dr.bobby muscle relaxant

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    MuscleRelaxants

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    Muscle Relaxants

    • What are they used for? –

    Facilitate intubation of thetrachea – Facilitate mechanical

    ventilation – Optimized surgical working

    conditions

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    Muscle Relaxants• ow skeletal muscle relaxation

    can be achieved? – igh doses of volatile anesthetics – Regional anesthesia – !dministration of neuromuscular

    blocking agents• "roper patient positioning on the

    operating table

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    Muscle Relaxants

    • Muscle relaxants must not begiven without ade#uate dosageof analgesic and hypnotic drugs

    • $nappropriately given % a patientis paralyzed but notanesthetized

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    Muscle Relaxants

    • ow do they work? – &euromuscular 'unction

    Nerve terminal• Motor endplate of a muscle• Synaptic cleft

    – &erve stimulation – Release of !cetylcholine (!ch) – "ostsynaptic events

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    &euromuscular *unction(&M*)

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    +inding of !ch to receptors on muscle end,plate

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    Muscle Relaxants• -epolarizing muscle relaxant

    – Succinylcholine•

    &ondepolarizing musclerelaxants – Short acting – Intermediate acting – Long acting

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    -epolarizing MuscleRelaxant

    • .uccinylcholine• What is the mechanism of action?

    – Physically resemble Ach – Act as acetylcholine receptor agonist – Not metabolized locally at NMJ – Metabolized by pseudocholinesterase in

    plasma – Depolarizing action persists Ach – !ontinuous end"plate depolarization causes

    muscle rela#ation

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    -epolarizing MuscleRelaxant

    • .uccinylcholine• What is the clinical use of

    succinylcholine? – Most often used to facilitate intubation

    • What is intubating dose ofsuccinylcholine?

    – /,/01 mg2kg – Onset 34,54 seconds6 duration 1,/4

    minutes

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    -epolarizing MuscleRelaxant

    • .uccinylcholine – What is phase $ neuromuscular

    blockade?

    – What is phase $$ neuromuscularblockade?

    • $esemble bloc%ade produced bynondepolarizing muscle rela#ant• Succinylcholine infusion or dose &"'

    mg(%g

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    -epolarizing MuscleRelaxant

    • .uccinylcholine – -oes it has side e7ects?

    • 8ardiovascular•

    Fasciculation• Muscle pain• $ncrease intraocular pressure• $ncrease intragastric pressure•

    $ncrease intracranial pressure• yperkalemia• Malignant hyperthermia

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    &ondepolarizing Muscle

    Relaxants• What is the mechanism ofaction?

    – !ompete )ith Ach at the binding sites – Do not depolarized the motor endplate – Act as competitive antagonist – *#cessive concentration causing

    channel bloc%ade – Act at presynaptic sites+ prevent

    movement of Ach to release sites

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    &ondepolarizing MuscleRelaxants

    • 9ong acting – Pancuronium

    • $ntermediate acting –

    Atracurium – ,ecuronium – $ocuronium – !isatracurium

    • .hort acting – Mivacurium

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    &ondepolarizing MuscleRelaxants

    • "ancuronium – Aminosteroid compound – -nset &"' minutes+ duration ./"0/

    minutes – Intubating dose /1/2"/134 mg(%g – *limination mainly by %idney 52'67+

    liver 53'67 – Side e8ects 9 hypertension+ tachycrdia+

    dysrhythmia+

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    &ondepolarizing Muscle

    Relaxants• :ecuronium – Analogue of pancuronium – much less vagolytic e8ect and shorter

    duration than pancuronium – -nset &"' minutes duration 4/"&'

    minutes – Intubating dose /1/2"/134 mg(%g –

    *limination :/6 by %idney+ ./6 by liver

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    &ondepolarizing MuscleRelaxants

    • !tracurium – Metabolized by

    • *ster hydrolysis• ;ofmann elimination

    – -nset &"' minutes+ duration 4'"&'minutes

    – Intubating dose /1' mg(%g – Side e8ects 9

    histamine release causing hypotension+tachycardia+ bronchospasm• Laudanosine to#icity

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    &ondepolarizing MuscleRelaxants

    • 8isatracurium – Isomer of atracurium – Metabolized by ;ofmann elimination – -nset &"' minutes+ duration 4/"&'

    minutes – Intubating dose /13"/14 mg(%g – Minimal cardiovascular side e8ects – Much less laudanosine produced

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    &ondepolarizing MuscleRelaxants

    • Rocuronium – Analogue of vecuronium – $apid onset 3"4 minutes+ duration 4/"&'

    minutes – -nset of action similar to that of

    succinylcholine – Intubating dose /1. mg(%g – *limination primarily by liver+ slightly by

    %idney

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    !lteration of responses• ;emperature• !cid,base balance•

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    !lteration of responses• 8oncurrent diseases

    – Neurologic diseases – Muscular diseases

    • Myasthenia gravis• Myasthenic syndrome 5*aton"Lambert

    synrome7 –

    Liver diseases –

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    !lteration of responses• -rug interactions

    – Inhalation agents – Intravenous anesthetics – Local anesthetics – Neuromuscular loc%ing drugs – Antibiotics –

    Anticonvulsants – Magnesium

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    Monitoring &euromuscularFunction

    What are the purposes ofmonitoring? – !dminister additional relaxant as

    indicated – -emonstrate recovery

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    Monitoring &euromuscularFunction

    ow to monitor?• !linical signs• =se of nerve stimulator

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    Monitoring &euromuscularFunction

    • 8linical signs – Signs of ade>uate recovery

    • Sustained head lift for ' seconds• Lift the leg 5child7• Ability to generate negative inspiratory

    pressure at least 4' cm; 2 -+ able to s)allo)and maintain a patent air)ay

    • -ther crude tests 9 tongue protrusion+ armlift+ hand grip strength

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    Monitoring &euromuscularFunction

    • =se of nerve stimulator – Single t)itch 9 single pulse /14 msec – ?etanic stimulation – ?rain"of"four 9 series of : t)itch+ /14

    msec long+ 4 ;z fre>uency+ administerevery 3/"3' seconds

    – Double burst stimulation – Post tetanic count

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    ierarchy of &euromuscular +lockade

    Fraction of receptoroccupied by

    nondepolarizingmuscle relaxant

    Response to nervestimulator

    Whole body signs

    00"3// &o response Flaccid6 extremerelaxation0' "osttetanic facilitationpresent

    -iaphragm moves6hiccough possible

    0/ One of four twitch of;OF present

    !bdominal relaxationade#uate for most

    prcedure

    @' Four twitch of ;OFpresent6 ;OF ratio 40>;idal volume and vitalcapacity normal

    '/ /44, z tetanussustained"asses inspiratorypressure test

    &/44, z tetanus

    sustainedead lift and hand,grip

    sustained

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    !ntagonism of&euromuscular +lockade

    *8ectiveness of anticholinesterases dependson the degree of recovery present )henthey are administered

    • !nticholinesterases – Neostigmine

    • -nset &"' minutes+ elimination hal ife @@minutes

    • Dose /1/:"/1/@ mg(%g – Pyridostigmine – *drophonium

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    !ntagonism of&euromuscular +lockade

    • What is the mechanism of action? – Inhibiting activity of acetylcholineesterase – More Ach available at NMJ+ compete for

    sites on nicotinic cholinergic receptors – Action at muscarinic cholinergic receptor

    • Bradycardia• ;ypersecretion• Increased intestinal tone

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    !ntagonism of&euromuscular +lockade

    • Muscarinic side e8ects are minimizedby anticholinergic agents

    – Atropine• Dose /1/3"/1/4 mg(%g

    – Scopolamine – glycopyrrolate

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