Gender-associated differences in pharmacokinetics and anti-arrhythmic effects of flecainide in Japanese patients with supraventricular tachyarrhythmia

Eur J Clin Pharmacol. 2007 Oct;63(10):951-7. doi: 10.1007/s00228-007-0348-7. Epub 2007 Jul 31.

Abstract

Objective: We examined the effect of gender-associated differences in pharmacokinetics on the anti-arrhythmic effects of flecainide in Japanese patients with supraventricular tachyarrhythmia and in healthy subjects.

Methods: The study population comprised 72 outpatients (52 males and 20 females) treated with oral flecainide for supraventricular tachyarrhythmias. Serum flecainide concentrations were determined by use of high-performance liquid chromatography. The anti-arrhythmic efficacy of flecainide was assessed for at least 2 months through evaluation of symptomatology, electrocardiograms, and Holter monitoring. Pharmacokinetics of flecainide after a single 50-mg dose was examined in 14 healthy subjects (7 males and 7 females).

Results: The daily dose of flecainide did not differ between males and females (2.87 +/- 0.68 versus 2.92 +/- 0.90 mg/kg). The serum flecainide concentration was significantly lower in males than in females (315 +/- 151 versus 408 +/- 184 ng/mL, P < 0.05). Clinically relevant efficacy of flecainide was achieved significantly (P < 0.05) less often in male patients (31 of 52; 60%) than in female patients (19 of 20; 95%). We confirmed that nonrenal clearance of flecainide among healthy subjects was significantly higher in males than in females (0.77 +/- 0.16 versus 0.57 +/- 0.06 L h(-1) kg(-1), P < 0.05).

Conclusions: Our results suggest that the anti-arrhythmic efficacy of flecainide differed between males and females because of gender-associated differences in pharmacokinetics.

Publication types

  • Clinical Trial
  • Comparative Study

MeSH terms

  • Adult
  • Aged
  • Anti-Arrhythmia Agents / blood
  • Anti-Arrhythmia Agents / pharmacokinetics*
  • Anti-Arrhythmia Agents / therapeutic use*
  • Asian People*
  • Chromatography, High Pressure Liquid
  • Cross-Sectional Studies
  • Cytochrome P-450 CYP2D6 / genetics
  • Cytochrome P-450 CYP2D6 / metabolism
  • Electrocardiography, Ambulatory
  • Female
  • Flecainide / blood
  • Flecainide / pharmacokinetics*
  • Flecainide / therapeutic use*
  • Genotype
  • Haplotypes
  • Humans
  • Japan
  • Male
  • Middle Aged
  • Muscle Proteins / genetics
  • Muscle Proteins / metabolism
  • NAV1.5 Voltage-Gated Sodium Channel
  • Promoter Regions, Genetic
  • Sex Factors
  • Sodium Channels / genetics
  • Sodium Channels / metabolism
  • Tachycardia, Supraventricular / drug therapy*
  • Tachycardia, Supraventricular / genetics
  • Tachycardia, Supraventricular / metabolism
  • Tachycardia, Supraventricular / physiopathology
  • Time Factors
  • Treatment Outcome

Substances

  • Anti-Arrhythmia Agents
  • Muscle Proteins
  • NAV1.5 Voltage-Gated Sodium Channel
  • SCN5A protein, human
  • Sodium Channels
  • Cytochrome P-450 CYP2D6
  • Flecainide