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Pharmacology - Fall > Lecture 8 - Opioids & Pain Control > Flashcards

Lecture 8 - Opioids & Pain Control Flashcards

1
Q

What is the mechanism of action for opioids?

A
  • Hyperpolarization of nerves by opening K and Ca channels in 1st and 2nd order neurons
  • Inhibition of ascending pathways in CNS
  • Excitation of descending adrenergic and serotonergic pathways
  • Decrease emotional connectivity to pain
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2
Q

Which processes of pain do opioids decrease?

A

Transmission and maybe transduction

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3
Q

What are the pharmacological effects of opioids?

A
  • Inhibition of pain and pain perception
  • Sedation and anxiolysis (before surgery)
  • Depression of respiration
  • Cough suppression
  • Decrease in intestinal motility
  • Pupillary constriction and nausea and vomiting
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4
Q

Why are opioids given as anxiolytics?

A

To decrease the amount of anesthetic needed

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5
Q

What is the main cause of death from opioid overdose?

A

Respiration depression

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6
Q

Which opioid is used to treat diarrhea?

A

Codeine

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7
Q

What is a key symptom of opioid overdose?

A

Pupil constriction

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8
Q

Can a px be on both acetaminophen and morphine?

A

Yes b/c they work via different mechanisms

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9
Q

___ dosing is less effective than IV

A

Oral

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10
Q

Why should opioids be given by the mouth?

A
  • Oral dosing has longer term effect requiring less frequent doses
  • Oral dosing avoids the “highs” and thus is less addictive
  • Oral dosing is safer in terms of overdose
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11
Q

Why should opioids be given by the clock?

A
  • Uses less drug
  • Avoids euphoria associated w/ release of pain, so less addictive potential
  • Avoids development of chronic pain syndromes
  • Do not reward px w/ opioids for having pain
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12
Q

Why should opioids be given by the ladder?

A
  • Assures safest and least potent drug is used

- Avoids addictive potential b/c opioids aren’t used until required

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13
Q

What is the weakest commonly used opioid?

A

Codeine

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14
Q

What is codeine used for?

A
  • Pain
  • Diarrhea
  • Coughing
  • Inhibit breathing
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15
Q

What is special about tramadol?

A

Has 2 complementary mechanisms

  • Activates u-opioid receptor (like other opioids)
  • Weak inhibitor of NE and serotonin reuptake
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16
Q

IV morphine is ____ as potent as oral

A

Twice as potent

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17
Q

Is morphine considered a strong opioid?

A

No

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18
Q

What is the potency of oxycodone compared to morphine?

A

Oxycodone has equal or slightly higher potency

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19
Q

A 10 mg dose of morphine is equivalent to how much oxycodone?

A

5 mg

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20
Q

What is the slow-release form of oxycodone?

A

OxyContin

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21
Q

What is percocet?

A

Oxycodone and tylenol

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22
Q

What is the danger w/ oxycodone?

A

Repression of breathing

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23
Q

Hydromorphone is ___ times more potent as morphine

A

5

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24
Q

When is hydromorphone used?

A

Surgical settings for moderate to severe pain (cancer, bone trauma, burns)

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25
Q

Fentanyl is ___ times more potent as morphine

A

80

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26
Q

What is sublingual fentanyl used for?

A

Acute but temporary pain (ex: debriding wounds)

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27
Q

What is transdermal fentanyl used for?

A

More severe pain (cancer, palliative)

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28
Q

Sufentanyl is ___ times more potent than fentanyl

A

About 10

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29
Q

What is the most common opioid given intravenously?

A

Morphine

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30
Q

What is naltrexone?

A

Oral opioid inhibitor

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31
Q

What is the function of naltrexone and what is it effective at?

A
  • Reverse psychomimetic effects of opiate agonists, reverses hypotension and CV instability
  • Effective in treating alcohol addiction, but not opioid addiction
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32
Q

What is naloxone?

A
  • Potent opioid antagonist

- Blocks all major effects of opioids including pain control

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33
Q

When is naloxone used?

A

Emergency situations (respiratory depression in clinical situation of heroin overdose)

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34
Q

Methadone is ___ times more potent than morphine

A

At least 10 (highly variable per px)

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35
Q

What is methadone used for?

A

Addiction medicine and palliative care where px has developed resistance or toxicity to other opioids

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36
Q

Why does methadone work?

A

Only a partial agonist, so a high enough dose of methadone reverses opioid effects

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37
Q

What should be considered when prescribing opioids?

A
  • Titrate dose based on response and side effects until max. analgesia and function are attained w/ tolerable side effects
  • If possible, switch short acting opioid to a long-acting opioid at equianalgesic dose b/c long-acting opioids decrease peaks and valleys of pain control
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38
Q

What should be noted when switching from one opioid to another?

A

The new opioid seems to be about 50-70% more effective than it should be b/c body is responding differently, so initial dose should be 50-70% less

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39
Q

When should opioid therapy be discontinued?

A
  • Intolerable or unacceptable side effects w/ little to no analgesia
  • High doses w/o analgesia
  • Evidence of addiction
  • No evidence of px trying to increase function in the face of reasonable analgesi
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40
Q

What is tolerance?

A

Decrease potency of analgesic effects of opioids following repeated administration

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41
Q

Is tolerance common in px w/ cancer pain?

A

No

42
Q

What type of opioids should be given to px in a great deal of pain?

A

Slow release

43
Q

What is physical dependence?

A

Normal response to chronic opioid administration

44
Q

What is addiction?

A

Psychological dependence (craving)

45
Q

What are common symptoms of opioid withdrawal?

A
  • Yawning
  • Sweating
  • Tremor
  • Fever
  • Increased heart rate
  • Insomnia
  • Muscle/abdominal cramps
  • Dilated pupils
46
Q

How can you deal w/ tolerance?

A
  • Avoid increasing dose

- Take a medication holiday following slow withdrawal to allow opioid receptors to go back up

47
Q

What is central sensitization?

A

Decreased brain sensitivity to pain

48
Q

Which NTs are pain mediators?

A

NE and serotonin

49
Q

What do tricyclic antidepressants do for pain?

A

Increase serotonin and/or NE in synapse by inhibiting reuptake

50
Q

What type of pain are TCAs used for and why?

A

Chronic pain b/c takes 1-3 weeks for pain control

51
Q

Which type of antidepressants are most effective for diabetic neuropathy?

A

TCAs

52
Q

Will TCAs given for pain have any effect on depression?

A

No b/c a low dose

53
Q

Can SSRIs be given for pain in a px already on a high dose of antidepressants for depression?

A

No

54
Q

Which 2 TCAs are given for pain?

A

Nortriptyline and amitriptyline

55
Q

Which 3 SSRIs are given for pain?

A

Paroxetine, fluoxtine, and sertraline

56
Q

What are SNRIs?

A
  • Serotonin and NE reuptake inhibitors

- Potent inhibitor of neuronal serotonin and NE reuptake and weak dopamine reuptake

57
Q

Are TCAs or SNRIs more effective for pain?

A

TCAs

58
Q

What are the 2 SNRIs used for pain and which types of pain is each used for?

A
  • Venlafaxine - neuropathic pain

- Duloxetine - diabetic neuropathy, fibromyalgia

59
Q

What do alpha 2 adrenergic agonists do to decrease pain?

A
  • Stimulates alpha-adrenoreceptors in brainstem causing activation of inhibitory neurons thus decreasing symp outflow
  • Prevent pain signal transmission
60
Q

What are the 2 alpha 2 adrenergic agonists used for pain and which types of pain is each used for?

A
  • Clonidine - neuropathic pain that is not responding to other tx (last line of tx in this class)
  • Tizanidine - tension-type headache, back pain, neuropathic pain (better tolerated than clonidine b/c less likely to cause hypotension)
61
Q

What are the medication classes that help w/ peripheral sensitization?

A
  • Carbamazepine
  • TCAs
  • Topiramate
  • Lidocaine
62
Q

What is carbamazepine?

A
  • Anticonvulsant
  • Limits influx of Na across cell membrane
  • *Inhibits firing of a nerve b/c decreases influx of sodium ions
63
Q

What is topiramate?

A
  • Anticonvulsant

- Limits influex of Na across cell membrane and antagonizes glutamate receptors

64
Q

What are common adverse reactions of topiramate?

A

Dizziness, ataxia, psychomotor slowing

65
Q

What does topical application of lidocaine do for pain?

A

Decreases discharge of small afferent nerve fibres by blocking voltage-gated Na channels

66
Q

What effect does increased Ca transport have on pain?

A

Causes spontaneous action potentials, sending a pain message to the brain

67
Q

What are some medications that decrease Ca channel activity?

A
  • Gabapentin and pregabalin

- First choice for neuropathic pain; pregabalin is 1st line therapy

68
Q

What are some medications that are NMDA antagonists?

A
  • Ketamine
  • Dextromethorphan
  • Methadone
69
Q

What does ketamine do?

A
  • Decreases central sensitization and modulation by decreasing the threshold for nerve transduction and decreases effects of substance P
  • Targets opioid receptors and Na and K channels to decrease pain
70
Q

What is a common adverse reaction w/ ketamine?

A

Local skin reaction

71
Q

Can ketamine stack w/ opioids?

A

Yes

72
Q

When is ketamine generally used?

A

Surgery

73
Q

What is dextromethoprhan?

A

Low affinity uncompetitive NMDA antagonist

74
Q

What is methadone?

A

Mu and delta opioid agonist but also blocks NMDA receptor and inhibits NE reuptake

75
Q

1 mg of methadone = __ mg of morphine

A

10

76
Q

Does methadone have active metabolites?

A

No, so less incidence of side effects

77
Q

What causes gout?

A

Accumulation of uric acid crystals in joints

78
Q

What can gout cause?

A

Gouty arthritis

79
Q

Which joint is gout most common in?

A

Joint of big toe

80
Q

What is uric acid produced from and which enzyme catalyzes this process?

A
  • Xanthine

- Xanthine oxidase

81
Q

What are some medications used to treat gout?

A
  • Colchicine
  • Allopurinol
  • Probenecid
  • NSAIDs
82
Q

What is colchicine?

A

Weak anti-inflammatory

83
Q

Colchicine should be dosed to _____

A

Toxicity

84
Q

What is allopurinol?

A

Xanthine oxidase inhibitor

85
Q

What is the drug of choice for gouty arthritis?

A

Indomethacin

86
Q

What is probenecid?

A

A uricosuric (inhibits reabsorption of uric acid)

87
Q

What is local anesthetic?

A
  • *Sodium channel blocker

- Agent that interrupts pain impulses in a specific region of the body w/o loss of px consciousnesss

88
Q

Do local anesthetics produce any side effects?

A

No b/c only used in a specific area (only need to be concerned if enters bloodstream and reaches the brain)

89
Q

What is surface anesthesia?

A

Accomplished by application of a local anesthetic to skin or mucous membranes

90
Q

What is surface anesthesia used for?

A

To relieve itching, burning, and surface pain

91
Q

What is a nerve block?

A

Local anesthetic is injected around a nerve that leads to the operative site

92
Q

A nerve block is exactly like ____

A

Lidocaine

93
Q

What is peridural anesthesia?

A

Injection of a local anesthetic into peridural space

94
Q

What is the peridural space?

A

One of the coverings of spinal cord

95
Q

What is spinal anesthesia?

A

Local anesthetic injected into subarachnoid space of spinal cord

96
Q

What are the effects of local anesthetics?

A
  • First, autonomic activity is lost
  • Then, pain and other sensory functions are lost
  • Motor activity is last to be lost
  • As local agents wear off, they do so in reverse order
97
Q

What are local anesthetics used for?

A
  • Surgical, dental, and diagnostic procedures

- Treatment of certain types of pain

98
Q

What is infiltration anesthesia used for?

A

Minor surgical and dental procedures

99
Q

What is infiltration anesthesia?

A

Injection of anesthesia intradermally, subcutaneously, or submucosally across path of nerves supplying target area

100
Q

What are nerve blocks used for?

A
  • Surgical, dental, and diagnostic procedures

- Therapeutic management of pain

101
Q

When will adverse effects result from a local anesthetic?

A
  • Inadvertent intravascular injection
  • Excessive dose or rate of injection
  • Slow metabolic breakdown
  • Injection into highly vascular tissue
102
Q

How can you determine a local anesthetic based on name?

A

All end in “aine”

Pharmacology - Fall (15 decks)

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