Opioids Flashcards

1
Q

What is nociception?

A

The neural processing of particular sensory information that results in pain perception.

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2
Q

Name the four processes involved in nociceptive pain.

A

Transduction Transmission Perception Modulation.

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3
Q

What stimuli activate TRPV1 and TRPV2 receptors?

A

Thermal stimuli (>42°C), low extracellular pH, vanilloid chemical ligands such as capsaicin.

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4
Q

Which ion channels are activated by mechanical stimuli?

A

ASIC, ATP sensitive P2X P2Y and kinin-sensitive B1 or B2 receptors.

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5
Q

What is the role of voltage-gated sodium channels in nociceptive transmission?

A

They convert depolarization of the peripheral terminal into an action potential.

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6
Q

What neurotransmitters are released by primary afferent neurons in the dorsal horn?

A

Glutamate Substance P CGRP.

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7
Q

How do gabapentin and pregabalin affect nociceptive transmission?

A

They modulate CNS transmission by acting on the α2δ subunit of Ca channels.

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8
Q

What are the major inhibitory neurotransmitters in the dorsal horn of the spinal cord?

A

Opioid peptides norepinephrine serotonin glycine GABA.

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9
Q

What is placebo analgesia?

A

Reduced sensation of pain due to belief in receiving a pain-suppressing drug involving endogenous opioid peptides.

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10
Q

What are the primary clinical uses of opioids?

A

Relief of severe pain treatment of major diseases trauma and surgery.

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11
Q

What receptors do endogenous opioid peptides primarily act on?

A

Dynorphins on κ-receptors, enkephalins and β-endorphin on μ and δ receptors.

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12
Q

How do opioids cause hyperpolarization of nerve cells?

A

By interacting with opioid receptors increasing K efflux and reducing Ca influx.

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13
Q

What effect does morphine have on the release of substance P?

A

It decreases its release modulating pain perception in the spinal cord.

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14
Q

What is opioid-induced hyperalgesia (OIH)?

A

Paradoxical increase in pain sensitivity due to excessive opioid use.

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15
Q

How is respiratory depression caused by opioids?

A

By reducing the sensitivity of respiratory center neurons to CO2.

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16
Q

What is the primary cause of death in acute opioid overdose?

A

Respiratory depression.

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17
Q

How do morphine and codeine suppress the cough reflex?

A

By unknown mechanisms independent of their analgesic effects.

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18
Q

What characteristic effect does morphine have on pupils?

A

Miosis (pupillary constriction) through stimulation of μ and κ receptors.

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19
Q

What effect does morphine have on the gastrointestinal tract?

A

Decreases motility increases tone of smooth muscle relieves diarrhea and causes constipation.

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20
Q

How does morphine affect the cardiovascular system at high doses?

A

Causes hypotension and bradycardia due to medullary action.

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21
Q

What effect does histamine release from morphine have?

A

Bronchoconstriction, hypotension, urticaria.

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22
Q

Name two opioid antagonists.

A

Naloxone and Naltrexone.

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23
Q

What is the primary use of opioid antagonists?

A

Treatment of opioid overdose.

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24
Q

How do opioid receptors generally affect ion channels?

A

Increase K efflux reduce Ca influx leading to hyperpolarization and reduced transmitter release.

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25
What is the mechanism of action of μ-opioid receptor agonists in the spinal cord?
Decreasing the release of substance P and inhibiting excitatory transmitter release.
26
What is the clinical significance of morphine's effect on the biliary tract?
Increases pressure due to gall bladder contraction and biliary sphincter constriction contraindicated in biliary colic.
27
What are the pharmacological actions of strong opioid agonists like morphine?
Analgesia, euphoria, sedation, respiratory depression, cough suppression, miosis, nausea, constipation.
28
How do moderate/low opioid agonists differ from strong agonists?
They are less potent and often used in combination with other analgesics.
29
What are the effects of mixed agonist-antagonist opioids?
Provide analgesia with a lower risk of dependence and respiratory depression.
30
Name a partial opioid agonist.
Buprenorphine.
31
What is the role of endogenous opioid peptides in pain modulation?
Inhibit synaptic transmission and are released in response to noxious stimuli.
32
How does naloxone reverse opioid effects?
By blocking opioid receptors reversing respiratory depression and analgesia.
33
What is the clinical use of methadone?
Treatment of opioid dependence and chronic pain management.
34
What is the effect of opioid agonists on the cough reflex?
Suppress the cough reflex with codeine being a common antitussive.
35
What is tramadol and its dual mechanism of action?
A weak centrally acting opioid that also inhibits norepinephrine and serotonin reuptake.
36
What are the primary symptoms of opioid withdrawal?
Agitation anxiety muscle aches increased tearing insomnia runny nose sweating yawning.
37
How is acute opioid toxicity managed?
Administering opioid antagonists like naloxone and supportive care.
38
What is the function of the nociceptive pathway?
Processing and transmitting pain signals from the periphery to the brain.
39
Name two novel opioids.
Oliceridine and PZM21.
40
How does opioid use affect fertility in females?
Inhibits cilia motility in the ovary tubes potentially leading to sterility.
41
What are the effects of opioids on the respiratory system?
Respiratory depression and increased risk of hypoxia.
42
What is the primary effect of kappa opioid receptor activation?
Analgesia at the spinal level sedation miosis dysphoria hallucinations.
43
What is the action of dynorphins?
Primarily act on κ-receptors modulating pain and emotional responses.
44
How do opioids influence neurotransmitter release?
Inhibit release by hyperpolarizing nerve terminals and reducing calcium influx.
45
What is the role of naloxone in opioid overdose?
Reverses opioid-induced respiratory depression and other effects.
46
How do serotonin and norepinephrine influence pain perception?
They modulate descending inhibitory pathways affecting pain transmission.
47
What is the role of endogenous opioids in stress response?
They modulate pain and stress responses through receptor activation.
48
What is the clinical use of buprenorphine?
Management of opioid dependence and moderate to severe pain.
49
How do opioids affect gastrointestinal motility?
Decrease motility and increase smooth muscle tone leading to constipation.
50
What is the primary mechanism of opioid-induced euphoria?
Stimulation of the ventral tegmentum and μ receptors.
51
How does opioid use lead to respiratory depression?
Reduces the sensitivity of respiratory center neurons to CO2.
52
What is the effect of opioid antagonists like naloxone on placebo analgesia?
Reduce placebo analgesia by blocking endogenous opioid peptides.
53
What is the role of μ-opioid receptors in pain relief?
Mediating analgesia euphoria sedation respiratory depression and dependence.
54
How do opioids cause sedation?
By additive effects with other CNS depressants and influencing neurotransmitter release.
55
What are the primary side effects of opioid use?
Constipation nausea vomiting respiratory depression euphoria miosis.
56
How is opioid-induced constipation managed?
Using laxatives stool softeners or opioid receptor antagonists specific to the gut.
57
What is the clinical significance of morphine's effect on the anal sphincter?
Increases tone leading to potential urinary retention especially in intoxicated patients.
58
How do opioids affect histamine release?
Trigger release from mast cells causing bronchoconstriction hypotension and urticaria.
59
What is the effect of opioids on the cardiovascular system at therapeutic doses?
Minimal effect but high doses can cause hypotension and bradycardia.
60
What is the role of enkephalins in pain modulation?
Act on μ and δ receptors modulating pain and stress responses.
61
How do opioids interact with G-protein coupled receptors?
Inhibit adenylyl cyclase activate MAP kinase pathways and influence ion channel activity.
62
What is the clinical use of fentanyl?
Management of severe pain often in surgical or chronic pain settings.
63
How do opioids cause euphoria?
Through stimulation of μ receptors and the ventral tegmentum.
64
What are the effects of opioid-induced hyperalgesia?
Increased sensitivity to pain despite opioid use.
65
How does naloxone affect opioid-induced respiratory depression?
Reverses it by blocking opioid receptors restoring normal respiratory function.