Absorption kinetics and pharmacodynamics of two oral dosage forms of flecainide in patients with an episode of paroxysmal atrial fibrillation

Abstract

The probability of cardioversion after an oral loading dose of flecainide in patients with AF is dependent on ka. Rapid loading of the effect compartment, i.e. the atria, appears to be critical to reach cardioversion. Higher flecainide serum concentrations and a more rapid absorption does not increase interindividual variability of pharmacokinetics and pharmacodynamics, which is important when safety is considered.

Baseline NT-ProBNP level predicts success of cardioversion of atrial fibrillation with flecainide

“…Flecainide is a class 1C antiarrhythmic drug which possesses the ability to block the cardiac sodium channel. Flecainide may also facilitate arrhythmias by slowing conduction of electrical stimuli through the heart [ 25 , 26 ]. In patients with AF, the slowing of electrical conduction may be reflected as prolongation of QRS interval duration during flecainide infusion.…”

Liquid chromatographic tandem mass spectrometric validated method for pharmacokinetic estimation of flecainide in human plasma

“…Following oral administration, the absorption of flecainide is nearly complete. Peak plasma levels are attained at about 3 hours in most individuals (range: 1 to 6 hours) (1,5). Flecainide does not undergo any consequential presystemic biotransformation (first-pass effect).…”

CYP2D6 genotype affects age-related decline in flecainide clearance

“…The concentration-time profile of flecainide was modeled using a one-compartment model with first-order absorption, according to a previous report [17]. Considering the limited data available for the absorption phase, the absorption rate constant (K a ) and distribution volume (V/F) were fixed at reported values of 0.62/h and 6.0 l/kg, respectively [17,18]. The first-order conditional estimation extended least squares method was used throughout the analysis.…”