Local Anesthetics

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Can you name the Local Anesthetics?

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

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Created Sep 18, 2011ReportNominate
Tags:Nintendo, local