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?

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
What is the DOC for opioid overdose?
Naloxone (Narcan)
26
How does Naloxone (Narcan) differ from Naltrexone?
- Naloxone (Narcan) = short DOA (2 hours) | - Naltrexone = longer DOA (24 hours)
27
What is the primary use of Naltrexone? What other use can it provide?
Used in tx of opioid addicts (especially in HC) | - Can decrease cravings in recovering alcoholics
28
What medication will precipitate withdrawal in patient dependent opioids (i.e. can cause withdrawal as drug is eliminated from body)?
Naltrexone
29
What two opioids are partial agonists? What are they often combined with, and why?
Combined with Naloxone to reduce abuse potential - Pentazocine/Naloxone - Buprenorphine