Local Anesthetics

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Can you name the Local Anesthetics?

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

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