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Spasmolytics

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Spasmolytics Chronic neurologic diseases Cerebral Palsy, Multiple Sclerosis Acute Injury Spinal cord damage, muscle inflamation Goal of therapy: Reduce spasticity and ... – PowerPoint PPT presentation

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Title: Spasmolytics


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
Dantrolene Sodium (Dantrium)
  • Interferes with excitation-contraction 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

9
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
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
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