Muscle relaxants: Kruse

Question 1

what are the Centrally acting spasmolytics?

Answer 1

• Baclofen
• Carisprodol
• cyclobenzaprine
• Diazepam
• Tizanidine

Question 2

What are the Non-centrally acting spasmolytics?

Answer 2

• Dantrolene

- Botulinum toxin

Question 3

What are the immunologic drugs for MS?

Answer 3

• Glucocorticoids
• Glatiramer acetate
• Interferons (beta-1a and beta-1b)
• Mitoxantrone

Question 4

MOA of Baclofen?

Answer 4

-agonist at GABAb receptors –>hyperpolarization and inhibition of excitatory neurotransmitter release in the brain and spinal cord

Question 5

Adverse effects of Baclofen?

Answer 5

• Drowsiness
• increased seizure activity in epileptic patients (withdrawal must be done slowly)
• vertigo, dizziness, psychiatric disturbances, insomnia, slurred speech, ataxia, hypotonia, muscle weakness

Question 6

what is baclofen used for

Answer 6

spasticity associated with MS or spinal cord lesions

Question 7

what is Carisprodol used for?

Answer 7

• short term (2-3 weeks) treatment of msk pain
• metabolized by CYP2C19; used with caution when coadministered with CYP450 inhibitors
• can treat anxiety and depression also

Question 8

high yield for cyclobenzaprine

Answer 8

• may caused visual hallucinations
• used for acute, painful, msk conditions . . ineffective in treating muscle spasm due to cerebral palsy or spinal cord injury
• metabolized by CYP450
• Xerostomia

Question 9

MOA of Benzodiazepine

Answer 9

-promote binding of major inhibitory neurotransmitter in the CNS GABA

Question 10

common uses for Diazepam?

Answer 10

• management of anxiety disorders
• ethanol withdrawal symptoms
• treatment of convulsive disorders
• sedation and amnesia

Question 11

what is the disadvantage to used benzodiazepines

Answer 11

• risk of dependence
• depression of CNS functions
• amnestic effects

Question 12

MOA of Tizanidine?

Answer 12

-alpha2 adrenergic agonist, decresases excitatory input to alpha motor neurons

Question 13

MOA of Dantrolene

Answer 13

• causes inhibition of RyR Ca channel; blocks release of calcium through the sarcoplasmic reticulum and muscle contraction is impaired
• Cardiac and smooth muscle unaffected

Question 14

what is a side effect/contraindication of Dantrolene

Answer 14

hepatitis

Question 15

What is dantrolene used for?

Answer 15

-treatment of spasticity associated with upper motor neuron disorders and management of malignant hyperthermia

Question 16

MOA of Botulinum toxin

Answer 16

-cleaves components of the core SNARE complex involved in exocytosis, preventing release of ACh

Question 17

What is Botulinum toxin used for clinically?

Answer 17

• treatment of strabismus and blepharospasm associated with dystonia
• cervical dystonia
• temporary improvement in appearance of lines/wrinkles of face
• severe primary axillary hyperhidrosis
• prophylaxis of chronic migraine headaches

Question 18

MAO of Glatiramer acetate

Answer 18

• a mixture of random polymers of 4 aa that is antigenically similar to myelin basic protein which is an important component of myelin sheath nerves
• thought to induce and activate T lymphocyte suppressor cells specific for a myelin antigen

Question 19

MOA of Mitoxantrone

Answer 19

-intercalates into DNA resulting in crosslinks and strand breaks