Muscle Relaxants, Kinder Flashcards

1
Q

What are the centrally acting spasmolytics

A

baclofen
tizanidine
diazepam

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2
Q

What drugs are used for local muscle spams

A

carisoprodol

cyclobenzaprine

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3
Q

what are the non-centrally acting spasmolytics

A

dantrolene

botulinum toxin

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4
Q

what are the Immunologic drugs used for MS

A

Interferons: beta1a beta1b
Glatiramer acetate
Mitoxantrone
Glucocorticoids

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5
Q

Spasticity

A

increase in tonic stretch reflexes and flexor muscle spasms with muscl eweakness

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6
Q

negative effects of spasticity

A

pain
decreased mobility
contractures
muscle spasms

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7
Q

mech of spasticity

A

UMN lesions

hyperexcitability of alpha motor neurons in cord

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8
Q

ways to modify reflex arc

A

reduce activity of Ia fibers that excite primary motor neuron
enhance activity of inhibitory internuncial neurons

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9
Q

MOA baclofen

A

agonist GABAb R
results in hyperpolarization from closing presynaptic CaCh, inc K postsynaptic Ch, inhibits dendritic Ca influx
suppress Ia sensory afferents interneurons and motor neurons
may reduce substance P

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10
Q

baclofen vs diazepam

A

baclofen as effective and less sedation side effect

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11
Q

adverse effects baclofen

A

drowsiness
increased seizure activity in epileptic patients(slow withdrawal)
confusion, dizziness, hypotonia, psych disturbances, insomnia, slurred speech, ataxia and muscle weakness

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12
Q

use baclofen

A

spascticiy in MS or spinal cord lesions

intrathecal for intractable spasticity from cord lesion, MS or spinal diseases

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13
Q

MOA Tizanidine

A

a2 agonist that reinforeces presynaptic and postsynaptic inhibition in cord
inhibits nociceptive transmission in dorsal horn

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14
Q

adverse effects tizanidine

A

less muscle wekaness but has drowsiness (take at night)

hypotension, dizziness, dry mouth asthenia and hepatotoxicity!!

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15
Q

use tizanidine

A

muscle spasticity

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16
Q

MOA diazepam

A

benzo that promotes binding to GABAa R and enhances those currents increasing inhibition and reduce spasticity

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17
Q

use diazepam

A

sedation, hypnotic effects, muscle relaxant, anxiolytic, anticonvulsant
anxiety disorders, ethanol withdrawal Sx, convulsive disorders, operation sedation and amnesia

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18
Q

adverse effects diazepam

A

CNS depression and sedation
risk of dependence with use
amnestic effects

19
Q

what drugs are used for relief of acute muscl spasm caused by local tissue trauma or muscle strain

A

carisoprodol and cyclobenzaprine

work at brainstem

20
Q

MOA carisoprodol

A

CNS depressant

metabolized to meprobamate which is sedative and anxiolytic

21
Q

use of carisoprodol

A

short term Tx

2-3 weeks MSK pain

22
Q

adverse effects carisoprodol

A

drowsiness and dizziness

addictive

23
Q

MOA cyclobenzaprine

A

reduce tonic somatic motor activity by influencing alpha and gamma motor neurons

24
Q

therapeutic use cyclobenzaprine

A

muscle spams with acute, painful MSK conditions (no longer than 2-3 weeks)
not useful for spinal cord injury or cerebral palsy

25
Q

adverse effects cyclobenzaprine

A

like tricyclic antidepressant, has antimuscarinic effects like sedation confusion and transient hallucinations
dizziness and xerostomia

26
Q

What arc does dantrolene interfere with

A

the excitation-contraction coupling

27
Q

MOA dantrolene

A

inhibit Ryanodine R Ca channel blocking Ca release form ST and contraction then impaired
Does NOT affect cardiac and smooth muscles

28
Q

therapeutic use dantrolene

A

spasticity with UMN disorders and management malignant hyperthermia!!!

29
Q

adverse effects dantrolene

A

muscle weakness, sedation, hepatitis

30
Q

CI dantrolene

A

hepatitis

31
Q

what can trigger malignant hyperthermia

A

volatile anesthetics

Neuromuscular blocking drugs like succinylcholine

32
Q

what happens in malignant hyperthermia

A

after triggered by agent large amounts Ca released causing massive muscle contraction, increased temp and lactic acid production
hence why dantrolene is administered

33
Q

MOA botulinum

A

zinc endopeptidase cleaves specific proteins in needed for vesicular fusion that allow Ach release. so blocks this release

34
Q

use of botulinum toxin

A

cervical dystonia, blepharospasm, severe primary axillary hyperhirosis
prophylaxis chronic migraines
Tx incontinence from overactive bladder

35
Q

adverse effects botulinum

A

focal muscle weakness

36
Q

MOA interferons used in MS

A

enhance suppressor T cell activity
reduces proinflammatory cytokines
down regulates Ag presentation
reduces trafficking of lymphocytes into CNS

37
Q

effects of interferons in MS

A

improves MRI lesions, decrease relapse rate and dec severity

38
Q

adverse effects interferons in MS

A

injection site reactions, flu like Sx, high prevalence of asymptomatic liver dysfunction
leukopenia, anemia and suicide

39
Q

MOA glatiramer acetate

A

mixture polymers of 4 amino acids
L alanine, L glutamic acid, L Lysine, L tyrosine
similar to myelin basic protein
“decoy”

40
Q

adverse effects to glatiramer acetate

A

local injection site reactions, transient systemic postinjection reactions(chest pain, flushing, dypsnea, palpitations, anxiety)

41
Q

what type of drug is Mitoxantrone

A

antineoplastic used for MS, AML and prostate CA

42
Q

MOA mitoxantrone

A

intercalates into DNA causing breakage

43
Q

bad side effect of mitoxantrone and how is it used

A

cardiac toxicity

reserved for rapidly advancing disease who failed other Tx

44
Q

Glucocorticoid in MS

A

monthly IV bolus used to Tx primary or secondary progressive MS alone or in combo with other immunomodulatory or immunosuppressive medications