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What receptor does diazepam inhibit?
Where is diazepam effective and what disorders is it used in?
- Skeletal muscle (due to injury)
- Upper motor neuron disorders (cerebral palsy, paraplegia, etc.)
- Affects spinal cord (reduces spasticity in pts. with spinal cord injuries)
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)
What happens when GABA-B receptors (located on CNS nerve terminals) are activated?
Inhibition of NT release
This drug can be given intrathecally by a pump.
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
This is a centrally acting alpha2 agonist
Tizanidine increase presynaptic and postsynaptic _____.
Inhibition of motor neurons
How often should you be dosed with tizanidine?
TID; tizanidine is short acting
What are the AEs of Tizanidine?
- Dry Mouth
Tizanidine should not be mixed with _____ or _____, which are potent inhibitors of CYP 1A2
This is a centrally acting muscle relaxant related to tricyclic antidepressants.
This drug doesn't relax muscle tone or decrease neuronal conduction. It possibly acts in the brainstem to reduce motor function.
Relief of cyclobenzaprine is probably due to _____, rather than _____.
- CNS depression/sedation
- Skeletal muscle relaxation
This centrally acting muscle relaxant's main metabolite is meprobomate, a common sedative-hypnotic drug.
It is unclear what the primary effect of carisoprodol is. In what diseases is it ineffective?
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