Local Anesthetics

9.2
Local Anesthetics

  • Structure
    • Ester or amide linkage (Figure 9.1)
    • Esters have one I in their name
      • Procaine
      • Benzocaine
    • Amides have two I’s in their name
      • Lidocaine
      • Articaine
      • Mepivacaine
An illustration of a chemical bond reads amine bond and ester bond.

Figure 9.1

  • Mechanism of Action (Figure 9.2)
    • Antagonize neuronal Na+ channels to prevent signal transmissions
    • Must cross the cell membrane and inactivate the channel intracellularly

Pharmacokinetics

  • ↑ Potency
    • ↑ Lipid solubility
  • ↓ Onset of Action
    • ↑ Concentration
    • ↑ Lipid solubility
      • Easier to diffuse through cellular membranes
    • pKa closer to physiologic pH
  • ↑ Duration
    • Presence of vasoconstrictors
    • ↑ Protein binding
A schematic diagram of a mechanism of action in antagonising neuronal. It reads N plus ions, intracellular, extracellular and local anaesthetic.

Figure 9.2

Physiologic Effects

  • Cerebral
    • IV
      • ICP on intubation
      • ↓ MAC
        • Except cocaine
  • Cardiovascular
    • Lidocaine
      • Class 1B antidysrhythmic
    • Bupivacaine
      • Complete cardiac conduction block with overdose or accidental intravascular injection
    • Regional
      • If vasoconstrictors are included, may transiently increase CO, MAP, and HR
  • Pulmonary
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Oct 16, 2024 | Posted by in Oral and Maxillofacial Surgery | Comments Off on Local Anesthetics

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