Effect of congestive heart failure on mexiletine pharmacokinetics in a Japanese population

Biol Pharm Bull. 2006 Nov;29(11):2267-9. doi: 10.1248/bpb.29.2267.

Abstract

Objective: The goal of this study was to evaluate the influence of congestive heart failure (CHF) on the clearance of mexiletine.

Methods: The mexiletine clearance/bioavailability (CL/F) ratio was estimated in 584 inpatients receiving mexiletine therapy. The study population consisted of 210 patients with CHF [CHF group; 116 inpatients with New York Heart Association (NYHA) class I-II (group NYHA I-II) CHF and 94 inpatients with NYHA class III-IV (group NYHA III-IV) CHF] and 374 inpatients without CHF (Non-CHF group). Serum levels of mexiletine were determined by high performance liquid chromatography (HPLC).

Results: Mexiletine clearance was significantly lower in the CHF group when compared with the Non-CHF group (0.264+/-0.093 vs. 0.393+/-0.082 l/h/kg, mean+/-S.D., p<0.05). Further, the CL/F ratio was 50% lower in group NYHA III-IV when compared with the Non-CHF group, and the CL/F ratio tended to change in inverse proportion to NYHA class.

Conclusion: CHF status significantly affects mexiletine clearance. Therefore, dose adjustments and careful monitoring are likely required in CHF patients receiving mexiletine.

Publication types

  • Clinical Trial
  • Comparative Study

MeSH terms

  • Administration, Oral
  • Anti-Arrhythmia Agents / administration & dosage
  • Anti-Arrhythmia Agents / pharmacokinetics
  • Anti-Arrhythmia Agents / therapeutic use
  • Asian People
  • Biological Availability
  • Chromatography, High Pressure Liquid
  • Drug Administration Schedule
  • Drug Monitoring / methods
  • Female
  • Heart Failure / drug therapy*
  • Heart Failure / metabolism*
  • Humans
  • Inpatients
  • Male
  • Metabolic Clearance Rate
  • Mexiletine / blood
  • Mexiletine / pharmacokinetics*
  • Mexiletine / therapeutic use
  • Severity of Illness Index

Substances

  • Anti-Arrhythmia Agents
  • Mexiletine