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      Flecainide: A New Class Ic Antidysrhythmic

      Drug Intelligence & Clinical Pharmacy
      SAGE Publications

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          A classification of antiarrhythmic actions reassessed after a decade of new drugs.

          The past decade has seen the introduction of many new class 1 drugs, restricting fast inward current. Confirmative evidence has been obtained that the antiarrthymic action of lidocaine and diphenylhydantoin is indeed due to their effect as class 1 agents depressing conduction. The original class 3 drug, amiodarone, is increasingly in use as an antiarrhythmic of first choice for WPW and for arrhythmias associated with hypertrophic myopathy, and as a reserve drug in resistant arrhythmias of other types. Other compounds delaying repolarization have proved to be clinically effective as antiarrhythmics. In addition to their class 2 antiarrhythymic action exhibited acutely, on long-term treatment beta blockers have a class 3 action, which might be, at least in part, responsible for the protection of postinfarction patients against sudden death. Recent research suggests that inhibition of slow inward current may lead, as a secondary consequence of lowered [Ca]i, to improved cell-to-cell conduction. Finally, all but one of the new antiarrhythmic drugs, none of which existed in 1972, have turned out to possess one or more of the four classes of action originally described. This can hardly be a coincidence. The single exception, alinidine, a selective bradycardic agent, may restrict anionic currents, which would constitute a fifth class of action, but this is far from proved.
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            Metabolism of flecainide.

            After oral administration in healthy human subjects, flecainide absorption is prompt (average peak level at 3 to 4 hours) and nearly complete (at least 90%); flecainide does not appear to undergo consequential presystemic biotransformation. Oral absorption in patients with cardiac arrhythmias, renal disease and congestive heart failure (CHF) is also good. Plasma levels of flecainide are proportional to dose within the therapeutic range. Neither food nor antacid affect the extent of flecainide absorption. In healthy subjects, the plasma half-life of unchanged flecainide is relatively long (mean 13 hours after single doses and 16 hours after multiple dosage). For patients with ventricular premature complexes, the half-life is longer (mean 20 hours), and twice-daily oral dosage is effective. The rate of flecainide elimination from plasma may possibly be reduced in older patients. Overall, the plasma pharmacokinetics of flecainide appear to be reasonably linear (not dose- or concentration-dependent). In humans, most (mean 86%) of a single oral dose is excreted in urine as flecainide and its metabolites; only a small portion (mean 5%) is found in feces. Thus, flecainide does not appear to undergo extensive biliary excretion. A substantial portion (mean 27%) of a dose is excreted in urine as unchanged flecainide. Under alkaline urinary conditions, flecainide elimination may be decreased. Only 2 major and 2 or 3 minor metabolites are found in human urine. The 2 major urinary metabolites possess little or no detectable antiarrhythmic activity and are also the major metabolites present in human plasma (primarily conjugated); since free metabolite levels are very low in plasma, metabolites are not likely to contribute any consequential pharmacologic activity. The rate of flecainide elimination from plasma is somewhat slower in patients with moderate renal failure and in patients with CHF than that for healthy persons, and is markedly slower in some patients with end-stage renal disease. Urinary excretion of unchanged flecainide is somewhat less in moderate renal patients and is markedly less in end-stage renal patients, but is not altered in CHF patients. Dosage should be reduced in patients with more severe renal disease and, if indicated, in some CHF patients. Hemodialysis is not an effective means for removal of unchanged flecainide, but does provide more substantial removal of metabolites. Flecainide is not extensively bound (mean 40%) to human plasma proteins in vitro and binding is independent of total drug level.(ABSTRACT TRUNCATED AT 400 WORDS)
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              Oral flecainide acetate for the treatment of ventricular arrhythmias.

              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.
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                Author and article information

                Journal
                Drug Intelligence & Clinical Pharmacy
                Drug Intelligence & Clinical Pharmacy
                SAGE Publications
                0012-6578
                August 30 2016
                October 1985
                August 30 2016
                October 1985
                : 19
                : 10
                : 703-707
                Article
                10.1177/106002808501901001
                d550db9b-b63d-4e16-a57f-f2f296d920c2
                © 1985

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