Oral Flecainide Acetate for the Treatment of Ventricular Arrhythmias

Abstract

The antiarrhythmic efficacy and safety of oral flecainide acetate were assessed during a controlled, short-term dosage-maintenance study. Thirteen patients with chronic ventricular ectopy entered a placebo control period, and 11 with persistent, frequent (greater than 600 per 12 hours) premature ventricular complexes (PVCs) advanced to drug therapy. Of 10 patients completing a trial of different doses, nine responded completely, with a mean PVC suppression of 98,3 per cent. Repetitive PVCs were eliminated. The mean effective dose was 189 mg per 12 hours, and the effective plasma concentration before administration of a dose averaged 635 ng per milliliter. One patient responded partially (68 per cent of PVCs suppressed). Flecainide continued to be effective and well tolerated at the end of a two-week outpatient trial in the nine complete responders, maintaining an average PVC suppression of 94.6 per cent. The PR and QRS intervals were mildly prolonged. The echocardiographic ejection fraction was unchanged during treatment. The elimination half-life was long - 18.8 +/- 3.8 hours. Flecainide thus appears to be a highly effective and well-tolerated antiarrhythmic agent with favorable pharmacokinetics.

Effects of flecainide on isolated vascular smooth muscles of rat

“…Flecainide acetate is a class Ic antiarrhythmic drug effective both in experimental and clinical ventricular and supraventricular tachyarrhythmias (Anderson et al, 1981;Duff et al, 1981;Campbell, 1983a;Hellestrand et al, 1984;Holmes & Heel, 1985;Somberg & Tepper, 1986). In cardiac muscle fibres, flecainide exhibits both very slow onset kinetics and recovery from V.ax block (Campbell & Vaughan Williams, 1983;Campbell, 1983a,b;Delpon et al, 1991) due to its high affinity for the activated and inactivated states of the Na channels (Anno & Hondeghem, 1990).…”

Comparative haemodynamic effects of intravenous lignocaine, disopyramide and flecainide in uncomplicated acute myocardial infarction

“…The absence of trend of change in any of the baseline haemodynamic variables during the control period confirmed the haemodynamic stability of each group. The therapeutic ranges for plasma levels of lignocaine, disopyramide and flecainide are 1-5 ,ug ml-', 2-5 ,ug ml-' and 200-800 ng ml-1 respectively (Bigger, 1980;Grossman et al, 1969;Niarchos, 1976;Koch-Weser, 1979;Anderson et al, 1981;Duran et al, 1982;Hellestrand et al, 1982;Hodges et al, 1982). These were achieved throughout the study, with plasma disopyramide close to the upper limit.…”

“…Flecainide, a new class 1C antiarrhythmic agent is an effective broad spectrum anti-arrhythmic (Hellestrand et al, 1982;Hodges et al, 1982;Anderson et al, 1981;Duff et al, 1981;Duran et al, 1982;Anderson et al, 1984). In common with other class 1 agents it induces mild depression of cardiac function in stable coronary artery disease (Legrand et al, 1983;Serruys et al, 1983;Josephson et al, 1984).…”

Targeting ryanodine receptors for anti-arrhythmic therapy

“…Flecainide initially showed promise as an antiarrhythmic agent against both ventricular [59] and atrial arrhythmias [60] . Because a predomi- [36] .…”