Local Anesthetics Flashcards
What is the mechanism of local anesthetics?
LA block voltage gated sodium channels preventing the influx of sodium ions, thus preventing an action potential
Local anesthetics bind Na channels in the _______ state
activated
How do local anesthetics affect resting and threshold potentials?
not altered
Which nerves are more easily blocked?Myelinated or unmyelinated?small or large fibers?resting or rapidly firing channels?proximal or distal?
Easier:MyelinatedSmallrapidly firingproximal
What are the three groups in the LA molecule?
Lipophilic group (benzene ring) and hdyrophilic group (tertiary amine) linked together with either an ester or amide
Name the amide LAs
LidocainemepivacainePrilocaineBupivacaineRopivacaineEtidocainei before the caine
Name the ester linked LAs
Procaine Chloroprocainetetrocainecocainebenzocaine
Where are the amides metabolized?
liver
Where are esters metabolized? Exception?
esters are metabolized by plasma cholinesterases, except cocaine which is met in liver
Which are more potent, esters or amides? What determines potency?
Esters are more potent. Potency determind by lipid solubility
what properties determine onset?
lipid solubility and pKa
What is the measure of local potency for LA that is similar to MAC?
Cm
What factors determine the absorption of LA?
DosageSite of injectionDrug-tissue bindingLocal blood flowvasoconstrictors
What side effect can metabolites of prilocaine and benzocaine have?
methemoglobinemia (ortholuidine)
What is the metabolite of esters that may cause an allergic rxn?
para aminobenzoic acid (PABA)
What is the physiologic effect of methemoglobinemia?
decreases O2 and CO2 carrying capacity of hemoglobin
Which group of pts have a higher risk for methemoglobinemia?
neonates due to fetal hemoglobin
What is normal methemoglobinemia?
<1%
What are the S & S of methemoglobinemia?
SOBcyanosischocolatey-brown arterial blood pulse ox that always reads 85%
What is the treatment for methemoglobinemia?
1-2 mg/kg methylene blue
Does addition of vasoconstrictors affect onset of LA?
no
Vasoconstrictors _________ duration of LA by limiting systemic _________ and maintaining the drug concentration at the _______.
increasesabsorptionnerve
Addition of epi (increases/decreases) the chance of systemic toxicity?
decreases
What is concentration of epi used with LA?
1:200,000 or 5 mcg/ml
How much does epi prolong the effect of bupivicaine?
epi has very little effect with bupivicaine
what factors influence the possibility of absorption leading to systemic toxicity?
DoseVascularity of sitepresence of epiproperties of the drug
Subcutaneous, intravenous, sciatic, tracheal, intercostal, brachial plexus, caudal, epidural paracervical. Arrange from most to least vascular
intravenous>tracheal>intercostal>caudal>paracervical>epidural>brachial plexus>sciatic>subcutaneous