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MOHD4: Exam 4 Drugs > Opioids > Flashcards

Opioids Flashcards

1
Q

Common structure of all opioids

A

Phenyl group/aromatic ring + ionized amine

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2
Q

Name 2 naturally occurring opioids

A

Morphine

Codeine

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3
Q

Which of the following is NOT a synthetic drug?
A. Levorphanol/butorphanol
B. Methadone
C. Pentazocine
D. Buprenorphine
E. Meperidine
F. Fentanyl/sufentanil/alfentanil/remifentanil

A

D. Buprenorphine is a semisythetic

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4
Q

Name the opioid receptor:
Causes a number of side effects including sedation, vomiting, respiratory depression, pruritis, euphoria, anorexia, urinary retention, physical dependence

A

Mu2

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5
Q

Name the opioid receptor:

Analgesia effects

A

Mu1 mostly

Mu2 but w/ lots of side effects

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6
Q

Name the opioid receptor:
Causes pain
Weak analgesia
Causes respiratory depression, euphoria, dysphoria, miosis, psychomimetric effect

A

Kappa

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7
Q

Name the opioid receptor:
Blocks opioid analgesia
Causes HYPERalgesia

A

ORL-1: Opioid Like Receptor

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8
Q

Where are peripheral opioid receptors synthesized?

A

dorsal root ganglion

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9
Q

Endogenous opioids are secreted by ____

A

leukocytes

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10
Q

A118G SNP of OPRM1 (human nu opioid receptor gene) is associated with:

A

higher pain score –> need more opioids

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11
Q

Name the opioid that is effective transdermally/topically and transmucosally.

A

Fentanyl (92%)

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12
Q

T/F: Oxycodone stays in circulation for a long time b/c it bypasses first pass metabolism.

A

False. 87% of oxycodone goes through 1st pass metabolism –> pulled out of circulation very fast

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13
Q

Name the opioid that has HIGH lipophilicity

A

Fentanyl

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14
Q 
Which of the following drugs does NOT use P-glycoprotein to get through BBB and bypass ABC transporters?
A. Buprenorphine
B. Morphine
C. Methadone
D. Loperamine
A

A

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15
Q

Name the 2 drugs that are metabolized by both CYP2D6 and CYP3A4

A

Tramadol

Oxycodone

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16
Q 
Which TWO of the following is NOT a good alternative for patients with renal impairment?
A. Fentanyl
B. Methadone
C. Morphine
D. Low dose oxycodone/hydrocodone
E. Oxymorphone
F. Hydromorphone
A

C, F

Both morphine and hydromorphone should be reduced in dose in renal impairment due to the glucuronide metabolites they make.

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17
Q

What drug should be AVOIDED with renal impairment?

A

Meperidine

Its metabolite, normeperdine, can cause seizures in healthy kidneys.

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18
Q

T/F: Sedation from opioids is more common with chronic use.

A

False. Common with initiation and dose escalation

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19
Q

List in order the receptors from most to least problematic in respiratory depression:
Kappa, mu, delta

A

Mu > delta > kappa

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20
Q

T/F: Pruritis presents in 100% of pts receiving IV opioids.

A

False. 100% of pts receiving intraspinal opioids.

10-50% of pts receiving receiving IV opioids

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21
Q

Pruritis is caused by ___

A

Central mu receptor activation

Maybe also by peripheral histamine release

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22
Q

Myoclonus/seizure is caused by (2) ___

A

High doses of opioids (Tramadol, morphine, hydromorphone, meperidine)
Accumulation of metabolites (M3G, H3G, normeperdine)

Improves with dose reduction

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23
Q

Opioid induced endocrine changes by (increase/decrease) in LH, FSH, Estrodiol, Testosterone.

A

Decrease

Causes osteopenia/osteoporosis in both male and female

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24
Q

Opioid induced hyperalgesia caused by all of the following EXCEPT:
A. CCK release from rostral ventromedial medulla
B. Increased inflammatory infiltrate
C. Increased expression of dynorphin
D. Enhanced release of excitatory neurotransmitters
E. Activation of NMDA receptors

A

B

25
Q

All of the following are involved in the rewarding effect of opioids EXCEPT:
A. ventral tegmental area in midbrain
B. nucleus accumbens (medium spinal neurons in ventral striatum)
C. Subthalamic nucleus
D. ventral pallidum

A

C

o Mu receptor in ventral tegmental area in midbrain consists of dopaminergic, GABAergic and glutamatergic neurons
o VTA communicates w/ nucleus accumbens (=medium spinal neurons in ventral striatum) → receive input from both dopaminergic neurons of VTA and glutamatergic neurons of hippocampus, mygdala, medial prefrontal cortex → medium spiny neurons release GABA onto ventral pallidum → drives mesolimbic system

26
Q

Name the partial mu receptor agonists (2)

A

Tramadol

Buprenophine

27
Q

Which of the following about Tramadol is TRUE?
A. Enhances re-uptake of serotonin and norephinephrine
B. Metabolized by CYP2C19 and CYP3A5
C. Does not have any drug interactions
D. It’s a prodrug
E. It’s a strong analgesic

A

D

A. Inhibit re-uptake
B. CY2D6, CYP3A4
C. Has several drug interactions
E. It is a weak analgesic like other partial mu receptor agonists.

28
Q

T/F: Partial Mu receptor agonists have high affinity for MOR and have full efficacy, making it a strong analgesic.

A

False. High affinity, partial efficacy, weak analgesic

29
Q

Name the drug:

Antagonist against KOR

A

Buprenophine

30
Q

Which of the following about Buprenophine is TRUE?
A. Its an atypical opioid
B. Low MOR affinity
C. Full agonist effect
D. Used for opioid addition
E. Not recommended for pts at risk for respiratory depression

A

D. High binding affinity makes it good for opioid addition

A. Its an agonist-antagonist: if given too much, has antagonist effect
B. High MOR affinity
C. Partial agonist effect
E. Ceiling effect on analgesia and respiratory depression makes it good to use for pts at risk for respiratory depression

31
Q 
Which of the following is NOT a agonist-antagonist?
A. Pentazocine
B. Naltrexone
C. Nalbuphine
D. Butorphanol
A

B. Naltrexone is an antagonist

32
Q

Name the drug:
Used to reverse some opioid adverse effects (pruritis w/ neuraxial opioids)
Used in labor pain b/c it spares fetal respiratory depression

A

Nalbuphine (agonist-antagonist)

33
Q 
Which of the following is TRUE about Butorphanol?
A. Low MOR affinity
B. Full MOR efficacy
C. Causes dysphoria instead of euphoria 
D. KOR antagonist
A

C. Used to reduce effect on mesolimbic dopamine reward pathway

A. High MOR affinity
B. POOR MOR efficacy
D. KOR agonist

34
Q

T/F: Antagonists are competitive at MOR and KOR w/ high affinity for KOR and have partial efficacy.

A

False. @ MOR, DOR, KOR
High affinity for MOR
No efficacy

35
Q

Used to rescue from overdose

A

Naloxone

36
Q

Which of the following is TRUE about Naloxone?
A. Good oral absorption
B. Blocks KOR in gut
C. SubQ administration
D. Short half life
E. Paired w/ Pentazocine to prevent abuse
F. It is a partial agonist.

A

D. Also very fast onset (within seconds)

A. NO oral absorption
B. Blocks MOR in gut –> may help w/ constipation?
C. IM or IV to block peripheral and central MOR
E. Paired w/ buprenorphine to prevent abuse
F. Antagonist

37
Q

T/F: Naltrexone is a antagonist that is well absorbed, has short duration of action and used for opioid addition.

A

False. Longer duration of action than Naloxone

Mixed w/ long acting opioids to deter abuse

38
Q 
Name the class of drugs:
Used for opioid induced constipation
A

Peripherally Acting Mu Receptor Antagonist (PAMORA)

39
Q

Name the Peripherally Acting Mu Receptor Antagonist (PAMORA) (3)

A

Methylnaltrexone
Naloxegol
Alvimopan (NOT FDA approved)

40
Q

Methylnaltrexone administration

A

SubQ

41
Q

Name the drug:

Used for bad constipation if not responding to other drugs

A

Naloxegol

42
Q

Naloxegol administration

A

Oral

43
Q

Triptans treat ___

A

migraines

You got it! You’re going to be ok! =)

44
Q

5HT1B receptors are found in ___

A

smooth mm of meningeal arteries

45
Q

5HT1B agonists cause ____

A

vasoconstriction in cranial nerves = desired effect

46
Q

5HT1D preceptors found on ____

A

trigeminal nerves

vascular smooth mms

47
Q

5HT1D agonists act by ____

A

subduing release of inflammatory inducing nerve stimulants

48
Q

Triptans work by blocking neurological inflammation in CNS and trigeminal nerve causing what 3 effects?

A

Vasoconstriction
Trigeminal inhibition
Decreased pain transmission

49
Q

2 of the fastest onset triptan

A

Sumatriptan Subcutaneous, intranasal: 15 min
Sumatriptan Oral: 30 min

Zolmitriptan intranasal: 10-15 min

50
Q

2 of the longest acting triptans

A

Eletriptan oral: 18 hours

Frovatriptan oral: 24 hours

51
Q

Serotonin syndrome is caused by:

A

Excess serotonin caused by:
weak re-uptake
increased intrasynaptic release by inhibiting GABA

52
Q

All of the following are symptoms of Serotonin Syndrome EXCEPT:
A. Mental status changes
B. Neuromuscular overactivity
C. Dizziness/vertigo
D. Blood pressure/heart rate fluctuations

A

C. It is an adverse effect of Triptan but not Serotonin Syndrome specifically

53
Q

Senna is used to help with _____

A

peristalsis

54
Q

T/F: Sedation tolerance will not develop unless doses are escalated quickly.

A

False. WILL develop unless

55
Q 
If sedation persists, which of the following SHOULD be done?
A. Hold 3-4 doses of opioid
B. Reduce dose by 50% 
C. Decrease frequency of administration 
D. Consider opioid rotation
A

D

A. Hold 1-2 doses of opioid
B. Reduce dose by 25%
C. Increase frequency of administration

56
Q 
All of the following are treatments for nausea/vomiting EXCEPT:
A. Promethazine
B. Prochlorperazine
C. Mu receptor antagonist
D. 5-HT3 antagonist
A

C

57
Q 
All of the following are treatments for pruritis EXCEPT:
A. Antihistamines
B. 5HT3 antagonists
C. Dopamine D2 antagonist
D. Mu receptor antagonists
A

C. Dopamine D2 agonist

58
Q

Name the 3 mu receptor antagonists used to treat pruritis

A

Nalbuphine
Naloxone
Naltrexone

MOHD4: Exam 4 Drugs (5 decks)

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