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Namespace Prefixes

PrefixIRI
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Statements

Subject Item
n2:DB00700
rdf:type
n3:Drug
n3:description
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.
n3:dosage
n9:271B491A-363D-11E5-9242-09173F13E4C5 n9:271B491B-363D-11E5-9242-09173F13E4C5 n9:271B491C-363D-11E5-9242-09173F13E4C5 n9:271B491D-363D-11E5-9242-09173F13E4C5
n3:group
approved
n3:halfLife
4-6 hours
n3: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.
n3:manufacturer
n6:271B4914-363D-11E5-9242-09173F13E4C5 n6:271B4915-363D-11E5-9242-09173F13E4C5 n6:271B4913-363D-11E5-9242-09173F13E4C5
owl:sameAs
n14:DB00700 n23:DB00700
dcterms:title
Eplerenone
adms:identifier
n18:PA164749044 n20:31547 n21:DB00700 n22:Eplerenone n24:0185-5368-30 n25:C12512 n26:D01115 n27:2876 n28:2876
n3: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.
n3:packager
n6:271B4910-363D-11E5-9242-09173F13E4C5 n6:271B490E-363D-11E5-9242-09173F13E4C5 n6:271B490F-363D-11E5-9242-09173F13E4C5 n6:271B490C-363D-11E5-9242-09173F13E4C5 n6:271B490D-363D-11E5-9242-09173F13E4C5 n6:271B4912-363D-11E5-9242-09173F13E4C5 n6:271B4911-363D-11E5-9242-09173F13E4C5
n3:patent
n12:6863902 n12:6410524
n3:synonym
Epoxymexrenone Inspra
n3: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.
n3:volumeOfDistribution
* 43 to 90 L
n3:proteinBinding
50%
n3:synthesisReference
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.
n7:hasConcept
n8:M0371594
foaf:page
n16:ins1681.shtml n29:eplerenone.html n30:inspra.htm
n3:IUPAC-Name
n4:271B4922-363D-11E5-9242-09173F13E4C5
n3:InChI
n4:271B4928-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n4:271B4927-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B4924-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n4:271B4925-363D-11E5-9242-09173F13E4C5
n3:SMILES
n4:271B4926-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n4:271B4938-363D-11E5-9242-09173F13E4C5 n4:271B4920-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B4921-363D-11E5-9242-09173F13E4C5 n4:271B4939-363D-11E5-9242-09173F13E4C5 n4:271B491E-363D-11E5-9242-09173F13E4C5
n3:logS
n4:271B491F-363D-11E5-9242-09173F13E4C5
n10:hasATCCode
n11:C03DA04
n3:H-Bond-Acceptor-Count
n4:271B492E-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n4:271B492F-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n4:271B4929-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n4:271B492A-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n4:271B492C-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n4:271B492B-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n4:271B492D-363D-11E5-9242-09173F13E4C5
n3:absorption
The absolute bioavailability of eplerenone is unknown.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
107724-20-9
n3:category
n3:clearance
* Apparent plasma cl=10 L/hr
n3:containedIn
n5:271B4917-363D-11E5-9242-09173F13E4C5 n5:271B4918-363D-11E5-9242-09173F13E4C5 n5:271B4916-363D-11E5-9242-09173F13E4C5 n5:271B4919-363D-11E5-9242-09173F13E4C5
n3:Bioavailability
n4:271B4934-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n4:271B4936-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n4:271B4937-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n4:271B4933-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n4:271B4932-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n4:271B4935-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n4:271B4923-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n4:271B4930-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n4:271B4931-363D-11E5-9242-09173F13E4C5