The influence of the sparteine/debrisoquin phenotype on the disposition of flecainide

• DOI: 10.1038/clpt.1989.73
• Publication Date: 2010-08-30T12:47:04Z
• Authors: Gerd Mikus; Annette S Gross; Jürgen Beckmann; Rita Hertrampf; Ursula Gundert-Remy; Michel Eichelbaum
• Keywords: Flecainide; Disposition; Sparteine

The pharmacokinetics and urinary excretion of flecainide (50 mg administered orally) were investigated in five extensive metabolizers (EMs) poor (PMs) the sparteine/debrisoquin type polymorphism under conditions controlled pH. Flecainide disposition was altered PMs. AUC higher (1462 ± 407 versus 860 256 hr ng/ml), elimination half-life prolonged (11.8 6.8 hours), amount excreted urine (26.7 7.2 15.4 1.3 mg) PMs compared with EMs (p < 0.05). Oral clearance reduced 0.019) (600 139 1041 307 ml/min EMs). renal similar > 0.05) (308 70 ml/min) (315 69 and, consequently, had a lower 0.008) metabolic (292 136 726 240 Under uncontrolled flow pH, will be difference greater. In impairment, accumulation to very high serum concentrations may anticipated, this result proarrhythmic effects. Clinical Pharmacology Therapeutics (1989) 45, 562–567; doi:10.1038/clpt.1989.73