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Pharm 6 > Muscle Relaxants > Flashcards

Muscle Relaxants Flashcards

0
Q

Drugs used to treat Spasticity

A
  • Baclofen
  • Tizanidine
  • Botulinum toxin
  • Dantrolene Sodium
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1
Q

Drugs used to treat spasm:

A
  • Cyclobenzaprine (flexeril)
  • Chlorzoxazone (Paraflex)
  • Orphenadrine (Norflex)
  • Methocarbamol (Robaxin)
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2
Q

All spasmolytics drugs alleviate the symptoms of ____________ muscle spasms.

A

Localized

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3
Q

T/F: No one spasmolytic is better than the other

A

True

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4
Q

Onset of action and duration and duration for:

1) Chlorzoxazone
2) Cyclobenzaprine
3) Methocarbamol
4) Orphenadrine

A

1) 60 min, 4-6 hr
2) 60 min (12-24 hr
3) 30 min, 1-2 hr
4) 60 min, 2-4 hr

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5
Q

MOA of spasmolytics

A

Depress polysynaptic reflexes (over monosynaptic reflexes) in the spinal cord.

  • Chlorzoxazone: unclear
  • Methocarbamol- unclear
  • Cyclobenzaprine: reduces tonic somatic motor activity influencing both alpha and gamma motor neurons.
  • Ophenadrine: Anticholinergic used to treat spasms of various etiologies
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6
Q

What drug is pharmacologically related to tricyclic antidepressants, and like TCA is serotonergic, noadrenergic (also anticholinergic and antimuscarinic). Short term treatment of skeletal muscle spasm, not effective for the treatment of spasticity.

A

Cyclobenzaprine

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7
Q

What drug is pharmacologically related to tricyclic antidepressants and the MOA is unclear but may be due to general CNS depression. Short term treatment for muscle spasms.

A

Methocarbamol

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8
Q

Most common Side effects for Cyclobenzaprine. High dose effects as well:

A

Drowsiness, loss of physical coordination, anticholinergic side effects, dizziness.
-High Doses: Areflexia, flaccid paralysis, resp. depression, tachycardia, hypotension

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9
Q

Most common side effects of Methocarbamol

A

Drowsiness, loss of physical coordination, light-headedness, dizziness, DISCOLORATION of URINE.
-High doses: CNS depression, resp. depression

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10
Q

Causes of spasticity

A
  • Accidental damage to brain or spinal cord
  • Ischemia (stroke)
  • MS
  • CP
  • Metabolic disease
  • Adrenoleukodystrophy
  • Amyotrophic lateral sclerosis
  • Phenylketonuria
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11
Q

Goals in treating spasticity

A
  • Reducing pain, frequency, irritating stimuli

- Improving gait, hygiene, activities of daily living, ease of care

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12
Q

Central acting treatment of Spasticity (Oral) and MOA:

A

Baclofen- GABAb receptor agonist
Tizanidine- alpha 2 adrenergic receptor agonist
Botulinum toxin
Gabapentin- act on N-type CA2+ channels to reduce neuropatic pain
Benzodiazepines: GABAa receptor agonist

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13
Q

Muscle acting treatment of spasticity

A

Dantrolene sodium (Dantrium)

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14
Q

Principal use of Oral Baclophen. Other uses:

A

to decrease spasticity caused by MS and spinal cord injury.

-Other: hiccups, neuropathic pain including trigeminal neuralgia, episodes of intense pain in face

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15
Q

What is intrathecal Baclofen and what are the advantages?

A

Pump surgically implanted under skin with catheter in intratecal space.
-Low dose, fewer side effects

16
Q

Uses of intrathecal baclophen

A
  • Cerebral palsy
  • Anoxic brain injury
  • MS
  • Stroke
  • Spinal cord injury
  • Arteriovenous malformation
  • Infection of spinal cord
17
Q

MOA of baclophen

A

Binding to pre-synaptic GABAb receptors

a. CA2+ influx through voltage-activated channels of type I a presynaptic terminals is inhibited
- Release of glutamate and aspartate are suppressed
b. Binding to post synaptic GABAb receptors causes:
- activation of K+ channels through a membrane-delimited pathyway
- Activation of 2nd messenger pathway involving arachidonic acid
c. Reduces substance P release from nociceptive afferent nerve terminals

18
Q

What is Tizanidine used for?

A

To decrease spasticity in patients with:

  • MS
  • Spinal cord injury
19
Q

What drug is this: Central acting at alpha 2 adrenergic agonist. Inhibits release of excitatory amino acids in spinal interneurons.

A

Tizanidine

20
Q

What drug is this: Used to treat spasticity caused by cerebral palsy, stroke, traumatic brain injury and advanced MS. Also treat patients with dystonia (oromandibular, cervical, laryngeal) and to treat excessive sweating.

A

Botulinum Toxin

21
Q

MOA of Botulinum toxin. Onset of muscle paralysis, max effect, and duration of paralysis.

A

Inhibits acetylcholine release from pre-synaptic nerve terminals, causing chemodenervation.
-Onset of focal muscle paralysis begins in 24 to 72 hours.
-Max effect in 5 to 14 days.
-Muscle paralysis can last 12-16 weeks.
Antibodies can develop lowering efficacy

22
Q

When is Botulinum toxin contraindicated

A

Excess weakness may result. Muscle paralysis may not be exact because toxin cannot be entirely contained.

23
Q

What drug is used to treat spasticity in patients with Upper motor neuron lesions, decrease spasticity in patients with strokes and spinal cord injuries, treat malignant hyperthermia, and treat neuroleptic malignant syndrome.

A

Dantrolene Sodium

24
Q

What Drug is this: Acts preferentially on fast muscle fibers to block muscle contraction. Reduces the depolarization-induced release of Ca2+ from the sarcoplasmic reticulum.

A

Dantrolene sodium

25
Q

Dantrolene sodium reaches peak concentration after ________ hour(s) following oral administration and is metabolized largely by ________, t1/2=15 hours

A

3-6 hours, the liver

26
Q

Contraindications of dantrolene sodium

A

Causes muscle weakness and may worsen overall functional capacity of the patient.
-SHOULD NOT BE used in patients with Amyotrophic lateral sclerosis where there is a low tolerance for muscle weakness.

27
Q

Adverse effect for Baclofen

A

Muscle weakness, sedation, fatigue, dizziness, nausea

28
Q

Adverse effects for Tizanidine

A

Drowsiness, dry mouth, dizziness, reversible dose-related elevation in liver transaminases.

29
Q

Adverse effect for Dantrolene

A

Hepatotoxicity, weakness, sedation, diarrhea

30
Q

Monitoring for Baclofennd special attention

A

Periodic liver function tests. Abrupt cessation associated with seizures.

31
Q

Monitoring and special attention for tizanidine

A

Periodic liver fxn tests. Not to be used with antihypertensives or clonidine.

32
Q

Monitoring and special attention for Dantrolene

A

Periodic liver fxn tests. Hepatotoxicity.

Pharm 6 (9 decks)

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