Opioids (Exam #1) Flashcards

1
Q

What is the general MOA of all opioid receptors (3)? What additional mechanism is seen with mu receptors?

A
  • Decrease cAMP via Gi proteins
  • Close presynaptic Ca channels
  • Decrease NT release

Mu also OPEN K channels = hyper polarization

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2
Q

What are the four major effects of opioids, and with which might you develop tolerance?

A
  • Analgesia = develop tolerance
  • Sedation/mental clouding
  • Euphoria vs. Dysphoria
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3
Q

Which opioid is most likely to induce N/V?

A

Morphine (injected)

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4
Q

What two opioids are utilized as cough suppressants, and which can also be used as a very mild analgesic?

A
  • Codeine (MILD analgesic also)

- Dextromethorphan

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5
Q

What AE is more common in overdose, and in what population should opioids be avoided for this reason?

A

Respiratory depression

- Avoid in asthmatics/pulm disease

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6
Q

With what opioid effect is there NO tolerance, and what drug is the exception to this? What other two effects have NO tolerance (no exceptions with these)?

A

Miosis (pupil constriction) = can always tell on PE
- Meperidine because also an anticholinergic

Also, constipation and seizures

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7
Q

What GI AE is most common with opioids? What GU AE is most common with opioids?

A
  • GI: Constipation

- GU: urinary retention

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8
Q

What two findings are commonly seen with injected Morphine?

A
  • N/V

- Histamine release (flushing, itching, sweating)

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9
Q

What two opioids should NOT be combined with MAOIs?

A
  • Meperidine

- Dextromethorphan

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10
Q

Which two opioids should NOT be combined with CYP2D6 inhibitors, and what is an example of an inhibitor? What opioid could be used as an alternative in this scenario?

A

Fluoxetine = CYP2D6 inhibitor

  • Codeine
  • Oxycodone

Can use Oxymorphone with Fluoxetine

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11
Q

What is the major CI associated with opioids, and why is this?

A

Use of a partial agonist with a full agonist

- Can induce withdrawal

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12
Q

What is the prototype opioid drug, and what receptors does it stimulate - how does this affect its effects?

A

Morphine

  • Stimulates ALL receptors
  • Produces ALL effects of opioids (good for severe pain)
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13
Q

In what population would you use Hydromoprhone (Dilaudid) over Morphine, and why?

A

Renal dysfunction

- Metabolites don’t accumulate

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14
Q

What is the primary use of Methadone (Dolophine), and why is this?

A

Long-term pain control

- Long DOA and half-life (most others are short)

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15
Q

What is the MOA of Methadone (Dolophine) (2)?

A
  • Block glutamate receptors

- Inhibit 5-HT reuptake

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16
Q

What are the two major CIs associated with Meperidine, and what AE can result if not followed?

A

Can cause seizures

  • 48+ hours of use
  • Renal failure
17
Q

What two signs/sxs are seen with Meperidine use (different from most opioids)?

A
  • Pupil dilation

- Tachycardia

18
Q

What opioid has a very high abuse potential due to its high potency?

A

Fentanyl

19
Q

What are the two “work horse” opioids, and what are they often combined with? What is their primary use?

A

Moderate/severe pain

  • Hydrocodone
  • Oxycodone

Often combined with Acetaminophen

20
Q

What can be added to Oxycodone to prevent opioid effects if injected?

A

Naloxone/Naltrexone

21
Q

What opioid is a kappa receptor agonist and mild mu receptor partial agonist? What effect may be seen?

A

Pentazocine/Naloxone

- May see dysphoria (due to kappa)

22
Q

What medication can be used to treat opioid addiction, and how does it do this?

A

Buprenorphine

- Reduces cravings

23
Q

What is the MOA of Tramadol?

A

Weak mu agonist

- Inhibits NE and 5-HT reuptake

24
Q

What AE may be seen if Tramadol is combined with antidepressants? What AE is seen with MAOIs, TCAs, SSRIs?

A
  • Antidepressants = seizures

- MAOIs/TCAs/SSRIs = Serotonin Syndrome

25
Q

What is the DOC for opioid overdose?

A

Naloxone (Narcan)

26
Q

How does Naloxone (Narcan) differ from Naltrexone?

A
  • Naloxone (Narcan) = short DOA (2 hours)

- Naltrexone = longer DOA (24 hours)

27
Q

What is the primary use of Naltrexone? What other use can it provide?

A

Used in tx of opioid addicts (especially in HC)

- Can decrease cravings in recovering alcoholics

28
Q

What medication will precipitate withdrawal in patient dependent opioids (i.e. can cause withdrawal as drug is eliminated from body)?

A

Naltrexone

29
Q

What two opioids are partial agonists? What are they often combined with, and why?

A

Combined with Naloxone to reduce abuse potential

  • Pentazocine/Naloxone
  • Buprenorphine