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Pharm > Pain Management: Opioids > Flashcards

Pain Management: Opioids Flashcards

1
Q

opiate

A

any of the narcotic alkaloids found in the poppy

including morphine, codeine, and thebaine.

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2
Q

opioid

A

any substance, endogenous or synthetic, that produces morphine-like actions which can be blocked by naloxone.

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3
Q

thebaine is the precursor to (3)

A

precursor for oxycodone, hydromorphone, oxymorphone

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4
Q

3 classes of opioids

A

morphine like
meperidine like
methadone like

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5
Q

derivatives of morphine: full agonists (3)

A

heroin
hydromorphone
oxymorphone

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6
Q

derivatives of morphine: partial agonists (2)

A

codeine

hydrocodone

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7
Q

opioid antagonist examples

A

naltrexone
naloxone
buprenorphine

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8
Q

mixed agonist antagonist

A

buprenorphine: acts as an agonist at one subtype of opioid receptor and an antagonist at another.

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9
Q

meperidine class

A

fentanyl
sufentanil
alfentanil

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10
Q

heroin is morphine with

A

two acetyl groups added to it

diacetyl morphine

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11
Q

the active ingredient in heroin is

A

morphine

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12
Q

why do people with opioid use disorder prefer heroin to morphine?

A

the 2 acetyl groups make heroin get into the brain faster than morphine does because it is much more lipophilic.

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13
Q

fentanyl vs heroin

A

more potent
more lipophilic
gets into the brain faster

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14
Q

which type of receptors do opioids work through?

A

G protein coupled receptors

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15
Q

true or false: endogenous and exogenous opioids both work through G protein coupled receptors

A

true

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16
Q

the opioid receptors

A

mewe
delta
kappa
ORL1

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17
Q

Which type of G protein do all 4 of the opioid receptors couple to?

A

Gi

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18
Q

opioid receptors are expressed both

A

pre synaptically an post synaptically

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19
Q

opioid receptors are coupled to calcium channels on which side of the synapse?

A

pre synaptic terminal

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20
Q

when calcium enters the pre synaptic terminal,

A

the axon terminal releases its neurotransmitter into the synaptic cleft.

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21
Q

what happens when you activate opioid receptors on pre synaptic terminals?

A

By activating the Gi protein, inhibiting calcium channels and keeping Ca from entering the pre synaptic terminal, which stops NT release. (halting pain transmission)

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22
Q

opioid receptors are coupled to potassium on which side of the synapse?

A

post synaptic side

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23
Q

Opioid receptors on the post synaptic side do what?

A

open potassium channels, causing K to flood out of the neuron.

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24
Q

pre synaptic and post synaptic mechanism act to

A

shut down pain transmission at the level of the synapse

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25
Q

By activating the opioid receptors on the presynaptic and postsynaptic terminals,

A

neuron is inhibited from transmitting a pain signal to another neuron

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26
Q

effects of opioids on the CNS(7)

A 
analgesia
euphoria
sedation
resp depression
cough depression
n/v
pupillary constriction
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27
Q

gold standard for treating moderate to severe pain, especially for nociceptive/inflammatory pain

A

opioids

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28
Q

because of ____, you can keep increasing the dose of opioids

A

tolerance

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29
Q

diagnostic tool for diagnosing an opioid overdose

A

pupillary constriction (armyosis)

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30
Q

opioid effects on GI tract (4)

A

increased tone, decreased motility
delay in gastric emptying
constipation
increase in intrabiliary pressure

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31
Q

opioids: pruritis

A

histamine release from mast cells

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32
Q

immune suppression: opioids

A

occurs with long term use.
Reduced hypothalamic pituitary adrenal (HPA) access and direct effects on immune cells themselves. immune cells have mew opioid receptors.

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33
Q

opioids: endocrinopathies

A

chronic long term use

decrease circulating sex hormones. can lead to osteroporosis

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34
Q

opioids: hyperalgesia

A

extreme response to pain from chronic prescribing of opioids

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35
Q

pure agonists: morphine like

Scientific name

A

phenanthrenes

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36
Q

example of morphine like pure agonists (phenanthrenes) 7

A 
morphine 
codeine
oxycodone
oxymorphone
hydromorphone
etorphine
dimorphine
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37
Q

examples of meperidine-like phenylpiperidines

A 
meperidine
fentanyl
alfentanyl
sufentanyl
remifentanyl
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38
Q

example of methadone-like (diphenylheptanes)

A

methadone
loperamide
tramadol
tapentadol

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39
Q

mixed agonists-antagonist (4)

A

buprenorphine
butorphanol
nalbuphine
pantazocine

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40
Q

buprenorphine and butorphanol

receptors

A

partial agonists at mew opioid receptors

antagonists at kappa opioid receptors

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41
Q

nalbuphine and pentazocine

Antagonize/agonize where?

A

antagonist at mew receptors

agonist at kappa receptors

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42
Q

mixed agonist-antagonist can be used

A

as analgesics

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43
Q

mainstay treatment for chronic moderate/severe nociceptive or inflammatory pain

A

pure agonists

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44
Q

opioids in neuropathic or functional pain

A

no efficacy

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45
Q

opioids having no clinically relevant ceiling effect to analgesia is related to

A

tolerance with repeated administration

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46
Q

true or false - morphine is superior to other mu agonists

A

false

variation exists among all pure agonist

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47
Q

MoA morphine

pre and post synaptic

A

activation of mu, kappa, and delta.

pre synaptic - block calcium channels and reduce NT release

post synaptic - open K channels, cause hyperpolarization of post synaptic neuron, leading to a decrease in cell firing.

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48
Q

PO bioavailability of morphine

A

25%

low

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49
Q

low bioavailability of morphine means

A

you have to give a much higher dose po to achieve the same effect that you would IV

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50
Q

M6G

A

the active metabolite of morphine

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51
Q

M3G

A

neurotoxic metabolite of morphine

if metabolism of morphine is changed, we have to be careful about M3G.

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52
Q

renal impairment and morphine

A

you will have a buildup of m6G and m3G.

toxicity.

53
Q

half-life of morphine

A

~2 hr

54
Q

adverse effects of morphine

A 
resp depression
N/V
dizziness
mental clouding
dysphoria
pruritis
constipation
urinary retention
hypotension
55
Q

Contraindications for morphine are related to (4)

A

impaired liver function
impaired response function
asthma
hypotension

56
Q

drug:drug interactions with morphine

A

any drugs with major significance relating to additive effects of morphine.

57
Q

half lives of oxy, hydromorphine, oxymorphone, codeine

A

relatively short

58
Q

which opioid is preferred for those with renal insufficiency and why?

A

hydromorphone as it does not have a lot of active metabolites.

59
Q

notable side effect of hydromorphone

A

chest pain

60
Q

codeine metabolism

A

phase I via CYP2D6

converts to morphine

61
Q

ultrametabolizers of codeine

A

cyp2d6
codeine poisoning

converting to morphine at dangerous levels
may be seen in breastfed infants

62
Q

meperidine class drug example

A

fentanyl

63
Q

half life of meperidine

A

short

64
Q

meperidine as compared to morphine

A

less constipation

more lipophilic and gets to the brain quicker, doesn’t effect peripheral tissues.

65
Q

meperidine for chronic pain

A

not recommended because of the metabolite toxicity

66
Q

med that is contraindicated with meperidine

A

MAOI

67
Q

Meperidine and tachycardic patients

A

contraindicated. can raise HR further

68
Q

routes of admin for fentanyl

A

paraenteral
transdermal
transmucosal

69
Q

potency of fentanyl

A

high, about 100x morphine potency

70
Q

half life of fentanyl

A

high

71
Q

lipophilicity of fentanyl

A

high

which makes it a good candidate for transdermal route.

72
Q

why isn’t there po fentanyl?

A

it goes through significant first pass effect and does not reach systemic circulation

73
Q

T or F: fentanyl and its congeners are devoid of active metabolites

A

true

74
Q

carfentanyl potency

A

1000x morphine

100x fentanyl

75
Q

why is fentanyl safe to give those with renal impairment?

A

lack of active metabolites

76
Q

advantages of fentanyl (4)

A

speed of analgesia in the setting of spontaneous breakthrough pain (given transmucosal)
transdermal
preferred to morphine in renal insufficiency
less prone to constipation

77
Q

who cannot be prescribed transdermal or oral transmucosal fentanyl?

A

opioid naive patients

78
Q

transdermal fentanyl is inappropriate for what kind of pain?

A

acute, intermittent, or mild

79
Q

transmucosal fentanyl is always dosed

A

in the lowest dose in an opioid tolerant patient

80
Q

methadone is

A

a long acting agonist

81
Q

half life of methadone

A

20-35 hours

82
Q

does methadone have active metabolites?

A

no

83
Q

opioids safe for renal impaired patients

A

hydromorphone
fentanyl
methadone

84
Q

EKG changes with methadone

A

possibility of QTc interval prolongation

85
Q

neuropathic pain and methadone

A

more effective than other opioids

86
Q

why does methadone produce less tolerance?

A

because it antagonizes NMDA receptors, altering glutamate levels in the CNS. tolerance does not develop at the same rate.

87
Q

why is methadone usable for neuropathic pain?

A

because it antagonizes NMDA receptors, altering glutamate activity.

88
Q

pharmacokinetic drug:drug interactions of methadone

A

many drugs induce or inhibit CYP3A4

methadone itself induces 3A4

89
Q

pharmacodynamic drug:drug interactions of methadone

A
  • anything that may cause CNS depression

- anything that may cause QTc prolongation

90
Q

what are the two opioids that are lipophilic enough to be given transdermally?

A

buprenorphine

fentanyl

91
Q

which 2 opioids are not available PO?

A

buprenorphine

fentanyl

92
Q

which 4 opioids can be given extended release?

A

hydromorphone
morphine
oxycodone
oxymorphone

93
Q

which opioids can be given as suppositories?

A

hydromorphone

morphine

94
Q

which 2 opioids are not offered injectable?

A

codeine

oxycodone

95
Q

which is the only opioid that is given transmucosally?

A

fentanyl

96
Q

which opioids stand out for breakthrough pain?

A

fentanyl

methadone

97
Q

opioid tolerance

A

progressive loss of effect with sustained administration of an opioid receptor agonist

98
Q

tolerance can be up to

A

30-fold

99
Q

tolerance to a particular opioid is comprised of either

A
  • tolerance unique to that opioid

- tolerance that extends to other opioid agonists

100
Q

cross tolerance

A

tolerance that extends to other opioid receptor agonists

101
Q

different responses to an opioid develop tolerance at different rates, ie:

A

tolerance to respiratory depression happens quickly, while tolerance to constipation never really happens.

102
Q

tolerance to a drug is combatted with

A

higher doses

watch for adverse effects

103
Q

opioid induced tolerance (4) characteristics

A

progressive decrease in efficacy
increased dose decreases pain
adverse effects with increased dosing
*decreased sensitivity to opioid analgesics(

104
Q

opioid induced hyperalgesia (4) characteristics

A

paradoxical increase in sensitivity to painful stimuli
increased dose increases pain
may be a different pain altogether
increased sensitivity to pain

105
Q

why is methadone spot blank on equianalgesic chart?

A

because tolerance is nonlinear in methadone. you’ll need to see a chart specific to methadone.

106
Q

what is the issue with equianalgesic tables?

A
  • single dose studies in opioid naive patients with acute pain
  • variables such as bioavailability are not taken into account
  • undirectional vs bidirectional equivalencies *pay attention to sedation when going from one drug to another
107
Q

when changing from IR to ER

A

start with the same daily total dose

108
Q

if changing from one opioid to another, what must you do with the new dose?

A

reduce the new med dose by 25-50% to begin with

109
Q

breakthrough pain types (4)

A

spontaneous
incidental volitional
incidental nonvolitional
end of dose

110
Q

volitional pain

A

pain under the patients control. ie raising arm after shoulder surgery would cause volitional pain

111
Q

Non volitional pain

A

unpreventable pain. ie coughing after surgery

112
Q

management of spontaneous, volitional, and volitional breakthrough pain

A

IR opioid PRN

113
Q

management of end of dose breakthrough pain

A

increase the dose or frequency of the around the clock analgesic

114
Q

breakthrough pain dosinf

A

10-15% total daily dose of the same opioid

115
Q

management of volitional pain

A

consider premeditating 30-45 min in advance of anticipated pain trigger

116
Q

what medications might you consider in the case of spontaneous or non volitional pain that comes on quickly

A

transmucosal fentanyl
or
PO methadone

117
Q

onset of analgesia is directly related to

A

lipophillicity

118
Q

oral transmucosal fentanyl black box warning

A
  • only dosed by titration, beginning with 100 mcg

- use only in opioid tolerant individuals

119
Q

opioid receptor antagonists

A

naloxone
naltrexone
methylnaltrexone
alvimopan

120
Q

short acting opioid receptor antagonist

A

naloxone

121
Q

long acting opioid receptor antagonist

A

naltrexone

122
Q

naloxone and naltrexone are antagonists of

A

mu kappa and delta

123
Q

naloxone is given ____ while naltrexone is given ____

A

naloxone - IM, IV, intranasal

naltrexone - oral

124
Q

naloxone and naltrexone block ____ and exacerbate ____

A

block stress induced analgesia

exacerbate clinical pain

125
Q

what rebound effects do you need to monitor for after use of naloxone

A

htn
tachycardia
ventricular arrhythmias

126
Q

what can naloxone and naltrexone also reverse

A

gi immotility/constipation

127
Q

opioid receptor antagonists that do not cross the BBB

and what does this mean?

A

methylnaltrexone
alvimopan

adverse effects may be reversed but analgesia will not ie you can relieve constipation without reversing pain control

128
Q

buprenorphine can be abused and require naloxone. how many attempts of naloxone may it take?

A

3-4

129
Q

Suboxone SL

how it works

A

you’ll only feel the agonist, not the antagonist part.
it’s buprenorphine and naloxone.
if you crush it and inject it, you can’t get high bc the naloxone blocks it.

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