- Molecular NameEplerenone
- SynonymEpoxymexrenone
- Weight414.498
- Drugbank_IDDB00700
- ACS_NO107724-20-9
- Show 3D model
- LogP (experiment)2.445
- LogP (predicted, AB/LogP v2.0)1.68
- pkaN/A
- LogD (pH=7, predicted)1.68
- Solubility (experiment)Slightly soluble
- LogS (predicted, ACD/Labs)(ph=7)-3.68
- LogSw (predicted, AB/LogsW2.0)0.01
- Sw (mg/ml) (predicted, ACD/Labs)0.09
- No.of HBond Donors0
- No.of HBond Acceptors6
- No.of Rotatable Bonds2
- TPSA91.43
- StatusFDA approved
- AdministrationN/A
- PharmacologyAn aldosterone antagonist used as an adjunct in the management of chronic heart failure. It is similar to spironolactone, though it may be more specific for the mineralocorticoid receptor and is specifically marketed for reducing cardiovascular risk in patients following myocardial infarction.
- Absorption_valueN/A
- Absorption (description)N/A
- Caco_2N/A
- Bioavailability69.0
- Protein binding46.5
- Volume of distribution (VD)0.6~1.3 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmEplerenone is converted (reversibly) to an inactive ring-open hydroxy acid. Both eplerenone (E) and the hydroxy acid (EA) circulate in plasma; concentrations of E are much higher than EA. Irreversible metabolism is catalyzed predominantly by CYP3A4.
- Half life4~6 h
- Excretion67% renal 32% biliary
- Urinary Excretion7
- Clerance2.4 ml/min/kg
- ToxicityThe 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.
- LD50 (rat)N/A
- LD50 (mouse)N/A