Opioids - Dr. C Flashcards
(95 cards)
1
Q
True or false: sigma receptor is an opioid receptor.
A
False! Only mu, kappa, and delta are opioid receptors.
2
Q
Which of the following is NOT an opioid receptor? A. Mu B. Kappa C. Sigma D. Delta
A
C. Sigma
3
Q
True or false: morphine produces analgesia without anesthesia.
A
True
4
Q
Which of the following is morphine more effective against?
A. Dull, throbbing pain
B. Sharp, cutaneous pain
A
A. Dull, throbbing pain
5
Q
Which of the following is morphine less effective against?
A. Dull, throbbing pain
B. Sharp, cutaneous pain
A
B. Sharp, cutaneous pain
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.
7
Q
________ is chronic pain condition characterized by instances of increased pain with no apparent change in opiate concentrations.
A
“Breakthrough” pain
8
Q
The sedation and stupor effects of morphine come from its interaction with which receptor?
A
Mu
9
Q
Respiratory depression is caused by _______ receptor activation.
A
Mu
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
11
Q
What are the 3 opioid receptors?
A
Mu, kappa, delta
12
Q
Respiratory depression comes as a result of actions on Mu opiate receptors in _______ respiratory centers,
A
Medullary
13
Q
What is the most common cause of death in relation to opiate overdose?
A
Respiratory depression
14
Q
What fraction of patients receiving opiates will experience nausea and emesis (vomiting)?
A
About 1/3
15
Q
True or false: opioids have an antitussive effect.
A
True
16
Q
This is a side effect of opiates that causes pupillary constriction.
A
Miosis (aka pinpoint pupils)
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
18
Q
Most opium was and still is produced in _____.
A
Afghanistan
19
Q
True or false: the 3 opiate receptors have similar amino acid sequences.
A
True
20
Q
True or false: Endogenous opiates are cleaved from the same peptide.
A
True
21
Q
What are the 5 classes of opiates?
A
Phenanthrene class Levorphanol class Meperidine class Fentanyl class Methadone class
22
Q
Morphine falls under which opiate class?
A
Phenanthrene class
23
Q
Which opiates fall under the phenanthrene class of opiates?
A
Morphine, dihydromorphone, and codeine
24
Q
Which meds fall under the levorphanol class of opiates?
A
Levorphanol and dextromethorphan
25
Which drugs fall under the meperidine class of opiates?
Meperidine and mCPP
26
Which drugs fall under the fentanyl class of opiates?
Fentanyl, alfentanyl, and sufentanyl
27
Which meds fall under the methadone class of opiates?
Methadone, LAAM, and propoxyphene
28
What is the prototype and the gold standard of opiate agonist agents?
Morphine
29
True or false: opiate agonist agents can be direct-acting agents, Reuptake blockers, synthesis inhibitors, or neuron activators.
FALSE! They are all direct-acting agonists!!!*
30
Can someone grow tolerance to the miosis effect of opiates?
No
31
Can someone grow tolerance to the constipation effect of opiates?
No
32
Explain the cardiovascular effects of morphine.
Reduced SNS tone and reflexes so:
Hypotension due to reduced vascular resistance so vasodilation
Orthostatic hypotension due to blunted baroreceptor reflex action
33
What are the 2 primary cardiovascular effects of morphine?
Hypotension
| Orthostatic hypotension
34
One of the cardiovascular effects of morphine is hypotension. It is primarily due to:
A. Reduced vascular resistance
B. Blunted baroreceptor reflex actions
A. Reduced vascular resistance
35
One of the cardiovascular effects of morphine is orthostatic hypotension. It is primarily due to:
A. Reduced vascular resistance
B. Blunted baroreceptor reflex actions
B. Blunted baroreceptor reflex actions
36
True or False: One of the GI effects of morphine is delayed gastric emptying secondary to decreased GI motility.
True
37
True or false, if someone is a chronic user of opioids, they will show tolerance to the constipation effect.
False! Constipation gets worse actually.
38
True or false: Opioids cause decreased tone of anal sphincter.
False! Increased tone, which is why you can't poop :(
39
Morphine (increases OR decreases) bladder external sphincter contraction, which increases bladder volume and reduces voiding.
Increases
40
The sphincter of Oddi is also known as ________.
The hepatobiliary sphincter
41
The morphine effect on smooth muscle can cause (increased OR decreased) biliary pressure?
Increased (up to 10X)
42
True or false: Morphine causes paradoxical worsening of gall stone and kidney stone pain.
True! Due to its effect on smooth muscle (so its effects on sphincters)
43
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.
False!! Primary issue with opioids and respiration is respiratory depression! (brainstem mediated respiratory depression! so it is a CNS effect).
44
True or false: Morphine can cause histamine release.
True
45
In acute overdose, what 3 things make up the opiate triad?
1. Respiratory depression
2. Comatose
3. Miosis
46
```
Which of the following is NOT a part of the opiate triad?
A. Constipation
B. Miosis
C. Respiratory depression
D. Comatose
```
A. Constipation
47
How do you treat acute opioid overdose?
IV Naloxone
48
Which has more efficacy?
A. Codeine
B. Morphine
B. Morphine
49
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.
Slow metabolizer
50
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.
Fast metabolizer
51
Codeine is metabolized to morphine by CYP ____.
2D6
52
Another name for diacetyl morphine is _____.
Heroin
53
_____ has to deacytelated twice by your body to form morphine, which is the active metabolite in your body.
Heroin
54
True or false: Heroin is a prodrug
True
55
True or false: Codeine is a prodrug
True
56
True or false: Morphine is a prodrug
False!
57
Which isomer of levorphanol has efficacy and profile similar to morphine?
A. L-isomer
B. D-isomer
A. L-isomer
58
Which Levorphanol isomer doesn't have an opiate mechanism but does produce antitussive effects?
A. L-isomer
B. D-isomer
B. D-isomer
59
The D-isomer of Levorphanol is called ______.
Dextromethorphan
60
Put the following in order from highest efficacy to lowest.
A. Morphine
B. Meperidine
C.Codeine
1. Morphine
2. Codeine
3. Meperidine
61
Why is meperidine not being used anymore?
Because its metabolite, normeperidine, causes seizures, can worsen serotonin syndrome, and has other bad side effects.
62
True or false: Meperidine carries a lower risk for effects on smooth muscle, respiratory depression, and addiction.
False! It carries lower risk for respiratory depression and addiction, but same effect on smooth muscle
63
Normeperidine has __X the analgesic potency and __X the toxicity of meperidine.
1/2x the analgesic potency and 2x the toxicity.
64
A meperidine derivative that people on the street used to get high is called ___.
MPTP
65
When someone poorly made MPTP, the resulting metabolite, called ____, killed dopamine neurons in the brain, resulting in early onset of Parkinson's in patients.
MPP+
66
```
Put the following in order from highest efficacy to lowest.
A. Morphine
B. Meperidine
C. Fentanyl
D. Codeine
```
1. Fentanyl
2. Morphine
3. Codeine
4. Meperidine
67
This class of opioids has different formulations including patches, intrathecal injection, and anesthesia.
Fentanyl class
68
China white is called a designer drug because _______.
It was made in someone's home, not legally by a chemist.
69
China white is a derivate of ____ and was produced in someone's home to be used as a street drug.
Fentanyl
70
What is the main contribution of China White?
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
Methadone has:
A. Lower efficacy than morphine
B. Similar efficacy as morphine
C. Higher efficacy than morphine
B. Similar efficacy as morphine
72
```
Put the following in order from highest efficacy to lowest.
A. Morphine
B. Meperidine
C. Fentanyl
D. Codeine
E. Propoxyphene
```
1. Fentanyl
2. Morphine
3. Codeine
4. Meperidine
5. Propoxyphene
73
```
Put the following in order from highest efficacy to lowest.
A. Morphine
B. Meperidine
C. Fentanyl
D. Codeine
E. Propoxyphene
F. Methadone
```
1. Fentanyl
2. Morphine
2. Methadone (= efficacy to morphine)
3. Codeine
4. Meperidine
5. Propoxyphene
74
Propoxyphene belongs to this class of opiates.
Methadone class
75
True or False: Propoxyphene doesn't activate opioid receptors even tho it is an opioid drug.
True
76
Respiratory depression can occur through which of the following receptor(s)?
A. Mu
B. Kappa
C. Delta
Only through mu
77
Psychomimetic effects can occur through which of the following receptor(s)?
A. Mu
B. Kappa
C. Delta
B. Kappa only
78
Constipation can occur through which of the following receptor(s)?
A. Mu
B. Kappa
C. Delta
A. Mu
&
B. Kappa
79
Abuse related to euphoria can occur through which of the following receptor(s)?
A. Mu
B. Kappa
C. Delta
A. Mu
80
Of the 3 opioid receptors, which receptor currently has no drug treatments that target it?
Delta
81
Nalorphine is a mu receptor _____ and kappa receptor ______.
Mu receptor antagonist and kappa receptor agonist.
82
True or false: Nalorphine had no abuse liability.
True (bc it's a mu receptor antagonist)
83
Why did people not like using nalorphine?
Too much kappa activity, so too much dysphoric/psychomimetic activity.
84
Pentazocine (Talwin) is a mu partial agonist and weak kappa agonist, and was advertised as bring abuse-free. Was that the case?
No! It was still abused.
85
Which drug is known to have a "sticky effect" on mu receptors and was considered a miracle drug as a result?
Buprenorphine (mixed agonist antagonist activity)
86
True or false: nuprenorphine is abuse free.
False! Not abuse free because still a mu agonist, but less abuse due to its sticky dissociation effect on mu.
87
Naloxone is an opiate receptor (agonist OR antagonist?)
Antagonist!
88
Naloxone has (short half life OR long half life?)
Very short half life, which is why it's only used as IV.
89
If someone comes in and is suspected of an opiate overdose, what do you do?
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
Why is naltrexone used for prevention of relapse in opiate abusers?
Because it has a long half life and is orally effective (it is a mu receptor antagonist)
91
True or false: If you give a patient too much IV naloxone, you can actually cause a withdrawal effect.
True
92
What is the negative aspect of naltrexone therapy?
It blocks endogenous opiates as well, so no normal good feelings are experienced.
93
True or False: Spinal (intrathecal) administration of fentanyl has addiction risk.
False! No addiction risk because it is localized. No respiratory risk either!
94
Tramadol is a weak mu receptor (agonist OR antagonist?) and has weak 5HT and weak NE reuptake blockade as well.
Agonist
95
______ can be used for opiate-induced constipation.
Methylnaltrexone (bc it doesn't cross BBB)
