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Pharmaceutisch Weekblad

, Volume 11, Issue 3, pp 92–94 | Cite as

The action of flecainide acetate and its enantiomers on mammalian non-myelinated nerve fibres

  • Loraine Lie-A-Huen
  • Jan van den Akker
  • Adriaan den Hertog
  • Dirk K. F. Meijer
Article

Abstract

The effects of flecainide acetate racemate and its two enantiomers on voltage-operated sodium and potassium channels and on the sodium pump activity of non-myelinated fibres of the guinea-pig vagus nerve were studied with the sucrose-gap method. The racemic mixture as well as theR enantiomer andS enantiomer in a concentration range of 3·10−5−3·10−4M caused suppression of the compound action potential, a diminished propagation velocity and a reduction of the post-tetanic potential (PTH), which was also observed with lidocaine. There was no significant difference in the effect caused by the enantiomers seperately. TheR enantiomer tended to evoke a stronger effect compared with theS enantiomer. However, the magnitude of the action is concentration-dependent. At a concentration<10−4M the action of the racemate was stronger than an equimolar concentration of the enantiomers. The activity of the sodium pump, defined by the time constant of post-tetanic potential decay, was affected at a concentration of 10−4M of the racemate, in contrast to lidocaine. The racemate and both enantiomers of flecainide acetate possess a similar local anaesthetic action, as reflected by the inhibition of voltage-operated sodium channels.

Keywords

Action potentials Enantiomers Flecainide acetate Nerve fibres, non-myelinated Sodium pump, electrogenic Structure-activity relationship 

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Copyright information

© Bohn, Scheltema & Holkema 1989

Authors and Affiliations

  • Loraine Lie-A-Huen
    • 1
  • Jan van den Akker
    • 2
  • Adriaan den Hertog
    • 2
  • Dirk K. F. Meijer
    • 3
  1. 1.Department of Clinical PharmacySt. Antonius HospitalCM Nieuwegeinthe Netherlands
  2. 2.Department of Pharmacology and Clinical PharmacologyUniversity of GroningenAW Groningenthe Netherlands
  3. 3.Department of Pharmacology and TherapeuticsUniversity of Groningenthe Netherlands

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