Anesthesia · single question

What is the mechanism of action of local anesthetics?

  1. Sodium channel blocker
  2. Potassium channel opener
  3. GABA receptor enhancer
  4. Calcium channel blocker
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Correct answer: A. Sodium channel blocker

  • A. Local anesthetics (lidocaine, articaine, bupivacaine, etc.) work by BLOCKING VOLTAGE-GATED SODIUM CHANNELS in nerve membranes. In their uncharged free-base form, they cross the lipid bilayer; once inside the neuron, they convert to the charged (ionized) form that blocks the Na+ channel from INSIDE. This prevents the Na+ influx needed for action potential generation and propagation, blocking nerve conduction. No Na+ influx = no action potential = no pain signal.
  • B. Opening K+ channels would cause hyperpolarization — but local anesthetics work by BLOCKING Na+ channels, not opening K+ channels.
  • C. GABA receptor enhancement is the mechanism of benzodiazepines and barbiturates — NOT local anesthetics.
  • D. Calcium channel blockers (like verapamil) affect cardiac and vascular smooth muscle — NOT the mechanism of local anesthetic action.

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