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PHTH 561 - Pharm > Hyperexcitable muscle disorders, antispasm and antispastic medications - Study guide > Flashcards

Hyperexcitable muscle disorders, antispasm and antispastic medications - Study guide Flashcards

1
Q

Order of process of muscle contraction

A
  1. entry of Na+ = intiate action potential thru sarcolemma and T-tubules
  2. activate voltage-sensitive receptors = trigger Ca2+ release into cytosol
  3. Ca ions bind to troponin -> changes shape -> removes block of tropomyosin -> active sites exposed
  4. contraction by myosin heads attaching and detaching with release of energy
  5. Removal of Ca2+ by active transport into the SR
  6. blocking respored and fibers relax
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2
Q

What is the difference between upper motor neuron and lower motor neuron lesion?

A
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3
Q

What is spasticity?

A

Velocity dependent increase in muscle tone
- because of increased excitability of the muscle stretch reflex

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4
Q

What is a muscle spasm?

A

Involuntary muscle contraction

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5
Q

What are the common neurologic disorders associated with spasticity?

A

MS
Stroke
Cerebral palsy
spinal cord and brain injuries
Neurodegenerative diseases affecting the:
- uppermotor neuron
- pyramidal
- extrapyramidal pathways

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6
Q

What are the sx of severe spasticity?

A
  • muscle stiffness
  • muscle spasm
  • rapid muscle contraction (clonus)
  • fixed joints (contractions)
  • exaggerated muscle jerks
  • pain or tightness around the joint
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7
Q

What are the primary goals of skeletal muscle relaxants?

A
  • selective decrease in skeletal muscle excitability
  • decrease pain w/o causing a profound decrease in muscle function
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8
Q

What are the agents used for skeletal muscle relaxants?

A

anti-spasticity or antispasmodic

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9
Q

What is brand name of baclofen?

A

Lioresal

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10
Q

What is the brand name of chlorzoxazone?

A

Parafon forte

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11
Q

What is the brand name of cyclobenzaprine?

A

Flexeril

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12
Q

What is the brand name for Dantrolene?

A

dantrium

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13
Q

What is the brand name of diazepam?

A

valium

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14
Q

What is the brand name of tizanidine?

A

zanaflex

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15
Q

What is the brand name of metaxalone?

A

Skelaxin

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16
Q

What is the mechanism of action for baclofen?

A

Acts on the GABA which facilitates spinal inhibition of motor neuron = inhibits reflexes and decrease spasticity

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17
Q

What are the uses for baclofen?

A
  • treat spasticity with SC lesions
  • for MS
  • doesn’t cause as much generalized muscle weakness
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18
Q

What are the adverse effects of baclofen?

A
  • transient drowsiness (goes away in a few days)
  • confusion and hallucinations with CVA or elderly
  • nausea
  • mm weakness
  • headaches
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19
Q

What is the route of administration of baclofen?

A

Oral
Intrathecal

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20
Q

What is the mechanism of action for cyclobenzaprine?

A

poorly understood inhibition of muscle stretch reflex in the spinal cord

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21
Q

What are the adverse of effects of cyclobenzaprine?

A

blurred vision
dizziness
drowsiness
lightheadness
dryness of the mouth

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22
Q

What is the uses for cyclobenzaprine?

A

relief of muscle spasms

23
Q

What is the route of administation for cyclobenzaprine?

A

oral route is the usual way but can also be intravenous

24
Q

What is the mechanism of action for tizanidine?

A
  • stimulates alpha-2 receptors in the spinal interneurons
  • cause interneuron inhibition = decrease excitatory input into the alpha motor neuron
  • decreases excitatability by both pre and post synaptic inhibition
25
Q

What are the uses for tizanidine?

A
  • control spasticity from spinal lesions and central lesions
  • as effective as others
  • milder side effects and less generalized mm weakness
  • doesn’t cause as much hypotension and other CV side effects compared to clonidine
26
Q

What are the adverse effects of tizanidine?

A

sedation
dizziness
dry mouth
Less generalized weakness than baclofen or diazepam

27
Q

What is the route of administration for tizanidine?

A

oral or can also be intraveous

28
Q

What is the mechanism of action for diazepam?

A

facilitate GABAergic transmission in the CNS

increases GABA-mediated inhibition of alpha motor neuron -> less excitability -> muscle relaxation

29
Q

What are the uses of diazepam?

A

Extensively in treating spasms associated with musculoskeletal injuries

30
Q

What are the adverse effects of diazepam?

A
  • sedation and general reduction in psychomotor ability
  • long term use also limited by tolerance and dependence
  • sudden use withdrawl = seizues, anxiety, agitation, tachycardia and even death
  • overdose of diazepam = coma or death
31
Q

What is the mechanism of dantrolene?

A

stops the release of Ca from skeletal muscle into the SR

32
Q

What are the uses of dantrolene?

A

Treating severe spasticity

not presribed to treat mm spasms caused by musculoskeletal injury

Used in traumatic cord lesions, advanced MS, cerebral palsay, CVA

33
Q

What are the adverse effects of dantrolene?

A
  • generalized muscle weakness is the most common
  • severe hepatoxicity
  • fatal hepatitis
34
Q

How is dantrolene use be counterproductive?

A

increased motor function with a decreased spasticity is offset by generalized mm weakness

35
Q

What are the uses for metaxalone?

A

mod to strong muscle relaxant used in symptomatic treatment of musculoskeletal pain

36
Q

What is the mechanism of action of metaxalone?

A

Has not yet been established but is possibly due to general CNS depression

37
Q

What are the adverse effects of metaxalone?

A

drowsiness
irritability
upset stomach

There’s a crap load but these are the most common (???)

38
Q

What is the route of administration for metaxalone?

A

oral route
taken 3-4x per day

39
Q

What is the use of chlorzoxazone?

A

relax certain muscles in the body to get relief caused by acute musculoskeletal disfunctions

40
Q

What is the mechanism of action for chlorzoxazone?

A

MOA is unknown but might act @ the spinal cord and subcortical levels of the brain
- this slows multisynaptic reflex arcs that has to do with muscle spasms

41
Q

What are some adverse effects of chlorzoxazone?

A

Drowsiness, dizziness, lightheadedness, tiredness, upset stomach, or headache may occur

42
Q

What is the route of administration for chlorzaxazone?

A

Oral route

43
Q

What is a patient controlled analgesia?

A

safe way for people to give themselves intravenous and pain medicine when they need

44
Q

What are the benefits of PCA?

A
  • allows for better pain control with less side effects
  • but does need patient awareness and cognitive ability
  • increases patient satisfaction
45
Q

What is nociceptive pain?

A

pain coming from actual or threatened damage to non-neural tissue
= activation of nociceptors

46
Q

What is neuropathic pain?

A

pain from neurons or somatosensory nervous system

47
Q

What is the difference between nociceptive vs neuropathic pain?

Picture

A
48
Q

What are the causes of acute pain?

A

generally known what caused the pain

49
Q

What are the causes of chronic pain?

A

often unknown

50
Q

What is the duration of pain for acute pain?

A

short
well-characterized

51
Q

What is the duration of pain for chronic?

A

Persistent after healing
greater than 3 months

52
Q

What is the treatment approach of acute pain?

A

When the cause is fixed = pain goes away
- usually self limiting

53
Q

What is the treatment approach of chronic pain?

A

the underlying cause and pain disorder
- pain control is the goal and not cure

PHTH 561 - Pharm (6 decks)

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