Local Anesthetics Flashcards
Nerve Effects
Small Fibers easier to block
Heavily Myelinated nerves easier
Nerve bundles are harder to block
Resting sodium channels have low affinity
Cardiac cells can be susceptible to blockade
Lipophilic group
Benzene Ring
Hydrophilic group
Tertiary Amine
Ester vs amide linkage
classification
Amide Vs Ester Classification
Amides have an I before the “caine” and metabolized by the liver
Esters (except cocaine) are metabolized by plasma cholinesterase
Potency
Lipid solubility
More lipid soluble is more potent
Onset
Lipid solubility and pKa
More lipid solubility is faster onset and closer to tissue pH is faster onset
Cm (minimum concentration)
Measurement of the potency. Minimum concentration for anesthetic to work.
Para-aminobenzoic Acid (PABA)
Metabolite of Ester local anesthetic metabolism.
This is generally what people are allergic to when they are allergic to LA
Also in sunscreen
Methemoglobinemia
Prilocaine/Benzocaine: Ortholuidine
Normal metHgB <1%
Pulse oximeter will go down to 85%
Treat with 1-2mg/kg of methylene blue
Vasoconstrictor
Used to increase duration of action by limiting absorption
Common epinephrine 5mcg/mL (1:200,000) mixed in
Systemic Toxicity Causes
IV Injection (Most Common)
Absorption from injection site
Depends on: Dose administered, vascularity of site, presence of epi, properties of the drug.
Vascularity (From top to least)
Tracheal Intercostal Caudal Paracervical Epidural Brachial Plexus Sciatic Subcutaneous
CNS Systemic Toxicity
Circumoral numbness
Restlessness
Slurred Speech
Seizure
CV Systemic Toxicity
Hypotension Decreased Cardiac Conduction Ventricular Arrythmias Bupivicaine (most cardiotoxic) Treatment is 1.5 mg/kg IV over 10 minutes
Systems in order
Circumoral Numbness Tinnitus Lightheadedness Visual Disturbances Muscle Twitching Unconsciousness convulsions Respiratory Depression Cardiovascular Collapse
Toxic Doses
Lidocaine: 5mg/kg or 7mg/kg with epi
Bupivicaine: 2.5mg/kg
Cocaine
Blocks sodium channels, but crosses the BBB easily
Also a vasoconstrictor by blocking reuptake of norepinephrine
IV/smoked onset is 5 minutes
30 minute onset nasal
Spinal Anesthesia Lidocaine
Duration: 1.5 hours
5% with 7.5% dextrose
Transient Neurologic Symptoms
Spinal Anesthesia Bupivicaine
2-2.5 hours
0.5% and 0.75% with or without dextrose
Spinal Anesthesia Tetracaine
2-3 hours up to 5 with epi
1% solution, can be mixed with 10% dextrose
Bier Block
Unknown Mechanism of Action
50mL 5% lidocaine or prilocaine
Dose of prilocaine not sufficient for methemoglobinemia
EMLA (eutectic mixture of local anesthetic)
Onset: 45-60 minutes
Duration: about an hour
Contraindications: broken skin or baby <12 months]
Dose: 1-2gm/cm^2