Local Anesthetics

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Can you name the Local Anesthetics?

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

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Created Sep 18, 2011ReportNominate
Tags:Nintendo, local