Local Anesthetics

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Can you name the Local Anesthetics?

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Nerve selectivity: rapid firing, small diameter 'C' fibers and medium diameter, myelinated B sympathetic preganglionic fibers.
Long duration amide
Mepivacaine class
Short duration ester
Medium duration ester
Class P-kinetics cont: Most bound by plasma PRO, which effects clinical effects and toxicity.
SE: metabolized to products which can cause methemoglobinemia (treat with methylene blue)
Prilocaine 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
Class of P-kinetics cont: pH dependent (HH principles) ionization important. Hydrolyzed relatively rapidly via butyrylcholinesterase (except benzocaine which is topical only)
SE: similar to tetracaine. However more cardiotoxic (arrythmias and hypotension), may be irreversible. Tx with epi, atropine, and bretylium.
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.
Medium duration amide
Long duration ester
HintAnswer
Surface active ester
Lidocaine class
Benzocaine class
Ropivacaine 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)
Bupivacaine class
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
Class P-kinetics: Similar in absorption & distribution and ionization to esters. Metabolism via CYP in liver (longer duration), liver function important in metabolism.
SE: similar to tetracaine
SE cont: All are vasodilators (except cocaine). Heart block, arrythmias, low BP. Can form metabolites that create hypersensitivity reactions.
Etidocaine class
Cocaine class
Procaine class

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Created Sep 18, 2011ReportNominate
Tags:Nintendo, local