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
 
 
 

- 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
 
 

Physiologic Effects
- Cerebral
- IV
- ↓ ICP on intubation
 - ↓ MAC
- Except cocaine
 
 
 
 - IV
 - 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
 
 
 - Lidocaine
 - Pulmonary
 
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