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Pharmacology > Opioids > Flashcards

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
Q

What is the mechanism of action of μ-opioid receptor agonists in the spinal cord?

A

Decreasing the release of substance P and inhibiting excitatory transmitter release.

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26
Q

What is the clinical significance of morphine’s effect on the biliary tract?

A

Increases pressure due to gall bladder contraction and biliary sphincter constriction contraindicated in biliary colic.

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27
Q

What are the pharmacological actions of strong opioid agonists like morphine?

A

Analgesia, euphoria, sedation, respiratory depression, cough suppression, miosis, nausea, constipation.

28
Q

How do moderate/low opioid agonists differ from strong agonists?

A

They are less potent and often used in combination with other analgesics.

29
Q

What are the effects of mixed agonist-antagonist opioids?

A

Provide analgesia with a lower risk of dependence and respiratory depression.

30
Q

Name a partial opioid agonist.

A

Buprenorphine.

31
Q

What is the role of endogenous opioid peptides in pain modulation?

A

Inhibit synaptic transmission and are released in response to noxious stimuli.

32
Q

How does naloxone reverse opioid effects?

A

By blocking opioid receptors reversing respiratory depression and analgesia.

33
Q

What is the clinical use of methadone?

A

Treatment of opioid dependence and chronic pain management.

34
Q

What is the effect of opioid agonists on the cough reflex?

A

Suppress the cough reflex with codeine being a common antitussive.

35
Q

What is tramadol and its dual mechanism of action?

A

A weak centrally acting opioid that also inhibits norepinephrine and serotonin reuptake.

36
Q

What are the primary symptoms of opioid withdrawal?

A

Agitation anxiety muscle aches increased tearing insomnia runny nose sweating yawning.

37
Q

How is acute opioid toxicity managed?

A

Administering opioid antagonists like naloxone and supportive care.

38
Q

What is the function of the nociceptive pathway?

A

Processing and transmitting pain signals from the periphery to the brain.

39
Q

Name two novel opioids.

A

Oliceridine and PZM21.

40
Q

How does opioid use affect fertility in females?

A

Inhibits cilia motility in the ovary tubes potentially leading to sterility.

41
Q

What are the effects of opioids on the respiratory system?

A

Respiratory depression and increased risk of hypoxia.

42
Q

What is the primary effect of kappa opioid receptor activation?

A

Analgesia at the spinal level sedation miosis dysphoria hallucinations.

43
Q

What is the action of dynorphins?

A

Primarily act on κ-receptors modulating pain and emotional responses.

44
Q

How do opioids influence neurotransmitter release?

A

Inhibit release by hyperpolarizing nerve terminals and reducing calcium influx.

45
Q

What is the role of naloxone in opioid overdose?

A

Reverses opioid-induced respiratory depression and other effects.

46
Q

How do serotonin and norepinephrine influence pain perception?

A

They modulate descending inhibitory pathways affecting pain transmission.

47
Q

What is the role of endogenous opioids in stress response?

A

They modulate pain and stress responses through receptor activation.

48
Q

What is the clinical use of buprenorphine?

A

Management of opioid dependence and moderate to severe pain.

49
Q

How do opioids affect gastrointestinal motility?

A

Decrease motility and increase smooth muscle tone leading to constipation.

50
Q

What is the primary mechanism of opioid-induced euphoria?

A

Stimulation of the ventral tegmentum and μ receptors.

51
Q

How does opioid use lead to respiratory depression?

A

Reduces the sensitivity of respiratory center neurons to CO2.

52
Q

What is the effect of opioid antagonists like naloxone on placebo analgesia?

A

Reduce placebo analgesia by blocking endogenous opioid peptides.

53
Q

What is the role of μ-opioid receptors in pain relief?

A

Mediating analgesia euphoria sedation respiratory depression and dependence.

54
Q

How do opioids cause sedation?

A

By additive effects with other CNS depressants and influencing neurotransmitter release.

55
Q

What are the primary side effects of opioid use?

A

Constipation nausea vomiting respiratory depression euphoria miosis.

56
Q

How is opioid-induced constipation managed?

A

Using laxatives stool softeners or opioid receptor antagonists specific to the gut.

57
Q

What is the clinical significance of morphine’s effect on the anal sphincter?

A

Increases tone leading to potential urinary retention especially in intoxicated patients.

58
Q

How do opioids affect histamine release?

A

Trigger release from mast cells causing bronchoconstriction hypotension and urticaria.

59
Q

What is the effect of opioids on the cardiovascular system at therapeutic doses?

A

Minimal effect but high doses can cause hypotension and bradycardia.

60
Q

What is the role of enkephalins in pain modulation?

A

Act on μ and δ receptors modulating pain and stress responses.

61
Q

How do opioids interact with G-protein coupled receptors?

A

Inhibit adenylyl cyclase activate MAP kinase pathways and influence ion channel activity.

62
Q

What is the clinical use of fentanyl?

A

Management of severe pain often in surgical or chronic pain settings.

63
Q

How do opioids cause euphoria?

A

Through stimulation of μ receptors and the ventral tegmentum.

64
Q

What are the effects of opioid-induced hyperalgesia?

A

Increased sensitivity to pain despite opioid use.

65
Q

How does naloxone affect opioid-induced respiratory depression?

A

Reverses it by blocking opioid receptors restoring normal respiratory function.

Pharmacology (8 decks)

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