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MCMP 407 Spasmolytics Chronic neurologic diseases
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MCMP 407 Spasmolytics Chronic neurologic diseases

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  • 1. Spasmolytics
    • Chronic neurologic diseases
      • Cerebral Palsy, Multiple Sclerosis
    • Acute Injury
      • Spinal cord damage, muscle inflamation
    Goal of therapy: Reduce spasticity and pain, while retaining function
  • 2. Spasmolytics
    • Benzodiazepines (Diazepam, etc.)
    • GABA A Receptors
    • CNS and Spinal Cord
    • Side Effects: Sedation
    Diazepam (Valium)
  • 3. Spasmolytics
    • GABA B receptor agonist
    • Activation of K + channels
    • CNS and Spinal cord
    • (-)-Baclofen is the active isomer
    • Less sedation than BZDs
    • Intrathecal pumps now used in chronic conditions
    • Warning for severe withdrawal syndrome from intrathecal use
      • Altered mental status, hyperpyrexia, exaggerated spasticity, muscle rigidity, and rhabdomyolysis
    Baclofen (Lioresal
  • 4. Spasmolytics
    •  2 adrenergic receptor agonist
    • Congener of clonidine
    • Presynaptic inhibition of motor neurons
    • 1/10-1/50th potency as clonidine in lowering blood pressure
    • Side Effects: Drowsiness, hypotension, dry mouth
    Tizanidine (Zanaflex)
  • 5. Spasmolytics
    • Tricyclic structure
    • May act at level of brain stem
    • Strong antimuscarinic effects (sedation)
    • Ineffective in the treatment of chronic neurological disorders
    • Use: Relief of acute muscle spasm due to injury or strain
    Cyclobenzaprine (Flexeril)
  • 6. Atropine vs. Cyclobenzaprine
  • 7. Spasmolytics
    • Other drugs similar to Cyclobenzaprine (Flexeril)
    • Chlorzoxazone (Paraflex, Parafon)
    • Orphenadrine (Norflex)
    • Carisprodol (Soma)
  • 8. Spasmolytics
    • Interferes with excitation-contraction coupling
    • Reduces release of Ca ++ from the sarcoplasmic reticulum
    • Blocks contraction
    Dantrolene Sodium (Dantrium)
    • Side Effects: Muscle weakness, sedation, rare hepatitis
    • Uses: Cerebral palsy, multiple sclerosis
    • Also Malignant Hyperthermia
  • 9. Ca 2+ Motor neuron Na + ACH ACH ACH ACH ACH ACH ACH ACH ACH ACH ACH ACH ACH Na + Skeletal Muscle ACHEsterase Neuromuscular Blockers Action Potential         
  • 10. Properties of neuromuscular blockers Drug Elimination via Duration of action (minutes) Short-acting Mivacurium Plasma AChE 10-20 Intermediate-acting Atracurium Spontaneous 20-35 Vecuronium Hepatic and renal 20-35 Rocuronium Hepatic and renal 20-35 Long-acting Pancuronium Renal 60 Succinylcholine Plasma AChE 5-10
  • 11. Clinical use of neuromuscular blockers
    • Muscle relaxation during surgical procedures
    • Endotracheal intubation
    • Maintain controlled ventillation
  • 12. Clinical problems associated with neuromuscular blockers
    • Potentiated by inhaled anesthetics (Isoflurane)
    • Potentiated by aminoglycosides and calcium channel blockers
    • Can block autonomic ganglia at higher doses
    • Respiratory paralysis