Opioids - Dr. C Flashcards

1
Q

True or false: sigma receptor is an opioid receptor.

A

False! Only mu, kappa, and delta are opioid receptors.

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2
Q
Which of the following is NOT an opioid receptor?
A. Mu
B. Kappa
C. Sigma
D. Delta
A

C. Sigma

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3
Q

True or false: morphine produces analgesia without anesthesia.

A

True

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4
Q

Which of the following is morphine more effective against?
A. Dull, throbbing pain
B. Sharp, cutaneous pain

A

A. Dull, throbbing pain

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5
Q

Which of the following is morphine less effective against?
A. Dull, throbbing pain
B. Sharp, cutaneous pain

A

B. Sharp, cutaneous pain

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6
Q

True or False: opioids have anti-inflammatory effects.

A

False! NSAIDs do, but opioids don’t because the pain relief is primarily via reduced perception of the pain at the brain and spinal cord level.

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7
Q

________ is chronic pain condition characterized by instances of increased pain with no apparent change in opiate concentrations.

A

“Breakthrough” pain

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8
Q

The sedation and stupor effects of morphine come from its interaction with which receptor?

A

Mu

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9
Q

Respiratory depression is caused by _______ receptor activation.

A

Mu

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10
Q
When it comes to respiratory depression with morphine, all of the following are true EXCEPT:
A. Decreased minute volume
B. Decreased tidal exchange
C. Increased respiratory rate
D. Diminished response to increased pCO2
A

C. Increased respiratory rate

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11
Q

What are the 3 opioid receptors?

A

Mu, kappa, delta

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12
Q

Respiratory depression comes as a result of actions on Mu opiate receptors in _______ respiratory centers,

A

Medullary

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13
Q

What is the most common cause of death in relation to opiate overdose?

A

Respiratory depression

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14
Q

What fraction of patients receiving opiates will experience nausea and emesis (vomiting)?

A

About 1/3

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15
Q

True or false: opioids have an antitussive effect.

A

True

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16
Q

This is a side effect of opiates that causes pupillary constriction.

A

Miosis (aka pinpoint pupils)

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17
Q

_____ are 3 classes of endogenous opiates that your body releases, like when you experience a runner’s high and what not.

A

Endorphins, enkephalins, dynorphins

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18
Q

Most opium was and still is produced in _____.

A

Afghanistan

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19
Q

True or false: the 3 opiate receptors have similar amino acid sequences.

A

True

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20
Q

True or false: Endogenous opiates are cleaved from the same peptide.

A

True

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21
Q

What are the 5 classes of opiates?

A
Phenanthrene class
Levorphanol class
Meperidine class
Fentanyl class
Methadone class
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22
Q

Morphine falls under which opiate class?

A

Phenanthrene class

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23
Q

Which opiates fall under the phenanthrene class of opiates?

A

Morphine, dihydromorphone, and codeine

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24
Q

Which meds fall under the levorphanol class of opiates?

A

Levorphanol and dextromethorphan

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25
Q

Which drugs fall under the meperidine class of opiates?

A

Meperidine and mCPP

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26
Q

Which drugs fall under the fentanyl class of opiates?

A

Fentanyl, alfentanyl, and sufentanyl

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27
Q

Which meds fall under the methadone class of opiates?

A

Methadone, LAAM, and propoxyphene

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28
Q

What is the prototype and the gold standard of opiate agonist agents?

A

Morphine

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29
Q

True or false: opiate agonist agents can be direct-acting agents, Reuptake blockers, synthesis inhibitors, or neuron activators.

A

FALSE! They are all direct-acting agonists!!!*

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30
Q

Can someone grow tolerance to the miosis effect of opiates?

A

No

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31
Q

Can someone grow tolerance to the constipation effect of opiates?

A

No

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32
Q

Explain the cardiovascular effects of morphine.

A

Reduced SNS tone and reflexes so:
Hypotension due to reduced vascular resistance so vasodilation
Orthostatic hypotension due to blunted baroreceptor reflex action

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33
Q

What are the 2 primary cardiovascular effects of morphine?

A

Hypotension

Orthostatic hypotension

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34
Q

One of the cardiovascular effects of morphine is hypotension. It is primarily due to:
A. Reduced vascular resistance
B. Blunted baroreceptor reflex actions

A

A. Reduced vascular resistance

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35
Q

One of the cardiovascular effects of morphine is orthostatic hypotension. It is primarily due to:
A. Reduced vascular resistance
B. Blunted baroreceptor reflex actions

A

B. Blunted baroreceptor reflex actions

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36
Q

True or False: One of the GI effects of morphine is delayed gastric emptying secondary to decreased GI motility.

A

True

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37
Q

True or false, if someone is a chronic user of opioids, they will show tolerance to the constipation effect.

A

False! Constipation gets worse actually.

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38
Q

True or false: Opioids cause decreased tone of anal sphincter.

A

False! Increased tone, which is why you can’t poop :(

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39
Q

Morphine (increases OR decreases) bladder external sphincter contraction, which increases bladder volume and reduces voiding.

A

Increases

40
Q

The sphincter of Oddi is also known as ________.

A

The hepatobiliary sphincter

41
Q

The morphine effect on smooth muscle can cause (increased OR decreased) biliary pressure?

A

Increased (up to 10X)

42
Q

True or false: Morphine causes paradoxical worsening of gall stone and kidney stone pain.

A

True! Due to its effect on smooth muscle (so its effects on sphincters)

43
Q

True or false: The major problem in terms of respiration with opioids is due to the bronchiolar airway passage constriction due to the morphine effect on smooth muscle.

A

False!! Primary issue with opioids and respiration is respiratory depression! (brainstem mediated respiratory depression! so it is a CNS effect).

44
Q

True or false: Morphine can cause histamine release.

A

True

45
Q

In acute overdose, what 3 things make up the opiate triad?

A
  1. Respiratory depression
  2. Comatose
  3. Miosis
46
Q
Which of the following is NOT a part of the opiate triad?
A. Constipation
B. Miosis
C. Respiratory depression
D. Comatose
A

A. Constipation

47
Q

How do you treat acute opioid overdose?

A

IV Naloxone

48
Q

Which has more efficacy?
A. Codeine
B. Morphine

A

B. Morphine

49
Q

If you are a (slow metabolizer OR fast metabolizer?) of morphine, you probably have subtherapeutic levels because morphine is not getting metabolized quickly by CYP 2D6.

A

Slow metabolizer

50
Q

If you are a (slow metabolizer OR fast metabolizer?) of morphine, you run the risk of overdose because there is increased morphine in your system.

A

Fast metabolizer

51
Q

Codeine is metabolized to morphine by CYP ____.

A

2D6

52
Q

Another name for diacetyl morphine is _____.

A

Heroin

53
Q

_____ has to deacytelated twice by your body to form morphine, which is the active metabolite in your body.

A

Heroin

54
Q

True or false: Heroin is a prodrug

A

True

55
Q

True or false: Codeine is a prodrug

A

True

56
Q

True or false: Morphine is a prodrug

A

False!

57
Q

Which isomer of levorphanol has efficacy and profile similar to morphine?
A. L-isomer
B. D-isomer

A

A. L-isomer

58
Q

Which Levorphanol isomer doesn’t have an opiate mechanism but does produce antitussive effects?
A. L-isomer
B. D-isomer

A

B. D-isomer

59
Q

The D-isomer of Levorphanol is called ______.

A

Dextromethorphan

60
Q

Put the following in order from highest efficacy to lowest.
A. Morphine
B. Meperidine
C.Codeine

A
  1. Morphine
  2. Codeine
  3. Meperidine
61
Q

Why is meperidine not being used anymore?

A

Because its metabolite, normeperidine, causes seizures, can worsen serotonin syndrome, and has other bad side effects.

62
Q

True or false: Meperidine carries a lower risk for effects on smooth muscle, respiratory depression, and addiction.

A

False! It carries lower risk for respiratory depression and addiction, but same effect on smooth muscle

63
Q

Normeperidine has __X the analgesic potency and __X the toxicity of meperidine.

A

1/2x the analgesic potency and 2x the toxicity.

64
Q

A meperidine derivative that people on the street used to get high is called ___.

A

MPTP

65
Q

When someone poorly made MPTP, the resulting metabolite, called ____, killed dopamine neurons in the brain, resulting in early onset of Parkinson’s in patients.

A

MPP+

66
Q
Put the following in order from highest efficacy to lowest.
A. Morphine
B. Meperidine
C. Fentanyl
D. Codeine
A
  1. Fentanyl
  2. Morphine
  3. Codeine
  4. Meperidine
67
Q

This class of opioids has different formulations including patches, intrathecal injection, and anesthesia.

A

Fentanyl class

68
Q

China white is called a designer drug because _______.

A

It was made in someone’s home, not legally by a chemist.

69
Q

China white is a derivate of ____ and was produced in someone’s home to be used as a street drug.

A

Fentanyl

70
Q

What is the main contribution of China White?

A

It was because of China white that the government changed its laws: they made it so that if a drug came on the market that has potential for abuse on the streets, they can make it illegal (schedule I drug) and then do testing of the product after.

71
Q

Methadone has:
A. Lower efficacy than morphine
B. Similar efficacy as morphine
C. Higher efficacy than morphine

A

B. Similar efficacy as morphine

72
Q
Put the following in order from highest efficacy to lowest.
A. Morphine
B. Meperidine
C. Fentanyl
D. Codeine
E. Propoxyphene
A
  1. Fentanyl
  2. Morphine
  3. Codeine
  4. Meperidine
  5. Propoxyphene
73
Q
Put the following in order from highest efficacy to lowest.
A. Morphine
B. Meperidine
C. Fentanyl
D. Codeine
E. Propoxyphene
F. Methadone
A
  1. Fentanyl
  2. Morphine
  3. Methadone (= efficacy to morphine)
  4. Codeine
  5. Meperidine
  6. Propoxyphene
74
Q

Propoxyphene belongs to this class of opiates.

A

Methadone class

75
Q

True or False: Propoxyphene doesn’t activate opioid receptors even tho it is an opioid drug.

A

True

76
Q

Respiratory depression can occur through which of the following receptor(s)?
A. Mu
B. Kappa
C. Delta

A

Only through mu

77
Q

Psychomimetic effects can occur through which of the following receptor(s)?
A. Mu
B. Kappa
C. Delta

A

B. Kappa only

78
Q

Constipation can occur through which of the following receptor(s)?
A. Mu
B. Kappa
C. Delta

A

A. Mu
&
B. Kappa

79
Q

Abuse related to euphoria can occur through which of the following receptor(s)?
A. Mu
B. Kappa
C. Delta

A

A. Mu

80
Q

Of the 3 opioid receptors, which receptor currently has no drug treatments that target it?

A

Delta

81
Q

Nalorphine is a mu receptor _____ and kappa receptor ______.

A

Mu receptor antagonist and kappa receptor agonist.

82
Q

True or false: Nalorphine had no abuse liability.

A

True (bc it’s a mu receptor antagonist)

83
Q

Why did people not like using nalorphine?

A

Too much kappa activity, so too much dysphoric/psychomimetic activity.

84
Q

Pentazocine (Talwin) is a mu partial agonist and weak kappa agonist, and was advertised as bring abuse-free. Was that the case?

A

No! It was still abused.

85
Q

Which drug is known to have a “sticky effect” on mu receptors and was considered a miracle drug as a result?

A

Buprenorphine (mixed agonist antagonist activity)

86
Q

True or false: nuprenorphine is abuse free.

A

False! Not abuse free because still a mu agonist, but less abuse due to its sticky dissociation effect on mu.

87
Q

Naloxone is an opiate receptor (agonist OR antagonist?)

A

Antagonist!

88
Q

Naloxone has (short half life OR long half life?)

A

Very short half life, which is why it’s only used as IV.

89
Q

If someone comes in and is suspected of an opiate overdose, what do you do?

A
  1. Give small bolus of IV naloxone.
  2. If no response, give another small bolus of IV naloxone.
  3. If still no response, then not opiate related overdose.
90
Q

Why is naltrexone used for prevention of relapse in opiate abusers?

A

Because it has a long half life and is orally effective (it is a mu receptor antagonist)

91
Q

True or false: If you give a patient too much IV naloxone, you can actually cause a withdrawal effect.

A

True

92
Q

What is the negative aspect of naltrexone therapy?

A

It blocks endogenous opiates as well, so no normal good feelings are experienced.

93
Q

True or False: Spinal (intrathecal) administration of fentanyl has addiction risk.

A

False! No addiction risk because it is localized. No respiratory risk either!

94
Q

Tramadol is a weak mu receptor (agonist OR antagonist?) and has weak 5HT and weak NE reuptake blockade as well.

A

Agonist

95
Q

______ can be used for opiate-induced constipation.

A

Methylnaltrexone (bc it doesn’t cross BBB)