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Clinical pharmacology and therapeutics > The pharmacology of pain control > Flashcards

The pharmacology of pain control Flashcards

1
Q

What is pain?

A

Subjective
Complex
“What the patient says hurts”

An unpleasant sensory and emotional experience associated with actual or potential tissue damage, or described in terms of such damage”

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2
Q

Describe acute pain

A

Minutes, hours, days
Well defined onset
Associated with objective and subjective physical signs
Hyperactivity of the autonomic nervous system
Responds well to analgesia and treatment of underlying problem

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3
Q

Describe chronic pain

A

Weeks, months
Associated with significant changes in lifestyle, function and personality
More challenging management

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4
Q

State a cause of somatic nociceptive pain

A

Activation of nociceptors in skin, muscle and bone

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5
Q

State a cause of visceral nociceptive pain

A

Activation of nociceptors from stretching, distension or inflammation

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6
Q

State a cause of neuropathic pain

A

Direct damage to PNS or CNS

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7
Q

What are the symptoms of somatic nociceptive pain

A

Localized, aching, throbbing, gnawing

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8
Q

What are the symptoms of visceral nociceptive pain

A

Poorly localized, deep aching, cramping, pressure

also referred pain

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9
Q

What are the symptoms of neuropathic pain

A

Burning, shooting, stabbing, electric shock. May be associated altered sensation. Often dermatomal

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10
Q

Give examples of neuropathic pain

A

Damage to nerve plexus, post herpetic neuralgia, spinal cord compression, diabetic neuropathy

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11
Q

Give examples of visceral nociceptive pain

A

Bowel obstruction, pancreatic cancer, liver metastases

(capsular pain)

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12
Q

Give examples of somatic nociceptive pain

A

Bone metastasis, tumour invasion into soft tissue, muscle spasticity

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13
Q

Name two types of pain classified in terms of pattern

A

Background pain

Breakthrough pain

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14
Q

What is total pain?

A

The cumulative of social, psychological, physical and spiritual pain

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15
Q

Describe the ascending pain pathways

A

Nociceptors (receptors)
A-delta fibres (fast transmission of sharp localised pain)
C-fibres (slow transmission of dull burning chronic pain)
Spinal ganglia
Dorsal horn (pain signal is modified)
Lateral spinothalamic tract
Pain perception point
Somatosensory cortex and other areas of the brain

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16
Q

Where does pain processing occur in the brain?

A

Somatosensory cortex
Prefrontal cortex
Thalamus

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17
Q

What factors play a role in pain processing?

A

Mood
Beliefs
Cognition
Genetics

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18
Q

Describe the descending pain pathway

A 
Cortex
Thalamus
Periaqueductal grey matter 
Rostral ventral medulla 
Dorsal root ganglia
Spinal cord
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19
Q

What do the periaqueductal grey matter and the rostral ventral medulla contain?

A

High levels of opioid receptors

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20
Q

What does the 5HT/NA neuron control?

A

Controls/inhibits communication between the 1st and 2nd order neuron in the ascending pathway

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21
Q

Describe the WHO analgesic ladder

A

Non-opioid analgesic +/- adjuvant
Weak opioid analgesic +/- Non-opioid analgesic +/- adjuvant
Strong opioid analgesic +/- Non-opioid analgesic +/- adjuvant

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22
Q

List some non opioid analgesics

A

NSAIDs
Paracetamol
Aspirin

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23
Q

List some weak opioid analgesics

A

Tramadol
Codeine
Dihydrocodeine

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24
Q

List some strong opioid analgesics

A 
Morphine
Oxycodone 
Fentanyl 
Diamorphine 
Alfentanil 
Hydromorphone
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25
Q

List some pharmacological adjuvants

A

Corticosteroids
Antidepressants - duloxetine, amitriptyline, mirtazapine
Antiepileptics - gabapentin, pregabalin
Antimuscarinics - Mebeverine and hyoscine
Benzodiazepines
Bisphosphonates
Ketamine

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26
Q

List some non-pharmacological adjuvants

A 
TENs 
Acupuncture 
Massage
Heat 
Psychological support and relaxation 
Radiotherapy 
Interventional techniques
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27
Q

What type of receptor are opioid receptors?

A

G protein coupled

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28
Q

Name the 3 main subtypes of opioid receptor

A

Mu
Kappa
Delta

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29
Q

Where are opioid receptors located?

A 
CNS - cortex, thalamus, PAG, RVM
Enteric plexus of the gut 
Peripheral sensory afferent nerves
Dorsal root cells 
Immune cells
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30
Q

Name the endogenous opioid of mu receptors

A

Beta-endorphins

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31
Q

Describe the drug effects of mu receptor binding

A

Analgesia - spinal cord and brain

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32
Q

Name the endogenous opioid of kappa receptors

A

Dynorphins

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33
Q

Describe the drug effects of kappa receptor binding

A

Analgesia - spinal cord
Dysphoria
Miosis
Diuresis

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34
Q

Name the endogenous opioid of delta receptors

A

Enkephalins

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35
Q

Describe the drug effects of delta receptor binding

A

Analgesia - spinal cord

Respiratory depression

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36
Q

List the effects of opioids

A 
Analgesia 
Psychotropic 
Respiratory depression 
Suppression of the cough reflex 
Constipation
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37
Q

Describe the analgesic effect of opioids

A

Anti-nociception and effect on emotional response
Direct inhibition of ascending pathway from spinal cord to dorsal horn
Activation of descending pathway from midbrain to dorsal horn

38
Q

Describe the psychotropic effect of opioids

A

Anxiolysis and euphoria may also help with analgesic properties

39
Q

When is an opioid used to induce respiratory depression?

A

SOB in a patient with end stage COPD (oramorph)

40
Q

When is an opioid used for its constipative effect?

A

High output stomas (codeine)

41
Q

List the adverse effects of opioids

A 
Constipation 
Nausea and vomiting
Sedation 
Dry mouth
Pruritus
42
Q

What are the symptoms of opioid toxicity?

A 
Drowsiness 
Myoclonic jerks 
Pinpoint pupils (miosis)
Respiratory depression 
Agitation
Confusion
Vivid dreams
Hallucinations 
Tolerance 
Addiction
Physical dependence
43
Q

Describe the management of mild to moderate toxicity

A

Reduce or stop opiod
Check renal and hepatic function
Ensure adequate hydration

44
Q

Describe the management of severe opioid toxicity

A

Naloxone

45
Q

What are the signs of severe opioid toxicity

A

RR <8
Decreased O2 sats
Unresponsive

46
Q

What is tolerance?

A

Increased dose required over time to produce a given pharmacological response. Related to receptor down regulation

47
Q

What is addiction?

A

Pattern of behaviour characterised by craving of the psychic effect of the drug or the need to avoid withdrawal

48
Q

Which receptor does codeine act on?

A

Mu receptor

49
Q

Which receptor does Dihydrocodeine act on?

A

Mu receptor

50
Q

Which receptor does tramadol act on?

A

Mu receptor

Monoaminergic

51
Q

State the dose of codeine

A

15-60mg PO qds

240mg/24hrs max

52
Q

What is the biggest side effect of codeine?

A

Constipation

53
Q

State the does of dihydrocodeine

A

15-60mg PO QDS

240mg/24hrs max

54
Q

What is the biggest side effect of codeine?

A

Constipation

55
Q

State the dose of tramadol

A

50-100mg PO QDS

400m/24hrs max

56
Q

What is the biggest side effect of tramadol?

A

Nausea and vomiting

Sedations

57
Q

Who do you have to be cautious of prescribing tramadol?

A

Elderly
Seizures
MAOIs

58
Q

What is the morphine equivalent of codeine?

A

/ 10

59
Q

What is the morphine equivalent of dihydrocodeine?

A

/ 10

60
Q

What is the morphine equivalent of tramadol?

A

/5-10

61
Q

Which strong opioid is the 1st line on step 3 of WHO analgesic ladder?

A

Morphine

62
Q

Describe the mechanism of action of morphine

A

Mu and kappa receptor agonist

63
Q

Where is morphine metabolised?

A

Liver

64
Q

How is morphine excreted?

A

Urine

65
Q

List some immediate release preparations of morphine

A

Oramorph (suspension)

Sevredol (tablets)

66
Q

List some modified release preparations of morphine

A

MST (tablets and suspension)

Zomorph (capsules)

67
Q

How long does morphine IR take to peak onset?

A

15-30 mins

68
Q

How long does morphine IR take for peak effect?

A

30mins-1hr

69
Q

What is the half life of morphine IR?

A

2-4hrs

70
Q

What is the duration of action of morphine IR ?

A

4hrs

71
Q

How long does morphine IR take to reach steady state?

A

24hrs

72
Q

How long does morphine SR take to peak onset?

A

2 hrs

73
Q

How long does morphine SR take for peak effect?

A

3-4hrs

74
Q

What is the half life of morphine SR?

A

2-4hrs

75
Q

What is the duration of action of morphine SR?

A

12hrs

76
Q

How long does morphine SR take to reach steady state?

A

24hrs

77
Q

Describe oxycodone

A

Semisynthetic

Full opioid agonist

78
Q

How is oxycodone metabolised?

A

By the liver

79
Q

How is oxycodone given?

A

Orally

80
Q

What preparations does oxycodone come in?

A

Immediate release

Modified release

81
Q

Describe the mechanism of action of hydromorphone

A

Similar mechanism of action to morphine (mu and kappa agonist) though more selective for mu receptor agonism

82
Q

Name a highly potent strong opiod that comes in a patch, lozenge or intranasally

A

Fentanyl

83
Q

How long do fentanyl depto patches remain in the skin for?

A

24hrs post removal

84
Q

What are fentanyl patches not suitable for?

A

Rapidly escalating/unstable pain

85
Q

Describe the lozenge/intranasal/SL fentanyl

A

Rapid onset of action
Shorter duration of action
No relationship between most effective dose and effective background dose

86
Q

Describe Alfentanil

A 
3rd line opioid used with specialist advice 
Very potent 
Short acting (half life 30mins)
Metabolised in liver 
Injectable
87
Q

What is the opioid of choice when eGFR <30ml/min

A

Alfentanil

88
Q

In whom may alfentanil clearance be reduced?

A

Liver impairment

Older patients

89
Q

What is the breakthrough dose of opioid?

A

1/6 total daily dose

90
Q

Which patients are required to have a breakthrough dose?

A

Any being prescribed a regular opioid

91
Q

How should opioids be switched?

A

Dosing varies greatly between different opioids

Therefore care must be taken when switching between different opioids

92
Q

Describe a method that opioids are administered

A

Opioid syringe pumps

Clinical pharmacology and therapeutics (27 decks)

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