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

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    MCMP 407 Spasmolytics Chronic neurologic diseases MCMP 407 Spasmolytics Chronic neurologic diseases Presentation Transcript

    • 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
    • Spasmolytics
      • Benzodiazepines (Diazepam, etc.)
      • GABA A Receptors
      • CNS and Spinal Cord
      • Side Effects: Sedation
      Diazepam (Valium)
    • 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
    • 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)
    • 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)
    • Atropine vs. Cyclobenzaprine
    • Spasmolytics
      • Other drugs similar to Cyclobenzaprine (Flexeril)
      • Chlorzoxazone (Paraflex, Parafon)
      • Orphenadrine (Norflex)
      • Carisprodol (Soma)
    • 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
    • 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         
    • 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
    • Clinical use of neuromuscular blockers
      • Muscle relaxation during surgical procedures
      • Endotracheal intubation
      • Maintain controlled ventillation
    • 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