- Molecular NamePropafenone
- SynonymPropafenona [INN-Spanish]; Propafenone HCl; Propafenone hydrochloride; Propafenone-HCl; Propafenonum [INN-Latin]
- Weight341.451
- Drugbank_IDDB01182
- ACS_NO54063-53-5
- Show 3D model
- LogP (experiment)3.34
- LogP (predicted, AB/LogP v2.0)3.75
- pka9.56
- LogD (pH=7, predicted)1.52
- Solubility (experiment)Slightly soluble
- LogS (predicted, ACD/Labs)(ph=7)-1.28
- LogSw (predicted, AB/LogsW2.0)0.84
- Sw (mg/ml) (predicted, ACD/Labs)0.11
- No.of HBond Donors2
- No.of HBond Acceptors4
- No.of Rotatable Bonds11
- TPSA58.56
- StatusFDA approved
- AdministrationN/A
- PharmacologyA class Ic anti-arrhythmic medication, which treats illnesses associated with rapid heart beats such as atrial and ventricular arrhythmias.
- Absorption_value95.0
- Absorption (description)Nearly completely absorbed following oral administration (90%). Systemic bioavailability ranges from 5 to 50%, due to significant first-pass metabolism. This wide range in systemic bioavailability is related to two factors: presence of food (food increases bioavailability) and dosage (bioavailability is 3.4% for a 150-mg tablet compared to 10.6% for a 300-mg tablet).
- Caco_2N/A
- Bioavailability35.0
- Protein binding97.0
- Volume of distribution (VD)1.5~5.7 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmPropafenone is metabolized primarily in the liver. Because of its short half-life, it requires dosing two or three times daily to maintain steady blood levels. The long-term safety of propafenone is unknown. Because it is structurally similar to another dangerous anti-arrhythmic medicine, flecainide, caution should be exercised in its use. Flecainide and propafenone, like other antiarrhythmic drugs have been shown to increase the occurrence of dangerous arrhythmias (5.3% for propafenone, Teva physician prescribing information), primarily in patients with underlying heart disease.
- Half life2~10 h
- ExcretionN/A
- Urinary ExcretionN/A
- CleranceN/A
- ToxicitySymptoms of propafenone overdose (usually most severe within the first 3 hours) may include convulsions (rarely), heartbeat irregularities, low blood pressure, and sleepiness.
- LD50 (rat)N/A
- LD50 (mouse)N/A