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Pharmacology > Part 3 - Muscle Relaxants > Flashcards

Part 3 - Muscle Relaxants Flashcards

1
Q

Muscle Relaxants Primary Goals

A

Selectively decrease skeletal muscle excitability

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2
Q

Muscle Relaxants Primary Uses

A

Muscle Spasms and spasticity

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3
Q

Muscle Spasms

A

Usually injury to mm or peripheral nn causing tonic contraction

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4
Q

Spasticity

A

CNS lesion that causes an exaggerated stretch reflex. Often velocity dependent.

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5
Q

Types of agents used to treat muscle spasms

A

Centrally acting anti-spasm drugs

Diazapam (Valium)

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6
Q

Centrally acting anti-spasm drugs

A

Diverse group

Used commonly in back and neck spasms; other ortho injuries

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7
Q

Common Central antispasm drugs

A 
Carisoprodol
Chlorzoxazone
Cyclobenzaprine
Metaxalone
Methocarbarbamol
Orphenadrine Citrate
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8
Q

Centrally-acting anti-spasm drugs primary effect

A

Strong sedatives

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9
Q

Carisoprodol MOA

A

Enhances GABA inhibition in brain

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10
Q

Cyclobenzaprine MOA

A

Might increase serotonin in the brainstem

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11
Q

Antispasm drugs bottom line

A

Short term use for acute spasms
Patients may decide to take at bedtime
Combine with aggressive PT
Should be discontinued ASAP

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12
Q

Diazepam (Valium)

A

Developed originally as an antianxiety drug

Works in CNS to increase inhibitory effects of GABA

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13
Q

GABA Receptor

A

Has binding sites for GABA, Benzo, Barbituates
Chloride channel in the center
Chloride is normally inhibitory
Valium keeps GABA bound longer

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14
Q

Valium effects

A

Increases GABA mediated inhibition of alpha motor neuron
Less excitation leads to muscle relaxation
Used in spasms and spasticity, but causes sedation
Long-term use limited by tolerance and dependence

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15
Q

Agents used to treat spasticity

A 
Diazepam
Baclofen
Alpha-2 agonists
Gabapentin
Dantrolene
Botulinum toxin
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16
Q

Baclofen

A

Synthetic GABA
Stimulates GABA receptors in cord
Decreases excitation of alpha motor neuron
Can be administered intrathecally

17
Q

Intrathecal Baclofen

A

Used in severe spasticity
Catheter and pump deliver drug to subarachnoid space
May decrease spasticity with less drug, fewer side effects

18
Q

Intrathecal baclofen signs of OD

A

Decreased respiration
Decreased cardiac function
Stupor
Coma

19
Q

Intrathecal baclofen signs of withdrawal

A

Fever
Confusion
Hallucinations
Seizures

20
Q

Alpha-2 agonists

A

Primarily tizanidine
Stimulates alpha-2 receptors located on spinal interneurons
Causes inhibition of interneurons; decrease excitation on alpha motor neuron
Efficacy similar to oral baclofen but less generalized mm weakness

21
Q

Gabapentin (Neurontin)

A

Developed as antiseizure drug
Inhibits Ca++ entry presynaptic terminal; decreased release of glutamate
Used primarily in MS, SCI.
May cause sedation, dizziness, ataxia

22
Q

Dantrolene Sodium (Dantrium)

A

Only direct-acting muscle relaxant
Inhibits release of calcium from skeletal mm SR
Problems with liver toxicity; esp women over 35

23
Q

Botulinum toxin

A 
Muscle paralytic...Injected locally for severe spasms such as torticollis
Increased use in spasticity
7 serotypes, 2 used clinically
-Type A (Botox, Dysport, Xeomin)
-Type B (Myobloc)
24
Q

Botulinum toxin MOA

A

Inhibits release of ACh at skeletal neuromuscular junction by eating connection proteins so no exocytosis of ACh

25
Q

Botulinum toxin antispasticity effects

A 
Injected into selected muscle
Relaxation occurs within 3 to 7 days; lasts 2 to 3 months
Reduces spastic dominance
-Increases residual function
-Improved ADL, braces fit better, etc
26
Q

Botulinum toxin effects

A

BTX may be transported to CNS (retrograde transmission)

May produce carry-over & long term effects on activity in cord and brain

27
Q

Limitations of botulinum toxin

A

Local irritation at injection site
Potential for antibody production
Must limit total dose

28
Q

Botulinum toxin total dose

A

300-400 Units/tx Type A

2500-5000 Units/Tx Type B

29
Q

BTX signs of OD

A

Drooping eyes
Difficulty speaking/swallowing
General muscle weakness
Respiratory distress

30
Q

Muscle relaxants rehabilitation concerns

A

Generalized weakness
Sedation
Possible drastic change in spasticity over relatively short time span

Pharmacology (15 decks)

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