Pharmacology · Antiepileptics and CNS Drugs (Antipsychotics, Antidepressants, Sedatives)

Lignocaine (lidocaine) is used as a local anaesthetic. The mechanism by which it blocks nerve conduction is:

  • A It closes potassium channels, hyperpolarising the axonal membrane
  • B It antagonises calcium channels on Schwann cells, reducing myelin conduction
  • C It binds the intracellular face of voltage-gated Na+ channels in the open/inactivated state, blocking Na+ influx in a use-dependent manner
  • D It activates inhibitory GABA-B receptors on peripheral sensory neurons
Correct answer: C. It binds the intracellular face of voltage-gated Na+ channels in the open/inactivated state, blocking Na+ influx in a use-dependent manner

Explanation

Local anaesthetics are tertiary amines that penetrate the nerve membrane in the uncharged (free base) form, become protonated intracellularly, and then bind to a receptor site within the inner vestibule of the voltage-gated Na+ channel. They preferentially bind open and inactivated channel states (use-dependence/frequency-dependence), blocking Na+ influx and preventing action potential propagation. Small, unmyelinated C-fibres (pain) are blocked before large myelinated motor fibres.

Reference: KD Tripathi, Essentials of Medical Pharmacology, 8th ed.

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

Written and medically reviewed by the StethoPrep medical team.

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