Opioids Flashcards

(56 cards)

1
Q

What is the pathway of orofacial pain

A

Nociceptors on trigeminal nerve endings –> A-d fibers and C fiber –> Trigeminal ganglion –> Trigeminal nuclei on the brainstem –> Thalamus –> Limbic Systema and Cerebral cortex

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

T/F - Orofacial pain follows a path different than other pain pathways throughout the body

A

False - it’s the same

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

Where are nociceptors located?

A

Throughout the skin, oral mucosa, and tooth pulp

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

A-delta fibers

A

Faster, myelinated axons response first to noxious mechanical stimuli
Produce the initial sensation of sharp pain

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

C fibers

A

Slower, unmyelinated axons that respond to thermal, mechanical, and chemical assaults
Dull, aching, or burning pain

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

Are there more C or A-delta fibers in the body?

A

There are 5x more C fibers than A-delta

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

Nociceptor signaling

A

Nociceptors are molecular sensors
Different nociceptors respond to various noxious stimuli such as heat, cold, mechanical perburbations, or protons
Their activation leads to local depolarization which in turn initiates action potentials

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

How does inflammation cause pain?

A

Mediators such as prostaglandins, substance P, TNF-a, Il-16, and Il-6 interact with nociceptors and facilitate the transmission of pain signals

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

T/F - Tissue injury can lead to sensitization of the pain response

A

True

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

Where can pharmacologic intervention occur to diminish pain?

A

At the periphery
Periphery signaling to the CNS
CNS activity

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

Where do NSAIDs and SAIDs act to diminish pain?

A

Inhibition at the periphery

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

Where do local anesthetics act to diminish pain?

A

Inhibition of signaling to the CNS

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

Where do opioids act to diminish pain?

A

Inhibition at the periphery and

Inhibition of CNS activity

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

What are the four families of endogenous opioids?

A

Pro-opiomelanocortin peptides
Pro-enkephalin peptides
Prodynorphin peptides
Endomorphins

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

What are the three important opioids receptors?

A

Mu (u)
Kappa (k)
Delta (d)

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

Opioids receptors

A

GCPRs
Widely distributed in the CNS
They activate Gai

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

B-endorphin

A

31 amino acid peptide

Natural agonist of the u-opioid receptor

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

Where is B-endorphin made, and what is it made from?

A

Formed from processing of pro-opiomelanocortin (POMC)

Made in the pituitary and hypothalamus

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

Met-enkephalin

A

5 amino acid peptide (pentapeptide)
Derived from pro-enkephalin precursor
Found in the adrenal medulla and throughout the CNS
Natural agonist of the d receptor

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

Leu-enkephalin

A

5 amino acid peptide (pentapeptide)
Derived from pro-enkephalin and pro-dynorphin
Found throughout the CNS
Natural agonist of the d receptor

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

Dynorphin A

A

13 aa peptide
Derived from Pro-dynorphin precursor
Found throughout the CNS
Natural agonist of the k receptor

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

Dynorphin B

A

13 aa peptide
Derived from Pro-dynorphin precursor
Found throughout the CNS
Natural agonist of the k receptor

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

a/B neo-endorphin

A
10 aa peptide (a)
9 aa peptide (B)
Derived from Pro-dynorphin precursor
Found throughout the CNS
Natural agonist of the k receptor
24
Q

What do opioid receptors activate?

25
What does opioid activation of Gi do?
Inhibits adenyl cyclase activity, which reduces PKA, which reduces Ca entry Reduction in Ca entry prevents the synapse from working
26
What does opioid activation of GBGy do?
Activates a Cl channel, hyperpolarizing the postsynaptic terminal, inhibiting an AP on the synaptic membrane
27
T/F - Opioids can inhibit synaptic transmission pre and postsynaptically
True
28
What are the different forms of u receptors, and which are the most physiologically important?
u1*, u2*, u3
29
Where are u receptors found?
PAG Superficial dorsal horn of the spinal cord Nucleus ambiguous Amygdala Cerebral cortex GI tract (inhibit peristaltic action, causing constipation)
30
What is the natural agonist of the u-opioid receptor?
B-endorphin
31
What receptor do the majority of analgesic drugs act upon?
U receptors
32
What is the site of Analgesic action?
Inhibits the ascending pathway of pain - can inhibit the transmission of an impulse - can inhibit excitatory neurotransmitter release
33
How can analgesics inhibit the descending pathway of pain inhibition?
Opioids inhibit GABA release on the PAG | -by inhibiting the inhibitor, opioids activate the pathway that produces CNS mediated inhibition of pain
34
What is the clinical effects of opioids?
All opioids produce analgesia, respiratory depression, constipation, GI spasm, and physical dependence
35
What receptor does morphine target?
It is the prototypical full agonist for the u receptor (weak agonist for k)
36
What do patients report after taking morphine?
They report that the pain is still present, but it is no longer unpleasant
37
What is the most serious acute adverse effect of all opioids (especially morphine)
Respiratory depression
38
What is tolerance?
A state in which an organism no longer responds to a given dosage of a drug A higher dose is required to achieve the same effect
39
T/F - tolerance develops to all effects uniformly
False - tolerance firsts manifests as shortened or diminished analgesia
40
What does the rate of tolerance depend on?
Dose and the frequency of administration | Generally seen 5-7 days after treatment
41
T/F - If tolerance is developed, the toxic effects of a drug are also diminished
False - toxic effects remain even if tolerance develops
42
T/F - Dependece and tolerance are the same thing
False
43
What enzyme metabolizes morphine, and where is it?
UGT2B7 | In the liver as well as the brain
44
What is the primary product of morphine metabolism? The secondary?
``` 1' = Morphine-3-glucuronide (M-3-G) 2' = Morphine-6-glucuronide (M-6-G) ```
45
Which product of morphine can cross the BBB?
M-6-G
46
Which morphine product (along with morphine) can act on u receptors?
M-6-G
47
How does Codeine compare to morphine?
It is more effective orally than morphine | Codeine binds poorly to u receptors
48
What are the products of codeine metabolism?
Codeine-6-glucuronide (80%) | Morphine (5%)
49
What dosage of codeine is recommended? Why?
30-60mg daily | Side effects are minimal at this dose, and we usually don't see dependence at this dose either
50
T/F - Pain with an inflammatory component can be treated without an anti-inflammatory
False - pain with an inflammatory component should NOT be treated without an anti-inflammatory drug (we want to beat down the inflammation as well)
51
What do Dihydrocodeine, Oxycodone, and Hydrocodone have in common with morphine? What makes them different?
They're all methylated in the 3' position | These can be taken orally
52
Naloxone, naltrexone, and nalmefene are all what?
Opioid antagonists
53
What are opioid antagonists used for?
Used to treat opioid toxicity
54
Which opioid antagonists is injected and works rapidly?
Naloxone
55
Which opioid antagonists is effective orally and lasts a long time?
Naltrexone | But, Nalmefene can last even longer
56
Which opioids are used most commonly in dentistry?
Codeine, Hydrocodone, oxycodone, pentazocine