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    2 LOCAL ANAESTHETICS Egerton

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    Malueth Angui
    Local anaesthetics work by reversibly blocking sodium channels in nerve membranes, preventing the transmission of nerve impulses. They are used clinically to block pain or sympathetic responses in specific body areas without affecting consciousness. Newer local anaesthetics were developed to reduce irritation, toxicity, and have a faster onset and longer duration of action. They are administered via injection near nerves and their pharmacokinetics and pharmacodynamics allow for reversible nerve blockade depending on the specific agent used.

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    2 LOCAL ANAESTHETICS Egerton

    Uploaded by

    Malueth Angui
    19 views24 pages
    Local anaesthetics work by reversibly blocking sodium channels in nerve membranes, preventing the transmission of nerve impulses. They are used clinically to block pain or sympathetic responses in specific body areas without affecting consciousness. Newer local anaesthetics were developed to reduce irritation, toxicity, and have a faster onset and longer duration of action. They are administered via injection near nerves and their pharmacokinetics and pharmacodynamics allow for reversible nerve blockade depending on the specific agent used.

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    2 LOCAL ANAESTHETICS egerton

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    Local anaesthetics work by reversibly blocking sodium channels in nerve membranes, preventing the transmission of nerve impulses. They are used clinically to block pain or sympathetic responses in specific body areas without affecting consciousness. Newer local anaesthetics were developed to reduce irritation, toxicity, and have a faster onset and longer duration of action. They are administered via injection near nerves and their pharmacokinetics and pharmacodynamics allow for reversible nerve blockade depending on the specific agent used.

    Copyright:

    © All Rights Reserved
    Download as PPTX, PDF, TXT or read online from Scribd
    Download as pptx, pdf, or txt
    19 views24 pages

    2 LOCAL ANAESTHETICS Egerton

    Uploaded by

    Malueth Angui
    Local anaesthetics work by reversibly blocking sodium channels in nerve membranes, preventing the transmission of nerve impulses. They are used clinically to block pain or sympathetic responses in specific body areas without affecting consciousness. Newer local anaesthetics were developed to reduce irritation, toxicity, and have a faster onset and longer duration of action. They are administered via injection near nerves and their pharmacokinetics and pharmacodynamics allow for reversible nerve blockade depending on the specific agent used.

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    © All Rights Reserved
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    Download as pptx, pdf, or txt
    of 24

    LOCAL ANAESTHETICS

    DR. GATHIRI
    Introduction
    • Local anaesthetics reversibly block impulse
    conduction along nerve axons and other
    excitable membranes that utilise Na channels
    as the primary means of action potential
    generation.
    • A LA is a drug that can reversibly prevent
    transmission of the nerve impulse in the region
    to which it is applied without affecting
    consciousness.
    Contd…
    • This can be used clinically to block pain
    sensation or sympathetic vasoconstrictor
    impulses to specific areas of the body.
    Contd…
    • Historically, cocaine was the 1st in 1860.
    • Used as an ophthalmic anaesthetic but found
    to have addicting CNS actions.
    • 1905- procaine.
    • Goals of producing newer Las were to reduce
    local irritation and tissue damage, minimise
    systemic toxicity, faster onset of action and
    longer duration of action.
    Basic pharmacology
    chemistry
    • Most LAs consist of a lipophilic group (mostly
    an aromatic ring) connected by an chain-
    which includes an ester or amide to an
    ionizable group (usually a tertiary amine).
    classification
    esters amides
    • Cocaine • Lidocaine/xylocaine
    • Procaine • Mepivacaine
    • • Bupivacaine
    Tetracaine
    • Etidocaine
    • Benzocaine
    • Prilocaine
    • chloroprocaine • Ropivacaine
    • Levobupivacaine
    • Cinchocaine
    Pharmacokinetics
    • LAs are usually administered by an injection
    into the area of the nerve fibres to be blocked.
    • Of importance is determining the rate of offset
    of anaesthesia, and the likelihood of CNS and
    cardiac toxicity.
    a. absorption
    • Systemic absorption of injected LA from the
    site of administration depends on several
    factors:
     Dosage
     Site of injection
     Drug tissue binding
     Presence of vasoconstrictor substances
     Physicochemical properties of the drug
    Contd…
    • Application of LA to a highly vascular area eg.
    Trachea results in rapid absorption and thus
    higher blood levels than in a poorly perfused
    area.
    • Vasoconstrictor substances eg. epinephrine
    reduce systemic absorption of LAs from the
    depot site by decreasing blood flow in these
    areas.
    b. Distribution
    • Amide LAs are widely distributed after IV bolus
    administration.
    • After an initial rapid distribution phase,
    indicative of uptake into highly perfused
    organs eg. Brain, liver, kidney, heart, a slower
    distribution phase occurs with uptake into
    moderately well perfused tissues-muscle gut.
    c. Metabolism and excretion
    • LAs are converted in the liver or in plasma to
    more water soluble metabolites then excreted
    in urine.
    • Ester type LAs are hydrolysed rapidly in the
    body to by butyrylcholinesterase
    (pseudocholinesterase). Have a short T ½, Eg.
    Less than 1 minute for procaine and
    chloroprocaine.
    Contd…
    • Amide linkage of LAs is hydrolysed by liver
    microsomal cytochrome P450.
    • The metabolism varies.
    • Prilocaine(fastest)>etidocaine>lidocaine>mepi
    vacaine>bupivacaine(slowest).
    • :. Toxicity from the amide group is likely to
    occur in patients with liver disease.
    Contd…
    • Decreased hepatic removal of LAs should also
    be anticipated in patients with reduced
    hepatic blood flow.
    Pharmacodynamics
    A: mechanism of action
    • Blockade of voltage gated sodium channels
    leading to peripheral nerve blockade.
    • The excitable membrane of nerve axons and
    neuronal cell bodies maintains a
    transmembrane potential of -90 to -60mV.
    • With excitation, the Na channels open and a
    fast inward Na current depolarises the
    membrane toward the Na equilibrium potential
    (+40mV).
    Contd…
    • With depolarisation, Na channels close
    (inactivate) and potassium channels open.
    • The outward flow repolarises the membrane
    toward the potassium equilibrium potential
    (-95mV).
    • Repolarisation returns the Na channels to the
    rested state.
    Contd…
    • The Las block the Na channel.
    • With increased concentrations of the LA, the
    threshold for excitation increases, impulse
    conduction slows, the rate of rise of the AP
    declines, the AP amplitude decreases and
    then the ability to generate an AP is abolished.
    B: actions on nerves
    • Cause loss of sensation but also of motor
    paralysis.
    • Upon application of LA, the smaller B and C
    type fibres are blocked first.
    • The small type A delta fibres are blocked next.
    • Pain is blocked first and motor function last.
    Fibre type Fn Diameter myelination Conduction Sensitivity to
    μm velocity (m/s) block

    Type A Proprioception, 12-20 heavy 70-120 +


    Alpha motor

    Beta Touch, pressure 5-12 heavy 30-70 ++

    Gamma Muscle spindles 3-6 heavy 15-30 ++

    Delta Pain, 2-5 heavy 12-30 +++


    temperature

    Type B Preganglionic <3 light 3-15 ++++


    autonomic

    Type C Pain 0.4-1.2 none 0.5-2.3 ++++


    Dorsal root

    Sympathetic Postganglionic 0.3-1.3 none 0.7-2.3 ++++


    C: effects on other excitable tissues
    • LA s have weak neuromuscular blocking
    effects-little clinical importance.
    • Some are useful antiarrhythmic agents ant
    lower concentrations.
    Clinical pharmacology
    • Analgesia
    • Routes of admnistration: epidural, SAB,
    topical, within the vicinity of the peripheral
    nerve endings, major nerve trunks.
    Contd…
    • Choice depends on duration of action

    • Short acting
    • Procaine
    • Chloroprocaine
    Contd…
    • Intermediate acting
    • Lidocaine
    • Mepivacaine
    • Prilocaine
    • Long acting
    • Tetracaine
    • Bupivacaine
    • Etidocaine
    • Ropivacaine
    Additives
    • Vasoconstrictors eg epinepherine and
    phenylepherine.
    • Good for those with short to intermediate
    duration of action.
    • The vasoconstrictor retards the removal of the
    LA from the site.
    • Decreases blood level=reduced toxicity
    • Carbonates-accelerates the onset of action of LA
    Toxicity
    • CNS
    • CVS
    • Peripheral nervous system (neurotoxicity)
    • Blood

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