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Skeletal muscle relaxants & Spasmolytics dr abdul azeem

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lecture slides on skeletal muscle relaxants & spasmolytics by Dr. Abdul Azeem (RMC)

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Skeletal muscle relaxants & Spasmolytics dr abdul azeem

  1. 1. SKELETAL MUSCLE RELAXANTS & SPASMOLYTICS By Dr. Abdul Azeem
  2. 2. I) PERIPHERALLY ACTING 1) NEUROMUSCULAR JUNCTION BLOCKERS a) NON DEPOLARIZING NEUROMUSCULAR BLOCKERS  ISOQUINOLINE DERIVATIVES D- TUBOCURARINE GALLAMINE ATRACURIUM CIS ATRACURIUM ALCURIUM DOXACURIUM MIVACURIUM
  3. 3. • STEROID DERIVATIVES PANCURONIUM VECURONIUM RAPACURONIUM PIPECURONIUM ROCURONIUM b) DEPOLARIZING NEUROMUSCULAR BLOCKERS SUXAMETHONIUM (SUCCINYLCHOLINE) DECAMETHONIUM 2) DIRECTLY ACTING DANTROLENE
  4. 4. II) CENTRALLY ACTING MUSCLE RELAXANTS (SPASMOLYTICS) • BENZODIAZEPINES DIAZEPAM CHLORDIAZEPOXIDE CLONAZEPAM NITRAZEPAM • GABA ANALOGUES BACLOFEN PROGABIDE oALPHA 2 AGONIST TIZANIDINE
  5. 5. OTHERS GLYCINE MEPROBAMATE MEPHENESEN IDROCILAMIDE RILUZOLE BOTULINUM TOXIN
  6. 6.  NEUROMUSCULAR JUNCTION BLOCKERS  Classification according to duration of action › Short acting  Succinylcholine <8 min  Mivacurium 10-20 min › Intermediate acting  Atracurium 25-35 min  Cisatracurium 25-40 min  Rocuronium 25-35 min  Vecuronium 25-35 min
  7. 7.  Long acting  Doxacurium more than 35 min  Tubocurarine more than 35 min  Pancuronium more than 35 min  Pipecuronium more than 35 min
  8. 8. Nicotinic Transmission At NMJ
  9. 9. NEUROMUSCULAR JUNCTION
  10. 10. NICOTINIC ACETYLCHOLINE RECEPTOR
  11. 11. History Strychnos toxifera
  12. 12. Chemistry
  13. 13. • Pharmakokinetics
  14. 14. MOA Non Depolarizing / Competitive N.M Blockers- Tubocurarine etc.
  15. 15. Mechanism of Action: Non Depolarizing / Competitive N.M Blockers i.e . Tubocurarine etc. Competitive antagonist to Ach at Nicotinic (Nm) Receptor at MEP N.M Transmission is interrupted leading to N.M. Blockade. At Larger doses, some drugs also enter pore of ion channel of Nm , further decrease in N.M. Transmission.
  16. 16. Blockade is: Antagonised by: Anticholinesterases (Neostingmine, Edrophonium, Pyridostigmine )
  17. 17. Potentiated by:- • GA.(Ether, Enflurane, Halothane) • Amino glycoside Antibiotics. (Streptomycin, Gentamicyn) • Acidosis • L.A (Procaine) • Hypokalemia • Myasthenia gravis • Dehydration • Advanced age-Prolonged Effect
  18. 18. D-TUBOCURARINE (PROTOTYPE) Non depolarizing N.M. Blocker. Source: Chief alkaloid of curare Obtained from Chondrodendron & Strychnos Chemistry: Mono quaternary Ammonium Compound.
  19. 19. Pharmacokinetics: Not Abs. from GIT. Given I/V It is redistributed. Not metabolised. Excreted unchanged by kidney 40 % / Bile 60 % Crosses Placenta but not harmful. It does not cross BBB. Mechanism of action: O.O.A : 4 min. D.OA: more than 35 min
  20. 20. Pharmacological effects No central effects Skeletal muscle relaxation. First weakness & then paralysis. Sequence of Paralysis of Skeletal Muscles: Eye, Jaw, Facial muscles . Muscles of Neck, Limbs , Trunk. Interocostal muscles Diaphragm Recovery in reverse order. Ganglionic blockade: Mild in high doses
  21. 21. CVS: Hypotension due to Release of Histamine.Vasodilatation, decreased PR , decreased BP. Bronchoconstriction due to Histamine release Ganglionic Blockade (Vasodilatation) in larger doses.  PANCURONIUM › Steroidal quaternary ammounioum compund › 6 times more potent than Tubocurarine › Quick onset of action › No effect on ganglia › Vagolytic effect › Moderate increase in Blood Pressure › No effect on CNS › No effect on foetus › No Histamine release › ›
  22. 22. • ATRACURIUM • Isoquinoline • Intermediate acting • Metabolism – Hepatic • Hofmann Elimination • Laudanosine Seizures • Cis-Atracurium • Mivacurium: Shortest duration of action. Metabolised by pseudocholine esterase
  23. 23. Depolarizing Skeletal Muscle Relaxant (Succinylcholine) • Pharmakokinetics
  24. 24. M.O A of Depolarizing drugs (Succinylcholine) The Blockade occurs in 2 Phases  Phase I (depolarizing) Phase I block: is augmented by anticholinestrase & not reversed
  25. 25. Phase I (depolarizing) 1. Succinylcholine reacts with nicotinic receptors 2. Ion channels are opened → depolarization of motor end plate. 3. Depolarization spreads to adjacent membrane 4. Result in disorgansed / generalized contraction of motor unit. 5. Not hydrolyzed in synapse → persistent depolarization → flaccid paralysis
  26. 26. Phase II Block (Desensitizing Block) With continued exposure—Initial end plate depolarization decreases and membrane is re polarized but unresponsive/ desensitized to Ach. due to: Blockade of channel. Development of in excitable area in muscle membrane immediately surrounding the M.E.P which prevent the spread of impulses or desensitization of membrane occurs .
  27. 27. MOA OF SUCCINYLCHOLINE
  28. 28.  SUCCINYLCHOLINE › Hydolysed by plasma & liver Pseudochlone & butyryl cholinesterases › Duration of action is very short (8 min)  DIBUCAINE NUMBER TEST
  29. 29. Adverse Effects • Non Depolarising Drugs • Histamine Release • Vagolytic Effect • Depolarising Drugs (Succinyl choline) • Malignant Hyperthermia • Apnea • Hyperkalamia • Increased intra gastric pressure • Increased IOP • Muscular Aches & Pain •
  30. 30. Drug Interactions
  31. 31. • Uses of NMJ Blockers • Surgical operations • Endotracheal intubation ,laryngoscopy • Orthopedic manipulation • Convulsive disorders • Electroconvulsive therapy (ECT) • For assisted ventilation
  32. 32. SUGAMMADEX  When given post operatively there is rapid recovery from even profound degree of Neuro muscular blockade.  It rapidly inactivate the steroidal neuro muscular blocking drugs by forming an in active complex which is excreted in urine
  33. 33. DANTROLENE MOA: It reduces the release of activator calcium from the sarcoplasmic reticulum
  34. 34. DANTROLENE MOA PHARMACOKINETICS ADVERSE EFFECTS THERAPEUTICS USES Spasmolytic Malignant hyperthermia DOSE
  35. 35. PHARMACOKINETICS 1/3 of oral dose is absorbed t ½ is 8 hrs. ADVERSE EFFECTS •Muscle Weakness •Sedation •Occasionally hepatitis THERAPEUTICS USES Spasmolytic Malignant hyperthermia DOSE: As Spasmolytic Initially 25mg / day gradually increase over 7 weeks to a maximum of 100 mg 4 times a day For Malignant Hyperthemia
  36. 36. Botulinum Toxin MOA
  37. 37. Uses Strabismus Blepharospasm Hemifacial spasm Spasm associated with lower esophageal sphincter and anal fissure
  38. 38. Dystonias e.g. cervical dystonia, Oromandibular dystonia Generalized spastic disorders( cerebral palsy) Hyperhidrosis of palms and axillae
  39. 39. Cosmetic procedure for wrinkles of the face
  40. 40. Central Spasmolytics • Spasticity is increased muscle tone. • increase in tonic stretch reflexes and flexor muscle spasm with muscle weakness • Often observed in – Cerebral palsy – Multiple sclerosis – Stroke – ALS (Amyotrophic lateral sclerosis) • Aim • Reduction of excessive skeletal muscle tone without reduction of muscle strength.
  41. 41. DIAZEPAM MOA: It facilitates the action of GABA in CNS.
  42. 42. USES: Muscle Spasm (local truma to tetanus) DOSE: Oral dose initially 5 mg / day and gradually increase to maximum of 60 mg / day. ADVERSE EFFECTS Sedation
  43. 43. BACLOFEN MOA: GABA B Agonist ADVERSE EFFECTS • Drowsiness • Increase in seizure activity in epileptic patients • Excessive somnolence • Respiratory depression • Coma THERAPEUTICS USES – Relieves muscles spasm. Most useful agent for symptomatic treatment of spasticity – Prevention of migraine – Reduces craving in recovering alcoholics
  44. 44. TIZANIDINE MOA: Centrally acting Alpha 2 agonist Inhibits release of excitatory amino acids in the spinal interneurons It re-inforces both pre-synaptic & post- synaptic inhibition in the cord ADVERSE EFFECTS Drowsiness Hypotension Dry mouth Asthenia
  45. 45. GABAPENTIN Antiepileptic drug is a good spasmolytic agent in patient with multiple sclerosis PRE GABALIN Newer analogue of gabapentin usefull in muscle spasm PROGABIDE Gaba A and Gaba B agonist and has active metabolites including GABA itself
  46. 46. Riluzole • Pharmacokinetics – Absorption orally – Highly protein bound – Half life 12 hours – Metabolism --- in liver by both cyotchrome P450-mediated hydroxylation and glucurnidation MOA – it inhibits glutamate release – It also blocks postsynaptic NMDA- and kainite-type glutamate receptors and inhibits voltage-dependent sodium channels
  47. 47. Uses • ALS Dose • 50 mg every 12 hours Adverse effect • Nausea • Diarrhea • Hepatic injury
  48. 48. GLYCINE inhibitory neurotransmitter. When Given crosses BBB IDROCILAMIDE Newer drugs for treatment of ALS MOA Inhibit glutamatergic transmission in CNS
  49. 49. • Seditive, Hypnotic and Anti anxiety drug Carisoprodal • Its active metabolite is meprobamate. Cyclobenzaprine
  50. 50. DIAZEPAM MOA USES DOSE ADVERSE EFFECTS
  51. 51. BACLOFEN MOA ADVERSE EFFECTS THERAPEUTICS USES – Relieves muscles spasm. Most useful agent for symptomatic treatment of spasticity – Prevention of migraine – Reduces craving in alcoholics
  52. 52. TIZANIDINE MOA It re-inforces both pre-synaptic & post- synaptic inhibition in the cord ADVERSE EFFECTS Drowsiness Hypotension Dry mouth Asthenia
  53. 53. Meprobamate • Saditive, Hypnotic and Anti anxiety drug Carisoprodal • Its active metabolite is meprobamate. Glycine

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