Muscle Relaxants, Kinder Flashcards by Amanda Beach

What are the centrally acting spasmolytics

baclofen
tizanidine
diazepam

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What drugs are used for local muscle spams

carisoprodol

cyclobenzaprine

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what are the non-centrally acting spasmolytics

dantrolene

botulinum toxin

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what are the Immunologic drugs used for MS

Interferons: beta1a beta1b
Glatiramer acetate
Mitoxantrone
Glucocorticoids

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Spasticity

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

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negative effects of spasticity

pain
decreased mobility
contractures
muscle spasms

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mech of spasticity

UMN lesions

hyperexcitability of alpha motor neurons in cord

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ways to modify reflex arc

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

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MOA baclofen

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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baclofen vs diazepam

baclofen as effective and less sedation side effect

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adverse effects baclofen

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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use baclofen

spascticiy in MS or spinal cord lesions

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

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MOA Tizanidine

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

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adverse effects tizanidine

less muscle wekaness but has drowsiness (take at night)

hypotension, dizziness, dry mouth asthenia and hepatotoxicity!!

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use tizanidine

muscle spasticity

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MOA diazepam

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

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use diazepam

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

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adverse effects diazepam

CNS depression and sedation
risk of dependence with use
amnestic effects

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

carisoprodol and cyclobenzaprine

work at brainstem

MOA carisoprodol

CNS depressant

metabolized to meprobamate which is sedative and anxiolytic

use of carisoprodol

short term Tx

2-3 weeks MSK pain

adverse effects carisoprodol

drowsiness and dizziness

addictive

MOA cyclobenzaprine

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

therapeutic use cyclobenzaprine

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

adverse effects cyclobenzaprine

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

What arc does dantrolene interfere with

the excitation-contraction coupling

MOA dantrolene

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

therapeutic use dantrolene

spasticity with UMN disorders and management malignant hyperthermia!!!

adverse effects dantrolene

muscle weakness, sedation, hepatitis

CI dantrolene

hepatitis

what can trigger malignant hyperthermia

volatile anesthetics | Neuromuscular blocking drugs like succinylcholine

what happens in malignant hyperthermia

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

MOA botulinum

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

use of botulinum toxin

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

adverse effects botulinum

focal muscle weakness

MOA interferons used in MS

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

effects of interferons in MS

improves MRI lesions, decrease relapse rate and dec severity

adverse effects interferons in MS

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

MOA glatiramer acetate

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

adverse effects to glatiramer acetate

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

what type of drug is Mitoxantrone

antineoplastic used for MS, AML and prostate CA

MOA mitoxantrone

intercalates into DNA causing breakage

bad side effect of mitoxantrone and how is it used

cardiac toxicity | reserved for rapidly advancing disease who failed other Tx

Glucocorticoid in MS

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