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MCMP 407 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 MCMP 407 Spasmolytics O H3C N N Cl Diazepam (Valium) Benzodiazepines (Diazepam, etc.) GABAA Receptors CNS and Spinal Cord Side Effects: Sedation MCMP 407 Spasmolytics H2N CO2H Cl Baclofen (Lioresal 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 MCMP 407 Spasmolytics N S N H N Cl Tizanidine (Zanaflex) N N H 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 MCMP 407 Spasmolytics CHCH2CH2N(CH3)2 Cyclobenzaprine (Flexeril) 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 MCMP 407 Atropine vs. Cyclobenzaprine MCMP 407 Spasmolytics Other drugs similar to Cyclobenzaprine (Flexeril) Chlorzoxazone (Paraflex, Parafon) Orphenadrine (Norflex) Carisprodol (Soma) MCMP 407 Spasmolytics O O O2N H C N NN Na + O Dantrolene Sodium (Dantrium) Interferes with excitationcontraction coupling Reduces release of Ca++ from the sarcoplasmic reticulum Blocks contraction Side Effects: Muscle weakness, sedation, rare hepatitis Uses: Cerebral palsy, multiple sclerosis Also Malignant Hyperthermia MCMP 407 Neuromuscular Blockers Motor neuron ACHEsterase Skeletal Muscle MCMP 407 Properties of neuromuscular blockers Drug Elimination via Duration of action (minutes) Short-acting Succinylcholine Mivacurium Plasma AChE Plasma AChE 5-10 10-20 Intermediate-acting Atracurium Spontaneous Vecuronium Hepatic and renal Rocuronium Hepatic and renal 20-35 20-35 20-35 Long-acting Pancuronium 60 Renal MCMP 407 Clinical use of neuromuscular blockers Muscle relaxation during surgical procedures Endotracheal intubation Maintain controlled ventillation MCMP 407 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