LOCAL ANAESTHESIA

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General Propertiest

Machanism of action

  • LAs block both the generation and the conduction of the nerve impulses
  • The blockage results from biochemical changes caused by the drug on the lipotropic film of cell membrane.

 

Pharmacological Actions

  1. On CVS :
  • Myocardiac depressants
  • Heart rate ¯ ed
  • Excitability and refractory period are ­
  • Produce hypotension

 

  1. On CNS :
  • Cause light – headedness, dizziness and blurred vision
  • Restlessness, tremors and convulsions
  • Higher does causes CNS stimulation followed by depression

 

  1. Other actions :
  • Direct spasmolytic action on smooth muscle.
  • Can produce neuro-muscular blockade in large doses

 

Absorption, Fate & Excretion

  • LA’s are not absorbed from unbroken sking
  • Absorption is more rapid from the trachea than the pharynx while it is poor through the urinary bladder.
  • Metabolized by hydrolysis in both liver and plasma.
  • The amide like LA’s are degraded by liver microsomes.

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