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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 |