SM_236a, 240a: Pharmacology, Opioids, and Pain Concepts I and II Flashcards Preview

MSK/Derm > SM_236a, 240a: Pharmacology, Opioids, and Pain Concepts I and II > Flashcards

Flashcards in SM_236a, 240a: Pharmacology, Opioids, and Pain Concepts I and II Deck (43)
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1

Describe the opioid receptors

Opioid receptors

  • Mu, kappa, delta
  • One gene codes for each
  • Subtypes come from splice variants
  • All involved in brain, spinal, GI sites

2

The opioid receptors are _____, _____, and _____

The opioid receptors are mu, happa, and delta

3

Mu opioid receptor is responsible for ____, ____, ____, ____, ____, ____, and ____

Mu opioid receptor is responsible for analgesia, euphoria, dependence, respiratory depression, miosis, GI effects, and pruritis

 

(named after morphine)

4

Kappa opioid receptor is responsible for ____, ____, and ____

Kappa opioid receptor is responsible for mild analgesia, less respiratory depression, and pyschomimetic effects (unlike euphoria)

5

Delta opioid receptor function is ____

Delta opioid receptor function is unknown

6

Opioid receptors are found in the ____, ____, and ____

Opioid receptors are found in the brain, spinal cord, and gut

7

Describe the location of opioid receptors in the brain

  • Amygdala - emotion
  • Brainstem - ventilation
  • Area postrema - vomiting
  • Periaqueductal gray - inhibitory pathway

 

(gate control theory, periaqueductal gray inhibits pain transmission in dorsal horn via a relay in the rostral ventral medulla)

8

Opioid receptors work via ____, which ____, ____, ____, and ____

Opioid receptors work via G receptor proteins, which inhibit cellular adenylyl cyclase, increase K+ currents and decrease Ca2+ currents, cause hyperpolarization, and decrease nociceptive transmission

9

Opioids work on ____ and ____ receptors

Opioids work on presynaptic and postsynaptic receptors

10

Opioids activate the ____, triggering ____ and releasing ____

Opioids activate the periaqueductal gray, triggering the descending inhibitory pathways and releasing endorphins

 

 

(descending pathway modulates pain in transmission in the ascending pathway)

11

Opioids ____ the GABA neuron, which allows for ____ of the pain inhibitory neuron

Opioids inhibit the GABA neuron, which allows for activation of the pain inhibitory neuron

12

Opiate is a _____

Opiate is a drug derived from opium

13

Opioid is ____

Opioid is all drugs, both natural and synthetic, that bind to opioid receptor

14

Narcotic is ____, ____, and ____

Narcotic is any substance that induces sleep, acts on opioid receptors, and any illicit substance

15

Opioids that are agonists are _____ and include _____, _____, and _____

Opioids that are agonists are mu receptor agonists and include morphine, merepiridine, and hydromorphone

16

Opioids that are antagonists are _____ and include _____ and _____

Opioids that are antagonists are mu receptor antagonists and include naloxone and naltrexone

17

Opioids that are agonist/antagonists are _____ and include _____ and _____

Opioids that are agonist/antagonists are kappa agonists / mu antagonists and include butorphanol and nalbuphine

18

Opioids that are partial agonists are _____ and _____ and include _____

Opioids that are partial agonists are partial mu agonists with high affinity and meaningless kappa antagonists and include buprenoprhine

19

Describe opioids that are agonist/antagonists

Agonist/antagonist opioids

  • Analgesia is kappa mediated
  • Weak mu receptor antagonist 
  • Ceiling effect
  • Less GI side effects
  • Kappa: less respiratory depression / sedation / euphoria but makes person nuts
  • Can trigger withdrawal so do not use in opioid tolerant patient
  • Can reverse opioid side effects at low dose

 

20

Describe opioids that are partial agonists

Partial agonist opioids

  • Only partial mu agonist
  • Ceiling effect for agonism
  • Binds mu with high affinity: higher than most opioids, prevents other opioids from binding, makes naloxone reversal difficult in overdose
  • Current use: opioid maintenance, not so much for chronic pain

21

Partial agonist opioids are used for ____

Partial agonist opioids are used for opioid maintenance

22

Describe neurologic effects of opioids

Neurologic effects of opioids

  • Analgesia: supraspinal and spinal cord level, not reliably associated with loss of consciousness, better for nociceptive pain (pain caused by stimulation of nociceptive receptors) than neuropathic pain (pain caused by damaged neural structures)
  • Miosis (pinpoint pupil): seen with all opioid agonists
  • No tolerance to this: useful in overdose diagnosis, even in tolerant addicts

23

____ is the major way that opioids kill

Respiratory depression is the major way that opioids kill

 

(hold if sedated)

24

Describe respiratory effects of opioids

Respiratory effects of opioids

  • Therapeutic effects: prevent hyperventilation from pain and anxiety, opioids can be used for their antitussive actions, can help avoid increases in bronchomotor tone in asthma
  • Adverse effect: respiratory depression is most serious, activation of mu opioid receptor in caidal medullary raphe region inhibits the ventilatory response to hypercapnia

25

Direct cardiac actions are _____ than for other inhalational or IV anesthetics

Direct cardiac actions are lower than for other inhalational or IV anesthetics

26

GI effects of opioids include ____ and ____

GI effects of opioids are slowed peristalsis and nausea/vomiting

 

  • Slowed peristalsis: via enteric NS opioid receptors
  • Nausea/vomiting: via chemoreceptor trigger zone

27

Tolerance to opioids does NOT include ____ and ____

Tolerance to opioids does NOT include miosis and constipation

 

(tolerant to euphoria, sedation, analgesia, N/V, respiratory depression)

28

Opioid withdrawal contains symptoms of ____

Opioid withdrawal contains symptoms of sympathetic overdrive

 

  • Anxiety, insomnia, diaphoresis, yawning, rhinorrhea, lacrimation
  • HTN, tachycardia
  • Hyperventilation
  • Mydriasis
  • Also diarrhea and abdominal cramps

29

Opioid overdose symptoms include ____, ____, and ____

Opioid overdose symptoms include respiratory depression / arrest, sedation or unresponsiveness, and miosis

 

 

(ABCs - support ventilation, use naloxone as the antagonist)

30

List the agonist, antagonist, agonist/antagonist, and partial agonist opioids

Opioids

  • Agonists: morphine, codeine, hydrocodone, oxycodone, merperidine, fentanyl, hydromorphone, methadone, tramadol
  • Antagonists: naloxone, naltrexone
  • Agonist/antagonist: nalbuphine
  • Partial agonist: buprenorphine

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