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Local Anesthetics

Pharmacology

Local Anesthetics
Structure tertiary amine attached to aromatic ring with either an ester or amide linkage; basic; termed aminoesters or aminoamides
Mechanism of Action when electrostatic forces cause sodium channels to open, the local anesthetic, in its charged form, binds to its channel receptor and blocks the channel; local anesthetics can only enter through the lipid membrane in its uncharged form
Potency potencies are compared through their minimal blocking concentration, or Cm; Cm is the drug concentration that just halts impulse traffic over an in vitro 10 mm length of nerve
Duration of Action associated with drug's affinity for plasma alpha-1 acid glycoprotein
Concept of Differential Block A, B, and C nerve fibers; small B and unmyelinated C fibers require a lesser concentration of local anesthetic to produce conduction block than do the thicker myelinated A fibers
Organization of Nerves into Bundles nervve fibers are grouped into bundles; motor fibers are usually in the periphery, while sensory fibers are in the core; motor block will often be seen before sensory block
Routes of Metabolism aminoesterases are metabolized by cholinesterases in the plasma and liver; aminoamides are metabolized by the liver
CNS Effects excitatory; lightheadedness, dizziness, muscle twitching, seizures
Cardiovascular Effects depresses myocardial conduction
Bupivacaine 70x more potent than lidocaine in depressing myocardial conduction
Local Anesthetics Procaine, Lidocaine, Mepivacaine, Tetracaine, Bupivacaine
Created by: DrCutiepie
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