Local Anesthetics

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Can you name the Local Anesthetics?

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

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