Local Anesthetics

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Can you name the Local Anesthetics?

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Class P-kinetics: Similar in absorption & distribution and ionization to esters. Metabolism via CYP in liver (longer duration), liver function important in metabolism.
Cocaine class
Short duration ester
Prilocaine class
SE: similar to tetracaine
Long duration ester
SE cont: All are vasodilators (except cocaine). Heart block, arrythmias, low BP. Can form metabolites that create hypersensitivity reactions.
Long duration amide
Benzocaine class
Class P-kinetics cont: Most bound by plasma PRO, which effects clinical effects and toxicity.
SE: similar to tetracaine. However more cardiotoxic (arrythmias and hypotension), may be irreversible. Tx with epi, atropine, and bretylium.
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)
Class P-kinetics: systemic absorption is proportional to vascularization, widely distributed in not locally injected.
Medium duration amide
Nerve selectivity: large diameter, slow firing, myelinated 'A' type motor neuron fibers
Lidocaine class
Procaine 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.
Etidocaine class
Medium duration ester
Ropivacaine class
Surface active ester
Mepivacaine class
Tetracaine class
Bupivacaine 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)
Nerve selectivity: rapid firing, small diameter 'C' fibers and medium diameter, myelinated B sympathetic preganglionic fibers.
SE: Can also block NE --> vasoconstriction and CV toxicity (HTN, cerebral hemorrhage, arrhythmias, and MI's)

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