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Pharmacology > Chapter 20: Opioid Analgesics > Flashcards

Chapter 20: Opioid Analgesics Flashcards

1
Q

opioids act at several points throughout the pain pathway, what is a disadvantage of this?

A

can cause a wide variety of ADRs

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2
Q

t/f opioids have been used as analgesics for thousands of years

A

t

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3
Q

what is an example of a naturally occurring opioid?

A

morphine

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4
Q

codeine is isolated from the ___

A

opium poppy

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5
Q

oxycodone, buprenorphine and heroin are all ____ forms of opioids

A

semi-synthetic

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6
Q

___ is the prototypic opioid

A

morphine

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7
Q

fentanyl and methadone are ___ type opioids

A

fully synthetic

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8
Q

what are the 3 types of opioid receptors?

A

mu, delta, and kappa

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9
Q

all opioid receptors are coupled to either ___ or ___ g proteins

A

Gi/Go

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10
Q

what are the endogenous agonists of opioid receptors?

A

endorphins, enkephalins, and dynorphins

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11
Q

endorphins act primarily on ___ opioid receptors

A

Mu

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12
Q

enkephalins act primarily on ___ opioid receptors

A

delta

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13
Q

dynorphins act primarily on ___ opioid receptors

A

kappa

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14
Q

the ___ opioid receptor is the most clinically targeted for pain relief

A

mu

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15
Q

peripheral nerves sense pain, carries it to the spinal cord, where ___ and ___ are released

A

glutamate and neuropeptides

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16
Q

release of glutamate from the presynaptic neuron causes __ in the postsynaptic neuron

A

depolarization by opininf Na channels and AP to be carried to the brain

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17
Q

what happens when mu opioid receptors are activated in the periphery?

A

opens K channels, causing hyper polarization, helping to stop the AP that would cause the brain to recognize the pain

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18
Q

in the spinal cord, mu receptors are located on the ___ neuron and their activation prevents the opening of ___ channels with results in a decrease in ___ release

A

presynaptic; Ca; NT

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19
Q

activation of mu receptors on postsynaptic neurons causes the ____ channels to be open longer, causing the neuron to become ___ and require a stronger stimulus to activate

A

K; hyperplarize

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20
Q

opioids cause the closing of ___ channels and the opening of ___ channels

A

ca; K

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21
Q

outline the anatomical pathway of ascending pathways

A

primary afferent neurons receives pain stimuli, spinal cord, brain stem, cortex for processing

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22
Q

opioids cause an increase in the DA ____ pathway

A

reward

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23
Q

opioid modulation of mu receptors in the cortex likely plays a role in dampening the perception of ____ attached to painful stimuli

A

emotion

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24
Q

pain stimuli are transmitted to the ___ horn of the spinal cord

A

dorsal

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25
Q

t/f in the descending pathway, stimuli are processed in the cortex and signal is sent back to the periphery

A

t

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26
Q

stimulation of mu receptors enhances the descending inhibitory signals by reducing ___ release into the inhibitory circuit

A

GABA

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27
Q

t/f inhibiting signals from moving from the spinal cord helps prevent pain

A

true

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28
Q

stimulation of mu receptors in the ___ enhances inhibition of signal in the spinal cord

A

midbrain

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29
Q

mu receptors in the __ are responsible for autonomic function

A

midbrain

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30
Q

mu receptors in the ___ are responsible for baroreceptor reflex and respiration

A

medulla

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31
Q

bc mu receptors are present in many brain regions, opioids can have systemic effects such as :

A

sedation, respiratory suppression, nausea, decreased GI motility, CV (bradycardia and hypotension)

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32
Q

t/f sedative effects of opioids are significant and shouldn’t be mixed with other drugs that have sedative effects

A

t

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33
Q

should benzodiazepams / alcohol be used when using opioids?

A

no, too much sedative

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34
Q

what is the most serious and life threatening effect of opioids that occurs in OD?

A

respiratory suppression

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35
Q

Naloxone MOA

A

competitive antagonist of mu opioid receptor, removing opioid during overdose to restore respiration (available as nasal spray)

36
Q

Naloxone reverses the effects of opioid OD within ___ (time)

A

2-3 minutes

37
Q

what is the duration action for naloxone?

A

short, 1-2 hours (important to monitor pt incase opioid still present after this time)

38
Q

naltrexone has a half life of ___ and onset time of ___

A

10 hrs; 30 min-1hr

39
Q

what is the role of naltrexone in OD treatment?

A

used once respiratory suppression has been reversed by naloxone and acts to prevent reoccurrence should naloxone be cleared before the opioid

40
Q

the full agonists: ___, ___ , ___, and ___ all have high potency at the mu receptor and strong analgesic activity

A

morphine, oxycodone, fentanyl, methadone

41
Q

fantanyl is approximately ____ x more potent than morphine

A

100

42
Q

oxycodone and methadone have similar potency to morphine, but have higher ___

A

oral bioavailability

43
Q

buprenorphine is a agonist at ___opioid receptors and an antagonist at __ and ___ opioid receptors, making it a mixed opioid receptors

A

mu; kappa; delta

44
Q

it is not well known, but it is thought that blocking kappa and delta opioid channels reduces risk of ___

A

opioid dependence / abuse

45
Q

codeine is known as a ___mu receptor opioid ___ agonist

A

weak; partial

46
Q

the majority of the analgesic effects of codeine come from its biotransformation to ___

A

morphine

47
Q

what is the benefit of administering codeine with caffeine and acetaminophen?

A

al these together have a synergistic effect on pain lowering, so less opioid is needed

48
Q

how does caffeine in Tylenol 3 help reduce risk of addiction?

A

offsets sedative effect

49
Q

a small amount of codeine is metabolized by the ___ enzyme to morphine in the liver

A

CYP 2d6

50
Q

codeine has __% oral bioavialbility and ___% is metabolized to morphine

A

50, 10

51
Q

t/f there is a popular polymorphism of the CYP2d6 enzyme, so different groups of people may turn codeine to morphine to a greater or lesser extent than expected

A

t

52
Q

give 2 examples of opioids that rely less on CYP2D6 metabolism

A

morphine and oxycodon

53
Q

which is more potent and has a higher oral bioavailability, morphine or oxycondone?

A

oxycondone

54
Q

oxycodone is primarily metabolized by the ___ enzyme

A

CYP3A4

55
Q

oxycodone is indicated for what pain level?

A

severe (7-10)

56
Q

small doses of oxycodone in combination w/ non-opioid analgesics are indicated for what level of pain?

A

moderate

57
Q

___ is the brand name for the combination of oxycodone and acetaminophen

A

percocets

58
Q

t/f Percocet was discontinued in Canada (still exists as endocet etc)

A

t

59
Q

___ is the most well known brand name of oxycodone

A

oxycontin

60
Q

oxycontin is in a ___ type formulation which allows for __

A

controlled release; longer action

61
Q

what is the duration of action for oxycontin?

A

12hrs

62
Q

t/f their is a lot of controversy around oxycontin and possibly paying prescribers

A

t

63
Q

what is the issue with the CR formulation of oxycontin by Perdue pharma?

A

easily crushed which causes immediate high, especially if dissolved and injected

64
Q

if crushed oxycontin is injected, it has a similar effect as __

A

heroin

65
Q

explain the formulation of Oxyneo form of oxycodone

A

difficult to crush and not water soluble, making it harder to abuse

66
Q

t/f very little (micrograms) of fentanyl is needed to achieve analgesic

A

t

67
Q

what is the indication for fentanyl?

A

severe pain in patients tolerant to other opioids (ex: cancer pain)

68
Q

what is opioid tolerance?

A

loss of effectiveness even with repeated dosing when used for extended period of time

69
Q

t/f opioid tolerant patients are also more resistant to respiratory suppression

A

t

70
Q

t/f the exact mechanism of opioid tolerance is unknown

A

treu

71
Q

what altered pharmacokinetics may be involved in opioid tolerance?

A

altered metabolism, increased clearance

72
Q

how might altered opioid receptor signalling be involved in opioid tolerance>

A

receptor desensitization, altered downstream signalling pathways

73
Q

how might altered neuronal circuitry be involved in opioid tolerance?

A

increased depression of NMDA receptors

74
Q

fentanyl is often given as a ___ formulation because it has poor oral bioavailability

A

parenteral

75
Q

for rapid onset of analgesic, ___ and __ formulations of fentanyl may be used

A

SL and IV

76
Q

___ formulations of fentanyl are useful to allow slow absorption over many hours to get stable long-lasting analgesic effect

A

transdermal patch

77
Q

t/f fentanyl is contraindicated in patients who do nat have opioid tolerance / are opioid naive

A

t

78
Q

when opioids are abused, it is typically the ___ at the inset of the dose that is desired by the patient

A

euphoric high

79
Q

the rapid decrease in opioids that have a quick onset and short duration can cause a ____ that leads to drug-seeking behaviour

A

“crash”

80
Q

drugs that have a wearing off effect where a patient may experience pain between dosing can lead to ___

A

overuse and drug seeking and tolerance

81
Q

what types of drugs are best for management of opioid use disorder>

A

opioid agonists with long duration of action and slower onset to reduce addictive qualities while also helping prevent severe withdrawal

82
Q

what is a downside of methadone?

A

it is a full agonist of mu and can itself be abused

83
Q

a specific formulation of buprenorphine called ___ includes a small dose of naloxone to discourage abuse

A

suboxone

84
Q

how does the addition of naloxone in suboxone discourage abuse?

A

if excess is taken in an attempt to get high, the naloxone will antagonize these effects

85
Q

buprenophine is a ___ of the mu receptor that may help its taper off opioids while reducing withdrawal symptoms

A

partal agonsit

Pharmacology (49 decks)

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