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.
SE: metabolized to products which can cause methemoglobinemia (treat with methylene blue)
Class P-kinetics cont: Most bound by plasma PRO, which effects clinical effects and toxicity.
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.
Tetracaine class
Class P-kinetics: systemic absorption is proportional to vascularization, widely distributed in not locally injected.
Mepivacaine class
Benzocaine class
Procaine 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: Can also block NE --> vasoconstriction and CV toxicity (HTN, cerebral hemorrhage, arrhythmias, and MI's)
SE: light headedness, sedation, restless, nystagmus, tonic-clonic convulsions (tx with sedative hypnotics). Resp and CV collapse. High [ ] may permanent damage nerves.
Long duration ester
Class P-kinetics cont: Weak base which must be lipophilic to pass through cell membrane to internally block channels and hydrophilic to bind channel.
HintAnswer
Ropivacaine class
Nerve selectivity: large diameter, slow firing, myelinated 'A' type motor neuron fibers
Lidocaine 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
Prilocaine class
Etidocaine class
Medium duration amide
Cocaine class
Surface active ester
Bupivacaine class
SE: similar to tetracaine. However more cardiotoxic (arrythmias and hypotension), may be irreversible. Tx with epi, atropine, and bretylium.
Medium duration ester
SE: similar to tetracaine
Long duration amide

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