Eplerenone
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| Pronunciation | /ɛpˈlɛrənoʊn/ |
| Trade names | Inspra |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a603004 |
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| Routes of administration |
Oral (tablets) |
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| Pharmacokinetic data | |
| Bioavailability | ~70% |
| Protein binding | ~50% (33–60%) (primarily to α1-acid glycoprotein) |
| Metabolism | Liver (CYP3A4) |
| Metabolites | 6β-OH-EPL, 6β,21-OH-EPL, 21-OH-EPL, 3α,6β-OH-EPL (All inactive) |
| Biological half-life | 4–6 hours |
| Excretion | Urine (67%), feces (32%) |
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| Synonyms | SC-66110; CGP-30083; 9-11α-Epoxymexrenone; 9,11α-Epoxy-7α-methoxycarbonyl-3-oxo-17α-pregn-4-ene-21,17-carbolactone |
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| ECHA InfoCard | 100.106.615 |
| Chemical and physical data | |
| Formula | C24H30O6 |
| Molar mass | 414.49 |
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Eplerenone (INN) is a steroidal antimineralocorticoid of the spirolactone group that is used as an adjunct in the management of chronic heart failure. It is similar to the diuretic spironolactone, though it is much more selective for the mineralocorticoid receptor in comparison (i.e., does not possess any antiandrogen, progestogen, glucocorticoid, or estrogenic effects), and is specifically marketed for reducing cardiovascular risk in patients following myocardial infarction. Eplerenone is a potassium-sparing diuretic, meaning that it helps the body get rid of water but still keep potassium.
Eplerenone was developed by Pharmacia Corporation, which was acquired by Pfizer in 2002. It was marketed by Pfizer under the trade name Inspra. The US Food and Drug Administration (FDA) approved the drug for sale in the United States in 2002. Eplerenone is currently approved for sale in the US, EU, Netherlands and Japan. Relative to dosage, eplerenone costs an estimated $2.93 per day when treating congestive heart failure and $5.86 per day when treating hypertension.
Eplerenone is specifically indicated for the reduction of risk of cardiovascular death in people with heart failure and left ventricular dysfunction within 3–14 days of an acute myocardial infarction, in combination with standard therapies and as treatment against hypertension. A variant of the spirolactone group, Eplerenone was developed to contradict the depletion of essential potassium and magnesium levels that are common amongst other mineralocorticoid receptor antagonists. It is a more expensive alternative to spironolactone.
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