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NMSP Exam 3 > Opioids > Flashcards

Opioids Flashcards

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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
What happens when opioids and alcohol or other CNS depressants are mixed?
- Intensify the opioid-induced sedation and respiratory depression
26
What is a class of drugs that needs to be avoided in people taking opioids?
- Anticholinergic because these drugs can exacerbate opioid induced constipation and urinary retention
27
What is the triad of symptoms of an opioid overdose?
- Coma - Respiratory depression - Pinpoint pupils
28
How does fentanyl compare to morphine?
- 100x more potent - Same adverse effects - CYP3A4 substrate
29
What are some notable formulations of fentanyl?
- IM - IV - Transderm - Transmucosal - Nasal spray - Lozenge on stick - Buccal tabs
30
How do the potencies of alfentanil, remifentanil, and sufentanil compare to morphine?
- Alfentanil: 10x - Remifentanil: 100x - Sufentanil: 1000x
31
What are alfentanil, remifentanil, and sufentanil used for?
- Induction of anesthesia - Maintenance of anesthesia in combo with other drugs - Sole anesthetic agents
32
What is meperidine?
- Shares major properties of morphine | - Was considered first line drug for moderate to severe pain but use has declined
33
Why is meperidine not used now?
- 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
How was it abused by healthcare workers?
- Lacks anticholinergic effects so there is no pinpoint pupils in patients
35
What is methadone?
- Shares major properties of morphine - Has long duration of action - Used to treat pain increased 7x from 1997-2004
36
Who is best to use/administer methadone? Why?
- Professionals - Prolongs QT interval --> torsades de pointes - Need to be careful if given with other drugs that prolong the QT interval
37
What is heroin?
- Has higher lipid solubility than morphine, giving a greater high when injected by facilitating access of morphine to brain
38
What is the use of hydromorphone?
- Moderate to severe pain
39
What are the adverse effects of hydromorphone?
- Similar to morphine | - Reversed by naloxone
40
What is special about hydromorphone?
- Water soluble so it can be diluted in a smaller volume for ingection
41
What is codeine?
- Prototype for moderate to strong opioid agonists
42
How is codeine usually given?
- PO
43
What is special about the metabolism of codeine?
- Metabolized to morphine by CYP2D6 which is required for analgesia - If a person lacks this gene, codeine is ineffective
44
How is codeine formulated?
- Alone and with nonopioid analgesics
45
What is an effective use of codeine?
- Cough suppressant
46
What is oxycodone?
- Moderate to strong opioid agonist similar to codeine
47
How is oxycodone metabolized?
- By CYP3A4 making it susceptible to induces or inhibitors
48
What was one way that people abused oxycodone? How is this prevented now?
- Used to crush and snort | - Prevented now by the powder turning into gel when mixed with water or alcohol
49
What are some adverse effects of oxycodone?
- Drowsiness - Dizziness - Pruritus - Constipation - Nausea - Vomiting
50
What is hydrocodone?
- Moderate to strong opioid agonist similar to codeine
51
What is the most prescribed form of hydrocodone?
- Acet + hydro
52
What is pentazocine?
- Prototype for the agonist-antagonist opioids used to treat mild to moderate pain (not used in US anymore)
53
How does pentazocine and butorphanol affect the perception of pain?
- Causes inhibition of ascending pain pathways, altering the perception of and response to pain
54
What effects do pentazocine and butorphanol cause?
- Analgesia - Sedation - Respiratory depression
55
Why is the abuse potential low with pentazocine?
- Due to unpleasant reactions (anxiety, strange thoughts, nightmares)
56
What does pentazocine and butorphanol do in someone physically dependent on mu agonists?
- Precipitates withdrawal
57
How is pentazocine and butorphanol toxicity reversed?
- Higher levels of naloxone
58
What is butorphanol?
- Prototype for the agonist-antagonist opioids used to treat mild to moderate pain
59
What is the nasal spray formulation of butorphanol used for?
- Migraines
60
What situation is butorphanol contraindicated in? Why?
- MI | - Increases cardiac work
61
What is buprenorphine?
- A kappa opioid receptor antagonist and partial agonist at mu receptors
62
What is buprenorphine primarily used for?
- Treat addicts (suboxone) | - Treat acute mild to moderate pain, not recommended for long term use
63
What effects does buprenorphine cause?
- Analgesia - Sedation - Respiratory depression (less than full mu agonists)
64
Does naloxone work against buprenorphine?
- No because it binds very tightly
65
What adverse effects can buprenorphine cause?
- Prolongs QT interval | - Spasm of sphincter of Oddi which poses risk for patients with pancreatitis or biliary disease
66
What is naloxone?
- Pure opioid antagonist
67
What is naloxone used for?
- Can reverse most effects of opioid agonists including respiratory depression, coma, and anlagesia
68
What happens when naloxone is administered in the absence of opioids?
- No significant effects
69
What happens in people are physically dependent on opioids?
- Precipitates immediate withdrawal reaction
70
What are some opioid withdrawal symptoms?
- 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
What is naltrexone?
- Pure opioid antagonist used for alcohol and opioid abuse | - Prevents euphoria from opioids but does not prevent craving
72
How does naltrexone work in alcoholics?
- Reduces the "high" alcoholics get when consuming alcohol
73
When can't naltrexone be used?
- When a patient is taking opioids for pain
74
What is methylnaltrexone?
- Mu-opioid antagonist that cannot readily cross blood-brain barrier
75
What is methylnaltrexone indicated for?
- For opioid-induced constipation in patients with end stage disease taking opioids continuously for pain
76
What is loperamide?
- Mu-opioid agonist that cannot readily cross blood brain barrier
77
What is loperamide indicated for?
- Acute and chronic diarrhea
78
What is pain?
- Subjective experience so you have to go based off the patient's description
79
What could lead to addictive behavior for opioids?
- High doses to treat pain for > 20 days
80
What are some indications for opioids?
- Postoperative pain - Obstetric analgesia - Myocardial infarction - Dyspnea
81
Why are opioids not used in head injuries?
- They cause ICP which will worsen head injury

NMSP Exam 3 (18 decks)

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