Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

PMCOL 200 > Opioids > Flashcards

Opioids Flashcards

1
Q

What is opium?

A

Dried latex obtained from the poppy.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What are opiates?

A

Any drug derived from opium.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What are opioids?

A

Any drug that binds to an opioid receptor.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What are narcotics?

A

Drugs that treat pain with sleep-inducing properties.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What kind of receptors are opioid receptors?

A

Inhibitory G-protein coupled receptors.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What does activation of opioid receptors cause?

A

Inhibition of calcium channels and activation of potassium channels, also inhibition of adenylyl cyclase.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What are the four types of opioid receptors?

A

Mu, kappa, delta, and ORL1.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Why do the opioid receptors produce differing effects when activated?

A
  1. Receptor distribution throughout the brain is different for each receptor.
  2. Ligands have different specificity for different receptors.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Where are mu receptors most densely located?

A

In the brainstem and limbic system.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Where are delta and kappa receptors most densely located?

A

In the cortex.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Where are ORL1 receptors located?

A

Across the entire brain.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What is ORL1 receptor activation thought to be involved in?

A

Fear processing.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What does agonism at the mu receptor cause?

A

Analgesia, euphoria, antitussive effects, respiratory depression, constipation.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What does antagonism at the mu receptor cause?

A

Aversive effects, prevent euphoria, block overdose.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What does agonism at the delta receptor cause?

A

No euphoria, no analgesia (except in chronic pain), possibly seizure-inducing.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What does antagonism at the delta receptor cause?

A

No obvious effects.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

What does agonism at the kappa receptor cause?

A

Aversive effects, hallucinations, produces anxiety.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

What does antagonism at the kappa receptor cause?

A

Potential antipsychotic and antidepressant effects.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

What are full mu opioid receptor agonists?

A

Morphine, methadone, fentanyl, heroin.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

What is the partial agonist at the mu opioid receptor used to treat substance use disorder?

A

Buprenorphine.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

What is buprenorphine?

A

Partial agonist at the mu receptor and antagonist at the delta and kappa opioid receptor. Common teatment for both pain and opioid addiction.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

What are beta-arrestins?

A

Family of intracellular proteins important for regulating signal transduction at GPCRs.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

What is the beta-arrestin signalling pathway?

A
  1. Receptor is activated.
  2. G-protein cleaves, GPCR is phosphorylated and signals beta-arrestin binding.
  3. Beta-arrestin blocks further signalling and redirects signalling to alternative pathways and targets receptors for internalization.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

What are the symptoms of beta-arrestin recruitment?

A

Respiratory depression and constipation.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

What is receptor selectivity?

A

Selectivity of a drug for different receptor subtypes.

26
Q

What is functional selectivity?

A

Selectivity of a bound receptor for different signalling pathways.

27
Q

What mu agonist opioid must undergo intensive first-pass metabolism?

A

Morphine.

28
Q

What mu agonist opioid is not affected by first-pass metabolism?

A

Codeine.

29
Q

Where are opioids most highly concentrated?

A

In tissues like the brain, lungs, liver kidneys, and spleen because they are highly perfused.

30
Q

How is morphine metabolized?

A

Phase 2 glucuronidation in the liver by UGT2B7 into M3G and M6G.

31
Q

What is M6G?

A

Morphine-6-glucuronide, an active metabolite that cna prolong effects of morphine.

32
Q

How is codeine metabolized into morphine?

A

By CYP2D6.

33
Q

How are polar metabolites excreted?

A

Mainly in the urine.

34
Q

What are the three types of endogenous opioid peptides?

A

Beta endorphins, enkephalins, dynorphins

35
Q

What is the function of endogenous opioid peptides?

A

To mediate pain, reward, learning, and memory/cognition.

36
Q

What is the common protein precursor for opioid peptides?

A

Tyr-Gly-Gly-Phe.

37
Q

What is the precursor for enkephalin?

A

Pro-enkephalin.

38
Q

What is the precursor for beta-endorphin?

A

Pro-opioimelanocortin.

39
Q

What is the precursor for dynorphins?

A

Pro-dynorphin.

40
Q

What is the affinity for opioid receptors of enkephalins?

A

Delta, Mu, kappa.

41
Q

What is the affinity for opioid receptors of endorphins?

A

Mu equal to deta, kappa.

42
Q

What is the affinity for opioid receptors of dynorphins?

A

kappa, mu is equal to delta.

43
Q

Where in the brainstem are opioid receptors localized? What does agonism in this area cause?

A

Rostroventral medulla. Assist in increasing diffusion of noxious inhibitory control.

44
Q

What is the noxious inhibitory circuit comprised of? Function?

A

Comprised of the descending excitatory and inhibitory neurons in the medulla that inhibit or activate pain synapses in the spinal cord.

45
Q

What receptors are located on the ON cells in the medulla?

A

Mu, delta.

46
Q

If the mu and delta receptors on the ON cells in the medulla were activated, what would be the effect?

A

Inhibition of ON cells, reduction in nociceptive signalling.

47
Q

Where are dopamine neurons primarily located?

A

Ventral tegmental area.

48
Q

Where are mu receptors located in the VTA?

A

On inhibitory GABAergic interneurons.

49
Q

When the mu receptors in the VTA are activated, what would be the effect?

A

Inhibition of inhibitory GABAergic interneurons causing release of dopamine.

50
Q

What is TRV250?

A

A delta opioid receptor biased agonist that is biased to the G-protein pathway over the beta-arrestin pathway.

51
Q

What is CR845?

A

Potent analgesics that are peripherally restricted os that they do not cross the BBB. Agonist of kappa receptors.

52
Q

What is tolerance?

A

Decreased response to the effects of a drug, necessitating ever-larger doses to achieve the same effect.

53
Q

What is the mechanism of opioid tolerance?

A

Following agonist binding and G-protein signalling, beta-arrestin is recruited to shut off signalling and produce desensitization.

Receptor is internalized for recycling.

54
Q

What is physical dependence?

A

Dependence on a drug such that withdrawal occurs when an individual stops administering.

55
Q

What are acute opioid withdrawal symptoms?

A

Runny nose, tearing eyes, chills, muscle aches, diarrhea, anxiety.

56
Q

What are the physical barriers of opioids used to prevent addiction?

A

Turning tablet into paste-like substance to prevent from snorting.

57
Q

How to chemical barriers help prevent opioid addiction?

A

Allow for the substance to resist extraction.

58
Q

What is agonist/antagonist combination?

A

Taking an opioid agonist with an antagonist to interfere with euphoria associated with abuse.

59
Q

What is agonist replacement therapy?

A

Replacing opioid agonists with opioids of lower efficacy/potency and with longer half-lifes to prevent adverse effects.

60
Q

What is methadone?

A

Full agonist at the mu-opioid receptor, long acting. Replacement therapy drug.

61
Q

What is naloxone?

A

non-selective competitive opioid receptor antagonist that treats acute intoxication via opioids.

PMCOL 200 (19 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions