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MSK II Midterm > Kruse DSA: Skeletal Muscle Relaxants > Flashcards

Kruse DSA: Skeletal Muscle Relaxants Flashcards

1
Q

What are the centrally acting spasmolytics?

A
  • Baclofen
  • Cariprodol
  • Cyclobenzaprine
  • Diazepam
  • Tizanidine
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2
Q

What are the non-centrally acting spasmolytics?

A
  • Danrtrolene

- Botulinum toxin

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3
Q

What are the immunologic drugs for Multiple sclerosis?

A
  • Glucocorticoids
  • Glatiramer acetate
  • Interferons 1a and 1b
  • Mitoxantrone
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4
Q

Baclofen MOA

A
  • agonist at GABA(B) receptors
  • results in hyperpolarization and inhibition of excitatory neurotransmitter release in the brain and spinal cord
  • increased K+ conductance
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5
Q

Adverse effects of Baclofen

A
  • drowsiness, which patients become tolerant to with chronic administration
  • increased seizure activity in epileptic pts (withdrawl must be done slowly)
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6
Q

What is Baclofen used to treat?

A
  • reversible spasticity associated with multiple sclerosis or spinal cord lesions
  • intrathecal administration is used for tx of intractable spasticity caused by spinal cord injury, ms, and other spinal disease
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7
Q

What does Carisprodol act as?

A
  • a CNS depressant

- short term tx (2-3 weeks) of msk pain

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8
Q

Adverse effects of Carisprodol?

A

-dizziness and drowsiness

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9
Q

What is Carisprodol metabolized by?

A
  • CYP2C19

- use with caution when coadministered with CYP450 inhibitors

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10
Q

What is carisprodol metabolized to?

A
  • meprobamate

- has anxiolytic and sedative effects

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11
Q

MOA or Chlorzoxazone?

A
  • acts on spinal cord and subcortical levels by depressing polysynaptic reflexes
  • used for symptomatic tx of muscle spasm and pain associated with acute msk conditions
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12
Q

What does cyclobenzaprine do?

A

-reduces tonic somatic motor activity by influencing both alpha and gamma motor neurons

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13
Q

What is cyclobenzaprine used to treat?

A
  • muscle spasm associated with acute, painful msk conditions

- ineffective in treating muscle spasm due to cerebral palsy or spinal cord injury

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14
Q

What is cyclobenzaprine metabolized by?

A
  • CYP450

- use with caution when coadministered with CYP450 inhibitors

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15
Q

Adverse effects of cyclobenzaprine?

A

-drowsiness, dizziness, and xerostomia

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16
Q

Diazepam MOA

A

-promote the binding of the major inhibitory neurotransmitter in the CNS GABA(a) receptor, enhancing GABA-induced ion currents; leads to increased inhibitory transmission and a reduction in spasticity

17
Q

common used of diazepam?

A

-management of anxiety disorders, ethanol withdrawal symptoms, skeletal muscle relaxation, tx of convulsive disorders, preoperative or preprocedural sedation, and amnesia

18
Q

Common adverse effects of diazepam?

A

-generalized CNS depression

19
Q

Disadvantages to using benzo’s

A
  • risk of dependence
  • depression of CNS functions
  • amnestic effects
  • additional CNS depression when combined with other drugs that depress the CNS
20
Q

Tizanidine MOA

A
  • alpha2 adrenergic agonist that decreases excitatory input to alpha motor neurons
  • used for tx of muscle spasticity
21
Q

adverse effects of Tizanidine?

A

-drowsiness, hypotension, dry mouth, and asthenia/muscle weakness

22
Q

What does Dantrolene do?

A

-in contrast to the centrally acting drugs, reduces skeletal muscle strength by interfering with excitation-contraction coupling in the muscle fibers

23
Q

MOA of Dantrolene

A

-causes inhibition of the RyR calcium channel; blocks the release of calcium through the sarcoplasmic reticulum and muscle contraction is impaired

24
Q

Why arent Cardiac and smooth muscle affected by Dantrolene?

A

-different RyR channel subtypes

25
Q

Side effects of Dantrolene

A

-generalized muscle weakness, sedation, and occasionally hepatitis (contraindicated in hepatitis patients)

26
Q

What do we use Dantrolene for?

A

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

27
Q

What is malignant hyperthermia?

A
  • rare heritable disorder that canbe triggered by a variety of stimuli, including the combination of general anesthetics and succinylcholine
  • patients at risk for this condition have a hereditary impairment in the ability of the sarcoplasmic reticulum to sequester calcium
  • after administration of a triggering agent, a sudden and prolonged release of calcium causes massive muscle contraction, lactic acid production, and increased body temperature
  • reduction of calcium is accomplished with administration of dantrolene
28
Q

MOA for botulinum toxin

A

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

29
Q

adverse effects of Botulinum toxin

A

-focal muscle weakness in the area of injection, which may last up to several months

30
Q

glucocorticoids

A

-monthly bolus IV glucocorticoids are used for tx of primary or secondary progressive MS alone or in combo with other immunomodulatory or immunosuppressive medications

31
Q

MOA of glatiramer acetate?

A

-a mixture of random polymers of four amino acids that is antigenically similar to myelin basic protein, which is an important component of the myelin sheath of nerves

32
Q

Interferons MOA

A
  • Acts on BBB by interferin with T-cell adhesion to the endothelium by binding VLA-4 on T cells or by inhibiting the T-cell expression of MMP
  • results in a reduction of relapses by one-third, a reduction of new MRI T2 lesions and the volume of enlarging T2 lesions, a reduction in the number and volume of Fd-enhancing lesions, and a slowing of brain atrophy
33
Q

What is Mitoxantrone?

A

-Antineoplastic agent used to tx MS, AML, and advanced hormonere-refractory prostate cancer

34
Q

MOA of Mitoxantrone?

A

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

MSK II Midterm (15 decks)

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