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RELAXANTS
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Classification on basis of site of action
and mechanism of action
A) PERIPHERALLY ACTING
Neuromuscular blockers
Non depolarizing agents
Isoquinoline derivatives steriod derivatives
Depolarizing agents
Suxamethonium (Succinylcholine)
Decamethonium
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Neuromuscular Junction
1: Cholinergic motor neurone,2:
motor end-plate, 3: vesicles, 4:
NMR, 5: mitochondrion
Depolarizing agents:
Succinyle choline
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B) Centrally acting (spasmolytic drugs)
Diazepam ( act through GABA A) receptors)
Baclofen (GABA B) receptors
Dantroline ( act directly by interfering release of
calcium from sarcoplasmic reticulum)
Note:
these drugs are used to control spastic muscle tone as
in epilesy ,multiple scelerosis ,cerebral palsy, stroke,
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Mechanism of Sk. muscle
contraction
Initiation of impulse
Release of acetylcholine
Muscle contraction.
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Presynaptically:
To inhibit acetylcholine synthesis or release (practically not used).
As they may have whole body unspecific nicotinic as well as
muscarinic effects
Postsynaptically:
To block the receptor activity.
To block ion channel at the end plate
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Non depolarizing (majority):
Act by blocking acetylcholine receptors.
Depolarizing:
act as agonists at acetylcholine receptors
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Mechanism of action
(non depolarizing agents)
a) At low doses:
These drugs combine with nicotinic receptors and prevent
acetylcholine binding.as they compete with acetycholine for
receptor binding they are called competitive blockers
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Their action can be overcome by increasing conc. of
acetylcholine in the synaptic gap(by inhibition of
acetyle choline estrase enzyme)
e.g.: Neostigmine ,physostigmine edrophonium
Anesthetist can apply this strategy to shorten the
duration of blockage or over come the overdosage.
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At high doses
These drugs block ion channels of the end plate.
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ACTIONS
All the muscles are not equally sensitive to blockade.
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Pharmacokinetics:
Administered intravenously
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Some (vecuronium, rocuronium) are acetylated in liver.( there
clearance can be prolonged in hepatic impairment)
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Drug interactions
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Unwanted effects
Fall in arterial pressure chiefly a result to ganglion
block , may also be due to histamine release this may
give rise to bronchospasm (especially with
tubocurarine ,mivacurium ,and atracurium)
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DEPOLARIZING AGENTS
DRUGS Suxamethonium ( succinylecholine)
Decamethonium
Mechanism of action:
These drugs act like acetylcholine but persist at the synapse at
high concentration and for longer duration and constantly
stimulate the receptor.
Pharmacokinetics:
Administered intravenously.
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SUCCINYLCHOLINE
• It causes paralysis of skeletal muscle.
Sequence of paralysis may be different from that of
non depolarizing drugs but respiratory muscles are
paralyzed last
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Characteristics of neuromuscular-blocking drugs
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Some properties of neuromuscular blockers
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Half life of the drug is 8-9 hours.
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Baclofen
It acts through GABA B receptors
It is less sedative
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