02 Local Anesthesia
02 Local Anesthesia
Anesthetics
Jason Ryan, MD, MPH
Local Anesthetics
• Amides
• Lidocaine
• Mepivacaine
• Bupivacaine
• Esters
• Procaine
• Cocaine
• Benzocaine
• Tetracaine
Cell
Membrane
X
B + H+ BH+
Key Points
1. Uncharged form crosses membrane
2. Charged form blocks Na channel
3. Drugs work on inside of cell membrane
4. Acidic environments = more drug needed for effect
Adding Epinephrine
• LA can be given with epinephrine
• Causes vasoconstriction
• Less bleeding
• Less washout → more local effect
Differential Blockade
• Small fibers > large fibers
• Myelinated > unmyelinated
Differential Blockade
• Different effects different senses
• Pain blocked first, pressure last
Local Anesthetics Uses
• Minor surgical procedures
• Epidural/spinal anesthesia
Local Anesthetics Side Effects
• CNS Stimulation
• Initial (excitation):Talkativeness, anxiety, confusion, stuttering
speech
• Later: Drowsiness, coma
• Cardiovascular
• Hypotension, arrhythmia, bradycardia, heart block
• Cocaine is exception: hypertension, vasoconstriction
• Bupivacaine most cardiotoxic
Methemoglobinemia
• Iron in hemoglobin normally reduced (Fe2+)
• Certain drug oxidize iron to Fe3+
• When Fe3+ is present → methemoglobin
• Fe3+ cannot bind oxygen
• Remaining Fe 2+ cannot release to tissues
• Acquired methemoglobinemia from drugs
• Local anesthetics (benzocaine)
• Nitric oxide
• Dapsone
• Treatment: methylene blue
Clinical Scenario
• Endoscopy patient
• Benzocaine spray used for throat analgesia
• Post procedure shortness of breath
• “Chocolate brown blood”
• O2 sat (pulse oximetry) = variable (80s-90s)
• PaO2 (blood gas) = normal
• Also premature babies given NO for pulmonary
vasodilation