Opioids Flashcards
1
Q
morphine is the
A
prototypic opioid agonist
2
Q
opioid
A
all compounds that work on opioid receptors
3
Q
opiate
A
naturally occurring alkaloid from the opium poppy
4
Q
when did the opioid crisis start
A
1990s-ish
5
Q
pain that occurs when nerve endings are activated by tissue damage or inflammation
A
nociceptive pain
6
Q
often a result of injury, protective response
A
nociceptive pain
7
Q
abnormal processing of stimuli from the peripheral or central nervous systems
A
neuropathic
8
Q
no functional purpose, described as burning, electric shock
A
neuropathic pain
9
Q
physical pain that is caused, increased, or prolonged by mental, emotional or behavioral factors
A
psychogenic pain
10
Q
pathophysiology of nociceptive pain (5 steps)
A
- site of injury
- chemicals release that allow neurotransmission along ascending nerve to dorsal horn
- impulse follows spinothalamic tract to brain
- pain perceived by brain
- impulse travels descending path to make a motor response
11
Q
opioid receptors are located in the
A
CNS, GI tract, bladder
12
Q
most of the adverse side effects are due to
A
peripheral stimulation of opioid receptors
13
Q
opioid receptors inhibits response at dorsal horn
A
dorsal root ganglia
14
Q
opioid receptors reduce neurotransmitter release and decreases signaling and inhibit post synaptic neuron signaling
A
dorsal root ganglia
15
Q
opioid receptors simulates endogenous opioid system
A
cerebral cortex
16
Q
controls pain, reward, and addicitive behaviors
A
cerebral cortex
17
Q
opioid receptors mimics the action of endorphins, enkephalins, dynomorphins in the
A
cerebral cortex
18
Q
what are the opioid receptor types
A
- Mu
- Delta
- Kappa
19
Q
what is the primary opioid receptor
A
Mu
20
Q
are specific agonists available for opioid receptors?
A
no
21
Q
this receptor is located in the CNS at supraspinal and spinal sites and the PNS in the GI tract, cardiovascular, and immune systems
A
Mu receptors
22
Q
primary use for opioid mu receptor
A
analgesia
23
Q
side effects of mu receptor
A
respiratory depression, sedation, pruritus, euphoria, miosis (pinpoint), decreased GI motility, urinary rentention, physical dependence, hormone changes, stimulate dopamine/acetylcholine release
24
Q
chronic use of opioids can lead to
A
immunosuppression
25
what opioid receptor is located primarily within the dorsal horn of the spinal cord and brain stem
Kappa receptor
26
effects of kappa opioid receptor
modest analgesia
27
adverse effects of kappa receptor (7)
diuresis, dysphoria, sedation, resp depression, bradycardia, decreased GI motility, hallucunations
28
what opioid receptor is primary located in the brain and is a binding site for endogenous peptides
Delta receptor
29
effects of delta receptor
some analgesia
30
adverse effects of delta receptor (6)
dysphoria, delusions, hallucinations, dependence, hormonal changes, dopamine release
31
pure opioid agonists stimulate the (which receptor)
mu receptor
32
pure opioid receptors are the most potent ____
analgesics
33
in a pure opioid agonist, as the dose increases the analgesia increases in a _____ _____ _____
log linear fashion
34
the degree of analgesia is limited by
side effects
35
start ____ and go ____
low, slow
36
you should start with a ____ ____ pure opioid agonist when prescribing medication
short acting
37
classes of pure opioid agonists
phenanthrene, phenylpiperidine, diphenylheptane
38
example of phenanthrene
morphine, oxycodone, hydrocodone
39
example of phenylpiperidine
fentanyl
40
example of diphenylheptane
methadone
41
things to consider when using opioids for pain management (5)
pharmacokinetic profile, ROA, setting, patient history, adverse effects
42
through what system are opioids metabolized?
CYP 450 system
43
by using the CYP 450 system to metabolize opioids, this causes an increase ____ for _____ _____
risk, drug interactions
44
many metabolites are excreted ____
renally
45
what type of medication is codeine
very weak mu receptor agonist
46
codeine is ingested as the "inactive" form of the drug, turning into ___ when activated. Codeine is known as a ____.
morphine, prodrug
47
where is codeine converted into morphine and how?
liver. Codeine --> CYP2D6 --> morphine
47
in normal metabolizers what percent of codeine is converted to morphine?
10%
48
what percentage of Caucasians and Asian/African Americans lack the ability to metabolize codeine into morphine?
6-10% Caucasians
2-5% Asian / African American
49
if someone lacks the ability to metabolize codeine into morphine there is no _____ ____
therapeutic benefit
50
what percent of people are ultra rapid metabolizers covert codeine to >10% morphine
1%
51
if you are an ultra rapid metabolizer, you are at increased risk for what
respiratory depression
52
contraindications of codeine? (2ish)
Children, children especially after a tonsillectomy
53
at lower doses codeine can suppress the ___ ____
cough reflex
54
what is made of Tylenol #3/#4
acetaminophen/codeine
(#3 = mg codeine, #4 = 60mg tylenol)
55
a complex response involving the central and peripheral nervous system as well as the smooth muscle of the bronchial tree
cough relfex
56
this opioid medication is known as the gold standard opioid
morphine
57
how is morphine available?
Oral, SQ, IV, IM, Intrathecal
58
if someone has chronic pain and has tried quite a few other pain medications, what type of morphine would you prescribe?
oral sustained release: MS contin (12 hours)
oral extended release: Kadian (12-24hrs)
59
is IV morphine short or long acting?
short acting, rapid onset
60
what types of morphine isnt really recommended due to
IM & SQ
61
what is peak onset time for IV morphine and its duration time?
onset is 20 minutes, duration is 3-5 hours
62
what is morphine used for (2)
pulmonary edema, pain relief
63
what opioid medication has lower affinity for mu receptor
hydrocodone
64
true or false: hydrocodone is mostly combined with something else
true
65
hydrocodone + acetaminophen =
Vicodin, Norco, Lorect
66
hydrocodone + ibuprofen =
Vicoprofen
67
hydrocodone is weaker than
oxycodone
68
what opioid medication has a higher affinity for the mu receptor
oxycodone
69
oxycodone + acetaminophen =
Percocet(pill), Roxicet (oral solution)
70
Oxycodone + ASA =
percodan
71
peak and duration for Percodan
1 hour, 4-5 hr duration
72
OxyContin is ___ ____
controlled release
73
what is peak and duration for OxyContin
3-4 hour peak, 12 hour duration
74
hydromorphone =
dliaudid
75
what opioid is a strong opioid agonist
hydromorphone
76
hydromorphone has similar _____ as morphine but a higher _____
efficacy, potency
77
how is hydromorphone available?
PO, SQ, IM, IV, PR
78
what method of admin is hydromorphone NOT recommended in?
IM
79
can hydromorphone be used in a PCA form?
YES
80
true/false: hydromorphone is also available in dilaudid HP
true
81
hydromorphone oral peak & duration
30-90 minutes, 4-5 hours
82
hydrmorphone IV peak
10-20 minutes
83
risk of hydromorphone
prolonged QT, increased risk of seizures
84
how is hydrmorphone eliminated
renally
85
contraindications of hydrmorphone?
kidney disease
86
meperidine =
demerol
87
meperidine uses what type of metabolism?
hepatic P450 metabolism
88
what product is made from the hepatic P450 metabolism in meperidine?
normeperidine
89
accumulation of normeperidine in the blood leads to
sezuires, renal failure
90
how is meperidine administered?
PO, IM, SQ, IV
91
when can meperidine (demerol) be fatal?
when used with MAOIs
92
is meperidine recommended as a first line agent?
NOOOO
93
what is one unique factor regarding overdose of meperidine?
naloxone does not reverse metabolite (can worsen seziures)
94
fentanyl =
duragesic, fentora (DANGER)
95
what opioid is a very potent agent, 50-100 times more potent than morphine and 30-50 times more potent than heroin?
fentanyl
96
should you give fentanyl to an opiate naive patient for chronic pain treatment?
absolutely NOT
97
IV effect time/duration
immediate effect, 30-60 min duration
98
duragesic ROA =
transdermal
99
duragesic has a (short/long) halflife and the patch is worn for ___ hours
long, 72 hours
100
fentora ROA =
buccal
101
fentora is often used for
breakthrough pain in oncology patients
102
what is unique about fentanyl? (and also crazy scary for doctors and first responders)
absorbed through the skin
103
what opioid is used in managing chronic pain and treating opioid addiction
methadone
104
mechanism of action of methadone (3)
1. Mu agonist
2. N-methyl-D-aspartate (NMDA antagonist)
3. NE and 5HT re-uptake inhibitor
105
half life of methadone
12-40 hours
106
adverse side effects methadone
pronlonged QT, conversion between products NOT linear
107
what opioid is a non-opioid synthetic analgesic and barely stimulates the mu receptor?
tramadol (ultram)
108
mechanism of action of tramadol
1. very mild mu agonist
2. reduces re-uptake of NE and 5-HT
109
what are some positives to taking tramadol vs other opioids?
1. less resp depression
2. less histamine release
110
side effects of tramadol
1. N/V
2. constipation
3. HA & dizzy
4. SERATONIN SYNDROME
4. SEIZURES
111
contraindications of tramadol
a patient who takes SSRI's
112
potentially life-threatening condition associated with increased serotonergic activity in the CNS
serotonin syndrome
113
clinical manifestations of serotonin syndrome (2)
1. AMS
2. Agitation
114
Autonomic symptoms of Serotonin Syndrome (5)
1. Tachycardia
2. Hyperthermia
3. sweating
4. diarrhea
5. mydriasis (dilated pupil)
115
neuromuscular hyperactivity in serotonin syndrome =
hyperreflexia
116
higher doses of opioids are associated with higher risk of ______
overdose
117
a value assigned to opioids to represent their relative potencies
Miligram Morphine Equivalent (MME)
118
what is the reason for calculating the MME?
can assess how much opioids a patient is recieving
119
if >50 MME/day the risk of overdose _____
doubles
120
#1 opioid side efecct
constipation
121
why do opioids cause constipation? (3)
1. decreases intestinal secretions
2. decrease peristalsis
3. increased smooth muscle tone
122
does a tolerance develop with constipation and taking opioids?
NO
123
treatments for constipation while taking opioids (4)
1. scheduled stimulant laxative
2. increase fluid intake
3. exercise
4. peripherally acting opioid antagonists
124
what opioid side effect stimulates receptors of the medulla called the chemoreceptor trigger zone
Nausea/Vomiting
125
does N/V while taking opioids get worse with constipation?
yes
126
can you build a tolerance to opioid caused N/V?
yes, 3-4 days
127
what opioid side effect should you start at a low dose to avoid?
sedation
128
name the opioid side effect based on these factors:
1. CNS depressant
2. dose dependent
3. tolerance builds in 1-3 days
sedation
129
pathognomonic sign of opioid overdose =
miosis (pinpoint pupils)
130
are there any major side effects of the cardiac system at low doses
usually not
131
high doses of opioids can cause these cardiac symptoms (2)
1. bradycardia
2. hypotension
132
do you develop a tolerance to urinary retention when taking opioids?
either/or, its a surprise :)
133
what is the main cause of death from an opioid overdose?
respiratory depression
134
does tolerance develop in respiratory depression
yes
135
respiratory depression is ____ _____
dose dependent
136
treatment of adverse opioid side effects (2)
1. hold opioid
2. naloxone
137
Mechanism of action of naloxone
1. antagonizes both mu 1&2
2. rapid onset, short half-life
138
gradual loss of effect with repeated doses =
tolerance
139
when is tolerance typically seen?
2-3 mo of use
140
patients on chronic opioid therapy should consider ___ ____ to avoid tolerance
opioid rotation
141
what side effects develop a tolerance
sedation, resp depression, N/V, +/- urinary retention
142
adaptation which produces withdrawal when drug is stopped
physical dependence
143
strong desire or a sense of compulsion to take a drug, progressive neglect of alternative pleasures of interests because of drug use, increased amount of time spent obtaining drug
psychological dependence or addiction
144
a primary chronic disease of brain reward, motivation, memory, and related circuitry
addiction (per the american society of addiction medicine)
145
what does addiction cause
pathologic pursuit of reward and relief through substance use and other behaviors
146
severity and duration depends on quantity, type, frequency, and duration of opioid use
withdrawal
147
symptoms of withdrawal occur with ____ cessation and ____ when on chronic opioids
abrupt, chronic
148
removal of inhibition =
increases neurotransmission
149
withdrawal symptoms
abd pain, diarrhea, HTN, lacrimation, rhinorrhea, goosebumps, pupillary dilation, hyperventilation, pain/irritability, dysphoria/depression, restlessness and insomnia, forgetfulness
150
diphenoxylate (lomotil) is used to treat
diarrhea
151
what type of license must you have to prescribe lomotil and what schedule drug is it?
DEA, its a schedule 5
152
what is in lomotil that makes it an opioid like product?
Diphenoxylate
153
Diphenoxylate is insoluble so it stays in the ____ _____
GI tract
154
what is loperamide (imodium) used for?
diarrhea treatment
155
loperamide is an ____ ______
opioid agonist
156
does loperamide stay in the GI tract?
yes
157
high doses of loperamide can interact with the ____
CNS
158
people often misuse ____ & ______ to get a small high and end up with ______
loperamide & diphenoxylate, f ton of constipation
159
what is dextromethorphan (delsym, DM) used for?
anti-tussive
160
what is in dextromethorphan?
dextro-isomer of codeine
161
effects of dextromethorphan are _____ by opioid antagonists but in high doses interacts with ____ and causes _____
unaffected, CNS, euphoria
162
what are 3 non-analgesic uses of opioids (3 meds)
1. Diphenoxylate
2. Loperamide
3. Dextromethorphan
163
opioid antagonists
compete with opioid receptors
164
what is the primary opioid antagonist?
mu
165
effects of opioid antagonists (3)
1. reverse agonists
2. deterrent to use
3. different medications have different pharmacokinetic profiles
166
examples of opioid antagonists (4)
1. naloxone
2. Naltrexone
3. Naloxegol
4. Methylnaltrexone
167
important characteristics about naloxone (4)
1. rapid reverse of opioid OD
2. Low PO bioavail (give nasal, IV, IM, etc)
3. rapid onset
4. SHORT duration of action (often give multiple doses)
168
side effects of naloxone (4)
1. projectile vomiting
2. agitation
3. HTN
4. Tachycardia
169
do you need a perscription for naloxone?
no, available at pharmacy, in most AEDs and EMTs/Police carry
170
important characteristics about Naltrexone (reVia, Vivitrol) (5)
1. opioid & alcohol addiction
2. NOT given with opioid agonists (reverses effect)
3. NOT for use during acute withdrawl
4. given for cravings
5. available oral and IM
171
side effects of naltrexone
depression, suicide risk, hepatotoxicity, insomnia, N/V
172
important charcateristics of Naloxegol (moveantik)
1. naloxone + polyethylene glycol polymer
2. works ONLY within GI (too large to leave)
3. available PO
173
important characteristics of methylnaltrexone (relistor)
1. quaternary derivative of naltrexone
2. works ONLY in GI (positive charge keeps in GI)
3. available SC
174
both Naloxegol and Methylnaltrexone treat opioid ______
constipation
