- Molecular NameDigoxin
- SynonymDigitalis Glycoside
- Weight780.949
- Drugbank_IDDB00390
- ACS_NO20830-75-5
- Show 3D model
- LogP (experiment)1.26
- LogP (predicted, AB/LogP v2.0)1.29
- pkaN/A
- LogD (pH=7, predicted)1.29
- Solubility (experiment)0.054 mg/ml
- LogS (predicted, ACD/Labs)(ph=7)-3.6
- LogSw (predicted, AB/LogsW2.0)0.06
- Sw (mg/ml) (predicted, ACD/Labs)0.2
- No.of HBond Donors6
- No.of HBond Acceptors14
- No.of Rotatable Bonds7
- TPSA203.06
- StatusFDA approved
- AdministrationOral, Intravenous
- PharmacologyDigoxin is widely used in the treatment of various heart conditions, namely atrial fibrillation, atrial flutter and sometimes heart failure that cannot be controlled by other medication.
- Absorption_value78.0
- Absorption (description)The absorption of digoxin after oral administration is variable and subject to bioavailability differences. Absorption occurs mainly in the small intestine and is delayed in the presence of food. Digoxin is rapidly distributed throughout the body and less than 20% of the total digoxin in the body is located in the blood. High concentrations are found in the heart, brain, and kidneys, but the skeletal muscles form the largest digoxin store. Concentrations in the myocardium are higher than in plasma. Digoxin is also found in the CSF and it also crosses the placenta.
- Caco_2N/A
- Bioavailability70.0
- Protein binding25.0
- Volume of distribution (VD)5~10 L/kg; or 3.12CLcr + 3.84
- Blood/Plasma Partitioning ratio (D_blood)Plasma:whole blood ratio, 0.93.
- MetabollsmDigoxin is metabolised by stepwise removal of the sugar moieties to form digoxigenin, which is further metabolised to inactive metabolites which may be excreted in the free or conjugated form. Reduction to dihydrodigoxin, which is relatively inactive, also occurs.
- Half life39 h
- ExcretionUp to 80% of a dose is excreted in the urine in 7 days with 27% of the dose in the first 24 h; the remainder is eliminated in the faeces via the bile. In most patients, 80 to 90% of the material excreted in the urine is unchanged, up to 10% is in the dihydro form, and a small amount includes digoxigenin and the mono- and bisdigitoxosides. In about 10% of patients, however, between 20 and 55% is excreted as metabolites, mainly dihydrodigoxin. Of the material excreted in the bile, about 50% is unchanged, about 25% is digoxin bisdigitoxoside, about 25% is digoxin monodigitoxoside, and about 1% is digoxigenin. Digoxin is a metabolite of deslanoside, digitoxin, lanatoside C, and metildigoxin.
- Urinary Excretion60
- Clerance1~4 ml/min/kg; or 0.88CLcr + 0.33
- ToxicityToxicity includes ventricular tachycardia or ventricular fibrillation, or progressive bradyarrhythmias, or heart block.
- LD50 (rat)N/A
- LD50 (mouse)LD50 = 7.8 mg/kg