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    Local Anaesthetics: Dr. R. Jamuna Rani MD, Professor & HOD, Department of Pharmacology

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    Aimee Ann Macaraeg
    Local anesthetics reversibly block nerve impulse generation and conduction. Cocaine was the first discovered local anesthetic in 1860. Procaine, a synthetic derivative, was introduced in 1905 due to cocaine's toxicity. Local anesthetics work by interacting with sodium channels and stabilizing nerve cell membranes to prevent impulse propagation. They are classified based on potency, duration, and whether they are natural, injectable, or for surface use. Adverse effects include delayed wound healing and arrhythmias when combined with vasoconstrictors.

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    Local Anaesthetics: Dr. R. Jamuna Rani MD, Professor & HOD, Department of Pharmacology

    Uploaded by

    Aimee Ann Macaraeg
    73 views25 pages
    Local anesthetics reversibly block nerve impulse generation and conduction. Cocaine was the first discovered local anesthetic in 1860. Procaine, a synthetic derivative, was introduced in 1905 due to cocaine's toxicity. Local anesthetics work by interacting with sodium channels and stabilizing nerve cell membranes to prevent impulse propagation. They are classified based on potency, duration, and whether they are natural, injectable, or for surface use. Adverse effects include delayed wound healing and arrhythmias when combined with vasoconstrictors.

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    6_LOCALANAESTHETICSDr_JRnew

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    Local anesthetics reversibly block nerve impulse generation and conduction. Cocaine was the first discovered local anesthetic in 1860. Procaine, a synthetic derivative, was introduced in 1905 due to cocaine's toxicity. Local anesthetics work by interacting with sodium channels and stabilizing nerve cell membranes to prevent impulse propagation. They are classified based on potency, duration, and whether they are natural, injectable, or for surface use. Adverse effects include delayed wound healing and arrhythmias when combined with vasoconstrictors.

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    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    73 views25 pages

    Local Anaesthetics: Dr. R. Jamuna Rani MD, Professor & HOD, Department of Pharmacology

    Uploaded by

    Aimee Ann Macaraeg
    Local anesthetics reversibly block nerve impulse generation and conduction. Cocaine was the first discovered local anesthetic in 1860. Procaine, a synthetic derivative, was introduced in 1905 due to cocaine's toxicity. Local anesthetics work by interacting with sodium channels and stabilizing nerve cell membranes to prevent impulse propagation. They are classified based on potency, duration, and whether they are natural, injectable, or for surface use. Adverse effects include delayed wound healing and arrhythmias when combined with vasoconstrictors.

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    of 25

    LOCAL ANAESTHETICS

    Dr. R. Jamuna Rani MD,


    Professor & HOD,
    Department of Pharmacology
    LOCAL ANAESTHETICS
    „ Local anaesthetics reversibly block
    generation and conduction of nerve
    impulses
    „ Cocaine is the first naturally derived local
    anaesthetic agent discovered in 1860
    „ It was introduced in the clinical use by
    Koller by 1884
    „ Because of toxicity produced by cocaine a
    synthetic derivative procaine was
    discovered by EINHORN 1905
    „ 1943 lidocaine was synthesized by
    LOFGREN
    CHEMISTRY
    „ Most local anaesthetics contains
    hydrophilic group on one side and
    liphopilic aroamtic group on the other are
    connected by the alkyl chain through an
    amide or ester linkage
    „ They are weak bases
    MECHANISM OF ACTION
    „ The local anaesthetics interact with LA
    receptor situated in the voltage sensitive
    sodium channel and reduce the entry of
    sodium ions
    „ They produce membrane stabilizing
    action. The action affecting the process of
    depolarization leading to failure of
    propagation of impulse without affecting
    the resting potential
    PHARMACOKINETICS
    „ The ester type local anaesthetics are
    metabolized by pseudocholinesterase
    present in the plasma.
    „ The amide linked local anaesthetics are
    metabolized in the liver by dealkylation
    and hydrolysis
    LOCAL ACTIONS
    „ They affect both sensory and motorfibres.
    „ Autonomic fibres are more susceptible than
    somatic fibres.
    „ Small fibres are affected first than the larger
    fibres.
    „ Non myelinated fibres are blocked easily than
    myelinated fibres.
    „ Among the somatic afferents order of blockade
    is pain – temperature – touch – deep pressure
    „ Applied to the tongue bitter taste is lost first
    followed by sweet and salt taste is last of all
    LA & VASOCONSTRICTORS
    „ Adrenaline (1:50000 – 1:200000)
    „ Ephedrine, felypressin
    „ The LA is given along with the
    vasoconstrictor agent
    „ Prolongs duration of action of LA by
    decreasing their rate of removal from the
    local site into the circulation
    „ Reduces systemic toxicity
    „ Provides more bloodless field for surgery
    (Contd…)
    „ Side effects:
    „ It delay wound healing
    „ Raise BP and promote arrhythmias in
    susceptible individuals
    „ C/I: LA + vasoconstrictor combination is
    contraindicated in the surgery of toes,
    fingers, pinna and penis.
    SYSTEMIC ACTIONS
    „ All LA are capable of producing CNS
    stimulation followed by depression
    „ The stimulation is due to inhibition of
    inhibitory neurons
    CLASSIFICATION
    „ I. NATURAL
    Cocaine

    „ II. Synthetic
    Injectable
    „ INJECTABLE
    Low potency, short duration
    Procaine (ester)
    Chloroprocaine (ester)
    „ INTERMEDIATE POTENCY AND DURATION
    Lignocaine (Lidocaine)
    Prilocaine
    „ HIGH POTENCY, LONG DURATION
    Tetracaine (Amethocaine) (ester)
    Bupivacaine
    Ropivacaine
    Dibucaine (Cinchocaine)
    Bucricaine (Acridine derivative)
    „ SURFACE ANAESTHETIC:
    „ Soluble
    NATURAL: Cocaine
    „ Synthetic:
    Lignocaine
    Tetracaine
    Benoxinate
    „ Insoluble
    Benzocaine (ester)
    Butylaminobenzoate (Butamben)
    Oxethazaine
    BUCRICAINE
    „ Bucricaine is a new LA derived from acridine has
    inherent vasopressor action produce longer duration
    of action less cardiotoxic. Used in opthalmic, dental
    and surgical procedures
    „ Procaine is not a good surface anaesthetic because
    it does not penetrate into the intact skin and
    mucous membrane
    „ D/I: Procaine contains PABA which decreases the
    antimicrobial action of sulphonamides.
    Anticholinesterases increase the duration of action
    of procaine
    „ It forms poorly soluble salt with benzyl penicillin
    procaine penicillin injected IM acts for 24 hrs.
    „ Tetracaine and lignocaine produce skeletal
    muscle relaxation very useful in cautery
    „ Cocaine is a protoplasmic poison, drug of
    addiction, cause dryness of cornea,
    increase blood pressure, produce
    mydriasis. It is banned because it is a
    drug of addiction
    „ Chlorprocaine produce neurotoxicity
    „ Bupivacaine popularly used in obstetrics
    practice (Mother can actively cooperate in
    vaginal delivery) administered epidurally, less
    likely to reach the foetus to produce neonatal
    depression
    SHOULD NOT BE GIVEN IV. because it
    produces prolongation of QT interval and
    induce ventricular tachycardia
    „ Ropivacaine, bupivacaine congener less
    cardiotoxic
    „ Dibucaine is a longest acting LA more toxic
    occasionally used for spinal anaesthesia
    available as ointment, injection, ear drops
    „ Benoxinate good surface anaesthetic for
    eye (tonometry) available as 0.4% eye
    drops
    „ Benzocaine and butylaminobenzoate PABA
    derivative can antagonise sulphonamide
    locally. Used as lozenges for stomatits,
    sore throat, dusting powder/ointment for
    wound and ulcer and as suppository for
    anorectal lesion
    „ Oxethazaine (mucaine) it is administered
    along with antacids for the symptomatic
    relief of gastritis drug induced gastric
    irritation, GO reflux and heart burn in
    pregnancy. It desensitizes the gastrocolic
    reflex and reduce PP urgency in irritable
    bowel syndrome
    „ Eutectic lignocaine/prilocaine it is applied
    under occlusive dressing for 1hr before IV
    cannulation, split skin graft harvesting and
    venesection. It bridges between surface and
    infiltration anaesthesia
    METHODS OF APPLICATION OF
    LA
    „ Surface anaesthesia: Endoscopy, colonoscopy
    etc.
    „ Infiltration anaesthesia: Incisions, excisions,
    hydrocele.
    „ Nerve block anaesthesia: Tooth extraction and
    neuralgia
    „ Spinal anaesthesia: For abdominal, pelvic and
    orthopaedic procedures
    „ Epidural: Abdominal, pelvic, orthopaedic
    procedures and post operative cardiac pain
    „ IV regional anaesthesia: Upper limb surgery.
    SYSTEMIC USES OF LA
    „ Lignocaine, IV bolus used to terminate
    ventricular arrhythmias, pain due to
    cancer and severe pruritis
    „ Procainamide is used orally in ventricular
    arrhythmias
    COMPLICATIONS OF SPINAL
    ANAESTHESIA

    „ Headache, respiratory paralysis,


    hypotension, cauda equina syndrome,
    meningitis, nausea and vomiting
    DRUGS PRODUCING LA ACTION
    „ Some other drug, eg. Propranolol,
    chlorpromazine, H1 antihistaminics, quinine
    have significant LA activity, but are not
    used for this purpose because of local
    irritancy or other prominent systemic
    activity. Local anaesthesia can be produced
    by cooling as well, eg. application of ice,
    CO2 snow, ethylchloride spray
    TETRODOTOXIN & SAXITOXIN
    „ Biological toxins block the pore of the
    sodium channel – prevent depolarization
    „ Cause paralysis of respiratory muscles
    requires respiration support in severe
    cases
    „ Blockade of vasomotor nerves cause
    relaxation of VSM and responsible for
    hypotension
    TREATMENT
    „ Early gastric lavage & pressor support are
    indicated
    „ If the patient survives for 24 hours the
    prognosis is good with shellfish poisoning

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