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Summer Pharm - Exam 2 > Opioids > Flashcards

Opioids Flashcards

1
Q

opioids are classified into (3)

A

full agonists

partial agonists

antagonists

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2
Q

major target receptor for opioids

A

μ - mu

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3
Q

moa for opioids

A

mimic endogenous opioid peptides

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4
Q

where are endogenous opioid peptides found

A

regions associated w. pain transmission →

spinal cord

limbic system

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5
Q

3 endogenous opioid peptides

A

enkephalins

endorphins

dynorphins

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6
Q

enkephalins are found in the (2)

A

brain

adrenal medulla

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7
Q

endorphins are found in the (2)

A

brain

pituitary gland

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8
Q

t/f: opioid peptides can elicit all responses associated w. opioid drugs, including tolerance and dependence

A

T!

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9
Q

opioid analgesics interact w. __ opioid receptors (2)

to produce __ effects (2)

A

peripheral and CNS

therapeutic and adverse

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10
Q

primary moa of opioids

A

decreased NT release → decreased neuronal excitability

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11
Q

decreased NT release of opioids is __ linked

A

G protein

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12
Q

Mu (morphine receptor) mediates

A

spinal/supraspinal analgesia

respiratory dpn

reduced GI motility

miosis

euphoria

physical dependence

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13
Q

kappa (dynorphin) receptors mediate

A

spinal analgesia

miosis

sedation

dysphoria

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14
Q

delta (enkehalin) receptors mediate

A

similar to mu

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15
Q

subjective experience of pain =

A

perception + rxn

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16
Q

inhibitory effects of opioid action are associated with the __ pathway

A

descending

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17
Q

inhibitory effects of opioids include (3)

A

change in rxn to pain

increase in pain threshold

spinal analgesia

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18
Q

sensitization to pain and transduction of pain stimuli are associated w.

A

COX 2 → PG

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19
Q

perception of, and rxn to, pain is associated w. the __ pathway

A

ascending →

spinothalamic tract

limbic system

cortices

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20
Q

analgesic effect of elevation of pain threshold occurs at the

A

somatosensory cortex → activation of brain stem (descending inhibition)

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21
Q

presynaptic elevation of pain threshold occurs via decrease of __ from spinal cord neurons (2)

A

substance P

glutamate

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22
Q

postsynaptic decrease of pain threshold occurs via decreased response of __ neurons

A

2nd order pain transmission

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23
Q

change in subjective response to pain occurs in the __

via inducement of __ (2)

A

limbic system

tranquility/euphoria

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24
Q

opioid drugs are more efficacious but also more dangerous for relief of __ pain

A

mod-severe

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25
Q

analgesic effects of opioids are __,

whereas analgesic effects of NSAIDs exhibit a __

A

dose-dependent

ceiling effect

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26
Q

are opioids antipyretic or anti-inflammatory

A

no!

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27
Q

3 non analgesic uses of opioids

A

cough suppression

anti-diarrheal

MI

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28
Q

which opioid is used as a cough suppressant

A

dextromorphan

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29
Q

why is dextromorphan lower risk for abuse potential

A

lower doses required for cough suppression

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30
Q

which opioid is used as a anti-diarrheal agent

A

loperamide

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31
Q

why is loperamide low risk for parenteral abuse

A

low-solubility salts

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32
Q

which opioid is used for pain/anxiety relief for MI

A

fentanyl

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33
Q

does fentanyl have any effect on myocardial fxn

A

not really

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34
Q

opioids are first line for __ pain,

but NOT for __ pain

A

acute mod-sev

chronic

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35
Q

what is included in opioid use disorder (7)

A

respiratory dpn

n/v

sedation

dizziness

constipation

dry mouth

pruritis

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36
Q

mc affective response to pain w. opioids

A

euphoria

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37
Q

why are we worried about euphoria w. chronic opioid use

A

produces changes in brain-reward pathway → opioid use disorder

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38
Q

what percentage of people on longterm opioids for non cancer pain in PCP setting struggle w. addition

A

25%

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39
Q

most serious acute s.e of opioid drugs if pt does not follow dosing guidelines

A

respiratory dpn

rarely a problem if dosing guidelines are followed

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40
Q

moa for respiratory dpn w. opioids

A

decrease in sensitivity of respiratory centers to CO2

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41
Q

risk for respiratory dpn increases when (3)

A

opioids titrated rapidly

sleep apnea

co-administered w. benzos

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42
Q

__ precedes

__ w. respiratory dpn related to opioids

A

prominent sedation

significant dpn

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43
Q

how many ppl die daily from prescription opioid od’s

A

40+

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44
Q

classic triad of opioid od

A

coma

pinpoint pupils

respiratory dpn

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45
Q

tx for opioid od if somnolent but easily arousable

A

NO naloxone!

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46
Q

when do you administer naloxone for opioid od

A

symptomatic respiratory dpn

OR

progressive obtundation (alterness/consciousness)

decreased RR is imminent

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47
Q

t/f: duration of naloxone is shorter than agonists

A

T!

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48
Q

what might occur in addicts who are given naloxone

A

withdrawal sx →

sweating, increased RR, agitation

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49
Q

constipation caused by opioids is both __ (2)

A

direct

indirect

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50
Q

direct reduction of bowel motility w. opioids is mediated via

A

mu receptors → inhibit ENS fxn

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51
Q

indirect reduction in bowel motility of opioids is caused by

A

decrease in Ach release → anticholinergic effect

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52
Q

t/f: do pt’s on opioids develop tolerance to constipation

A

no!

constipation worsens as dose increases

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53
Q

pt’s on opioids must be given prophylactic pharm for

A

constipation

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54
Q

common first line prophylactic pharm for constipation dt opioids

A

daily senna (stool softener)

+/- docusate

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55
Q

is docusate effective alone for constipation

A

nope!

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56
Q

other tx to try for opioid constipation (besides senna)

A

PEG-sorbitol daily or PRN

bisacodyl enema

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57
Q

list drugs in order of effectiveness for prophylaxis of constipation

A

trick question!

they are equally effective

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58
Q

n/v related to opioids is controlled by __ stimulation

of the __

in the __

A

direct

CTZ

medulla

59
Q

n/v w. opioids is mc in __ pt’s

due to a __ component

A

ambulatory

vestibular

60
Q

moa of pharm management of n/v w. opioids

A

antagonists of receptors in periphery and at CTZ

61
Q

4 drugs used to n/v w. opioids

A

antihistamines → diphenhydramine/meclizine → H1 muscarinic

prokinetic D2 → metoclopramide

D2 antagonists (antipsychotics) → prochlorperazine or haloperidol

5HT3 antagonists → ondansetron

62
Q

what would you give to a pt on opioids if n/v is related to ambulation

A

antihistamine → diphenhydramine - meclizine

63
Q

what would you give to a pt on opioids if they c/o postprandial nausea or early satiety

A

prokinetic agents → metoclopramide

64
Q

s.e of metoclopramide that can be use limiting

A

sedation

EPSE (extrapyramidal) → tardive dyskinesia

65
Q

inexpensive first line option for n/v w. opioid use

A

D2 antagonists →

prochlorperazine

haloperidol

66
Q

what drug for opioid related n/v is reserved for tx failure

A

5HT3 antagonists → odansetron

expensive

67
Q

ADR of opioids induced by release of histamine (NOT IgE mediated)

A

pseudo-allergic phenomena →

hypotn

bronchospasm

68
Q

pseudo-allergic phenomena is tx w.

A

antihistamines

69
Q

t/f: true allergies to opioids are extremely rare

A

T!

most rxns are related to pseudo allergic phenomena

70
Q

sx of true opioid allergic rxn

A

rash

airway obstruction

face swelling

71
Q

if true opioid allergy, switch from __

to __

PLUS

__

A

semisynthetic (morphine)

synthetic (fentanyl/methadone)

PLUS

antihistamine and GC

72
Q

t/f: switching from semisynthetic to synthetic opioid for allergic rxn reduces cross sensitivity

73
Q

are sedation and CNS dpn seen w. non opioid analgesics

A

no! just opioids

74
Q

tolerance to opioids is mediated by both (2)

A

receptor

cellular level

75
Q

t/f: cross tolerance exists to some degree to all drugs that act as agonists at mu receptors

76
Q

tolerance is lost __ weeks after d.c of opioids

77
Q

repeated use of opioids that alters physiological state so that continued use is needed to prevent withdrawal

A

dependence

78
Q

dependence will be the same for opioids if (2)

A

equianalgesic

administered by same route

79
Q

physical dependence can develop for patients on as little as __

for __ days

A

3-4 therapeutic doses/day

3-7 days

80
Q

physical dependence w. opioids is common, but __ is rare

A

addiction

extreme compulsive use

81
Q

withdrawal symptoms of opioids can occur w. (2)

A

repetitive use → abrupt cessation

administration of antagonists

82
Q

sx of opioid withdrawal are related to

A

increase in SNS outflow

83
Q

what drug helps w. opioid withdrawal sx related to increased SNS outflow

84
Q

severity of opioid withdrawal depends on

A

t½ →

shorter t½ = more severe

85
Q

what drug suppresses opioid withdrawal by opioid maintenance therapy

86
Q

opioid withdrawal occurs over __ hr

87
Q

sx of opioid withdrawal from quickest → latest onset

A

vomiting

diarrhea

dpn

drug cravings

88
Q

additive CNS dpn is seen w. opioids PLUS __ (2),

which increases risk of __

A

benzos and etoh

lethality

89
Q

opioids PLUS __ (2)

can cause serotonin syndrome

A

MAO inhibitors

SSRIs

90
Q

SSRI and MAO inhibitor most dangerous w. opioids

A

meperidine

tramadol

91
Q

which 2 opioids are oral only

A

oxycodone

hydrocodone

undergo first pass hepatic metabolism

92
Q

which 3 opioids are available oral and IV

A

morphine

hydromorphone

oymorphone

93
Q

which opioid is parenteral only

94
Q

which opioid has highly variable dosing

95
Q

__ soluble opioids have more rapid onset

96
Q

which opioids have the most rapid onset

A

IV →

fentanyl

hydromorphone

morphine

97
Q

slowest onset of action route of opioid administration

98
Q

phase I oxidation in liver via CYP2D6 is activating for which 2 opioids

A

codeine

tramadol

99
Q

codeine is demethylated to

100
Q

tramadol is demethylated to

A

more active opioid

101
Q

2 types of genetic polymorphisms for metabolizers of codeine and tramadol

A

poor metabolizers (PM)

ultra-rapid metabolizers (UM)

102
Q

which type of metabolizer has greater risk for toxicity

A

ultra rapid metabolizers

103
Q

rec for people w. genetic polymorphisms

A

avoid opioids

104
Q

phase 1 oxidation in liver via CYP3A4 is inactivating for (3)

A

oxycodone

tramadol

methadone

105
Q

phase 2 conjugation in the liver via UGTB27 is inactivating for (3)

A

morphine

hydromorphone

oxymorphone

106
Q

__ can help manage opioid induced constipation

107
Q

most opioids are

A

full agonists at the mu receptor:

morphine → MS Contin

hydrocodone → vicodin

hydromorphone → dilaudid

oxycodone → percocet

oxymorphone → opana

108
Q

synthetic opioids

A

fentanyl

meperidine

diphenoxylate/loperamide

methadone

tramadol

109
Q

partial agonist opioid

A

buprenorphine

110
Q

mixed action opioid: full opioid agonist + NE5HT reuptake inhibitor

A

tramadol → ultram

111
Q

opioids used today are equally powerful and differ only in

A

potency (dose)

112
Q

drug dose =

113
Q

how do partial agonist opioids (ex buprenorphine) differ from full agonist opioids (ex morphine)

A

partial (buprenorphine) has a ceiling effect

full (morphine) do not

114
Q

what will happen if you give a pt dependent on a full opioid agonist a partial agonist OR an antagonist

A

they will have withdrawal sx

115
Q

what influences onset of action

A

route of administration

116
Q

what influences duration of action

117
Q

what influences onset-duration of action

A

formulations

118
Q

what determines clinical utility of opioids

A

side effects

119
Q

onset of action by route of administration

A

fastest → slowest:

IV

IM

SC

PO

120
Q

__ has the shortest duration of action

121
Q

immediate release opioids have no delay in full dose reaching plasma, so duration is based on

A

plasma t½

122
Q

what opioid has the shortest t½

123
Q

IR opioids are recommended for __

ER opioids are used for __

A

initial titration

chronic pain

124
Q

pro of combo opioid PLUS non opioid analgesic

A

increase in pain control

minimal increase in s.e

125
Q

pro of opioid PLUS NSAID

A

synergistic analgesia

PLUS

anti-inflammatory action

126
Q

pro of APAP PLUS opioid

A

synergistic analgesia

127
Q

vicodin is a combo of

A

hydrocodone

APAP

128
Q

morphine has rapid action in __ pain (2)

A

post-surgical

acute trauma

129
Q

extremely potent opioid w. rapid onset/offset beneficial for initial titration and severe pain

130
Q

fentanyl is useful for __ pain

A

perioperative and postoperative surgical pain

131
Q

__ can suppress opioid withdrawal syndrome if given orally

132
Q

extended duration methadone is useful in tx of __,

but has a long __ and can be toxic

A

chronic pain

t½

133
Q

which opioid can cause prolonged QT

134
Q

which opioid can be used parenterally and orally for severe pain

A

hydromorphone

135
Q

concern w. hydromorphone

A

unfamiliarity w. dosing and more potent than morphine → inadvertent o.d

136
Q

which opioid is often combined w. ASA or APAP to provide peripheral and central pain relief

137
Q

which opioid is particularly suited for relief of moderate pain in ambulatory pt’s

A

hydrocodone

138
Q

use of which opioid is declining and is contraindicated in kids

A

codeine

meperidine use also declining

139
Q

concern w. codeine

A

s.e increase more than pain relief at higher doses →

sedation, rash, miosis, vomiting

140
Q

what opioid is recommended via transdermal patch in adults w. mod-sev pain

A

buprenorphine

141
Q

what opioid is the drug of choice in opioid detoxification

A

initial: SL buprenorphine
maintenance: buprenorphine + naloxone

142
Q

which opioid is useful in chronic pain syndromes dt inhibition of NE and serotonin reuptake

143
Q

which opioid has abuse potential and increases suicide risk in addiction-prone pt’s

144
Q

bad s.e’s of tramadol

A

lowers sz threshold

ddi w. MAOI and SSRIs

Summer Pharm - Exam 2 (12 decks)

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