Pharm- Skeletal Muscle Relaxants Flashcards

1
Q

Categories of NM blocking drugs and examples of each

A

Depolarizing- succinylcholine
Polarizing Long Duration- tubocurarine
Polarizing short duration- mivacurium

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2
Q

Categories of SM spasmolytic drugs and examples

A

Acute- cyclobenzapine
Chronic CNS action (TBD)- baclofen, diazepam, tizanidine
Chornic Peripheral- dantrolene

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3
Q

Members of neuromuscular blockers that interfere with transmission at the neuromuscular end plate and are not centrally acting drugs.

A

Atracurium, pancuronium, gallamine

GAP

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4
Q

used to produce muscle paralysis in order to facilitate surgery or artificial ventilation.

A

NM blocking drugs

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5
Q

: A drug that reduces abnormally elevated muscle tone (spasticity) without paralysis

A

Spasmolytic

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6
Q

are sudden, violent, painful, involuntary contractions of a muscle or group of muscles.

A

Spasm

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7
Q

Action potentials by motor neurons are conducted directly to nerve terminals in muscle fibers that form synapses called ____________

A

neuromuscular junctions (NMJ)

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8
Q

________ is released from the nerve terminal and stimulated _______ receptors on the muscle, producing contraction

A

Acetylcholine, nicotinic

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9
Q

Increased muscle tone or muscle contractions that cause stiff, awkward movement.

A

Spasticity

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10
Q

Common causes of spasticity

A

head injuries, cerebral palsy, MS, stroke

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11
Q

What are the mediators for:
Spasm
Spasticity

A

Spasm– LMN

Spasticity– UMN

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12
Q

Difference between causes of spasm and spasticity

A

Spasm= acute, transient and treatable
Spasticity= chronic and permanent
(Slide 8 = list of causes)

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13
Q

Name 5 spasmolytic drugs, and how one of them differs

A

Baclofen, diazepam, tizanidine, and Dantrolene– only one that is peripheral acting/NOT centrally acting
Dan’s Bacterial Tie Dies and BOtulinum

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14
Q

What are the two major uses for spasmolytic drugs

A

Muscle Strain and Back Pain

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15
Q

What are the inhibitory NT’s released by interneurons?

A

GABA and glycine

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16
Q

What does Botulinum toxin target?

A

synaptins

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17
Q

What does diazepam target

A

GABAa receptors

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18
Q

What does tizanidine target

A

centrally acting alpha 2 receptors

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19
Q

Acts within the spinal cord to suppress hyperactive reflexes involved in regulation of muscle movement

A

Baclofen

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20
Q

Baclofen MOA and target

A

GABA analog, GABAb

21
Q

Difference in action of baclofen and diazepam

A

Baclofen– interferes with release of excitatory transmitters
Diazepam– facilitates GABA-mediated presynaptic inhibition

22
Q

baclofen can reduce spasticity associated with these 4 things

A

MS, spinal cord injury, and cerebral palsy.

23
Q

Baclofen is not effective for _____ and _____-

A

Parkinsons and Stroke

24
Q

CNS effects and contraindications of Baclofen

A

CNS depressant resulting in dizziness and drowsiness

Should not be used with other depressants, including alcohol

24
Q

the only benzodiazepine labeled for treating spasticity.

A

Diazepam

25
Q

can be used for treatment of spasms (LMN) and spasticity (UMN)/ can be used in patients with muscle spasm of almost any origin, including local muscle trauma

A

Diazepam

26
Q

enhances the effect of the neurotransmitterGABAby binding to the benzodiazepine site on theGABAareceptor(via the constituent chlorine atom) leading tocentral nervous systemdepression.[4]

A

Diazepam

27
Q

difference in when to use diazepam and dantrolene

A

Diazepam does not cause muscle weakness like dantrolene and should be used with patients already exhibiting muscle weakness. Be sure to use proper dose of diazepam as to not induce too much sedation

28
Q

Acts within the spinal cord to suppress hyperactive reflexes involved in regulation of muscle movement.

A

baclofen

29
Q

anti-anxiety agent that can be used as a spasmolytic drug

A

Diazepam

30
Q

It acts directly on skeletal muscle to relieve spasticity by Suppression of calcium release from sarcoplasmic reticulum (SR)

A

Dantrolene

31
Q

what specific Ca release mechanism does dantrolene act on

A

prevents opening of Ca channel vital to the Calcium Induced Calcium Release Mechanism

32
Q

Baclofen interacts with ______ to produce-_______

A

Alcohol, Antihistamines, CNS depressants, MAO inhibitors

Increased CNS depression; increased risk of hepatotoxicity with combination of chlorzoxazone and alcohol

33
Q

Chlorphenesin interacts with ______ to produce ____

A
Tricyclic antidepressants(eg., amitriptyline)
Increased CNS depression; increased risk of hepatotoxicity with combination of chlorzoxazone and alcohol
34
Q

Dantrolene has minimal effects on _______ meaning that

A

smooth and skeletal muscle, it will have no effect on BP and overall no effect on TPR

35
Q

Dantrolene can treat spasticity caused by_______ but causes________

A

MS, cerebral palsy, and spinal cord injury.

significant decrease in strength / ability of skeletal muscle to contract

36
Q

What can be used to treat malignant hyperthermia and how does it work

A

Dantrolene, blocks the release of Ca from the SR

37
Q

What drug can trigger malignant hyperthermia

A

Succinly choline

38
Q

Dantrolene adverse effects

A

dose related liver damage, most serious toxicity, dizzines, drowsiness, and urinary frequency

39
Q
Dantrolene + estrogen =  
                \+ CNS depressants=
                \+Clindamycin= 
                 \+ Verampil= 
                \+warfarin+clofibrate=
A
hepatotoxicity
sedation
increased NM blockade
hyperkalemia and cardiac depression
common metabolic enzymes
40
Q

93% protein binding with a half life of 1-3 days

A

Cyclobenzaprine

41
Q

30% protein binding

A

Baclofen, Carisoprodol, Metaxalone

tizanidine

42
Q

treat neuropathic pain, interefere with alpha 2

A

tizanidine

43
Q

inhibits H1, musacrinic, NMDA receptors as well as NE uptake, treat fibromyalgia and muscle pain

A

Orphenadril-

44
Q

> 90% protein binding, half life of 6-9 hours

A

Dantrolene

45
Q
Contraindication of:
Baclofen
Carisoprodol
Cyclobenzaprine
Dantrolene
A
  • rheumatoid arthritis
  • hypersensitivity to meprobamate
  • MI, cardiac conduction disorders, hyperthyroidism
  • hepatic disease, rheumatoid arthritis
46
Q

An α2 agonist

Hypotentsion, drowsiness, and dry mouth

A

tizanidine

47
Q

Spasticity from cerebral palsy

Cosmetics surgery

A

botulinum toxin