Opiates, Opioids Flashcards
1
Q
Opiates are made from ___
A
plants
2
Q
Opioids are made from ___
A
labs
3
Q
Active compounds of poppies (2)
A
Morphine, codeine (prodrug of morphine)
4
Q
what was soldier’s disease?
A
opium abuse
5
Q
opioid MOA
A
opioid receptor agonist:
- block release of pain neurotransmitters from nociceptive fibers (glutamate, substance P, and calcitonin gene-related peptide)
- activate presynaptic receptors on GABA neurons (inhibit GABA release)
6
Q
morphine MOA
A
Mu agonist
7
Q
where are Mu receptors located?
A
primarily brainstem and medial thalamus
8
Q
what is subtype Mu1 associated w/?
A
Mu1 related to analgesia, euphoria, and serenity
9
Q
what is subtype Mu2 associated w/?
A
Mu2 is related to respiratory depression, pruritus, prolactin release, dependence, anorexia, and sedation. These are also called OP3 or MOR (morphine opioid receptors).
10
Q
where are kappa (OP2, KOR) located?
A
limbic and other diencephalic areas, brain stem, and spinal cord
11
Q
delta receptors, located mostly in the brain, are associated w/ what?
A
not well studied, maybe psychomimetic and dysphoric effects
12
Q
name some full opioid agonists
A
Morphine Fentanyl Hydromorphone Codeine Oxycodone Methadone Heroin
13
Q
name 2 opioid partial agonists
A
Buprenorphine Butorphanol (Stadol)
14
Q
name 2 opioid antagonists
A
Naloxone (Narcan)
Naltrexone
15
Q
name a combo opioid partial agonist/antagonist
A
Suboxone (buprenorphine + naloxone)
16
Q
name some short-acting opioids
A
Codeine Hydrocodone Hydromorphone (Dilaudid) Morphine (MSIR, Roxanol) Oxycodone Oxymorphone (Opana) Fentanyl (Actiq)
17
Q
list some uses for short-acting opioids
A
Acute pain
Incident pain
Breakthrough pain
Activity (PT, travel)
18
Q
list some long-acting opioids
A
Fentanyl (transdermal) Levorphanol Methadone Morphine (MS Contin, Kadian, Avinza) Oxycodone (Oxycontin) Oxymorphone (Opana ER)
19
Q
what are some uses for long-acting opioids?
A
Chronic pain
Moderate to severe pain
20
Q
DEA scheduling 1-5 is ___ to ___ addictive
A
most to least
21
Q
opioid ADRs
A
Sedation, lethargy Constipation Respiratory depression N/V Pruritus/urticaria (direct histamine response, can also cause bronchospasm)
22
Q
triad of opioid OD
A
Miosis
Loss of consciousness
Respiratory depression
23
Q
opioid OD antidote
A
naloxone (Narcan)
24
Q
what is something that can exacerbate and opioid OD?
A
EtOH (or other CNS depressants)
25
does morphine cross the BBB?
yes
26
T/F there are a lot of drug int's w/ morphine
False
27
morphine ADRs
```
Direct histamine release
Respiratory depression
Orthostasis
Constipation
N/V
```
28
is codeine a strong or weak Mu agonist?
weak
29
when codeine is metabolized to morphine, it's potency is ___% that of morphine
50%
30
codeine metabolism
CYP 2D6 substrate
Inhibited by bupropion, cimetidine, celecoxib, cocaine
Warning for ultra-rapid metabolizers (nursing infants)
31
Oxycodone (roxicodone, oxycontin, percocet, etc.) is active at what receptors?
mu and kappa receptors
32
what enzyme metabolizes oxycodone?
CYP 2D6
33
fun facts about oxycodone
High potency analgesia
t1/2 = 2.5 - 3 hrs
Highly abused
34
what is the most commonly used opioid?
hydrocodone
35
T/F, hydrocodone has weak activity at mu receptor
true
36
what enzyme metabolizes hydrocodone?
CYP 2D6 (to hydromorphone)
37
name some combo hydrocodone meds
hydrocodone/acetaminophen (Lortab, Lorcet, Vicodin)
| Hydrocodone/ibuprofen (Vicoprofen)
38
Hydromorphone (Dilaudid, Exalgo) works at which receptors?
mu and delta receptors
39
T/F, hydromorphone is more potent than morphine
true
40
Oxymorphone (Opana) is ___ x more potent than morphine
10
41
T/F, oxymorphone is a P450 drug
false
42
name 2 opioids that are NOT metabl by 450
oxymorphone & hydromorphone
43
Fentanyl (Actiq, Duragesic) is a strong/weak mu agonist
strong
44
fentanyl is __ x more potent than morphine
80
45
what enzyme metabolizes fentanyl
CYP 3A4
46
what do we worry about for the fentanyl transdermal patch?
heat - causes dose dumping
47
Can you give fentanyl to a patient with a codeine allergy?
they are structurally different, so theoretically, yes
48
can you reverse effects of meperidine (demerol) w/ narcan?
no
49
meperidine (demerol) is a neurotoxic metabolite that can cause what?
Anxiety, tremors, seizures
50
pts taking meperidine should avoid taking what?
antcholinergics & MAOIs
51
Propoxyphene (Darvon, Darvocet) is/is not reversible w/ narcan
is; can cause neuro & cardiotoxicity
52
methadone MOA
NMDA antagonist, Serotonin-norepinephrine reuptake inhibitor (SNRI) - Neuropathic pain
53
methadone has a long half-life because it is
highly lipophilic
54
serious ADR of methadone
cardiotoxicity; torsades des pointes
| titrate slowly
55
metab enzymes of methadone
CYP3A4 and 2D6
56
buprenorphine MOA & use
Mu receptor partial agonist, Kappa receptor antagonist
Used for opioid/heroin addiction
(3A4 metab)
57
buprenorphine ADR
Sedation
N/V
Dizziness, HA
Respiratory depression
58
Butorphanol (Stadol)
| Levorphanol general info
Used for moderate to severe pain
Respiratory depression
Euphoria
Typical opioid ADRs
59
naloxone (narcan) ADRs
headache, myalgia, increased B/P, opioid withdrawal
60
naloxone (narcan) MOA, ind
mu receptor antagonist (admin IM, subQ, IV, intranasal)
Reverses respiratory depression, sedation, hypotension
(Works in 2 – 5 min, Lazarus effect)
Used as a reversal agent for opioid OD
61
Tramadol (Ultram, Ultracet, Ryzolt, Rybix) MOA
Synthetic codeine analog
Weak Mu receptor agonist
Inhibits NE and 5HT uptake (SNRI)
62
Tramadol (Ultram, Ultracet, Ryzolt, Rybix) warning
Warning for seizure risk at recommended and increased doses (higher incidence with SSRIs, TCAs, opioids, MAOI)
63
Tramadol (Ultram, Ultracet, Ryzolt, Rybix) serious ADRs
Suicide risk
| Serotonin syndrome risk
64
Tramadol (Ultram, Ultracet, Ryzolt, Rybix) ind
As effective as morphine for mild to moderate pain, labor pain - less effective for severe or chronic pain
65
Tramadol (Ultram, Ultracet, Ryzolt, Rybix) ADRs
Dizziness, vertigo, nausea, constipation, headache, somnolence, vomiting, pruritus
Supposedly less respiratory depression than morphine
66
Tramadol (Ultram, Ultracet, Ryzolt, Rybix) drug int
CYP2D6 and CYP3A4 inhibitors
Serotonergic drugs
Carbamazepine
67
Tapentadol (Nucynta, Nucynta ER) gen info
Mu opioid agonist, NE reuptake inhibitor
1st opioid specifically approved for diabetic neuropathy
Stronger than tramadol
No P450 metabolism
Potentially fatal if taken with EtOH
DEA CSA: CII
Same drowsiness/dizziness as oxycodone (less N/V and constipation)
68
opioid conversion guidelines
Calculate 24 hr total dose
Divide by dosing schedule
Reduce dose by 30% - 50%
Titrate to goal
69
warning signs of opioid addiction/abuse
Early refills
Requesting higher doses
Prescriber hopping
70
define opioid addiction
Use of medication outside normally accepted standard for the drug
Cravings and preoccupation with the drug
Loss of control of use
phys vs psych
71
opioid dependence parameters
> 3 behaviors over a 12-month period
72
signs & sx of opioid withdrawal
```
Mood lability -> irritability, anxiety, restlessness
Chills, sweating
Abdominal pain, nausea, diarrhea
Sneezing, rhinorrhea, dilated pupils
Muscle weakness, pains
Insomnia
```
73
time line of opioid withdrawl
8-16 hrs after last dose (peak 2 – 4 days)
resolves 7 – 14 days
Not life-threatening
74
red flags of dependency/addiction
post-op
requesting specific med/increased dose
don't want PE, testing
75
what is the CAGE questionnaire used for?
alcohol & drug dependency quick eval
76
opioid dependence tx
Detoxification (necessary for long-term abstinence)
can be slow (tapering via methadone) or rapid (via reversal med or d/c of opioids; naltrexone/buprenorphine, clonidine, anti-diarrheal, NSAIDs, muscle relaxants)
77
goals of opioid withdrawal tx
Prevent or reduce withdrawal symptoms
Prevent or reduce cravings
Avoid relapse
Restore normal physiological functions caused by opioid dep.
Improve impairments created by opioid dep
78
non-pharm withdrawal tx
Support groups (Narcotics Anonymous), psychotherapy, pain contracts, TROSA, family counseling
79
pharm withdrawal tx
Methadone
Buprenorphine
Naltrexone
80
2016 CDC Chronic Pain Guidelines when pain lasts > 1 yr
Nonopioid & nonpharm tx preferred
Consider opioids when benefit outweigh risk
Est tx goals before starting opioids
Discuss risks & realistic benefits
Start with IR opioids & lowest effective dosage (3 – 7 days for acute pain)
Evaluate treatment q 1-4 wks after starting or increasing dose; if dosing stable, evaluate q3 months
If harm > benefit, taper and d/c
Evaluate risk for harms
Sleep disorders, pregnancy, renal/liver insufficiency, 65 or older
Review history of controlled substance prescriptions
Urine drug testing prior to initiation and annually thereafter
Avoid concomitant use of BZDs
Arrange tx for opioid-use disorders
