- Molecular NameAprindine
- SynonymAprindin; Aprindina [inn-spanish]; Aprindinum [inn-latin]; Aprinidine
- Weight322.496
- Drugbank_IDDB01429
- ACS_NO37640-71-4
- Show 2D model
- LogP (experiment)4.9
- LogP (predicted, AB/LogP v2.0)4.87
- pka10.1
- LogD (pH=7, predicted)1.95
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)-2.24
- LogSw (predicted, AB/LogsW2.0)0.02
- Sw (mg/ml) (predicted, ACD/Labs)0.02
- No.of HBond Donors0
- No.of HBond Acceptors2
- No.of Rotatable Bonds8
- TPSA6.48
- StatusFDA approved
- AdministrationN/A
- PharmacologyA Class 1b antiarrhythmic agent.
- Absorption_valueN/A
- Absorption (description)Almost completely absorbed after oral administration.
- Caco_2N/A
- Bioavailability85.0
- Protein binding95.0
- Volume of distribution (VD)4 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmExtensively metabolised by aromatic hydroxylation and N-dealkylation followed by glucuronic acid conjugation; the monodesethyl metabolite, which can be detected in plasma after chronic administration, is active.
- Half lifePlasma half-life, 12 to 66 h (mean 30) in normal subjects but the half-life is apparently longer in patients with chronic ventricular arrhythmias and myocardial infarction (average, about 50 h)
- ExcretionLess than 1% of a dose is excreted in the urine as unchanged drug and about 40 to 65% as conjugated metabolites; 35 to 60% of the dose is eliminated in the faeces over a period of 5 days.
- Urinary ExcretionN/A
- ClerancePlasma clearance, about 2.5 mL/min/kg in normal subjects; decreased to about 1 mL/min/kg in patients with cardiac disease.
- ToxicityToxic effects are usually associated with plasma concentrations greater than 2 mg/L. Toxic effects were found in 9 patients whose plasma concentrations ranged from 1.2 to 4.9 mg/L (mean 2.6). [J. P. Van Durme et al.,Eur. J. Clin. Pharmacol.,1974, 7, 343–346.]
- LD50 (rat)N/A
- LD50 (mouse)N/A