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    Mechanism of Action of Local Anaesthetics

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    bcthejas
    Local anesthetics work by slowing the rate of depolarization and reducing the height and rate of rise of the action potential, which slows axonal conduction and ultimately prevents the propagation of action potentials without altering the resting membrane potential. They preferentially block small nerve fibers and nerves with higher firing frequencies or more positive membrane potentials. In nerve bundles, fibers located circumferentially are affected first. The effectiveness of local anesthetics is also affected by the pH of the application site. Local anesthetics bind to and inhibit many receptors and ion channels including sodium, potassium, and calcium channels as well as various enzymes and receptors.

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    Mechanism of Action of Local Anaesthetics

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    bcthejas
    10 views12 pages
    Local anesthetics work by slowing the rate of depolarization and reducing the height and rate of rise of the action potential, which slows axonal conduction and ultimately prevents the propagation of action potentials without altering the resting membrane potential. They preferentially block small nerve fibers and nerves with higher firing frequencies or more positive membrane potentials. In nerve bundles, fibers located circumferentially are affected first. The effectiveness of local anesthetics is also affected by the pH of the application site. Local anesthetics bind to and inhibit many receptors and ion channels including sodium, potassium, and calcium channels as well as various enzymes and receptors.

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    Local anesthetics work by slowing the rate of depolarization and reducing the height and rate of rise of the action potential, which slows axonal conduction and ultimately prevents the propagation of action potentials without altering the resting membrane potential. They preferentially block small nerve fibers and nerves with higher firing frequencies or more positive membrane potentials. In nerve bundles, fibers located circumferentially are affected first. The effectiveness of local anesthetics is also affected by the pH of the application site. Local anesthetics bind to and inhibit many receptors and ion channels including sodium, potassium, and calcium channels as well as various enzymes and receptors.

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    Attribution Non-Commercial (BY-NC)
    Download as PPT, PDF, TXT or read online from Scribd
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    10 views12 pages

    Mechanism of Action of Local Anaesthetics

    Uploaded by

    bcthejas
    Local anesthetics work by slowing the rate of depolarization and reducing the height and rate of rise of the action potential, which slows axonal conduction and ultimately prevents the propagation of action potentials without altering the resting membrane potential. They preferentially block small nerve fibers and nerves with higher firing frequencies or more positive membrane potentials. In nerve bundles, fibers located circumferentially are affected first. The effectiveness of local anesthetics is also affected by the pH of the application site. Local anesthetics bind to and inhibit many receptors and ion channels including sodium, potassium, and calcium channels as well as various enzymes and receptors.

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    Download as PPT, PDF, TXT or read online from Scribd
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    Mechanism of action of local

    anaesthetics
    Nerve cell membrane
    Action potential
    Action potential
    Mechanism of action
     slow rate of depolarization
     reduce height of action potential
     reduce rate of rise of action potential
     slow axonal conduction
     ultimately prevent propagation of action
    potential
     do not alter resting membrane potential
     increase threshold potential
    Mechanism of action
     Local anesthetics preferably block
    small nerve fiber.
     Nerves with higher firing frequency
    and more positive membrane
    potential are more sensitive to local
    anesthetic block (use-dependent
    block).
    Mechanism of action
     In nerve bundles, fibers that are
    located circumferentially are affected
    first by local anesthetics.
     Effectiveness of local anesthetics is
    affected by the pH of the application
    site.
    LAs bind and inhibit many
    differing receptors and
    channels

    Do not assume LA toxic side effects


    arise from Na channel inhibition!
    LAs bind and inhibit many
    differing receptors and
    channels

     Na, K, Ca channels
     G-protein modulation of channels
    LAs bind and inhibit many
    differing receptors and
    channels
     Many enzymes
     Adenylyl cyclase
     Guanylyl cyclase
     Lipases
     Many receptors
     Nicotinic acetylcholine
     NMDA
     β2-adrenergic

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