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Notes in
16 Local Anesthetics
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fillet-oven-grey-vermont-oklahoma-carolina
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Published
12/13/2023
Local anesthetics bind to the {{c1::alpha}} subunit of of voltage gated Na channels.
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In {{c1::phasic (use-dependent)}} blockade, local anesthetics have a faster onset with {{c2::frequent depolarization}} of a nerve.…
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Smaller diameter nerve fibers are {{c1::more::more/less}} sensitive to local anesthetics.
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A-alpha fibers are {{c1::less::more/less}} sensitive to local anesthetics than A-delta fibers.
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Small unmyelinated C fibers are relatively {{c1::resistant::sensitive/resistant}} to inhibition by local anesthetics compared to large myelinated fibe…
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Local anesthetics contain a {{c1::lipophilic}} benzene ring, {{c2::hydrophilic}} amine group, and an {{c3::ester}} or {{c3::amide}} intermediate chain…
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The lipophilic group of local anesthetics are usually {{c1::benzene rings}}.
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The hydrophilic group of local anesthetics are usually {{c1::tertiary amines}}.
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Local anesthetics are {{c1::weak::strong/weak}} {{c2::bases::acids/bases}}.
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The {{c1::nonionized}} form of local anesthetics is the form that crosses the neuronal membrane.
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The {{c1::ionized}} form of local anesthetics is the form that binds the voltage-gated Na+ channel.
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Highly {{c2::lipid}} soluble local anesthetics have a {{c1::longer::longer/shorter}} duration of action.
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There is increased {{c1::systemic}} absorption with increased vascularity of the injection site.
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The sites of injection ranked according to {{c11::vascularity and systemic absorption}} (greatest to least) can be memorized with the mnemonic IT…
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The addition of epinephrine to local anesthesia prolongs the uptake of {{c1::shorter}} acting agents like tetracaine and lidocaine.
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Epinephrine and clonidine can augment analgesia by local anesthetics through activation of {{c1::α2}} receptors.
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{{c2::Ester}} local anesthetics are predominantly metabolized by {{c1::pseudocholinesterases}}.
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Amide local anesthetics are metabolized by CYP-{{c1::3A4}} and {{c3::1A2}}.
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Oral symptoms of local anesthetic toxicity include {{c1::circumoral}} numbness, paresthesias of the {{c2::tongue}}, and a {{c3::metallic}} taste. …
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At {{c3::high::high/low}} concentrations, local anesthetics cause vaso{{c2::dilation}}, except {{c1::cocaine}}.
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{{c1::Neurologic::CV/Neuro}} signs and symptoms of local anesthetic toxicity occur BEFORE {{c1::cardiovascular::CV/Neuro}} ones.
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{{c2::Bupivacaine}} is a local anesthetic that is associated with severe {{c1::cardiovascular}} toxicity
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What populations are at increased risk for bupivacaine toxicity?{{c1::Pregnant women and children}}
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First line treatment for local anesthetic toxicity should be {{c1::20% lipid emulsion}}, which sequesters local anesthetics and reduces plasma co…
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Ropivacaine produces {{c1::less::more/less}} motor blockade than bupivacaine.
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Ester local anesthetics are {{c1::more::more/less}} likely to induce an allergic reaction than amide.
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{{c2::2-Chloroprocaine}} antagonitzes {{c1::μ and κ}} opioid receptors in the spinal cord.
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Which nerve fibers are unmyelinated? {{c1::C fibers}}
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Which nerve fibers are initially affected by local anesthetics?{{c1::B nerve fibers}}
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What modalities do the B nerve fibers serve?{{c1::Preganglionic sympathetic fibers}}
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Which fibers are the first fibers to recover from spinal anesthesia?{{c1::A-alpha}}
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What modalities do the A-alpha fibers serve?{{c1::Motor control (efferent)}}
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What modalities do the A-beta fibers serve?{{c1::Touch}} and {{c1::pressure}}
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What modalities do the A-gamma fibers serve?{{c1::Proprioception (muscle spindles)}}
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What modalities do the A-delta fibers serve?{{c1::temperature}} and {{c1::pain}}
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What modalities do the C fibers serve?{{c1::temperature}}, {{c1::pain}}
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What fibers are responsible for sensing pain?{{c1::A-delta, C}}
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What fibers are responsible for sensing temperature?{{c1::A-delta, C}}
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What fibers are responsible for proprioception?{{c1::A-gamma}}
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What fibers are responsible for motor control?{{c1::A-alpha}}
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The potency of local anesthetics is directly proportional to the {{c1::lipid solubility}}.
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The duration of action of local anesthetics is directly proportional to the {{c1::degree of protein binding}}.
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Local anesthetics with a {{c1::pKa}} closest to physiologic pH have the {{c2::fastest::slowest/fastest}} onset of action.
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Bupivacaine is a local anesthetic with an {{c1::amide}} structure.
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Lidocaine is a local anesthetic with an {{c1::amide}} structure.
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Tetracaine is a local anesthetic with an {{c1::ester}} structure.
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Allergic reactions to {{c2::ester}} local anesthetics are from the compound {{c1::PABA}}.
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Allergic reactions due to {{c2::amide}} local anesthetics are from the compound {{c1::methylparaben}}.
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Blurred vision, tinnitis, dizziness, metallic taste, and altered levels of conciousness are neurological signs of {{c1::local anesthetic}} toxici…
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What size of nerve fiber, small or large diameter, is affected first by local anesthetics?{{c1::Small-diameter fibers}}
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Which nerve fibers (size, myelination) are affected first by local anesthetics?{{c1::Small, myelinated fibers}}
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What type of local anesthetics are procaine, cocaine, tetracaine, and benzocaine?{{c1::Esters}}
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Would a small, unmyelinated or large, myelinated fiber be affected first by local anesthetics?{{c1::Small, unmyelinated}}
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What type of nerve fiber, myelinated or unmyelinated, is affected first by local anesthetics?{{c1::Myelinated fibers}}
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What type of local anesthetic are lidocaine, mepivacaine, and bupivacaine?{{c1::Amides}}
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What type of local anesthetics should be given to a patient who is allergic to ester local anesthetics (e.g. procaine)?{{c1::Amide anesthetics (e.g. l…
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12/13/2023
What drugs increases the risk of bupivacaine toxicity (3)?{{c1::β-blockersCalcium channel blockersDigoxin}}
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