Opiates and Opioids Flashcards

1
Q

Define nociception

A

ability to sense or perceive pain

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2
Q

Define analgesia

A

absence of pain in response to stimuli that are normally painful without loss of consciousness

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3
Q

Define hyperalgesia

A

extreme responsiveness to stimuli that are usually only modestly painful

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4
Q

Define allodynia

A

pain caused by a stimulus not normally evoking pain

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5
Q

Define the path of pain transmission

A

detection of painful stimulus at nociceptor > sensory afferents (Ad or C) > Dorsal root ganglion > spinal cord > spinothalamic tracts in brain > perception

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6
Q

What is Substance P?

A

an important neurotransmitter in pain from DRG afferents at tissue and level of spinal cord

  • pro-inflammatory
  • detected by tachykinin receptors (NK1, NK3)
  • activates pain pathway
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7
Q

How does acupuncture alleviate pain?

A

activates endogenous pathways that help suppress pain

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8
Q

What drug classes have a peripheral site of analgesic drug action?

A

NSAIDs and corticosteroids; act on the nociceptor

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9
Q

What drug classes have a nerve block site of analgesic drug action?

A

Local anesthetics; acts on the sensory afferents

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10
Q

What drug classes have an epidural site of analgesic drug action?

A

Opioids, alpha2 agonists, NMDA antagonists, local anesthetics; act at the level of the spinal cord

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11
Q

What drug classes have a CNS site of analgesic drug action?

A

Alpha2 agonists, NMDA antagonists, opioids, cannabinoids

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12
Q

What three opiates are used clinically?

A

morphine, codeine, and papaverine

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13
Q

What is the difference between opiates and opioids?

A

Opiates are naturally occurring alkaloids derived from opium (e.g. morphine, codeine, papaverine)

Opioids are drugs/substances that bind opioid receptors; used for their pain-relieving effects; includes natural and synthetic compounds

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14
Q

Which DEA-class of drugs have no currently accepted medical use?

A

Class I (heroin, bufotenine)

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15
Q

What are endogenous opioids?

A

“gut-brain” peptides released in response to painful stimuli, prolonged physical exertion, or during a fight or flight response that activate endogenous opioid receptors

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16
Q

What are the four classes of endogenous opioids?

A
  1. Enkephalins (met & Leu) - pentapeptides
  2. Endorphins (beta) - larger (31 amino acids)
  3. Dynorphins (A & B) - intermediate size
  4. Endomorphins (1 & 2) - tetrapeptides w/ mu specificity
17
Q

What are the CNS effects of endogenous opioids?

A

analgesia, nausea/vomiting (dogs), mood alteration, depressed breathing, sedation

18
Q

What are the GI effects of endogenous opioids?

A

constipation (decr propulsive activity)

19
Q

What are the cardiovascular effects of endogenous opioids?

A

cardiac depression, hypotension

20
Q

What are the 3 major receptors acted on by opioids?

A

Mu, kappa, and delta

21
Q

What G-protein do opioid receptors associate with?

A

Gi

22
Q

What are the general effects of opioids?

A

decrease the activities of the brain, GI system, and CVS

23
Q

Describe a mixed agonist-antagonist

A

a drug that stimulates some receptor subtypes, but antagonizes other subtypes of the same receptor family

24
Q

Describe the analgesic properties of opioids

A
  • decrease pain sensation without loss of consciousness
  • Requires two levels of action:
    • Spinal cord (modulation)
    • Supraspinal level (perception)
25
Q

Describe the spinal cord modulation effects of opioids that result in analgesia

A
  • decr substance P release from sensory afferents
  • decr postsynaptic actions of substance P
26
Q

Describe the supraspinal level (perception) effects of opioids resulting in analgesia

A
  • decr affective response to pain
  • decr fear/anxiety assoc. w/ pain
27
Q

Describe the sedative properties of opioids

A
  • initial calming effect that may be followed by sleep, coma, and then death
  • additive depressive effects when used with other CNS depressants
    • decreases anesthetic requirement in most animals
28
Q

Describe the ventilatory effects of opioids

A
  • doses that causes analgesia also cause ventilatory depression in most species
    • opioids depress brainstem sensitivity to PCO2 > drive to breath decreases
29
Q

Describe the emetic/nausea effects of opioids

A

Caused by triggering of chemoreceptor trigger zone in brainstem; species differences- dogs sensitive

30
Q

Do opioids have cough suppressant effects?

A

yes; species differences

  • dogs = codeine, butorphonal
  • cats = butorphonal
31
Q

What are the effects of opioids on the pupils?

A

Species-specific effect

  • dogs, rabbits, humans = miosis
  • cats, horses, sheep, non-human primates = mydriasis
  • birds = no change
32
Q

What type of effects do opioids have on mood?

A

variable (euphoria/dysphoria)

33
Q

What effects do opioids have on the GI tract?

A

GI stasis - involves CNS mechanisms and actions of the GI system, decreased propulsion

34
Q

What are the effects of opioids on the cardiovascular system?

A

cardiovascular depression; mild decr in heart functions

  • decr HR in dogs
  • decr blood pressure
35
Q

Is opioid tolerance common?

A

yes; involves CNS & peripheral organs

36
Q

What are the symptoms of opioid toxicity?

A

In dogs:

  • depressed ventilation
  • fixed pinpoint pupils
  • coma or marked CNS depression

Tx: naloxone and supportive therapy

37
Q

What are the general precautions for opiod use?

A
  • felines
  • pregnancy (decr newborn respiration)
  • shock (congestive heart failure)
  • pulmonary dz
  • liver dz (metabolized in liver)
38
Q

What are the signs of Opioid Withdrawal Syndrome?

A
  • anxiety
  • hypertension
  • nausea
  • diarrhea
  • dysphoria