to its binding to recombinant human glucocorticoid, progesterone and androgen receptors. (en)
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  • approved (en)
http://linked.open...drugbank/halfLife
  • 4-6 hours (en)
http://linked.open...ugbank/indication
  • For improvement of survival of stable patients with left ventricular systolic dysfunction (ejection fraction <40%) and clinical evidence of congestive heart failure after an acute myocardial infarction. (en)
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Title
  • Eplerenone (en)
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http://linked.open...mechanismOfAction
  • Eplerenone binds to the mineralocorticoid receptor and thereby blocks the binding of aldosterone (component of the renin-angiotensin-aldosterone-system, or RAAS). Aldosterone synthesis, which occurs primarily in the adrenal gland, is modulated by multiple factors, including angiotensin II and non-RAAS mediators such as adrenocorticotropic hormone (ACTH) and potassium. Aldosterone binds to mineralocorticoid receptors in both epithelial (e.g., kidney) and nonepithelial (e.g., heart, blood vessels, and brain) tissues and increases blood pressure through induction of sodium reabsorption and possibly other mechanisms. (en)
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  • Epoxymexrenone (en)
  • Inspra (en)
http://linked.open...drugbank/toxicity
  • The most likely symptoms of human overdosage would be anticipated to be hypotension or hyperkalemia. However, no cases of human overdosage with eplerenone have been reported. (en)
http://linked.open...umeOfDistribution
  • * 43 to 90 L (en)
http://linked.open...nk/proteinBinding
  • 50% (en)
http://linked.open...ynthesisReference
  • Bhaskar Reddy Guntoori, Svetoslav S. Bratovanov, Mohamed Ibrahim Zaki, Elena Bejan, Stephen E. Horne, "Process for the preparation and purification of eplerenone." U.S. Patent US20080234478, issued September 25, 2008. (en)
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  • The absolute bioavailability of eplerenone is unknown. (en)
http://linked.open.../affectedOrganism
  • Humans and other mammals (en)
http://linked.open...casRegistryNumber
  • 107724-20-9 (en)
http://linked.open...drugbank/category
  • (en)
http://linked.open...rugbank/clearance
  • * Apparent plasma cl=10 L/hr (en)
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