MCMP 407 Spasmolytics Chronic neurologic diseases

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MCMP 407 Spasmolytics Chronic neurologic diseases

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

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