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35 Cards in this Set
- Front
- Back
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clinical features of spasticity (2)
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skeletal muscle spasms
increase in tonic stretch reflexes, with muscle weakiness |
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mechanism of spasticity disease (involves dmg to where? results in what?)
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involves dmg to descending pathways of spinal cord
results in hyperexcitability of motor neurons |
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testing for spasticity (2)
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difficult to test: simple muscle tone/reflex tests provide little insight
more useful to do global clinical assessments (# of spasms per day) |
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evidence for antispasmodic oral drugs
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weak
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first smasmolytic drug
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antodyne
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antodyne led to dev of...
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mephesin
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mephenesin- MoA (what didn't it do?)
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selective depression of polysynaptic but not MONOsynaptic spinal cord reflexes
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mephenesin usage
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no longer used- used to be widely prescribed as centrally acting muscle relaxant (and used to derive them)
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pharmacology of mephenesin like muscle relaxants is similar to...
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sed-hyps
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difference between centrally acting muscle relaxants and sed-hyps
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spasmolytics are more selective for modulating fx mediated by spinal cord and therefore produce less sedation than sedative hypnotics
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AE of centrally acting muscle relaxants (4)
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reversible non specific CNS depression
sedation dizzy muscle weakness |
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3 main categories of CNS muscle relaxants (and 2 drugs that don't belong to any category)
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glycerol monoethers/derivatives
substituted alkanedioles/derivatives benzazoles orphenadrine citrate (orphan- misc. category) cyclobenzaprine (misc category) |
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3 glycerol monoether CNS muscle relaxants
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mephenesin
chlorphenesin methocarbamol |
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3 substituted alkanediols (CNS muscle relaxants)
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meprobamate
carisoprodol metaxalone |
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benzazole muscle relaxant
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chlorzoxazone
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2 "longer acting" (alleged) derivatives of mephenesin
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chlorphenesin
methocarbamol |
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carisoprodol- works for what?
similar to what drug |
modest efficacy for low back pain associated with sprain or strain
similar fx to benzos and have liability for abuse/dependency |
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CNS muscle drug that is not associated with abuse
how does it do this |
metaxolone
achieves relaxation without sedation (excessive) |
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chloroxazone- properties (3)
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hepatotoxicity
good muscle relaxant unclear if it helps spasms |
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orphenadrine- similar to what drugs?
receptor properties |
similar to antihistamines
has muscarinic receptor antagonist properties |
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valium (diazepam)- MoA (2)
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binds to GABAa and enhances GABA potency (modulates it) to open channel and increase Cl conductance
results in neuronal hyperpolarization |
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diazepam activity mediated by...
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activity is mediated by GABAa a2/a3 subunits
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diazepam relieves spasticity in what 2 types of pt
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relieves spasticity in some CP? patients or pt with spinal cord lesions
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valium (diazepam) AE (2)
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drowsy
fatigue |
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one of the most commonly used antispastics
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baclofen
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proposed baclofen MoA (3)
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proposed MoA: inhibit spinal cord mono/polysynaptic reflexes by ativating GABAb** (GABAb agonist)
this allows K+ channels to open, leading to hyperpolarization may also reduce release of excitatory NTs |
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AE of baclofen (4)
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sedation
weakness vertigo psych disturbances |
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baclofen indications - treats spasticity in...(3)
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treasts spasticity in para/quadruplegia
pt with MS/spinal cord trauma |
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baclofen routes (2)
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can be given orally or intrathecally with infusion pump if severe
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dantrolene proposed MoA (3)- acts where, what receptor, final effect
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peripheral acting
believed to act at sarcoplasmis reticulum of skeletal muscle cells by binding to ryanodine (calcium channels) receptor on SR to close channels and inhibit Ca++ release decreases contraction force |
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dantrolene indications (5)
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indications: spinal cord injury, stroke, cerebral palsy, MS, malignant hyperthermia
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tizanidine MoA (2)
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centrally acting a2 agonist
proposed to decrease release of NE/serotonin fron spinal interneurons that contain a2 receptors (negative feedback) |
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tizanidine indication
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indication: chronic spasticity conditions (MS mostly)
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AE of tizanidine (3)
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AE: hypotension/dizzy, falls, muscle weakness
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structure of tizanidine- similar to?
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SAR: similar structure to clonidine (-idine)
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