Eplerenone
Chemical compound / From Wikipedia, the free encyclopedia
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Eplerenone, sold under the brand name Inspra, is an aldosterone antagonist type of potassium-sparing diuretic that is used to treat chronic heart failure and high blood pressure, particularly for patients with resistant hypertension due to elevated aldosterone. It is a steroidal antimineralocorticoid of the spirolactone group and a selective aldosterone receptor antagonist (SARA).[6] Eplerenone is more selective than spironolactone at the mineralocorticoid receptor relative to binding at androgen, progestogen, glucocorticoid, or estrogen receptors.
Quick Facts Clinical data, Pronunciation ...
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Pronunciation | /ɛpˈlɛrənoʊn/ |
Trade names | Inspra, Epnone, Dosterep |
Other names | SC-66110; CGP-30083; 9-11α-Epoxymexrenone; 9,11α-Epoxy-7α-methoxycarbonyl-3-oxo-17α-pregn-4-ene-21,17-carbolactone |
AHFS/Drugs.com | Monograph |
MedlinePlus | a603004 |
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Routes of administration | By mouth (tablets) |
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Bioavailability | ~70%[2] |
Protein binding | ~50% (33–60%) (primarily to α1-acid glycoprotein)[2][3] |
Metabolism | Liver (CYP3A4)[2][3] |
Metabolites | 6β-OH-EPL, 6β,21-OH-EPL, 21-OH-EPL, 3α,6β-OH-EPL[2] (All inactive)[2] |
Elimination half-life | 4–6 hours[4] |
Excretion | Urine (67%), feces (32%)[5] |
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ECHA InfoCard | 100.106.615 |
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Formula | C24H30O6 |
Molar mass | 414.498 g·mol−1 |
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