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43 Cards in this Set
- Front
- Back
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When are muscle relaxants used?
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To treat conditions associated with hyperexcitable skeletal muscle
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What is the goal in using muscle relaxants?
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To normalize excitability without decreasing muscle function
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What are 2 types of skeletal muscle relaxants?
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1) Antispasmotics
2) Spasmolytic (Antispasticity) |
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What type of drug treats muscle spasms?
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Antispasmotics
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What types of drug treats spasticity?
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Spasmolytic (Antiaspasticity)
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How are drugs divided to Rx skeletal muscle relaxants?
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Drugs divided by what they treat
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What are muscle spasms?
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High in muscle tension
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What is spasticity?
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Increase in muscle excitability (velocity dependent CNS problem)
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What are 2 things that can cause muscle spasms?
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1) Musculoskeletal injury
2) Inflammation |
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What are 2 antispasmotic drugs?
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1) Polysynaptic inhibitors
2) Diazepam (Valium) |
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What drug is an example of a polysynaptic inhibitor?
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Cyclobenzaprine (Flexeril)
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What is the route that antispasmotic polysynaptic inhibitor is given?
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Oral
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What is the mechanism of a polysynaptic inhibitor?
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Decrease spinal cord polysynaptic reflex activity, thus decrease in alpha motor neuron excitability via altering interneuron activity
Not well understood |
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Why is Diazepam (Valium) not often used for muscle spasms?
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Because side effects at doses needed to relax muscles is too great (sedative)
Drug has muscle relaxant properties |
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What are 3 side effects using antispasmotics?
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1) Sedative--decrease in CNS activity
2) Physical dependence 3) Tolerance |
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Antispastmotics are usually indicated for...
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short-term use only
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What is usually used together with antispasmotics like Flexeril (polysynaptic inhibitors) and Diazepam (Valium)?
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PT treatment
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What are 5 spasmolytic (antispasticity) drugs?
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1) Baclofen (Lioresal)
2) Diazepam (Valium) 3) Dantrolene sodium (Dantrium) 4) Tizanidine (Zanaflex) 5) Botox A |
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What are the usually routes for administering Baclofen (Lioresal)?
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1) Oral
2) Intrathecal |
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What is the mechanism of Baclofen (Lioresal)?
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Gabba agonist that will bind to alpha motor neuron site (disinhibition of gabba neurotransmitters)
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How does Diazepam (Valium) work?
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Inhibits CNS, thus decreases spasticity but causes sedation
Long-term use avoided |
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What drug is long-term use avoid for spasticity?
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Diazepam (Valium)
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Drug that can be used on spasms or spasticity?
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Diazepam (Valium)
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What is neurotin used for?
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Anti-convulsant, inhibits gabba like Baclofen
Treated for SCI and MS |
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What diagnoses is neurotin used for?
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SCI and MS
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What are 2 side effects of neurotin?
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1) Fatigue
2) Ataxia |
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What is the mechanism of Dantrolene Sodium (Dantrium)?
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Blocks calcium release at the SR in the muscle (not CNS) to decrease muscle contraction
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What are 2 side effects of Dantrolene Sodium (Dantrium)
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1) Generalized weakness--not specific to one muscle
2) Liver toxicity |
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What does Tizanidine (Zanaflex) do?
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Inhibits spontaneous interneurons
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What is the mechanism of Tizanidine (Zanaflex)?
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Alpha-2 adrenergic agonist found at spinal interneurons
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When is Tizanidine (Zanaflex) used?
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After SCI, possible TBI but not in acute phase b/c can inhibit healing in the brain
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What drug has milder side effects with less generalized muscle weakness?
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Tizanidine (Zanaflex)
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What are 3 common side effects of Tizanidine (Zanaflex)?
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1) Sedation
2) Dizziness 3) Dry mouth |
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What are 3 indications for Botox A?
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1) Control localized muscle dystonias
2) Reduce spasticity in specific muscle groups 3) Control muscle hyperexcitability for other purposes |
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How is Botox A administered?
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Injected in skeletal muscles
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What is the mechanism of Botox A?
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Inhibits ACh release at NMJ
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What are the side effects of Botox A?
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Systemic use can cause widespread paralysis which can cause decrease respiratory muscle (decrease breathing)
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Botox cleaves what?
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Fusion proteins to keep ACh from releasing (temporary effects b/c nerves can sprout)
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What drug has only temporary effects for spasticity?
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Botox A--nerves can sprout back
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What are 2 cons to using Botox A?
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1) Does not cure spasticity
2) Limited number of muscle groups can be done at a time (otherwise dangerous systemic effects) |
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What happens if Botox A is used at too high of a dose?
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Can cause an immune response, must use Type B
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Botox A has a small incidence of...
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severe side effects, even though the drug is potentially lethal
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How are most skeletal muscle relaxants absorbed?
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Most are absorbed well from GI tract, metabolized in liver and excreted intact or as a metabolite
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