Mexiletine suppresses nodal persistent sodium currents in sensory axons of patients with neuropathic pain

Clin Neurophysiol. 2010 May;121(5):719-24. doi: 10.1016/j.clinph.2009.12.034. Epub 2010 Jan 22.

Abstract

Objective: To investigate changes in axonal persistent Na(+) currents in patients with neuropathic pain and the effects of mexiletine, an analogue of lidocaine, on axonal excitability properties.

Methods: The technique of latent addition was used to estimate nodal persistent Na(+) currents in superficial radial sensory axons of 17 patients with neuropathic pain/paresthesias before and after mexiletine treatment. Brief hyperpolarizing conditioning currents were delivered, and threshold change at the conditioning-test interval of 0.2 ms was measured as an indicator of the magnitude of persistent Na(+) currents.

Results: Threshold changes at 0.2 ms in latent addition were greater in the neuropathic patients than in the normal controls (p<0.001). After mexiletine treatment, there was a reduction in clinical pain scores (p<0.001), associated with decreased threshold changes at 0.2 ms (p<0.001).

Conclusions: In patients with neuropathy, nodal persistent Na(+) currents in large sensory fibers increase, and the abnormal currents can be suppressed by mexiletine. Pain reduction after mexiletine treatment raises the possibility that excessive Na(+) currents are also suppressed in small fibers mediating neuropathic pain.

Significance: Latent addition can be used for indirect in vivo monitoring of nodal Na(+) currents in large sensory fibers, and future studies using this approach in small fibers would provide new insights into the peripheral mechanism of neuropathic pain.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Axons / metabolism*
  • Electric Conductivity
  • Electrophysiological Phenomena
  • Female
  • Humans
  • Lidocaine / analogs & derivatives
  • Male
  • Mexiletine / therapeutic use*
  • Middle Aged
  • Neuralgia / drug therapy
  • Neuralgia / physiopathology*
  • Pain Threshold / drug effects
  • Paresthesia / drug therapy
  • Paresthesia / physiopathology*
  • Radial Nerve / metabolism*
  • Sensory Receptor Cells / metabolism*
  • Sodium Channels / drug effects*
  • Sodium Channels / metabolism

Substances

  • Sodium Channels
  • Mexiletine
  • Lidocaine