- Molecular NameEnoximone
- Synonymenoximone
- Weight248.306
- Drugbank_IDDB04880
- ACS_NO77671-31-9
- Show 3D model
- LogP (experiment)1.86
- LogP (predicted, AB/LogP v2.0)1.28
- pkaN/A
- LogD (pH=7, predicted)1.28
- Solubility (experiment)1.01 mg/ml
- LogS (predicted, ACD/Labs)(ph=7)-4.16
- LogSw (predicted, AB/LogsW2.0)0.96
- Sw (mg/ml) (predicted, ACD/Labs)0.02
- No.of HBond Donors2
- No.of HBond Acceptors4
- No.of Rotatable Bonds3
- TPSA83.5
- StatusFDA approved
- AdministrationIntravenous
- PharmacologyAn imidazole phosphodiesterase inhibitor. It is used in the treatment of congestive heart failure. Selective for phosphodiesterase 3
- Absorption_value80.0
- Absorption (description)N/A
- Caco_2N/A
- Bioavailability79.0
- Protein binding85.0
- Volume of distribution (VD)1.1 to 3.6 L/kg; 1.4 to 15.5 L/kg (median 3.8) (infants aged 0.6 to 49.7 weeks).
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmFollowing intravenous injection or infusion it undergoes metabolism in the liver to an active sulfoxide metabolite (piroximone).
- Half lifeIn healthy volunteers, 1 to 4 h, in patients with heart failure, 6 h (bolus injections), 8 h (continuous infusion); infants (0.6 to 49.7 weeks) 1.4 to 10.9 h (median 6.4); sulfoxide, 2.9 to 17.7 h (median 7.4).
- ExcretionIt is excreted primarily via the kidney, as metabolites in urine. After an intravenous dose, approx. 70% is excreted in urine as metabolites and 1% as the unchanged drug.
- Urinary ExcretionN/A
- Clerance3.7~13.0 ml/min/kg; 2.4 to 18.9 ml/min/kg (median 9.2) (infants aged 0.6 to 49.7 weeks)
- ToxicitySevere supraventricular and ventricular arrhythmias can occur.
- LD50 (rat)N/A
- LD50 (mouse)N/A