Pharmacopeia
FLECAINIDE
Core pharmacology
- Class Group
Antiarrhythmic –
Vaughan Williams Class Ic
Na channel blocker- Legacy Cicm Level
Level 3
- Introduction
Amide local anaesthetic
Class IC antiarrhythmic
Na channel blocker- Indications Uses
1. for the suppression of irritable foci, e.g. ventricular tachycardia and
ventricular ectopics
2. in the treatment of re-entry dysrhythmias, e.g. the
Wolff–Parkinson–White syndrome and
3. in the treatment of symptomatic paroxysmal atrial fibrillation intolerant
of other medication.- Presentation
As 50/100 mg tablets and as a 10 mg/ml solution of flecainide acetate for intravenous administration
- Mechanism of action
Flecainide reduces the maximum rate of depolarization in heart muscle and thereby slows conduction, particularly in the
His–Purkinje system. It has a profound effect on conduction in accessory
pathways, especially on retrograde conduction, and markedly suppresses
ventricular ectopic foci. It is a local anaesthetic agent which depresses membrane responsiveness and conduction velocity, with no effect on the duration of the action potential.- Physiological effects
CVS
Flecainide is generally well tolerated; the blood pressure and heart rate
usually remain unchanged. The drug has negative inotropic potential.CNS
Visual disturbances may occur and are probably a central effect of
the drug- Adverse Effects Toxicity
Reversible liver damage, dizziness, paraesthesiae,
headaches, and nausea may complicate the use of the drug.- Absorption
PO. Rapidly absorbed.
BA 85-90%- Protein binding
37-58%
- Volume of distribution
5.8-10 L/kg
- Metabolism
Liver
2 metabolites: metao-dealkylated flecainide and its lactam- Excretion
Urine (10-50% unchanged)
- Half-life
IV: 7-15hrs
PO: 12-27hrs- Route And Dose
PO 100-200mg Q12hrly
IV: Bolus 2mg/kg over 10min → Infusion 1.5mg/kg/hr for 1hr → 0.25 mg/kg/hr