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Pharmacology Exam 5 > Opioids > Flashcards

Opioids Flashcards

1
Q

MOA for opioid analgesia

A
  1. Inhibition of pain signaling

2. Reduce CNS response to pain signal (pro-analgesic)

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2
Q

One of the natural active constituents of opium, prototype

A

Morphine

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3
Q

IM, SC, IV, oral

Readily absorbed, effect in 5-15 minutes, 4-5 hr duration

A

Morphine (12 H DOA with sustained release)

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4
Q

Morphine: main metabolic pathway, active metabolites?

A

Glucuronidation (liver), morphine-6-B-glucuronide (long half-life) and morphine-3-B-glucuronide (seizures)

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5
Q

Are there dosing considerations for morphine with impaired liver or kidney function?

A

Yes

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6
Q

3 therapeutic effects of morphine:

A

Analgesia, sedation, euphoria

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7
Q

T/F: Sedation arising from morphine will lessen with use (tolerance).

A

True

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8
Q

MOA morphine analgesia (2)

A

Acts at peripheral and spinal levels to block pain transmission and acts at higher brain levels to block response to pain

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9
Q

5 major side effects of morphine

A

Respiratory depression, nausea/vomiting, constipation, pupillary constriction, itching

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10
Q

MOA of respiratory depression associated with morphine

A

Decreased sensitivity of chemoreceptor centers to plasma CO2 levels (hypoxic response still present)

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11
Q

T/F: Tolerance does NOT develop against respiratory depression.

A

False (tolerance develops)

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12
Q

CVD side effects of morphine

A

Mild, orthostatic hypotension due to histamine release (that also causes the itching)

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13
Q

Immune system side effects of morphine

A

Inhibition, minor unless someone is already immune compromised

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14
Q

Hormonal side effects of morphine

A

Altered effects, usually minor

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15
Q

Biliary & urinary tract side effects of morphine

A

Increased pressure, may worsen biliary colic and urinary tract obstruction

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16
Q

6 contraindications/limitations of morphine

A
  1. Patients with decreased respiratory reserve (asthma, emphysema, cor pulmonale)
  2. Head injuries
  3. CNS tumors
  4. Pregnancy
  5. Neonates & elderly (much more sensitive)
  6. Potential for dependence and misuse
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17
Q

DDIs for all opioid analgesics

A

Other CNS depressants (sedatives, ethanol, antidepressants, etc.)

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18
Q

Given orally, onset in 30-60 minutes, DOA 4-6 hours

A

Codeine

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19
Q

Potency of codeine (fraction)

A

1/10 (used for milder pain)

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20
Q

Metabolism of codeine (reaction, enzyme, product)

A

Demethylated by CYP2D6 to morphine

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21
Q

Clinical uses of codeine (3ish)

A
  1. Mild-moderate pain 2. With aspirin or APAP (additive effects)
  2. Cough suppression (lower doses)
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22
Q

Codeine vs. morphine: important differences (2)

A

More likely to cause constipation and less likely to cause addiction

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23
Q

Oral, IV, IM, transdermal, intranasal, sublingual

Onset times differ depending on route, but generally rapid onset and short DOA (ex: few minute onset for oral)

A

Fentanyl

24
Q

Clinical uses of fentanyl (what type of pain?)

A

Chronic and breakthrough pain

25
Q

Fentanyl vs. morphine: differences

A

Fentanyl does not promote histamine release (itching), affects the cardiovascular system less than morphine, more likely to produce truncal rigidity, VERY HIGH addiction potential (rapid onset, short duration)

26
Q

More potent and lipid soluble than morphine, allowing for rapid CNS entry

A

Heroin

27
Q

Synthetic opioid with very effective oral administration, but also given IV at low doses

A

Methadone

28
Q

Metabolism enzymes and duration of methadone

A

CYP3A4 and CYP2B6, slowly

29
Q

Onset ~15-30 minutes, half-life 15 H when acute, but 22 H when chronic
Longer DOA than morphine when used chronically

A

Methadone

30
Q

ADEs: serious cardiovascular events, like QT prolongation and torsades de pointes
Parenterally, causes euphoria and dependence, but NOT orally

A

Methadone (CV events when dose is too high)

31
Q

Effects of partial agonists/mixed agonists compared to full

A

Less analgesic action, but less respiratory depression

32
Q

T/F: Partial agonists act as antagonists when in the presence of full agonists.

A

True, can precipitate withdrawal

33
Q

What are mixed agonists-antagonists?

A

Drugs that are primarily agonists are ONE RECEPTOR subtype, but primarily antagonists at ANOTHER RECEPTOR subtype

34
Q

Kappa agonist, mu antagonist

A

Nalbuphine (kappa analgesia with ceiling on mu respiratory depression)

35
Q

Not given orally, similar potency as morphine, CIII

Onset 15 minutes, DOA 4-6 hours

A

Nalbuphine

36
Q

Partial agonist at mu receptors, antagonist at kappa receptors

A

Buprenorphine (mu analgesia & respiratory depression ceiling without kappa side effects)

37
Q

Not given orally, 30X more potent than morphine, CIII

A

Buprenorphine

38
Q

Major use for buprenorphine= opioid dependence and cocaine abuse, much like methadone. How does its use differ from methadone?

A

Its partial mu agonist (antagonist!) properties precipitates withdrawal in addicts using morphine, heroin, or other full agonists

39
Q

ADEs: QT prolongation and torsades de pointes

Available IV, IM, buccal film, or subdermal implant

A

Buprenorphine

40
Q

Anti-diarrheal agent that uses opioids unwanted constipating effects for therapy!

A

Loperamide (Imodium)

41
Q

Can be taken orally, as action is limited to GI tract

Onset 2-4 hours, DOA 10-15 hr

A

Loperamide

42
Q

Diphenoxylate difference from loperamide

A

CV, limited abuse potential (loperamide available OTC, no CNS actions, no abuse)

43
Q

Antitussive effects, like codeine

NOT analgesic, but can still be abused

A

Dextromethorphan (Robitussin)

44
Q

Dextromethorphan MOA (suspected)

A

CNS NMDA receptor antagonist for antitussive effect

45
Q

Opioid antagonist for treating opioid-induced constipation

A

Methylnaltrexone

46
Q

MOA of methylnaltrexone

Administration

A

Blocks GI opioid receptors that mediate constipation, SC injection daily

47
Q

T/F: Methylnaltrexone crosses the blood-brain barrier, but does not significantly contribute to CNS effects.

A

False, does not cross the BBB

48
Q

Naloxone MOA

A

Competitive antagonist at opioid receptors

49
Q

T/F: naloxone works with the same efficacy for full and partial agonists.

A

False, works better with full agonists (partial agonists are highly potent and slowly dissociate from receptors)

50
Q

Opioid antagonist:
Poor oral absorption, IV
Rapid onset 2-5 minutes, DOA 30 minutes- 2 hours

A

Naloxone (Narcan)

51
Q

Used to counteract effects of opioids, particularly in life-threatening events of respiratory depression 1. After surgery 2. After overdose

A

Naloxone (Narcan)

52
Q

T/F: Naloxone is NOT effective in treating respiratory depression due to non-opioid CNS depressants, like benzodiazepines.

A

True

53
Q

Opioid antagonist:
Very effective orally
Long DOA ~ 24 H

A

Naltrexone

54
Q

Used for treating opioid dependence…PREVENTING effects of opioids, so requires a strong patient commitment

A

Naltrexone

55
Q

Added to opioid products to prevent abuse. When taken orally, no effect. When taken parenterally, blocks opioid receptor (precipitates withdrawal and/or prevents opioid effect)

A

Naloxone

Pharmacology Exam 5 (8 decks)

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