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Spasmolytics

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

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Spasmolytics

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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.) • GABAA Receptors • CNS and Spinal Cord • Side Effects: Sedation Diazepam (Valium)

  3. Spasmolytics • GABAB 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 • a2 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. a a a b b b a a a Action Potential Neuromuscular Blockers Na+ Na+ Ca2+ ACH ACH ACH ACH ACH ACH ACH ACH ACH ACH Motor neuron ACH ACH ACH ACHEsterase Skeletal Muscle

  10. Properties of neuromuscular blockers Drug Elimination via Duration of action (minutes) Short-acting Succinylcholine Plasma AChE 5-10 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

  11. Muscle relaxation during surgical procedures Endotracheal intubation Maintain controlled ventillation Clinical use of neuromuscular blockers

  12. Potentiated by inhaled anesthetics (Isoflurane) Potentiated by aminoglycosides and calcium channel blockers Can block autonomic ganglia at higher doses Respiratory paralysis Clinical problems associated with neuromuscular blockers

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