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Related Experiment Videos

Local anesthetics.

F Yanagidate1, G R Strichartz

  • 1Pain Research Center, BWH/MRB611, 75 Francis Street, Boston, MA 02115-6110, USA.

Handbook of Experimental Pharmacology
|November 8, 2006
PubMed
Summary
This summary is machine-generated.

Local anesthetics block pain by inhibiting voltage-gated sodium channels and affecting various other molecular targets. These versatile drugs offer synergistic analgesic mechanisms for effective pain relief.

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Area of Science:

  • Neuroscience
  • Pharmacology
  • Pain Management

Background:

  • Local anesthetics are widely used for acute and chronic pain management.
  • Their analgesic effects stem from interactions with diverse molecular targets involved in pain processing.

Purpose of the Study:

  • To review the broad molecular actions of local anesthetics in pain processing.
  • To elucidate the mechanisms underlying their analgesic properties.

Main Methods:

  • Review of literature on local anesthetic actions on neuronal channels and receptors.
  • Analysis of molecular targets including voltage-gated sodium and calcium channels, and various receptors.

Main Results:

  • Local anesthetics block action potentials by inhibiting voltage-gated sodium channels, with higher affinity for open/inactivated states.

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  • They also inhibit voltage-gated calcium channels, suppress neurogenic inflammation, and affect receptors like TRPV1 and bradykinin B2.
  • Spinal local anesthetics inhibit glutamate receptors and mitogen-activated protein kinases, while intravenous administration can reverse neuropathic pain at sub-blocking concentrations.

    • Conclusions:

    • Local anesthetics exert analgesic effects through a synergistic combination of actions on multiple neuronal targets.
    • These mechanisms contribute to their broad efficacy in managing various pain conditions.