2. INTRODUCTION
• Skeletal muscle relaxant are drugs that reduce muscle tone either by
acting peripherally at the neuromuscular junction or centrally at
cerebrospinal axis or directly on the contractile mechanisms.
• The term muscle relaxant is used to refer to two major therapeutic
groups which are neuromuscular blockers and spasmolytic.
8. MECHANISM OF ACTION
• Bind to nicotinic receptors on the motor end plate and block
action of acetylcholine by competitive blockade.
• These compounds slowly dissociate from receptors and
transmission is gradually restored.
9. PHARMACOLOGICAL ACTIONS
SKELETAL MUSCLE- On IV administer-
action, it causes
Flaccid
paralysis
effect on small muscles of
eyes and fingers
effect on muscles of limbs, neck and
trunk
effect on intercostal muscles
paralysis of diaphragm
RESPIRATION STOPS
Muscle weakness
10. CONT.…
• Recovery occurs in reverse order i.e., the diaphragm is
first to recover.
• Its effect last for 30-60minutes.
AUTONOMIC GANGLIA- in high doses it can block
autonomic ganglia and adrenal medulla and causes
hypotension.
11. CONT…
• HISTAMINE RELEASE- it causes histamine release from mast
cells leading to bronchospasm, increased tracheobronchial and
gastric secretions. It also results in hypotension.
GASTROINTESTINAL TRACT- it may enhance post-operative
paralytic ileus after abdominal operations.
12. CONT.…
CARDIOVASCULAR SYSTEM- it causes significant fall in B.P.
due to
• Ganglionic blockade
• Histamine release
• Reduced venous return
13. PHARMACOKINETICS
• It is quaternary ammonium compound, hence not absorbed
orally.
• It is given IV and IM only.
15. TREATMENT OF TOXICITY
• NEOSTIGRNINE may be used to reverse the skeletal muscle
paralysis and it is the antidote in curare poisoning.
• ANTIHISTAMINE should be given to counter the effect of
histamine.
• SUGAMMADEX is an antidote for overdosage of rocuronium
and vecuoronium.
16. IMPORTANT FACTS
Pancuronium, atracurium, vecuronium, gallimine, doxacurium,
mivacurium, pipecuronium, rapacuronium, rocuronium are synthetic
neuromuscular blockers, whereas tubocuranine is natural
neuromuscular blocker(NMB).
Use of synthetic NMBs is preferred over natural NMBs due to
following reasons:
• Less or no histamine release
• Do not block autonomic ganglia hence cause less hypotension.
17. CONT…
• More potency.
• Agents like rapacuronium and rocuronium have rapid onset of
action
• Atracurium can be safely used in patients with renal
impairment because it is degraded by plasma esterases.
19. MECHANISM OF ACTION
• It stimulates nicotine receptors and depolarize skeletal muscle
membrane.
• Persistent depolarization causes flaccid paralysis.
• Its mechanism is not clearly known.
20. PHARMACOLOGICAL ACTIONS
SKELETAL MUSCLE- on IV administration onset of action is very
rapid i.e., within 1minute.
• Its initial action is muscular fasciculations and twitchings, mostly
in chest and abdominal regions are followed by skeletal muscle
paralysis.
CARDIOVASCULAR SYSTEM- initially hypotension and
bradycardia may results from stimulation of vagal ganglia. It is
followed by hypertension and tachycardia due to stimulation of
21. CONT…
• Higher doses can cause cardiac arrhythmias.
• It can also cause release of histamine if injected rapidly
22. PHARMACOKINETICS
• It is rapidly hydrolyzed by PSEUCDOCHOLINESTERASE enzyme
hence it is short acting about 5minutes.
• Some people might have abnormal synthesis of this enzyme
which is du to hereditary condition.
• In such people it doesn’t get hydrolyzed at last for several
hours resulting in apnea and paralysis.
23. ADVERSE ACTIONS
• Postoperative muscle pain (due to damage to muscle fiber)
• Hyperkalemia
• Cardiac arrhythmias
• Apnea (due to pseuducholinesterase)
24. USES OF PERIPHERALLY ACTING SKELETAL MUSCLE
RELAXANT
as have short acting property
• ET intubation
• Laryngoscopy
• Bronchoscopy
• Esophagoscopy
Orthopedic procedure like reduction of fractures
25. CONT.…
In electroconvulsive therapy (as it protects pt. from
convulsions and trauma)
To overcome spasm of tetanus, athetosis and status
epilepticus
26. DIRECTLY ACTING MUSCLE RELAXANT
They directly affect skeletal muscle contractile mechanism.
E.g. DANTROLENE
28. PHARMACOLOGICAL USES
• It is used in spastic disorders like hemiplegia, paraplegia, spinal
injuries, multiple sclerosis and cerebral palsy.
• Drug of choice in malignant hyperthermia is dantrolene.
• Quinine is used as antimalarial drug.
• Quinine is also used in myotonia congenital and nocturnal
muscle cramps.
30. CENTRALLY ACTING MUSCLE RELXANT
• These drugs act on higher centres and cause muscle
relaxation without loss of consciousness.
• They also have seductive properties.
41. NURSING IMPLICATIONS
• Respiration should be monitored while on SMRs.
• SMRs should not be withdrawn suddenly after long use
(as may cause hallucination, seizures).
• Patients should avoid driving after having SMRs due to
drowsiness and hallucinations.
• Patient vitals should be monitored every half hourly.
42. CONT…
• In patient with liver disease lower dose is given first
followed by gradual increase in further dose. It is
contraindicated in chronic liver disease patient or patient
with hepatotoxicity.
• Restriction in amount of dose in case patient has
developed psychological or physical dependence.
43. YOUR TURN!!!!!!
• How many types of muscle relaxants do we have?
2 i.e., peripheral acting and centrally acting
• Which type of muscle relaxant is better natural or synthetic?
And why?
Synthetic is better.
Because it has less side effects like less hypotension, fast acting,
no or less histamine release, etc.