Centrally Acting Muscle Relaxants

Question 1

Centrally acting spasmolytics

Answer 1

-Baclofen
-Carisprodol
-Cyclobenzaprine
-Diazepam
-Tizanidine
BCCDT

Question 2

Non-centrally acting spasmolytics

Answer 2

• Dantrolene

- Botulinum toxin

Question 3

Immunologic drugs for MS

Answer 3

• glucocorticoids
• Glatiramer acetate
• Interferon-beta-1a/b
• Mitoxantrone

Question 4

Baclofen- moa

Answer 4

• agonist at GABAb Rs- hyperpolarization (inc K conductance) and and inhibition of excitatory NT release in brain and spinal cord
• tx reversible spasticity assoc w MS or spinal cord lesoins

Question 5

Carisprodol- moa

Answer 5

• CNS depressant!!!
• short-term tx of musculoskeletal pain
• metabolite- Meprobamate

Question 6

Cyclobenzaprine

Answer 6

• reduces tonic somatic motor activity by infl both alpha and gamma motor neurons
• tx m spasm assoc w acute, painful musculoskeletal conditions

Question 7

Diazepam

Answer 7

• promote binding of major inhibiting Nt in the CNS (GABA) to the GABAa R- enhances GABA-induced ion currents (inc freq of channel openings) inc inhibitory transmission and a reduction in spasticity
• tx anxiety disorders, ethanol withdrawal sx’s, skeletal m relaxation, convulsive disordres, preop sedation, amnesia
• SE- generalized CNA depression

Question 8

Tizanidine

Answer 8

• alpha2-adrenergic agonist that dec excitatory input to alpha motor neurons
• tx of m spasticity

Question 9

Dantrolene

Answer 9

-reduces skeletal m strength by interfering w excitiation-contraction coupling in m fibers
-inhibition of RyR ca channel- blocks release of Ca thru SR and m contraction is impaired
tx- spasticity assoc w UMN disorders, malignant hypertthermia

Question 10

Botulinum toxin

Answer 10

• cleaves components of core SNARE complex involved in exocytosis, preventing the release of ACH
• tx- strabismus and blepharospasm assoc w dystonia; cervical dystonia; lines/wrinkles of face; severe primary axillary hyperhidrosis; focal spasticity; chronic migraine HA

Question 11

MS- Glatiramer acetate

Answer 11

• antigenically similar to myelin basic protein (important component of MS of n’s)
• induce and act T-lymphocyte suppressor cells specific for a mylein ag

Question 12

MS- interferons

Answer 12

-acts on BBB by interfering w T-cell adhesion to the endothelium by binding VLA-4 on T cells or by inhibiting the T-cell expression of MMP

Question 13

MS- mitoxantrone

Answer 13

-intercalates into DNA resulting in cross-inks and strand breaks