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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