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What receptor does diazepam inhibit?
GABA-A
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Where is diazepam effective and what disorders is it used in?
- Skeletal muscle (due to injury)
- Tetanus
- Upper motor neuron disorders (cerebral palsy, paraplegia, etc.)
- Affects spinal cord (reduces spasticity in pts. with spinal cord injuries)
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What is the MOA for Baclofen?
GABA-B agonist (presumed to decrease the release of excitatory NTs like glutamate from 1a afferents and upper motor neurons)
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What happens when GABA-B receptors (located on CNS nerve terminals) are activated?
Inhibition of NT release
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This drug can be given intrathecally by a pump.
Baclofen
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Besides sedation, dizzines, muscle weakness, and fatigue, what AEs are unique to Baclofen?
- Seizures or hallucinations on sudden withdrawal
- Black box warning associated with sudden withdrawal of intrathecal administration; led to high fever, altered mental status, rhabdomyolysis, and DEATH
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This is a centrally acting alpha2 agonist
Tizanidine
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Tizanidine increase presynaptic and postsynaptic _____.
Inhibition of motor neurons
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How often should you be dosed with tizanidine?
TID; tizanidine is short acting
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What are the AEs of Tizanidine?
- Hypotension
- Bradycardia
- Sedation
- Asthenia
- Dry Mouth
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Tizanidine should not be mixed with _____ or _____, which are potent inhibitors of CYP 1A2
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This is a centrally acting muscle relaxant related to tricyclic antidepressants.
Cyclobenzaprine
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This drug doesn't relax muscle tone or decrease neuronal conduction. It possibly acts in the brainstem to reduce motor function.
Cyclobenzaprine
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Relief of cyclobenzaprine is probably due to _____, rather than _____.
- CNS depression/sedation
- Skeletal muscle relaxation
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This centrally acting muscle relaxant's main metabolite is meprobomate, a common sedative-hypnotic drug.
Carisoprodol
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It is unclear what the primary effect of carisoprodol is. In what diseases is it ineffective?
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