Metabolism of flecainide

作者: Gordon J. Conard , Robert E. Ober

DOI: 10.1016/0002-9149(84)90501-0

关键词: Urinary systemPharmacokineticsHemodialysisFlecainideFlecainide AcetateInternal medicineMedicineEndocrinologyOral administrationIntestinal absorptionMetabolite

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

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