- Molecular NameFlecainide
- SynonymFlecainida [INN-Spanish]; Flecainide acetate; Flecainidum [INN-Latin]
- Weight414.346
- Drugbank_IDDB01195
- ACS_NO54143-55-4
- Show 3D model
- LogP (experiment)3.78
- LogP (predicted, AB/LogP v2.0)3.4
- pka9.3
- LogD (pH=7, predicted)0.87
- Solubility (experiment)0.0484 mg/ml
- LogS (predicted, ACD/Labs)(ph=7)-0.68
- LogSw (predicted, AB/LogsW2.0)0.04
- Sw (mg/ml) (predicted, ACD/Labs)0.36
- No.of HBond Donors2
- No.of HBond Acceptors5
- No.of Rotatable Bonds9
- TPSA59.59
- StatusFDA approved
- AdministrationN/A
- PharmacologyA class Ic antiarrhythmic agent used to prevent and treat tachyarrhythmias (abnormal fast rhythms of the heart). It is used to treat a variety of cardiac arrhythmias including paroxysmal atrial fibrillation (episodic irregular heartbeat originating in the upper chamber of the heart), paroxysmal supraventricular tachycardia (episodic rapid but regular heartbeat originating in the atrium), and ventricular tachycardia (rapid rhythms of the lower chambers of the heart). Flecainide works by regulating the flow of sodium in the heart, causing prolongation of the cardiac action potential.
- Absorption_value81.0
- Absorption (description)Flecainide is rapidly and almost completely absorbed after oral administration and peak plasma concentrations occur after 0.5 to 6 h.
- Caco_2N/A
- Bioavailability70.0
- Protein binding40.0
- Volume of distribution (VD)4.9 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmCYP2D6 (limited). It is extensively metabolised (subject to genetic polymorphism) mainly to m-O-dealkylated flecainide and the m-O-dealkylated lactam of flecainide, which both have some activity. m-O-dealkylated flecainide makes up to 20% of the drug's anti-arrhythmic activity. CYP2D6 is involved in its metabolism.
- Half life20 h (range 12-27 hours)
- ExcretionFlecainide is excreted mainly in urine (about 10 to 50% as the unchanged drug and the remainder as metabolites, depending on type of administration). About 5% is excreted in faeces. Excretion of flecainide is decreased in alkaline urine. Haemodialysis removes only about 1% of unchanged flecainide. It crosses the placenta and is distributed into breast milk.
- Urinary Excretion43
- Clerance5.6 ml/min/kg
- ToxicityOverdosing with flecainide is potentially life threatening and can cause or worsen supraventricular or ventricular arrhythmias and heart failure. Plasma levels above 0.7 to 1.0 mg/L are associated with increased likelihood of adverse experiences; the toxic concentration range is 1.5 to 3.0 mg/L.
- LD50 (rat)50-498 mg/kg
- LD50 (mouse)N/A