Local Anesthetics

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Can you name the Local Anesthetics?

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

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