MUSCLE RELAXANT

(NEUROMUSCULAR BLOCKING DRUGS)

Belinda Anabel (2015-061-002)

MECHANISM
Work at postsynaptic nicotinic cholinergic receptor
of the neuromuscular junction stop conduction of
nerve impulses skeletal muscle paralysis

TRANSMISSION
Association between a motor neuron and a muscle
cell occurs at the neuromuscular junction.
The cell membranes of the neuron and muscle fiber
are separated by a narrow (20-nm) gap, the synaptic
cleft.
As a nerves action potential depolarize its terminal,
an influx of calcium ions through voltage-gated calcium
channels into the nerve cytoplasm allows storage
vesicles to fuse with the terminal plasma membrane
and release their contents (acetylcholine [ACh]).

TRANSMISSION
The ACh molecules diffuse across the synaptic cleft
to bind with nicotinic cholinergic receptors on the
motor end-plate.
Each ACh receptor in the neuromuscular junction
normally consists of five protein subunits; two
subunits; and single , , and subunits. Only the
two identical subunits are capable of binding ACh
molecules.

CLASSIFICATION
Depolarizing
Non-Depolarizing

DEPOLARIZING
Mimic ACh by binding to the a-subunit of the nicotinic
cholinergic receptor keeping the ion channel open.
Cause prolonged depolarization which initially manifests
as diffuse muscle contractions known as fasciculations.
The depolarized, occupied membrane cannot react to
further release of ACh, thereafter causing muscle
paralysis.

DEPOLARIZING
SUCCINYLCHOLINE

SUCCINYLCHOLINE
Dosage : 11.5 mg/kg IV.
Onset : 30-60s
Only a small fraction of the injected dose ever
reaches the neuromuscular junction.
Because succinylcholine is not lipid soluble, it has
a small volume of distribution.
Used for rapid sequence induction when aspiration
is a risk (full stomach, trauma, diabetes mellitus,
hiatal hernia, obesity, pregnancy)

SUCCINYLCHOLINE
Adverse effects :
Bradycardia, junctional rhythm, cardiac arrest
due to SCh's action on cardiac muscarinic
receptors. More likely to occur when a second
dose of SCh is given minutes after the first.
Hyperkalemia

SUCCINYLCHOLINE

Allergic reaction anaphylactic shock

Malignant hyperthermia
Fasciculations post-op myalgia
Trismus
IOP
ICP

NON-DEPOLARIZING
Interfere with the actions of acetylcholine (ACh) at the NMJ,
which keeps ion channels closed so no depolarization can
occur.
Because NMBDs compete with ACh for receptor binding,
they are considered antagonist or competitive blockers.
NMBD action can be overcome by increasing ACh in the
synaptic cleft (the mechanism behind reversal of
neuromuscular blockade with acetylcholinesterase inhibitors).

NON-DEPOLARIZING
AMINOSTEROIDS
(PANCURONIUM, ROCURONIUM,
VECURONIUM)
BENZYLISOQUINOLINES
(ATRACURIUM, CISATRACURIUM)

PANCURONIUM
Dosage : 0.04-0.1 mg/kg IV
Maintenance : 0.01-0.05 mg/kg IV
Onset : 1-3 min
Duration of action 90 min
Tachycardia, BP CO
Elimination is mostly renal (increased duration in
renal disease, neonates, elderly)

PANCURONIUM
Adverse effects :
Tachycardia, hypertension
Allergic reaction anaphylactic shock
Bronchospasm, hypoventilation

ROCURONIUM
Dosage : 0.6-1.2 mg/kg IV
Maintenance : 0.06-0.6 mg/kg IV
Onset : 45-90s
Duration of action 35 min when dosing at 0.6 mg/kg
At a dose of 0.91.2 mg/kg, an onset of action that

approaches succinylcholine (6090 s), making it a

suitable alternative for rapid-sequence inductions.

ROCURONIUM
Does not release histamine or cause cardiovascular
effects
May promote muscarinic block
Metabolism : liver, kidney
Duration prolonged by severe hepatic failure and
pregnancy
Elderly patients may experience a prolonged
duration of action due to decreased liver mass

ROCURONIUM
Adverse effects :
Tachycardia, arrythmia
Bronchospasm, pulmonary hypertension

VECURONIUM
Dosage : 0.08-0.1 mg/kg IV
Maintenance : 0.01-0.05 mg/kg IV
Onset : < 3 min
Duration of action 35 min
Metabolism : liver, kidney
Satisfactory drug for patients with renal failure

VECURONIUM
Dose of 0.04 mg/kg initially followed by increments
of 0.01 mg/kg every 1520 min provides
intraoperative relaxation. Alternatively, an infusion
of 12 mcg/kg/min produces good maintenance of
relaxation

VECURONIUM
Does not release histamine or cause cardiovascular effects
Women seem to be approximately 30% more sensitive than

men, as evidenced by a greater degree of blockade and

longer duration of action
The duration of action prolonged in postpartum patients
Increased duration in hepatic disease, esp with repeated

dosing.
Side effect : opioid-induced bradycardia

VECURONIUM
Adverse effects :
Opioid-induced bradycardia
Hypoventilation

ATRACURIUM
Dosage : 0.3-0.5 mg/kg IV
Maintenance : 0.1-0.2 mg/kg IV
Onset : < 3 min
Metabolism : liver, kidney
Triggers dose-dependent histamine release that
becomes significant at doses above 0.5 mg/kg.
Cause a transient drop in systemic vascular
resistance

ATRACURIUM
Duration of action 35 min
Metabolism : liver, kidney
A dose of 0.5 mg/kg is administered intravenously
for intubation
May be shorter acting in children and infants than
in adults

ATRACURIUM
Dose-dependent
release
of
histamine
hypotension
Should be avoided in asthmatic patients
Prolonged by hypothermia

ATRACURIUM
Adverse effects :
Hypotension, sinus tachycardia
Bronchospasm, laryngospasm

CISATRACURIUM
Duration of action 35 min
Useful in patients with renal failure
Doesnt release histamine useful for asthmatic
patient