Opioids Flashcards
1
Q
opioids are classified into (3)
A
full agonists
partial agonists
antagonists
2
Q
major target receptor for opioids
A
μ - mu
3
Q
moa for opioids
A
mimic endogenous opioid peptides
4
Q
where are endogenous opioid peptides found
A
regions associated w. pain transmission →
spinal cord
limbic system
5
Q
3 endogenous opioid peptides
A
enkephalins
endorphins
dynorphins
6
Q
enkephalins are found in the (2)
A
brain
adrenal medulla
7
Q
endorphins are found in the (2)
A
brain
pituitary gland
8
Q
t/f: opioid peptides can elicit all responses associated w. opioid drugs, including tolerance and dependence
A
T!
9
Q
opioid analgesics interact w. __ opioid receptors (2)
to produce __ effects (2)
A
peripheral and CNS
therapeutic and adverse
10
Q
primary moa of opioids
A
decreased NT release → decreased neuronal excitability
11
Q
decreased NT release of opioids is __ linked
A
G protein
12
Q
Mu (morphine receptor) mediates
A
spinal/supraspinal analgesia
respiratory dpn
reduced GI motility
miosis
euphoria
physical dependence
13
Q
kappa (dynorphin) receptors mediate
A
spinal analgesia
miosis
sedation
dysphoria
14
Q
delta (enkehalin) receptors mediate
A
similar to mu
15
Q
subjective experience of pain =
A
perception + rxn
16
Q
inhibitory effects of opioid action are associated with the __ pathway
A
descending
17
Q
inhibitory effects of opioids include (3)
A
change in rxn to pain
increase in pain threshold
spinal analgesia
18
Q
sensitization to pain and transduction of pain stimuli are associated w.
A
COX 2 → PG
19
Q
perception of, and rxn to, pain is associated w. the __ pathway
A
ascending →
spinothalamic tract
limbic system
cortices
20
Q
analgesic effect of elevation of pain threshold occurs at the
A
somatosensory cortex → activation of brain stem (descending inhibition)
21
Q
presynaptic elevation of pain threshold occurs via decrease of __ from spinal cord neurons (2)
A
substance P
glutamate
22
Q
postsynaptic decrease of pain threshold occurs via decreased response of __ neurons
A
2nd order pain transmission
23
Q
change in subjective response to pain occurs in the __
via inducement of __ (2)
A
limbic system
tranquility/euphoria
24
Q
opioid drugs are more efficacious but also more dangerous for relief of __ pain
A
mod-severe
25
analgesic effects of opioids are \_\_,
whereas analgesic effects of NSAIDs exhibit a \_\_
dose-dependent
ceiling effect
26
are opioids antipyretic or anti-inflammatory
no!
27
3 non analgesic uses of opioids
cough suppression
anti-diarrheal
MI
28
which opioid is used as a cough suppressant
dextromorphan
29
why is dextromorphan lower risk for abuse potential
lower doses required for cough suppression
30
which opioid is used as a anti-diarrheal agent
loperamide
31
why is loperamide low risk for parenteral abuse
low-solubility salts
32
which opioid is used for pain/anxiety relief for MI
fentanyl
33
does fentanyl have any effect on myocardial fxn
not really
34
opioids are first line for __ pain,
but NOT for __ pain
acute mod-sev
chronic
35
what is included in opioid use disorder (7)
**respiratory dpn**
n/v
sedation
dizziness
constipation
dry mouth
pruritis
36
mc affective response to pain w. opioids
euphoria
37
why are we worried about euphoria w. chronic opioid use
produces changes in brain-reward pathway → opioid use disorder
38
what percentage of people on longterm opioids for non cancer pain in PCP setting struggle w. addition
25%
39
most serious acute s.e of opioid drugs if pt does not follow dosing guidelines
respiratory dpn
*rarely a problem if dosing guidelines are followed*
40
moa for respiratory dpn w. opioids
decrease in sensitivity of respiratory centers to CO2
41
risk for respiratory dpn increases when (3)
opioids **titrated rapidly**
**sleep apnea**
co-administered w. **benzos**
42
\_\_ precedes
\_\_ w. respiratory dpn related to opioids
prominent sedation
significant dpn
43
how many ppl die daily from prescription opioid od's
40+
44
classic triad of opioid od
coma
pinpoint pupils
respiratory dpn
45
tx for opioid od if **somnolent but easily arousable**
NO naloxone!
46
when do you administer naloxone for opioid od
symptomatic respiratory dpn
OR
progressive obtundation (alterness/consciousness)
*decreased RR is imminent*
47
t/f: duration of naloxone is shorter than agonists
T!
48
what might occur in addicts who are given naloxone
**withdrawal sx** →
sweating, increased RR, agitation
49
constipation caused by opioids is both __ (2)
direct
indirect
50
direct reduction of bowel motility w. opioids is mediated via
mu receptors → inhibit ENS fxn
51
indirect reduction in bowel motility of opioids is caused by
decrease in Ach release → anticholinergic effect
52
t/f: do pt's on opioids develop tolerance to constipation
no!
## Footnote
**constipation worsens as dose increases**
53
pt's on opioids must be given prophylactic pharm for
constipation
54
common first line prophylactic pharm for constipation dt opioids
**daily senna** (stool softener)
+/- docusate
55
is docusate effective alone for constipation
nope!
56
other tx to try for opioid constipation (besides senna)
**PEG-sorbitol** daily or PRN
## Footnote
**bisacodyl enema**
57
list drugs in order of effectiveness for prophylaxis of constipation
trick question!
they are equally effective
58
n/v related to opioids is controlled by __ stimulation
of the \_\_
in the \_\_
direct
CTZ
medulla
59
n/v w. opioids is mc in __ pt's
due to a __ component
ambulatory
vestibular
60
moa of pharm management of n/v w. opioids
antagonists of receptors in periphery and at CTZ
61
4 drugs used to n/v w. opioids
antihistamines → **diphenhydramine/meclizine** → H1 muscarinic
prokinetic D2 → **metoclopramide**
D2 antagonists (antipsychotics) → **prochlorperazine or haloperidol**
5HT3 antagonists → **ondansetron**
62
what would you give to a pt on opioids if n/v is related to ambulation
antihistamine → **diphenhydramine - meclizine**
63
what would you give to a pt on opioids if they c/o postprandial nausea or early satiety
prokinetic agents → **metoclopramide**
64
s.e of metoclopramide that can be use limiting
**sedation**
EPSE (extrapyramidal) → **tardive dyskinesia**
65
inexpensive first line option for n/v w. opioid use
D2 antagonists →
prochlorperazine
haloperidol
66
what drug for opioid related n/v is reserved for tx failure
5HT3 antagonists → **odansetron**
expensive
67
ADR of opioids induced by release of histamine (NOT IgE mediated)
pseudo-allergic phenomena →
hypotn
bronchospasm
68
pseudo-allergic phenomena is tx w.
antihistamines
69
t/f: true allergies to opioids are extremely rare
T!
most rxns are related to pseudo allergic phenomena
70
sx of true opioid allergic rxn
rash
airway obstruction
face swelling
71
if true opioid allergy, switch from \_\_
to \_\_
PLUS
\_\_
semisynthetic (morphine)
synthetic (fentanyl/methadone)
PLUS
antihistamine and GC
72
t/f: switching from semisynthetic to synthetic opioid for allergic rxn reduces cross sensitivity
F
73
are sedation and CNS dpn seen w. non opioid analgesics
no! just opioids
74
tolerance to opioids is mediated by both (2)
receptor
cellular level
75
t/f: cross tolerance exists to some degree to all drugs that act as agonists at mu receptors
T!
76
tolerance is lost __ weeks after d.c of opioids
1-2
77
repeated use of opioids that alters physiological state so that continued use is needed to prevent withdrawal
dependence
78
dependence will be the same for opioids if (2)
equianalgesic
administered by same route
79
physical dependence can develop for patients on as little as \_\_
for __ days
3-4 therapeutic doses/day
3-7 days
80
physical dependence w. opioids is common, but __ is rare
addiction
*extreme compulsive use*
81
withdrawal symptoms of opioids can occur w. (2)
repetitive use → abrupt cessation
administration of antagonists
82
sx of opioid withdrawal are related to
increase in SNS outflow
83
what drug helps w. opioid withdrawal sx related to increased SNS outflow
clonidine
84
severity of opioid withdrawal depends on
t½ →
## Footnote
**shorter t½ = more severe**
85
what drug suppresses opioid withdrawal by opioid maintenance therapy
methadone
86
opioid withdrawal occurs over __ hr
72
87
sx of opioid withdrawal from quickest → latest onset
vomiting
diarrhea
dpn
drug cravings
88
additive CNS dpn is seen w. opioids PLUS __ (2),
which increases risk of \_\_
benzos and etoh
lethality
89
opioids PLUS __ (2)
can cause serotonin syndrome
MAO inhibitors
SSRIs
90
SSRI and MAO inhibitor most dangerous w. opioids
meperidine
tramadol
91
which 2 opioids are oral only
oxycodone
hydrocodone
*undergo first pass hepatic metabolism*
92
which 3 opioids are available oral and IV
morphine
hydromorphone
oymorphone
93
which opioid is parenteral only
fentanyl
94
which opioid has highly variable dosing
methadone
95
\_\_ soluble opioids have more rapid onset
lipid
96
which opioids have the most rapid onset
IV →
fentanyl
hydromorphone
morphine
97
slowest onset of action route of opioid administration
oral
98
phase I oxidation in liver via CYP2D6 is activating for which 2 opioids
codeine
tramadol
99
codeine is demethylated to
morphine
100
tramadol is demethylated to
more active opioid
101
2 types of genetic polymorphisms for metabolizers of codeine and tramadol
poor metabolizers (PM)
ultra-rapid metabolizers (UM)
102
which type of metabolizer has greater risk for toxicity
ultra rapid metabolizers
103
rec for people w. genetic polymorphisms
avoid opioids
104
phase 1 oxidation in liver via CYP3A4 is inactivating for (3)
oxycodone
tramadol
methadone
105
phase 2 conjugation in the liver via UGTB27 is inactivating for (3)
morphine
hydromorphone
oxymorphone
106
\_\_ can help manage opioid induced constipation
naloxone
107
most opioids are
**full agonists at the mu receptor:**
morphine → MS Contin
hydrocodone → vicodin
hydromorphone → dilaudid
oxycodone → percocet
oxymorphone → opana
108
synthetic opioids
fentanyl
meperidine
diphenoxylate/loperamide
methadone
tramadol
109
partial agonist opioid
buprenorphine
110
mixed action opioid: full opioid agonist + NE5HT reuptake inhibitor
tramadol → ultram
111
opioids used today are equally powerful and differ only in
potency (dose)
112
drug dose =
potency
113
how do partial agonist opioids (ex buprenorphine) differ from full agonist opioids (ex morphine)
partial (buprenorphine) has a ceiling effect
full (morphine) do not
114
what will happen if you give a pt dependent on a full opioid agonist a partial agonist OR an antagonist
they will have withdrawal sx
115
what influences onset of action
route of administration
116
what influences duration of action
half life
117
what influences onset-duration of action
formulations
118
what determines clinical utility of opioids
side effects
119
onset of action by route of administration
fastest → slowest:
IV
IM
SC
PO
120
\_\_ has the shortest duration of action
fentanyl
121
immediate release opioids have no delay in full dose reaching plasma, so duration is based on
plasma t½
122
what opioid has the shortest t½
fentanyl
123
IR opioids are recommended for \_\_
ER opioids are used for \_\_
initial titration
chronic pain
124
pro of combo opioid PLUS non opioid analgesic
increase in pain control
minimal increase in s.e
125
pro of opioid PLUS NSAID
synergistic analgesia
PLUS
anti-inflammatory action
126
pro of APAP PLUS opioid
synergistic analgesia
127
vicodin is a combo of
hydrocodone
APAP
128
morphine has rapid action in __ pain (2)
post-surgical
acute trauma
129
extremely potent opioid w. rapid onset/offset beneficial for initial titration and severe pain
fentanyl
130
fentanyl is useful for __ pain
perioperative and postoperative surgical pain
131
\_\_ can suppress opioid withdrawal syndrome if given orally
methadone
132
extended duration methadone is useful in tx of \_\_,
but has a long __ and can be toxic
chronic pain
t½
133
which opioid can cause prolonged QT
methadone
134
which opioid can be used parenterally and orally for severe pain
hydromorphone
135
concern w. hydromorphone
unfamiliarity w. dosing and more potent than morphine → inadvertent o.d
136
which opioid is often combined w. ASA or APAP to provide peripheral and central pain relief
oxycodone
137
which opioid is particularly suited for relief of moderate pain in ambulatory pt's
hydrocodone
138
use of which opioid is declining and is contraindicated in kids
codeine
*meperidine use also declining*
139
concern w. codeine
s.e increase more than pain relief at higher doses →
sedation, rash, miosis, vomiting
140
what opioid is recommended via transdermal patch in adults w. mod-sev pain
buprenorphine
141
what opioid is the drug of choice in opioid detoxification
initial: SL buprenorphine
maintenance: buprenorphine + naloxone
142
which opioid is useful in chronic pain syndromes dt inhibition of NE and serotonin reuptake
tramadol
143
which opioid has abuse potential and increases suicide risk in addiction-prone pt's
tramadol
144
bad s.e's of tramadol
lowers sz threshold
ddi w. MAOI and SSRIs
