Chemistry of Local Anaesthetics

CHEMISTRY OF LOCAL ANAESTHETICS

Local anaesthetics are divided chemically into two groups:

  • Lengthening of intermediate chain or addition of Carbon atoms in the amine or aromatic increase in potency
  • Addition of butyl group to the amine or aromatic end → lipid solubility, protein binding → increased potency and long action

Structure activity relationship of local anaesthetics

Features of Amide LAs

  • More intense and longer lasting anaesthesia
  • Bind to plasma protein ( α1 acid glycoprotein)
  • Not hydrolysed by plasma esterases
  • Rarely cause hypersensitivity
  • Ester type LAs – cocaine, procaine, chloroprocaine, tetracaine, benzocaine
  • Amide type LAs – lidocaine (lignocaine), bupivacaine, dibucaine, prilocaine
Last modified: Tuesday, 15 May 2012, 11:50 AM