Opioid Analgesics Flashcards

1
Q

Three MoA of opioids

A
  1. Inhibit the transmission of nociceptive input from the periphery to the spinal cord
  2. Activate descending inhibitory pathways that modulate transmission in the spinal cord
  3. Later limbic system activity (pain perception)
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2
Q

What is each Mu receptor primarily responsible for?

A

Mu1 = analgesia

Mu2 = respiratory depression, Meiosis, reduced gastric motility, sedation, euphoria, pruritus, urinary retention, physical dependence

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3
Q

Which opioid is the most hydrophilic and which is the most lipophilic?

A

Morphine is the most hydrophilic, Fentanyl is the most lipophilic

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4
Q

Does tolerance develop equally to all opioid effects?

A

No, GI and Resp continue to be effected long after tolerance to the analgesic effect develops

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5
Q

What is the most serious AE w/opioid therapy?

A

Respiratory depression

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6
Q

Which opioid is associated with the greatest histamine release?

A

Morphine (oxycodone and fentanyl cause fewer)

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7
Q

What is the treatment for opioid toxicity?

A

Naloxone- pure opioid antagonist

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8
Q

Full agonists

A

Effectiveness is not limited by dose increases…pure agonist: do not antagonize the effects of other full agonists

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9
Q

Partial agonists

A

Medications have a ceiling analgesic effect whereas the pure agonists do not…meaning greater doses won’t increase analgesic effectiveness, only greater SEs

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10
Q

Partial/mixed agonist

A

Agonist for some receptors and antagonist for others

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11
Q

Antagonist

A

No analgesic effect, used to block the effect of opioids

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12
Q

Anti-tussive opioids work by inhibition of the coughing center in the medulla, but don’t cure the irritation, what are the three opioids used for this?

A

Codeine (MC)
Hydrocodone
Dextromethorphan

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13
Q

Phenanthrene opioids to remember

A
Morphine
Hydromorphone (Dilaudid)
Hydrocodone ER 
Hydrocodone/APAP (Vicodin, Lortab)
Levorphanol
Oxycodone (OxyContin)
Oxycodone/APAP (Percocet)
Oxymorphone (Opana)
Codeine
Codeine/APAP (Tylenol #3)
Mixed agonist/antagonist
   - Buprenorphine
   - Butorphanol
   - Nalbuphine
Heroin
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14
Q

Strong agonist, slow and erratic oral absorption, enters all body tissues, least lipophilic, crosses placenta…used for pain

A

Morphine

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15
Q

Two opioids that are metabolized to morphine

A

Heroin and codeine (so morphine in urine could mean exposure to morphine, heroin, or codeine)

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16
Q

AEs for this opioid: Increase in ICP, so significant caution in severe head injury…N/V, itching, hypotension

A

Morphine

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17
Q

Metabolite of morphine with better oral absorption, more fat soluble than morphine for moderate to severe pain…ER form is a Risk Evaluation and Mitigation Strategy (REMS) drug that requires provider training every 2 years

A

Hydromorphone (dilaudid)

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18
Q

Opioid that’s a moderate agonist, metabolized to hydromorphone for moderate to severe pain…there are two combination forms

A

Hydrocodone ER

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19
Q

Opioid metabolized to noroxycodone and oxymorphone (active metabolites)…several formulations: CR, IR (contact w/water turns it gummy for abuse protection), and Percocet/combined tabs

A

Oxycodone

20
Q

Synthetic Mu agonist w/greater analgesic profile than morphine for moderate/severe pain. The ER brand has an abuse-deterrent and the IR brand does not

A

Oxymorphone (Opana)

21
Q

Prodrug with no analgesic activity that gets metabolized to morphine, usually used as an antitussive unless combined w/another drug

A

Codeine

22
Q

BB warning: death related to ultra-rapid metabolism of this drug to morphine especially in the young

A

Codeine

23
Q

Codeine on its own
Codeine w/APAP
Codeine w/Guaifenesin

What class is each?

A

C-II
C-III
C-V

24
Q

AEs: This group of opioids precipitate opioid withdrawal in opioid-dependent patients, they have a ceiling effect on respiratory depression and analgesia, and a lower abuse potential

A

Mixed agonist/antagonists

25
Q

This mixed agonist/antagonist is a partial Mu receptor agonist and kappa receptor antagonist that’s used for opioid detoxification (as effective as methadone)

A

Buprenorphine (resistant to naloxone reversal due to long duration of action, limited access to physicians, caution in pregnancy)

26
Q

This opioid is a partial mu and kappa receptor agonist used for pain especially during labor if epidural is not possible

A

Butorphanol

27
Q

This non-controlled mixed agonist/antagonist is a partial mu antagonist and strong kappa agonist used for sedation w/ minimal respiratory depression and to reverse ventilator depression in opioid overdose while maintaining some analgesia

A

Nalbuphine (may be resistant to naloxone reversal)

28
Q

Phenylpiperidines to know

A

Meperidine (Demerol)
Fentanyl
Fentanyl derivatives (alfentanil, sufentanil, remifentanil)

29
Q

Mu and delta strong agonist with anticholinergic effects used to treat SHIVERING AND RIGORS, but shouldn’t be a first choice for pain

A

Meperidine (Demerol) - extensive hepatic metabolism, turns to normeperidine which is really cleared and have negative inotropic actions on the heart

30
Q

Meperidine (Demerol) is CI specifically in pts taking these types of meds (as are pretty much all opioids)

A

MAOIs

31
Q

Meperidine should be avoided in renal insufficiency and causes some strange AEs including?

A

Tachycardia, mydriasis, more frequent and profound hypotension than morphine, delirium and seizures, severe withdrawal syndrome

32
Q

Very potent synthetic opioid, lipophilic, rapid onset, short duration of action, available in transdermal product for chronic pain, IV, and Buccal for breakthrough pain and in the field/combat

A

Fentanyl

33
Q

Three fentanyl derivatives

A

Alfentanil (rapid onset, shorter doa)
Sufentanil (slower onset than fentanyl, same doa)
Remifentanil (rapid onset, shortest doa)

34
Q

Antagonist at NMDA receptor, inhibits serotonin/NE used for Chronic pain syndrome and detox of opioid addiction

A

Methadone (arrhythmias prolong QT interval)

35
Q

Partial mu agonist, full kappa agonist used, when IV only, for labor pain when epidural is not possible

A

Pentazocine

36
Q

Adjunct therapy to treat diarrhea symptoms ONLY

A

Diphenoxylate with atropine (lomotil)

37
Q

Serotonin and NE reputable inhibitor for moderate/severe pain associated with increased risk of serotonin syndrome and seizures

A

Tramadol (ultra-rapid metabolizers could lead to significant respiratory depression)

38
Q

ONLY OPIOID WITH INDICATION FOR DIABETIC PERIPHERAL NEUROPATHY

A

Tapentadol

39
Q

Opioid antagonist with no systemic effect when given orally

A

Naloxone

40
Q

Opioid antagonist used in opioid and alcohol addiction, 100% absorbed and active orally

A

Naltrexone (competes but does not displace opioids) - precipitates withdrawal

41
Q

Opioid antagonist that competes and displaces opioids, shorter duration of action

A

Naloxone (Narcan)

42
Q

How often can naloxone be given?

A

Every 2 to 5 minutes

43
Q

When tapering opioids, the goal is to taper by how much per week?

A

20-50%

44
Q

Dose at which two opioid agents are expected to produce similar analgesic effects

A

Equianalgesic opioid dosing

45
Q

Greater than expected potency in a new opioid, even in the same class of analgesic…risk is respiratory depression

A

Incomplete cross tolerance