Hosam Mohamed-
diazepam, baclofen
Which drugs potentiate GABA signaling? (2)
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tizanidine
Which drug agonizes A2-adrenergic receptors?
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increase neuronal inhibition; decrease muscle contractility
What are the 2 primary methods of treating Spasticity?
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a
Which receptor is a ligand-gated ion channel?
a) GABA A
b) GABA B
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b
Which receptor is a metabotropic GPCR?
a) GABA A
b) GABA B
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b
Which receptor activates K+ channels to cause hyperpolarization?
a) GABA A
b) GABA B
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a
Which receptor causes the influx of chloride ions into the cell?
a) GABA A
b) GABA B
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spinal cord
Both GABA A and GABA B are expressed in the __________.
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inhibitory
GABA is a major _________ amino acid NT.
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b
Which is 1st line for MS?
a) Diazepam
b) Baclofen
c) Tizanidine
d) Dantrolene
e) Botulinum Toxins
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a
Which is a Schedule IV?
a) Diazepam
b) Baclofen
c) Tizanidine
d) Dantrolene
e) Botulinum Toxins
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a, c
Which has both antispasticity and antispasmodic uses?
a) Diazepam
b) Baclofen
c) Tizanidine
d) Dantrolene
e) Botulinum Toxins
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b
Which has a BBW for AE's related to abrupt discontinuation?
a) Diazepam
b) Baclofen
c) Tizanidine
d) Dantrolene
e) Botulinum Toxins
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GABA analog that agonizes GABA B; causes hyperpolarization of presynaptic calcium channels and increased postsynaptic K+ conductance; suppressing activity of neurons
Baclofen MOA?
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analgesic-decreases substance P, less sedation than BZDs, poor peripheral distribution
What are other positive features of Baclofen? (3)
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elderly, renal/hepatic impairment
Who is at risk when using Diazepam? (2)
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increases GABA A activity via allosteric modulation
Diazepam MOA?
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sedation
Diazepam can relax muscle tone, but the dose required for this will cause _________.
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inhibits the release of presynaptic excitatory NT; reduces postsynaptic activation of the upper motor neuron; and potentiates glycine
Tizanidine MOA?
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inhibits RyR1 calcium channel in SR; inhibits calcium release; disrupting excitation and contraction coupling
Dantrolene MOA?
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d
Which has a BBW for hepatotoxicity?
a) Diazepam
b) Baclofen
c) Tizanidine
d) Dantrolene
e) Botulinum Toxins
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dantrolene, botulinum toxins
What are the direct-acting muscle relaxants? (2)
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cleave synaptic vesicle machinery (SNAPs and VAMPs); prevent ACh exocytosis and causes local muscle paralysis
Botulinum ToxinsMOA?
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a
Which has the longest half-life?
a) Diazepam
b) Baclofen
c) Tizanidine
d) Dantrolene
e) Botulinum Toxins
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a
Which causes CNS depression?
a) Diazepam
b) Baclofen
c) Tizanidine
d) Dantrolene
e) Botulinum Toxins
