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Muscle Relaxants


 Facilitate intubation of the
trachea
 Facilitate mechanical
ventilation
 Optimized surgical working
conditions
Muscle Relaxants
 How skeletal muscle relaxation can be
achieved?
 High doses of volatile anesthetics
 Regional anesthesia
 Administration of neuromuscular
blocking agents
 Proper patient positioning on the
operating table
Muscle Relaxants
 Muscle relaxants must not be given
without adequate dosage of
analgesic and hypnotic drugs

 Inappropriately given : a patient is
paralyzed but not anesthetized
Muscle Relaxants
 How do they work?
 Neuromuscular junction
 Nerve terminal
 Motor endplate of a muscle
 Synaptic cleft
 Nerve stimulation
 Release of Acetylcholine (Ach)
 Postsynaptic events
Neuromuscular Junction
(NMJ)
Binding of Ach to receptors on muscle end-plate
Muscle Relaxants
 Depolarizing muscle relaxant
 Succinylcholine
 Nondepolarizing muscle relaxants
 Short acting
 Intermediate acting
 Long acting
Depolarizing Muscle
Relaxant
 Succinylcholine
 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
 Continuous end-plate depolarization causes
muscle relaxation
Depolarizing Muscle
Relaxant
 Succinylcholine
 What is the clinical use of succinylcholine?
 Most often used to facilitate
intubation

 What is intubating dose of succinylcholine?
 1-1.5 mg/kg
 Onset 30-60 seconds, duration 5-10
minutes



Depolarizing Muscle
Relaxant
 Succinylcholine
 What is phase I neuromuscular
blockade?
 Sustained opening of receptor channels in
depolarized post-juntional membrane cannot
respond to further Ach
 What is phase II neuromuscular
blockade?
 Resemble blockade produced by
nondepolarizing muscle relaxant
 Succinylcholine infusion or dose > 3-5 mg/kg

Depolarizing Muscle
Relaxant
 Succinylcholine
 Does it has side effects?
 Cardiovascular
 Fasciculation
 Muscle pain
 Increase intraocular pressure
 Increase intragastric pressure
 Increase intracranial pressure
 Hyperkalemia
 Malignant hyperthermia
Nondepolarizing Muscle
Relaxants
 What is the mechanism of action?
 Compete with Ach at the binding sites
 Do not depolarized the motor endplate
 Act as competitive antagonist
 Excessive concentration causing channel
blockade
 Act at presynaptic sites, prevent movement
of Ach to release sites
Nondepolarizing Muscle
Relaxants
 Long acting
 Pancuronium
 Intermediate acting
 Atracurium
 Vecuronium
 Rocuronium
 Cisatracurium
 Short acting
 Mivacurium
Nondepolarizing Muscle
Relaxants
 Pancuronium
 Aminosteroid compound
 Onset 3-5 minutes, duration 60-90 minutes
 Intubating dose 0.08-0.12 mg/kg
 Elimination mainly by kidney (85%),
liver (15%)
 Side effects : hypertension, tachycrdia,
dysrhythmia,
Nondepolarizing Muscle
Relaxants
 Vecuronium
 Analogue of pancuronium
 much less vagolytic effect and shorter
duration than pancuronium
 Onset 3-5 minutes duration 20-35 minutes
 Intubating dose 0.08-0.12 mg/kg
 Elimination 40% by kidney, 60% by liver



Nondepolarizing Muscle
Relaxants
 Atracurium
 Metabolized by
 Ester hydrolysis
 Hofmann elimination
 Onset 3-5 minutes, duration 25-35 minutes
 Intubating dose 0.5 mg/kg
 Side effects :
 histamine release causing hypotension,
tachycardia, bronchospasm
 Laudanosine toxicity




Nondepolarizing Muscle
Relaxants
 Cisatracurium
 Isomer of atracurium
 Metabolized by Hofmann elimination
 Onset 3-5 minutes, duration 20-35 minutes
 Intubating dose 0.1-0.2 mg/kg
 Minimal cardiovascular side effects
 Much less laudanosine produced
Nondepolarizing Muscle
Relaxants
 Rocuronium
 Analogue of vecuronium
 Rapid onset 1-2 minutes, duration 20-35
minutes
 Onset of action similar to that of
succinylcholine
 Intubating dose 0.6 mg/kg
 Elimination primarily by liver, slightly by
kidney
Alteration of responses
 Temperature
 Acid-base balance
 Electrolyte abnormality
 Age
 Concurrent diseases
 Drug interactions
Alteration of responses
 Concurrent diseases
 Neurologic diseases
 Muscular diseases
 Myasthenia gravis
 Myasthenic syndrome (Eaton-Lambert
synrome)
 Liver diseases
 Kidney diseases

Alteration of responses
 Drug interactions
 Inhalation agents
 Intravenous anesthetics
 Local anesthetics
 Neuromuscular locking drugs
 Antibiotics
 Anticonvulsants
 Magnesium

Monitoring Neuromuscular
Function
 What are the purposes of monitoring?
 Administer additional relaxant as
indicated
 Demonstrate recovery
Monitoring Neuromuscular
Function
How to monitor?
 Clinical signs
 Use of nerve stimulator
Monitoring Neuromuscular
Function
 Clinical signs
 Signs of adequate recovery
 Sustained head lift for 5 seconds
 Lift the leg (child)
 Ability to generate negative inspiratory
pressure at least 25 cmH
2
O, able to swallow
and maintain a patent airway
 Other crude tests : tongue protrusion, arm lift,
hand grip strength


Monitoring Neuromuscular
Function
 Use of nerve stimulator
 Single twitch : single pulse 0.2 msec
 Tetanic stimulation
 Train-of-four : series of 4 twitch, 0.2 msec
long, 2 Hz frequency, administer every 10-
15 seconds
 Double burst stimulation
 Post tetanic count
Antagonism of
Neuromuscular Blockade
Effectiveness of anticholinesterases depends on
the degree of recovery present when they are
administered
 Anticholinesterases
 Neostigmine
 Onset 3-5 minutes, elimination halflife 77
minutes
 Dose 0.04-0.07 mg/kg
 Pyridostigmine
 Edrophonium


Antagonism of
Neuromuscular Blockade
 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
 Hypersecretion
 Increased intestinal tone


Antagonism of
Neuromuscular Blockade
 Muscarinic side effects are minimized by
anticholinergic agents
 Atropine
 Dose 0.01-0.02 mg/kg
 Scopolamine
 glycopyrrolate
Reversal of Neuromuscular
Blockade
 Goal : re-establishment of
spontaneous respiration and the
ability to protect airway from
aspiration