Local Anesthetics

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Can you name the Local Anesthetics?

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SE: Can also block NE --> vasoconstriction and CV toxicity (HTN, cerebral hemorrhage, arrhythmias, and MI's)
MOA: State dependent blockage of voltage dependent Na channels, prevent depolarization and conduction of APs in excitable cells esp. neurons when localized next to neurons
Medium duration ester
Procaine class
SE: similar to tetracaine
Short duration ester
Nerve selectivity: large diameter, slow firing, myelinated 'A' type motor neuron fibers
Class P-kinetics: Similar in absorption & distribution and ionization to esters. Metabolism via CYP in liver (longer duration), liver function important in metabolism.
Medium duration amide
Etidocaine class
Cocaine class
Class P-kinetics cont: Weak base which must be lipophilic to pass through cell membrane to internally block channels and hydrophilic to bind channel.
Benzocaine class
Prilocaine class
Class P-kinetics: systemic absorption is proportional to vascularization, widely distributed in not locally injected.
HintAnswer
Long duration amide
Tetracaine class
SE: metabolized to products which can cause methemoglobinemia (treat with methylene blue)
Surface active ester
Long duration ester
Bupivacaine class
Nerve selectivity: rapid firing, small diameter 'C' fibers and medium diameter, myelinated B sympathetic preganglionic fibers.
Mepivacaine class
Class P-kinetics cont: Most bound by plasma PRO, which effects clinical effects and toxicity.
SE cont: All are vasodilators (except cocaine). Heart block, arrythmias, low BP. Can form metabolites that create hypersensitivity reactions.
SE: light headedness, sedation, restless, nystagmus, tonic-clonic convulsions (tx with sedative hypnotics). Resp and CV collapse. High [ ] may permanent damage nerves.
SE: similar to tetracaine. However more cardiotoxic (arrythmias and hypotension), may be irreversible. Tx with epi, atropine, and bretylium.
Class of P-kinetics cont: pH dependent (HH principles) ionization important. Hydrolyzed relatively rapidly via butyrylcholinesterase (except benzocaine which is topical only)
Ropivacaine class
Lidocaine class

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