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NMSP Exam 3 > Opioids > Flashcards

Opioids Flashcards

1
Q

What is the metabolism of fentanyl, oxycodone, buprenorphine, and tramadol?

A
  • CYP3A4
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2
Q

What is the metabolism of codeine and hydrocodone?

A
  • CYP2D6
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3
Q

What is the metabolism of morphine, hydromorphone, and oxymorphone?

A
  • Glucuronidation
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4
Q

What are the three major classes of opioid receptors?

A
  • Mu
  • Kappa
  • Delta
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5
Q

How does morphine and other pure opioid agonists relieve pain?

A
  • Mimicking the action of endogenous opioid peptides, primarily at mu receptors but partly at kappa receptors
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6
Q

What can complement pain relief with opioid use?

A
  • Opioid-induced sedation and euphoria
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7
Q

What is the most serious adverse effect of opioids?

A
  • Respiratory depression
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8
Q

What are some other important adverse effects of opioids?

A
  • Constipation
  • Urinary retention
  • Orthostatic hypotension
  • Emesis
  • Birth defects
  • Elevation of intracranial pressure
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9
Q

What are the important responses to activation of Mu receptors?

A
  • Analgesia
  • Respiratory depression
  • Sedation
  • Euphoria
  • Physical dependence
  • Decreased GI motility
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10
Q

What are important responses to activation of Kappa receptors?

A
  • Analgesia
  • Sedation
  • Decreased GI motility
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11
Q

What are the actions at Mu and Kappa receptors of morphine, codeine, hydrocodone, meperidine, and other morphine-like drugs?

A
  • Mu: agonist

- Kappa: agonist

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12
Q

What are the actions at Mu and Kappa receptors of pentazocine?

A
  • Mu: Antagonist

- Kappa: Agonist

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13
Q

What are the actions at Mu and Kappa receptors of butorphanol?

A
  • Mu: partial agonist

- Kappa: agonist

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14
Q

What are the actions at Mu and Kappa receptors of buprenorphine?

A
  • Mu: Partial agonist

- Kappa: antagonist

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15
Q

What are the actions at Mu and Kappa receptors of naloxone, naltrexone, and others?

A
  • Mu: antagonist

- Kappa: antagonists

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16
Q

What are some examples of pure opioid agonists?

A
  • Morphine
  • Codeine
  • Hydrocodone
  • Meperidine
  • And other morphine-like drugs
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17
Q

What are some examples of agonist-antagonist opioids?

A
  • Pentazocine
  • Butorphanol
  • Buprenorphine
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18
Q

What are some examples of pure opioid antagonists?

A
  • Naloxone

- Naltrexone

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19
Q

What does sudden opioid withdrawal cause?

A
  • Abstinence syndrome that is unpleasant but not dangerous
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20
Q

How should opioids be withdrawn?

A
  • Gradually to minimize symptoms of abstinence
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21
Q

What occurs with prolonged use of opioids?

A
  • Tolerance develops to analgesia, euphoria, sedation, and respiratory distress
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22
Q

Which effect of opioids does tolerance not affect?

A
  • Constipation and miosis
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23
Q

Where are larger doses of opioids generally given?

A
  • Parentally
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24
Q

What are some precautions of opioid use?

A
  • Pregnancy
  • Labor and delivery
  • Head injury
  • Decreased respiratory reserve
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25
Q

What happens when opioids and alcohol or other CNS depressants are mixed?

A
  • Intensify the opioid-induced sedation and respiratory depression
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26
Q

What is a class of drugs that needs to be avoided in people taking opioids?

A
  • Anticholinergic because these drugs can exacerbate opioid induced constipation and urinary retention
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27
Q

What is the triad of symptoms of an opioid overdose?

A
  • Coma
  • Respiratory depression
  • Pinpoint pupils
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28
Q

How does fentanyl compare to morphine?

A
  • 100x more potent
  • Same adverse effects
  • CYP3A4 substrate
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29
Q

What are some notable formulations of fentanyl?

A
  • IM
  • IV
  • Transderm
  • Transmucosal
  • Nasal spray
  • Lozenge on stick
  • Buccal tabs
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30
Q

How do the potencies of alfentanil, remifentanil, and sufentanil compare to morphine?

A
  • Alfentanil: 10x
  • Remifentanil: 100x
  • Sufentanil: 1000x
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31
Q

What are alfentanil, remifentanil, and sufentanil used for?

A
  • Induction of anesthesia
  • Maintenance of anesthesia in combo with other drugs
  • Sole anesthetic agents
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32
Q

What is meperidine?

A
  • Shares major properties of morphine

- Was considered first line drug for moderate to severe pain but use has declined

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33
Q

Why is meperidine not used now?

A
  • Short half life
  • Adverse interactions with other drugs since it interacts with MAO inhibitors leading to coma or death
  • Continuous use leads to build up of a toxic metabolite
34
Q

How was it abused by healthcare workers?

A
  • Lacks anticholinergic effects so there is no pinpoint pupils in patients
35
Q

What is methadone?

A
  • Shares major properties of morphine
  • Has long duration of action
  • Used to treat pain increased 7x from 1997-2004
36
Q

Who is best to use/administer methadone? Why?

A
  • Professionals
  • Prolongs QT interval –> torsades de pointes
  • Need to be careful if given with other drugs that prolong the QT interval
37
Q

What is heroin?

A
  • Has higher lipid solubility than morphine, giving a greater high when injected by facilitating access of morphine to brain
38
Q

What is the use of hydromorphone?

A
  • Moderate to severe pain
39
Q

What are the adverse effects of hydromorphone?

A
  • Similar to morphine

- Reversed by naloxone

40
Q

What is special about hydromorphone?

A
  • Water soluble so it can be diluted in a smaller volume for ingection
41
Q

What is codeine?

A
  • Prototype for moderate to strong opioid agonists
42
Q

How is codeine usually given?

A
  • PO
43
Q

What is special about the metabolism of codeine?

A
  • Metabolized to morphine by CYP2D6 which is required for analgesia
  • If a person lacks this gene, codeine is ineffective
44
Q

How is codeine formulated?

A
  • Alone and with nonopioid analgesics
45
Q

What is an effective use of codeine?

A
  • Cough suppressant
46
Q

What is oxycodone?

A
  • Moderate to strong opioid agonist similar to codeine
47
Q

How is oxycodone metabolized?

A
  • By CYP3A4 making it susceptible to induces or inhibitors
48
Q

What was one way that people abused oxycodone? How is this prevented now?

A
  • Used to crush and snort

- Prevented now by the powder turning into gel when mixed with water or alcohol

49
Q

What are some adverse effects of oxycodone?

A
  • Drowsiness
  • Dizziness
  • Pruritus
  • Constipation
  • Nausea
  • Vomiting
50
Q

What is hydrocodone?

A
  • Moderate to strong opioid agonist similar to codeine
51
Q

What is the most prescribed form of hydrocodone?

A
  • Acet + hydro
52
Q

What is pentazocine?

A
  • Prototype for the agonist-antagonist opioids used to treat mild to moderate pain (not used in US anymore)
53
Q

How does pentazocine and butorphanol affect the perception of pain?

A
  • Causes inhibition of ascending pain pathways, altering the perception of and response to pain
54
Q

What effects do pentazocine and butorphanol cause?

A
  • Analgesia
  • Sedation
  • Respiratory depression
55
Q

Why is the abuse potential low with pentazocine?

A
  • Due to unpleasant reactions (anxiety, strange thoughts, nightmares)
56
Q

What does pentazocine and butorphanol do in someone physically dependent on mu agonists?

A
  • Precipitates withdrawal
57
Q

How is pentazocine and butorphanol toxicity reversed?

A
  • Higher levels of naloxone
58
Q

What is butorphanol?

A
  • Prototype for the agonist-antagonist opioids used to treat mild to moderate pain
59
Q

What is the nasal spray formulation of butorphanol used for?

A
  • Migraines
60
Q

What situation is butorphanol contraindicated in? Why?

A
  • MI

- Increases cardiac work

61
Q

What is buprenorphine?

A
  • A kappa opioid receptor antagonist and partial agonist at mu receptors
62
Q

What is buprenorphine primarily used for?

A
  • Treat addicts (suboxone)

- Treat acute mild to moderate pain, not recommended for long term use

63
Q

What effects does buprenorphine cause?

A
  • Analgesia
  • Sedation
  • Respiratory depression (less than full mu agonists)
64
Q

Does naloxone work against buprenorphine?

A
  • No because it binds very tightly
65
Q

What adverse effects can buprenorphine cause?

A
  • Prolongs QT interval

- Spasm of sphincter of Oddi which poses risk for patients with pancreatitis or biliary disease

66
Q

What is naloxone?

A
  • Pure opioid antagonist
67
Q

What is naloxone used for?

A
  • Can reverse most effects of opioid agonists including respiratory depression, coma, and anlagesia
68
Q

What happens when naloxone is administered in the absence of opioids?

A
  • No significant effects
69
Q

What happens in people are physically dependent on opioids?

A
  • Precipitates immediate withdrawal reaction
70
Q

What are some opioid withdrawal symptoms?

A
  • Pain in muscles/joints
  • Fast HR
  • Restlessness or sweating
  • General discomfort or anxiety
  • Dilated pupils, watery eyes
  • Diarrhea, vomiting, or nausea
  • Excessive yawning
  • Goose bumps
  • Insomnia
  • Tremor
71
Q

What is naltrexone?

A
  • Pure opioid antagonist used for alcohol and opioid abuse

- Prevents euphoria from opioids but does not prevent craving

72
Q

How does naltrexone work in alcoholics?

A
  • Reduces the “high” alcoholics get when consuming alcohol
73
Q

When can’t naltrexone be used?

A
  • When a patient is taking opioids for pain
74
Q

What is methylnaltrexone?

A
  • Mu-opioid antagonist that cannot readily cross blood-brain barrier
75
Q

What is methylnaltrexone indicated for?

A
  • For opioid-induced constipation in patients with end stage disease taking opioids continuously for pain
76
Q

What is loperamide?

A
  • Mu-opioid agonist that cannot readily cross blood brain barrier
77
Q

What is loperamide indicated for?

A
  • Acute and chronic diarrhea
78
Q

What is pain?

A
  • Subjective experience so you have to go based off the patient’s description
79
Q

What could lead to addictive behavior for opioids?

A
  • High doses to treat pain for > 20 days
80
Q

What are some indications for opioids?

A
  • Postoperative pain
  • Obstetric analgesia
  • Myocardial infarction
  • Dyspnea
81
Q

Why are opioids not used in head injuries?

A
  • They cause ICP which will worsen head injury

NMSP Exam 3 (18 decks)

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