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
What are the advantages of IV route?
rapid onset of action, reliable uptake, painless
26
What are the advantages of intramuscular route
reliable uptake
27
What are the advantages of subcutaneous route?
easy to perform
28
What are the advantages of oral transmucosal?
easy to perform
29
What are the advantages of transdermal route?
good for chronic use
30
What are the advantages of epidural/spinal route?
very effective analgesia for the right cases
31
What are the disadvantages of intravenous route?
need IV access
32
What are the disadvantages of intramuscular route?
painful- particularly large volumes
33
What are the disadvantages of subcutaneous route?
unreliable uptake
34
What are the disadvantages of oral transmucosal route?
only certain opioids (cat and buprenorphine)
35
What are the disadvantages of transdermal route?
no licensed products
36
What are the disadvantages epidural/spinal route?
no licensed opioids for this, technically difficult
37
What does the onset of action depend on?
- 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
What drugs are ultra-short acting?
fentanyl, alfentanil, sufentanil, remifentanil
39
What are short acting opioids?
butorphanol, pethidine
40
What are medium-acting opioids?
methadone and morphine
41
What are longer acting opioids?
buprenorphine
42
What is the duration of action for fentanyl
20 minutes
43
When might you use fentanyl?
during high stimulus part of surgery in addition to other opioid analgesia
44
When might you use a short acting opioid?
pre-med or sedative combo, multimodal analgesia regimen
45
When would you use medium and longer acting opioids?
part of multimodal analgesia regimen, postoperative analgesia, painful patient
46
What can generally affect duration of action?
higher dose, duration of action increased
47
How can you increase duration of action?
- oral sustained release formulations - IM or SC pellets, insoluble form, adding vasoconstrictor - transdermal delivery systems
48
What are common misconceptions with opioids?
- 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
Why might a cat become manic due to opioid admin/
if given as pre-med. high dose or pain free cat
50
What are the useful clinical effects of opioids?
analgesia, sedation, cough suppression
51
Why do side effects occur?
due to potency
52
What is the antagonist for opioids?
naloxone
53
What are the two main side efeects we worry about with opioid administration?
respiratory depression and bradycardia
54
How can bradycardia be treated?
atropine or glycopyrrolate
55
What are some less worrysome side effects of opioids?
- sedation when not desired - excitation - gut stasis - nausea and vomiting
56
What is the order of analgesia efficacy?
1. fentanyl (most) 2. methadone + morphine 3. pethidine 4. buprenorphine 5. butorphanol (least)
57
What are the effects of administering fentanyl?
- some respiratory depression when given during anaesthesia - induce bradycardia - useful as CRI as short acting
58
What are the effects of giving methadone?
- reduced nausea + vomiting compared to morphine - no concern for histamine release given IV - minimal CVS and respiratory side effects - NMDA receptor antagonist effects
59
What happens when pethidine is given?
- short acting - large volume needed so painful IM - histamine release of given IV
60
What happens when buprenorphine is given?
- good in cats - not very effective suncut - delayed onset of action - painful on injectionand not palatable when given oral transmucosally
61
What happens when butorphanol is given?
- analgesia short lived, higher dosses needed - may confound subsequent full mu-agonist - good sedation
62
How should you plan perioperative analgesia?
- base off patients current and anticipated pain - provide analgesia before it is needed - pain score regularly - consider other analgesics