Local Anesthetics

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Can you name the Local Anesthetics?

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

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