1 - Skeletal Relaxants Flashcards

1
Q

What are the two antispastic agents that are NOT centrally acting?

A

Dantrolene

Botulinum Toxin A

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2
Q

MOA for cyclobenzaprine (Flexeril)?

A

Cause a depressant effect of serotonergic neurons

Strong anticholinergic and antihistamine properties

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3
Q

Cyclobenzaprine (Flexeril) - clinical use?

A

Acute local muscle spasm

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4
Q

Cyclobenzaprine (Flexeril) is ineffective in treating muscle spasm due to:

A

Cerebral palsy or SCI

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5
Q

Cyclobenzaprine (Flexeril) can lower the ___ threshold, especially when combined with tramadol (Ultram)

A

Seizure

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6
Q

Clyclobenzaprine (Flexeril) - AE’s?

A
  1. Drowsiness
  2. Dry mouth
  3. Urinary retention
  4. Confusion (in elderly)
  5. SEROTONIN SYNDROME
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7
Q

Cyclobenzaprine (Flexeril) - CI’s?

A
  1. AMI
  2. MAOI’s
  3. ETOH
  4. Other CNS depressants
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8
Q

Cyclobenzaprine (Flexeril) - pregnancy?

A

No adverse events observed in animal studies

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9
Q

Orphenadrine (Norflex) - MOA?

A

Analog of BENADRYL

Antihistamine and anticholinergic properties

Euphoric and analgesic effects (unknown mechanism)

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10
Q

Orphenadrine (Norflex) - clinical use:

A

Tx of muscle spasm associated with acute painful musculoskeletal conditions

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11
Q

Orphenadrine (Norflex) - AE’s?

A

Anticholinergic effects (dry mouth, urinary retention, n/v, tachycardia)

Confusion (elderly)

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12
Q

Orphenadrine (Norflex) - CI’s?

A

Glaucoma, pyloric or duodenal obstruction, peptic ulcers, MG, BPH

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13
Q

Carisoprodol (Soma) C-IV - MOA?

A

Blocks interneuronal activity and depresses neuron transmission

Anxiolytic and sedative effects

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14
Q

Carisoprodol (Soma) - clinical use?

A

Relief of discomfort associated with acute, painful musculoskeletal conditions in adults

Short term use (2 to 3 weeks)

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15
Q

Carisoprodol (Soma) C-IV - AE’s?

A

Withdrawal symptoms can occur

Sedation, dizziness, HA, seizures

Confusion (elderly)

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16
Q

Carisoprodol (Soma) C-IV - pregnancy?

A

Adverse events have been observed in animal reproductive studies

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17
Q

Metaxalone (Skelaxin) - MOA?

A

Unknown - general depression of the nervous system

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18
Q

Metaxalone (Skelaxin) - Clinical use?

A

Relief of discomfort associated with acute, painful musculoskeletal conditions

Appears to cause less drowsiness than others

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19
Q

Metaxalone (Skelaxin) - AE’s?

A

Nausea, GI upset, sedation, HA, anxiety

Serotonin syndrome

Confusion (elderly)

20
Q

Methocarbamol (Robaxin) - MOA?

A

Suppresses spinal polysynaptic reflexes

21
Q

Methocarbamol (Robaxin) - Clinical use?

A

Adjunctive treatment of muscle spasm associated with acute painful musculoskeletal conditions

Treat muscle spasticity associated with tetanus poisoning

22
Q

Methocarbamol (Robaxin) - AE’s?

A

Urine discoloration (black, brown, or green)

Drowsiness

Confusion (elderly)

23
Q

Methocarbamol (Robaxin) - CI’s?

A

IV formulation in pt’s with renal impairment

Caution in hepatic impairment

24
Q

Tizanidine (Zanaflex) - MOA?

A

Centrally acting alpha-2 agonist

Reduces spasticity by increasing presynaptic inhibition of motor neurons

25
Q

Tizanidine (Zanaflex) - Clinical use?

A

Muscle spasticity

Short acting agent

26
Q

Tizanidine (Zanaflex) - AE’s?

A

Drowsiness

Dry mouth, HOTN, hepatotoxicity

Dosage adjustment for renal or hepatic insufficiency

27
Q

Baclofen (Lioresal) - MOA?

A

Orally active GABA-mimetic agent at the level of the spinal cord

Reduces Ca++ influx

Reduces excitatory transmitters

INHIBIT release of SUBSTANCE P

28
Q

Baclofen (Lioresal) - clinical use?

A

Drug of choice for multiple sclerosis

As effective is diazepam and causes less sedation

29
Q

Baclofen (Lioresal) - AE’s?

A

Drowsiness, nausea, confusion

Increased seizure activity in epileptic pt’s (must withdraw slowly)

30
Q

Diazepam (Valium) C-IV - MOA?

A

Benzodiazepine

Enhancement of the inhibitory effects of GABA

Antispasmotic AND antispasticity

31
Q

Diazepam (Valium) C-IV - clinical use?

A

Oral formulation used in cerebral palsy, MS, temporary muscle spasms, anxiety disorders, ETOH withdrawal

32
Q

Diazepam (Valium) C-IV - AE’s?

A

Drowsiness, fatigue, ataxia

Dependency and tolerance

33
Q

Diazepam (Valium) C-IV - pregnancy cat?

A

D

34
Q

Gabapentin (Neurontin) - MOA?

A

Inhibition of voltage-dependent Ca++ channels

Analog of GABA

35
Q

Gabapentin (Neurontin) - clinical use?

A

Generalized tonic-clonic seizures

Neuropathic pain and post herpetic neuralgia pain

Diabetic neuropathy (off-label)

36
Q

Gabapentin (Neurontin) - AE’s?

A

Drowsiness, fatigue, dizziness, HA, wright gain

Dose adjustment for renal/hepatic insufficiency

37
Q

Pregabalin (Lyrica) C-V - MOA?

A

Inhibition of voltage-dependent Ca++ channels

GABA derivative

38
Q

Pregabalin (Lyrica) C-V - clinical use?

A

Partial onset seizure (adjunct)

Non-epileptic neuropathic pain associated with: diabetic neuropathy, fibromyalgia, restless leg syndrome, social phobia

39
Q

Pregabalin (Lyrica) - AE’s?

A

Drowsiness fatigue GREATER THAN Gabapentin

Dizziness, weight gain, sexual dysfunction

40
Q

Pregabalin (Lyrica) C-V - discontinuation symptoms?

A

Insomnia, nausea, HA, diarrhea

41
Q

Dantrolene sodium (Rynodex) - MOA?

A

Reduces skeletal muscle strength by interfering with excitation-contraction coupling in the muscle fibers

42
Q

Dantrolene sodium (Rynodex) - clinical use?

A

IV DOC for tx of malignant hyperthermia (MH)

Oral - spasticity d/t SCI, stroke, MS

Not indicated for spasms d/t rheumatic d/o’s

43
Q

Dantrolene sodium (Rynodex) - AE’s?

A

Muscle weakness, sedation, hepatotoxicity

44
Q

Non-cosmetic uses for botulinum toxin?

A

Chronic migraines (2nd line agent)

Cervical dystonia

Blepharospasm

45
Q

BLUF on toxin A:

A

Slower onset
Longer duration of efficacy
Less pain of injection

46
Q

BLUF on toxin B:

A

Faster onset
Shorter duration of efficacy
More painful injection site
Generally for cervical dystonia only