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Pharmacology > Introduction to pain and analgesics > Flashcards

Introduction to pain and analgesics Flashcards

1
Q

IASP definition of pain

A

pain is an unpleasant sensory and emotional experience associated with actual or potential tissue damage or described in terms as such damage. Pain is perceived

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2
Q

what are the 3 pain fibers

A

1) Ab fiber
2) Ad fiber
3) C fiber

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3
Q

Ab pain fiber

A
  • myelinated
  • triggered with non-noxious stimuluses
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4
Q

Ad pain fiber

A
  • myelinated
  • triggered with noxious stimuluses
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5
Q

C pain fiber

A
  • non myelinated
  • dull achey pain
  • triggered with noxious heat and chemical stimuli
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6
Q

where are the 3 areas that you can modulate pain CNS

A

1) dorsal horn
2) cortex
3) PAG

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7
Q

what are the two pathways

A

1) spinothalamic tract (ascending)
2) spinobulbar tract (descending)

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8
Q

where does the spinothalamic relay

A

conveys discriminative/localization aspects of pain by projection to the thalamus

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9
Q

where does the spinobulbar tract relay too

A

convays the affective/intensity aspects of pain and is able to recruit descending controls via the periaqueductal gray, pontine locus coeruleus and rostroventriomedial medulla

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10
Q

what are the types of chronic pain

A
  • nocicpetive
  • neuropathic
  • mixed (nociceptive and neuropathic)
  • visceral
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11
Q

examples of nociceptive chronic pain

A

OA and RA

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12
Q

examples of neuropathic pain

A

Central
- post-stoke
- MS
- SCI
- Phantom pain
Peripheral
- Post-herpetic neuralgia
- Diabetic neuropathy
- HIV related neuropathic pain

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13
Q

examples of mixed chronic pain

A
  • Low back
  • Cancer
  • Fibromyalgia
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14
Q

examples of visceral chronic pain

A
  • Internal organs
  • Pancreatitis
  • Inflammatory bowel syndrome
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15
Q

Physical sensations of neuropathic pain

A
  • numbness
  • tingling
  • burning
  • paresthetic
  • paroxysmal
  • lancinating
  • electric like
  • raw skin
  • shooting
  • deep, dull, bone like ache
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16
Q

Allodynia

A

Pain from a stimulus that does not normally provoke pain

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17
Q

Hyperalgesia

A

exaggerated response to a painful stimulus

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18
Q

Hyperesthesias

A

exaggerated response to touch

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19
Q

hyperpathy

A

persistant pain event after the cause of pain has been removed

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20
Q

what an analgesic

A

painkiller
is divided into 2 categories: nonopioid analgestics and opioid analgesics

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21
Q

nonopioid analgestics

A

are comprised of drugs such as acetaminophen, aspirin, ibubrofen

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22
Q

opioid analgestics

A

naturally occuring semisynthetic and synthetic agests are are characterized by their ability to relieve moderate to severe pain.

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23
Q

what analgestics modulate at the brain

A
  • opioids
  • NSAIDs
  • Ketamine
  • TCA
  • Gabapentionoids
  • Benzodiazepines
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24
Q

what analgestics modulate at the SC

A
  • opioids
  • neuraxial local anesthetics
  • ketamine
  • alpha- agonist
  • TCA
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25
Q

what analgestics modulate at the peripheral nerve

A
  • opioids
  • TCA
  • alpha agonist
  • ketamine
  • nerve block with local anaesthetic
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26
Q

what analgestics modulate at the tissue

A
  • opioids
  • NSAIDs
  • local anesthetic infiltration
  • corticosteroid
  • cooling, immobilization, elevation
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27
Q

what conditions are muscle relaxants able to treat

A

hyper excitable skeletal muscle such as spasticity and muscle spasms.

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28
Q

where are the 3 areas that muscle relaxants can block at

A

1) SC level
2) neuromuscular junction
3) directly within the muscle fiber

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29
Q

what are some common symptoms of spasticity

A
  • muscle stiffness
  • muscle spasms
  • rapid muscle contractions (clonus)
  • fixed joints (contractures)
  • exaggerated muscle jerks
  • pain or tightness around joints
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30
Q

what is the primary goals for muscle relaxants?

A

1) decrease in skeletal muscle excitability
2) decrease pain

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31
Q

what are the 2 types of skeletal muscle relaxants

A

anti-spasticity or antispasmodic agents

32
Q

what is labeled for use only in epilepsy and postherpetic neuralgia but is also used as a muscle relaxant?

A

Gabapentin

33
Q

what is labeled only for the use of ALS but is also used as a muscle relaxant?

A

Riluzole

34
Q

what are the most common anti-spasticity drugs

A

1) Baclofen
2) Dantrolene
3) Tizanidine
4) Botulinum toxin

35
Q

what does Baclofen act on

A

Gaba-B receptors in the SC to inhibit reflexes and decrease spasticity

36
Q

what does Dantrolene act on

A

directly on the skeletal muscles inhibiting Ca2+ release

37
Q

what does Tizanidine act on

A

an alpha 2 adrenergic agonist that produces pre synaptic inhibition (CNS)

38
Q

what does Botulinum Toxin work at

A

the neuromuscular junction inhibiting acetylcholine release

39
Q

what are spasmolytics

A

muscle relaxants that inhibit muscle spasms (more for peripheral conditions)

40
Q

what are common spasmolytics?

A

1) Carisoprodol (soma)
2) Cyclobenzaprine (flexeril)
3) Methocarbamol (robaxin)
4) Orphenadrine (norflex)

41
Q

Carisoprodol (soma) acts on

A

believed to alter interneuronal activity in the SC and descending reticular formation.

42
Q

Cyclobenzaprine (Flexeril) acts on

A

the CNS by decreasing the activity in the brainstem

43
Q

Methocarbamol (Robaxin) acts on

A

the CNS

44
Q

Orphenadrine (Norflex) acts on

A

has anticholinergic properties but unsure of direct effect

45
Q

what are the key differences between anti-spasticity and spasmolytics?

A
  • anti-spasticity: for CNS conditions with increased muscle tone, have more specific targets, more chronic in nature
  • Spasmolytics: more PNS conditions, less clear targets, often used for acute conditions
46
Q

what are polysynaptic inhibitors

A

same as spasmolytics; theorized to work on the reflex arc decreasing alpha motor neuron excitability and therefore cause muscle relaxation

47
Q

what are the uses of polysynaptic inhibitors

A
  • Adjunts to rest and PT for releif of muscle spasms associated with acute painful MSK injuries
  • sometimes incorporated into the same tabel with an analgestic
48
Q

what are the adverse affects of polysynaptic inhibitors

A
  • drowsiness, dizziness
  • nauseas, lightheadesness, vertigo, ataxia, headache
  • tolerace and physical dependance
49
Q

what are agents that are used to treat spasticity

A

1) Baclofen
2) Ticanidine
3) Dantrolene
4) Botulinum toxin
5) Gabapentin
6) Diazepam (benzodiazepines)

50
Q

Diazepam (Valium) definition and what it works on

A
  • benzodiazepine agent
  • works by increasing the inhibitory effects at the CNS/SC synapses that use GABA. Less excited alpha motor neuron
51
Q

what are the 6 intrinsic benzoduazepine effects

A

1) anxiolysis
2) anterograde
3) amnesia
4) sedation/hypnosis
5) anticonvulsant
6) antiemesis and muscle relaxation

52
Q

what are the therapeutic uses of Diazepam (Valium)

A
  • treating muscle spasms
  • associated with inhibiting spasms of the larynx with the tentanus toxin
53
Q

what are the adverse effects of Diazepam (Valium)

A
  • sedation and reduction of psychomotor ability
  • long term use can lead to tolerance and dependance
  • sudden withdraw can lead to seizures, anxiety, agitation, tachycardia, and even death/coma
54
Q

what is a drug that can be used to reduce the effects of Diazepam (Valium) overdose

A

Flumazenil

55
Q

Baclofen (Lioresal) what is it and where does it effect

A
  • Derivative of the central inhibitory GABA
  • binds to GABA B receptors in the SC producing a less excited alpha motor neuron
56
Q

what are the uses of Baclofen

A
  • used to treat spasticity in SC lesions (paraplegia, quadriplegia, SC demyelination from MS)
  • does not cause as much generalized muscle weakness
57
Q

what are the adverse effects of Baclofen (Lioresal)

A
  • drowsiness
  • confusion and hallucinations
  • nausea, muscular weakness, headache
58
Q

what are the uses for Baclofen intrathecal (spinal) injections

A
  • used for severe spasticity
  • may decrease spasticity with a smaller dose with fewer systemic effects
59
Q

what are the uses for intrathecal baclofen pump

A

able to adjust to deliver the drug at a slow continuous rate. achieves best clinical reduction in spasticity

60
Q

intrathecal baclofen adverse effects

A
  • pump malfunction can cause withdrawal symptoms
  • increased delivery can cause overdose
  • pt can build up tolerance to drug
61
Q

what is the primary agent for adrenergic alpha 2 receptor agonists

A

Trizanidine (zanaflex)

62
Q

what do adrenergic alpha-2 receptor agonists? Tizanidine (Zanaflex) work to do

A
  • stimulate alpha 2 receptors in the spinal interneurons causing inhibition of the interneurons causing decrease in excitatory input to the alpha motor neurons
  • decreases excitability at both the pre and post synaptic inhibition
63
Q

what are the uses of Alpha-2 Agonists

A
  • control spasticity from UMN lesions
  • generally has milder side effects and produces less weakness
  • Tizanidine better then Clonidine due to less side effects
64
Q

what are the adverse effects of alpha-2 Agonists

A
  • sedation, dizziness, dry mouth
  • less generalized weakness
65
Q

Gabapentin (Neurontin)

A
  • developed as an anti-seizure med
  • Enhances GABA effect in the SC
66
Q

Uses of Gabapentin (Neurotin)

A
  • decrease spasticity with SCI and MS
  • best used in combo with other anti- spasticity agents
  • might be helpful in reducing chronic pain
67
Q

what are the adverse effects of Gabapentin (Neurotin)

A

sedation, fatigue, dizziness, ataxia

68
Q

Dantrolene Sodium (Dantrium)

A

only direct muscle relaxant

69
Q

what does Dantrolene Sodium (Dantrium) react on

A

inhibits the release of Ca2+ working directly on the sarcoplasmic reticulum

70
Q

what are the uses in Dantrolene Sodium (Dantrium)

A

treating severe spasticity (UMN lesions)

71
Q

what are the adverse effects of Dantrolene Sodium (Dantrium)

A
  • generalized muscle weakness
  • severe hepatotoxicity and fatal hepatitis
72
Q

Botulinum toxin (Botox)

A

muscle paralytic injected locally

73
Q

what are the serotypes of botulinum toxin

A

Type A (Botox) and Type B (Myobloc)

74
Q

what are the limitations of botulinum toxin

A
  • local irritation at injection
  • have a limit of total dose
75
Q

what is the mechanism of botox

A

inhibits Ach release at the NMJ causing paralysis within 3-7 days lasting 2-3 mo.

76
Q

what are the effects of botox injection wearoff

A

a new presynaptic terminal sprouts with new source of Ach, need a new injection again

Pharmacology (10 decks)

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