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13 Cards in this Set
- Front
- Back
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What is the mechanism of action for Local anesthetics
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Uncharged drug crosses nerve cytoplasm. Gets reprotonated in cytoplasm(active), binds sodium channel in open state. Stabilizes inactive state, prevents influx of sodium. No AP
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What is the general structure of Local Anesthetics
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Must contain an aromatic ring connected to chain via ester or amide linkage. Pka between 7.8-9.0. Closer to physio pH, more rapid onset. Inactivated by pseudocholinest -- not found in CSF
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subcutaneous injection to anesthetize a region distal to injection
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Field block
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injection of LA into or around individual peripheral nerves or plexi
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Nerve block
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injection of a LA directly into tissue disregarding course of cutaneous nervew
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Infiltration
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What can be used to prolong the duration of LA
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Epinephrine -- reduces blood flow to decrease rate of absorption and localize anesth. NOT used in areas of poor collateral circ -- figers, toes, ears, nose
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What are the ADE of LA
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CNS -- stimulation restless, tremers, Resp depressioin, Unbalanced excitation followed by depression. CV -- myocardial depression, all relax SM except cocaine. Hypersensitivity -- more likely from esters because derived from PABA
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used in the primary anesthesis of mucous membranes that has both local and CNS effects due to blocking catecholamine reuptake
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Cocaine -- Adrenergic phenomenon. Also increases the release of Catecholamines presynaptically.
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LA used in infiltration and dental proceedures. Has a slow onset and short half life
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Procaine -- hydrolyzed to PABA -- hypersens reactions. DDI with warfarin and MAOi
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Topical LA used in anesthesia of mucous membranes and insertion of medical devices that fits into pore of Na channel and keeps it in CLOSED form
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Benzocaine -- short acting and potent. Cream, aerosol, ointment. Contraind -- Methemoglobinemia. DDI -- SULFA drugs, caffeine, alcohol
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LA used in spinal and topical procedures due to its HIGH potency, fast action and prolonged efect due to the BUTYL group
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Tetracaine -- since prolonged time, increased possibility for tox
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LA used that is an amino linked, fast and widely used for topical, oral, epidural, infiltration and nerve blocks
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Lidocaine -- metabolites are also active anesthetics. DDI with many inhibitors/inducers of CYP
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LA used in epidurals because it blocks sensory function without blocking motor
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Bupivicaine
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