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QuickView for Eplerenone (compound)

Name: eplerenone
PubChem Compound ID: 443872
Molecular formula: C24H30O6
Molecular weight: 414.491 g/mol
CGP-30083; 107724-20-9; Eplerenone; Inspra; D01115; Epoxymexrenone; SC-66110; C12512; Eplerenone (JAN/USAN); Inspra (TN)
Name: eplerenone
Name (isomeric): DB00700
Drug Type: small molecule
Category: Aldosterone Antagonists, Antihypertensive Agents
CAS number: 107724-20-9
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.
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 overc...
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Mechanism of Action:
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 (...
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Absorption: The absolute bioavailability of eplerenone is unknown.
Protein binding: 50%
Biotransformation: Eplerenone is metabolized primarily by CYP3A4, however, no active metabolites have been identified in human plasma.
Half Life: 4-6 hours
Clearance: Apparent plasma cl=10 L/hr
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.
Affected organisms: Humans and other mammals
Drug interaction:
ClarithromycinThe macrolide, clarithromycin, may increase the effect and toxicity of eplerenone.
TelithromycinTelithromycin may reduce clearance of Eplerenone. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Eplerenone if Telithromycin is initiated, discontinued or dose changed.
VerapamilThis CYP3A4 inhibitor increases the effect and toxicity of eplerenone
ItraconazoleItraconazole may increase the effect and toxicity of eplerenone.
NefazodoneNefazodone increases the effect and toxicity of eplerenone
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