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    Local Anesthetics

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    Nia NaNa Try Faithful
    This document discusses local anesthetics, including their classification as esters or amides, mechanism of action by blocking sodium channels, and pharmacokinetics of absorption, distribution, and clearance. It describes the sequence of sensory and motor block from local anesthetics and factors that determine their potency and duration. Techniques for their use include infiltration, regional blocks like nerve blocks or epidurals, and surface anesthesia. Risks include local tissue toxicity and systemic toxicity from overdose.

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    Local Anesthetics

    Uploaded by

    Nia NaNa Try Faithful
    86 views35 pages
    This document discusses local anesthetics, including their classification as esters or amides, mechanism of action by blocking sodium channels, and pharmacokinetics of absorption, distribution, and clearance. It describes the sequence of sensory and motor block from local anesthetics and factors that determine their potency and duration. Techniques for their use include infiltration, regional blocks like nerve blocks or epidurals, and surface anesthesia. Risks include local tissue toxicity and systemic toxicity from overdose.

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    penting sekali

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    This document discusses local anesthetics, including their classification as esters or amides, mechanism of action by blocking sodium channels, and pharmacokinetics of absorption, distribution, and clearance. It describes the sequence of sensory and motor block from local anesthetics and factors that determine their potency and duration. Techniques for their use include infiltration, regional blocks like nerve blocks or epidurals, and surface anesthesia. Risks include local tissue toxicity and systemic toxicity from overdose.

    Copyright:

    © All Rights Reserved
    Download as PPT, PDF, TXT or read online from Scribd
    Download as ppt, pdf, or txt
    86 views35 pages

    Local Anesthetics

    Uploaded by

    Nia NaNa Try Faithful
    This document discusses local anesthetics, including their classification as esters or amides, mechanism of action by blocking sodium channels, and pharmacokinetics of absorption, distribution, and clearance. It describes the sequence of sensory and motor block from local anesthetics and factors that determine their potency and duration. Techniques for their use include infiltration, regional blocks like nerve blocks or epidurals, and surface anesthesia. Risks include local tissue toxicity and systemic toxicity from overdose.

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    © All Rights Reserved
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    Local anesthetics

    Objectives
    • Recall how an action potential is generated
    and propagated
    • Classify local anesthtics
    • Describe the machanism of action,
    pharmacokinetics and toxic effects of local
    anesthetics
    • Describe the different techniqes of use of LA
    • Describe the risks and benefits of using
    vasoconstrictors with LA
    Overview
    • Local anesthetics produce a transient
    and reversible loss of sensation
    (analgesia) in a circumscribed region
    of the body without loss of
    consciousness.

    • Normally, the process is completely


    reversible.
    ANESTHETICS
    • Local anesthetics - esters or
    amides
    –a lipophilic aromatic group
    –to a hydrophilic, ionizable
    amine.

    • Most are weak bases


    Classification of LA
    Esters

    • Benzocaine

    • Procaine/

    • Proparacaine
    Classification of LA
    Amide
    • Bupivacaine

    • Levobupivacaine

    • Lidocaine/Lignocaine

    • Mepivacaine
    Ionized
    • Local anesthetics gain access to the
    inner axonal membrane by

    1. traversing sodium channels while they


    are more often in an open
    configuration

    2. passage directly through the plasma


    membrane
    • Block inititation and
    propagation of action
    potential
    Sequence of clinical anesthesia

    •Sympathetic block (vasodilatation)


    •Loss of pain and temperature sensation
    •Loss of proprioception
    •Loss of touch and pressure sensation
    •Loss of motor function
    Anesthetic Potency

    • Potency = lipid solubility

    • Higher solubility = can use a


    lower concentration and reduce
    potential for toxicity
    DURATION OF ACTION

    • Duration = protein binding

    • Bupivacaine 95%
    Lidocaine 65%
    Pharmacokinetics
    • Effective within 5 min
    • Duration of action – 1-1.5 h
    • Activity is Ph dependent
    • Increased action in acidic ph
    CLEARANCE

    • ESTERS
    hydrolysis via cholinesterase

    • AMIDES
    metabolism via hepatic enzymes
    LA

    • Infiltration anesthesia

    • Regional anesthesia

    • Surface anesthesia
    LA

    • Infiltration anesthesia

    • Regional anesthesia

    • Surface anesthesia
    Gegional anaesthesia
    • Nerve block

    • Intravenous

    • Extradural

    • Intrathecal block/ spinal anaesthesia


    Nerve block
    • Inject a drug around
    the nerve

    • Anaesthetise a region
    Intravenous
    • 0.5-1% lidocaine
    without adrenaline
    Extradural/epidural
    • Thoracic, lumbar,
    sacral
    • Act on nerve roots
    • No hypotention
    Spinal anesthesia
    • Sympathetic nerve
    block
    • hypotension
    LA

    • Infiltration anesthesia

    • Regional anesthesia

    • Surface anesthesia
    • On intact skin – eutectic
    mixture of bases of
    prilocaine (EMLA)

    • Slow absorption
    Prolongation of action

    • Add vasoconstrictor –
    adrenaline

    • Can use a larger dose

    • Not to – fingers, toes, nose,


    penis
    Adverse effects

    • LA’s cause some vasodilatation at


    site

    • LA toxicity related to rate of


    absorption via blood flow
    Systemic Toxicity
    • Blockage of voltaged-gated Na
    channel affects action potential
    propagation throughout the body

    • Potential is present for systemic


    toxicity
    Effects of local anesthetics
    • Excitation – anxiety, agitation,
    restlessness

    • Convulsions

    • Reduced myocardial contractility

    • Vasodilatation

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