Opioids Flashcards

1
Q

What are the pharmacological effects of opioids?

A
  • analgesia
  • sedation
  • bradycardia
  • excitation
  • respiratory depression
  • nausea and vomiting
  • decreased GI motility
  • various urinary effects
  • antitussive?
  • minimal effect on inotrophy
  • effects on the pupil, miosis (dogs), mydriasis (cats)
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2
Q

What opioid receptors are found in the brain and spinal cord?

A
  • mu
  • kappa
  • delta
  • NOP (nociception opioid peptide) receptor
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3
Q

Whatare the three families involved in the endogenous opioid system that has naturally occuring peptides?

A
  • beta endorphin
  • leucine (leu)- and methionine (met) - enkephalins
  • dynorphins
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4
Q

What are neurotransmitters?

A

naturally occuring peptides

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5
Q

What is the endogenous ligand for the nociception opioid peptide?

A

nociceptin

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6
Q

What location is the delta receptir found?

A

brain and peropheral sensory neurones

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7
Q

What is the function of the delta receptor?

A
  • analgesia
  • antidepressant effects
    -convulsive effects
  • physical dependence
  • may modulate mu-opioid receptor-mediated respiratory depression
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8
Q

What is the location of the kappa receptor?

A

brain, spinal cord, peripheral sensory neurones

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9
Q

What are the functions of the kappa receptor?

A
  • analgesia
  • anticonvulsant effects
  • depression
  • dissociative/hallucinogenic effects
  • diuresis
  • miosis
  • dysphoria
  • neuroprotection
  • sedation
  • stress
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10
Q

What is the location of the mu receptor?

A

brain, spinal cord, periperal sensory neurones

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11
Q

What is the function of mu1 receptor?

A

analgesia and physical dependence

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12
Q

What is the function of the mu2 receptor?

A

respiratory depression, miosis, euphoria, reduced GI mortility, physical dependence

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13
Q

What is the function of the mu3 receptor?

A

possible vasodilation

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14
Q

What do full mu agonists do?

A

bind to and activate a receptor with the maximum response that an agonist can elicit at that receptor

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15
Q

What do partial agonists do?

A

bind to and activate a receptor but only have partial efficacy, even if they bind to all receptors

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16
Q

How will we know how the opioid will act?

A
  • what receptors/receptor subtypes they have
  • mechanism of action at these receptors (full or partialagonists, antagonitst)
  • pharmacokinetics
  • species differences
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17
Q

What are examples of a full mu agonist?

A

methadone and fentanyl

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18
Q

What are examples of partial agonists?

A

buprenorphine

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19
Q

What are examples of a mixed agonist-antagonist?

A

butorphanol

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20
Q

What are examples of antagonist?

A

naloxone

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21
Q

What is potency

A

how much you need to get an effect

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22
Q

What does efficacy meam?

A

how much effect you get

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23
Q

What can happen if you give pethidine IV?

A

allergic reaction

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24
Q

How can opioids be administered?

A

intramuscular, intravenous, subcutaneous, oral transmucosal/buccal, transdernal and epidural/spinal

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25
Q

What are the advantages of IV route?

A

rapid onset of action, reliable uptake, painless

26
Q

What are the advantages of intramuscular route

A

reliable uptake

27
Q

What are the advantages of subcutaneous route?

A

easy to perform

28
Q

What are the advantages of oral transmucosal?

A

easy to perform

29
Q

What are the advantages of transdermal route?

A

good for chronic use

30
Q

What are the advantages of epidural/spinal route?

A

very effective analgesia for the right cases

31
Q

What are the disadvantages of intravenous route?

A

need IV access

32
Q

What are the disadvantages of intramuscular route?

A

painful- particularly large volumes

33
Q

What are the disadvantages of subcutaneous route?

A

unreliable uptake

34
Q

What are the disadvantages of oral transmucosal route?

A

only certain opioids (cat and buprenorphine)

35
Q

What are the disadvantages of transdermal route?

A

no licensed products

36
Q

What are the disadvantages epidural/spinal route?

A

no licensed opioids for this, technically difficult

37
Q

What does the onset of action depend on?

A
  • route of administration
  • how quickly you see effect
  • IV quicker than IM because need to get into blood stream
  • peak effect when all drug is sitting on a receptor
  • how quickly the drug is removed from the receptors
38
Q

What drugs are ultra-short acting?

A

fentanyl, alfentanil, sufentanil, remifentanil

39
Q

What are short acting opioids?

A

butorphanol, pethidine

40
Q

What are medium-acting opioids?

A

methadone and morphine

41
Q

What are longer acting opioids?

A

buprenorphine

42
Q

What is the duration of action for fentanyl

A

20 minutes

43
Q

When might you use fentanyl?

A

during high stimulus part of surgery in addition to other opioid analgesia

44
Q

When might you use a short acting opioid?

A

pre-med or sedative combo, multimodal analgesia regimen

45
Q

When would you use medium and longer acting opioids?

A

part of multimodal analgesia regimen, postoperative analgesia, painful patient

46
Q

What can generally affect duration of action?

A

higher dose, duration of action increased

47
Q

How can you increase duration of action?

A
  • oral sustained release formulations
  • IM or SC pellets, insoluble form, adding vasoconstrictor
  • transdermal delivery systems
48
Q

What are common misconceptions with opioids?

A
  • cats become manic
  • cannot be re-dosed within their expended duration of action
  • respiraotyr depression can occur
  • cannot be combined with other classes of analgesic drug
49
Q

Why might a cat become manic due to opioid admin/

A

if given as pre-med. high dose or pain free cat

50
Q

What are the useful clinical effects of opioids?

A

analgesia, sedation, cough suppression

51
Q

Why do side effects occur?

A

due to potency

52
Q

What is the antagonist for opioids?

A

naloxone

53
Q

What are the two main side efeects we worry about with opioid administration?

A

respiratory depression and bradycardia

54
Q

How can bradycardia be treated?

A

atropine or glycopyrrolate

55
Q

What are some less worrysome side effects of opioids?

A
  • sedation when not desired
  • excitation
  • gut stasis
  • nausea and vomiting
56
Q

What is the order of analgesia efficacy?

A
  1. fentanyl (most)
  2. methadone + morphine
  3. pethidine
  4. buprenorphine
  5. butorphanol (least)
57
Q

What are the effects of administering fentanyl?

A
  • some respiratory depression when given during anaesthesia
  • induce bradycardia
  • useful as CRI as short acting
58
Q

What are the effects of giving methadone?

A
  • reduced nausea + vomiting compared to morphine
  • no concern for histamine release given IV
  • minimal CVS and respiratory side effects
  • NMDA receptor antagonist effects
59
Q

What happens when pethidine is given?

A
  • short acting
  • large volume needed so painful IM
  • histamine release of given IV
60
Q

What happens when buprenorphine is given?

A
  • good in cats
  • not very effective suncut
  • delayed onset of action
  • painful on injectionand not palatable when given oral transmucosally
61
Q

What happens when butorphanol is given?

A
  • analgesia short lived, higher dosses needed
  • may confound subsequent full mu-agonist
  • good sedation
62
Q

How should you plan perioperative analgesia?

A
  • base off patients current and anticipated pain
  • provide analgesia before it is needed
  • pain score regularly
  • consider other analgesics