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