Miscellaneous / Local Anesthetics

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Can you name the Local Anesthetics?

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HintAnswer
Ropivacaine class
Procaine class
SE: similar to tetracaine
SE: similar to tetracaine. However more cardiotoxic (arrythmias and hypotension), may be irreversible. Tx with epi, atropine, and bretylium.
Nerve selectivity: rapid firing, small diameter 'C' fibers and medium diameter, myelinated B sympathetic preganglionic fibers.
SE cont: All are vasodilators (except cocaine). Heart block, arrythmias, low BP. Can form metabolites that create hypersensitivity reactions.
Mepivacaine class
Long duration ester
Bupivacaine class
Benzocaine class
Surface active ester
Class P-kinetics cont: Most bound by plasma PRO, which effects clinical effects and toxicity.
SE: metabolized to products which can cause methemoglobinemia (treat with methylene blue)
SE: Can also block NE --> vasoconstriction and CV toxicity (HTN, cerebral hemorrhage, arrhythmias, and MI's)
Class P-kinetics: Similar in absorption & distribution and ionization to esters. Metabolism via CYP in liver (longer duration), liver function important in metabolism.
HintAnswer
Class P-kinetics cont: Weak base which must be lipophilic to pass through cell membrane to internally block channels and hydrophilic to bind channel.
Short duration ester
Long duration amide
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.
Lidocaine class
SE: light headedness, sedation, restless, nystagmus, tonic-clonic convulsions (tx with sedative hypnotics). Resp and CV collapse. High [ ] may permanent damage nerves.
Tetracaine class
Medium duration ester
Nerve selectivity: large diameter, slow firing, myelinated 'A' type motor neuron fibers
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
Medium duration amide
Prilocaine class
Cocaine class
Etidocaine class

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