Week 12-Analgesics Flashcards
1
Q
What are the non-opioid analgesics?
A
NSAIDs
acetaminophen
2
Q
What are the adjuvant analgesics?
A
anticonvulsants (gabapentin)
TCAs
SSRIs
SNRIs
3
Q
What are the opiate analgesics?
A
codeine
morphine
4
Q
What are the opioid analgesics?
A
propoxyphene tramadol hydromorphone oxycodone fentanyl meperidine methadone
5
Q
What is the MOA of NSAIDs
A
inhibition of cyclooxygenase (COX)
*most are non selective for COX 1 and 2
6
Q
COX 1 is _______
A
city protective
7
Q
COX 2 is ______
A
inflammatory
8
Q
What level of pain are NSAIDs given?
A
mild to moderate
9
Q
What is the ceiling effect associated with NSAIDs?
A
addition drug gives no additional analgesia, only increased side effects
10
Q
What are the NSAID class side effects? (4)
A
GI upset
GI irritation/ ulceration
edema
renal impairment
11
Q
What are the non Opioid NSAID classes? (6)
A
salicylic acid derivative propionic acids acetic acids fenamates oxicame cox-2 inhibitors
12
Q
what are the NSAID salicylic acid derivatives?
A
aspirin and salsalate
13
Q
What are the NSAID propionic acids?
A
ibuprofen
ketoprofen
naproxen
14
Q
What are the acetic acid NSAIDs?
A
keterolac
diclofenac
etodolac
indomethacin
15
Q
What is a oxicam NSAID?
A
meloxicam
16
Q
What is a COX 2 inhibitor NSAID?
A
Celecoxib (Celebrex)
17
Q
If one NSAID fails then _____
A
try another
18
Q
Why do NSAID combinations with dual MOAs work in synergy?
A
efficacy > sum of the individual components
19
Q
What is dose tritiation of NSAID combinations limited by?
A
the non-opioid
often the cause of unintended overdose
most hepatic failures are from excessive opiate/ APAP use
20
Q
What is the maximum dose of acetaminophen daily?
A
4 grams daily- soon to be 3g daily per FDA?
21
Q
What is the maximum dose of aspirin?
A
4 grand daily but higher for anti-inflammatory
22
Q
What is the maximum dose of ibuprofen?
A
3.2 grams daily
23
Q
What NSAID is a weak anti-inflammatory agent and contraindicated with less than 16 years old?
A
salicylic acids- aspirin
24
Q
What are salicylic acids (aspirin) contraindicated if less than 16 years of age?
A
Risk of Reyes Syndrome
25
What is the max daily dose of salicylic acid for anti-inflammatory?
3.6-5.4 grams daily
26
What NSAID is anti-inflammatory, anitypyretic and analgesic?
propionic acids-ibuprofen
27
What is the max dose of ibuprofen for fever/pain/dysmenorrhea?
max 1.2 grams daily
28
What is the only commonly available injectable NSAID used for moderate to severe pain?
keterolac (Toradol)
29
When is keterolac (Toradol) useful?
post- op pain
30
Why is keterolac (toradol) only used for 5 days?
increased risk of GI bleed
31
What is the usual dose of keterolac (toradol)?
30mg IVP q6h (max 120md/daily)
32
When should keterolac (toradol) dose be reduced to 15mg?
pts >65 years
body weight less than 50kg
"moderately" elevated serum creat (>2mg/dL)
33
What NSAID is for mild to moderate pain that is little used anymore?
fenamates-Mefenamic acid (Ponstel)
34
What NSAID should you avoid alcohol due to enhancing mucosal irritation?
fenamates-Mefenamic acid (Ponstel)
35
What NSAID is mainly used for acute & chronic RA and OA?
Oxicams- Piroxicam (Feldene) & Meloxicam
36
What is the advantage of oxicams?
long half life (45-50 hours)
| allows daily dosing
37
When should the dose of oxicams be reduced?
with hepatic dysfunction
38
What is the only remaining selective COX 2 inhibitor?
celecoxib (Celebrex)
39
What COX- 2 inhibitor was "voluntarily" removed in 2004? why?
Rofecoxib (Vioxx) due to increased number of "cardiac events" AMIs
40
When is celecoxib (Celebrex), a selective COX 2 inhibitor useful?
in non-cardiac patients (orthopedics)
41
What is a NON NSAID, Non-opioid analgesic that is an antipyretic agents with little anti-inflammatory activity?
acetaminophen (Tylenol)
42
What is the result of acetaminophen overdose?
hepatic failure
| avoid in pts with alcoholic liver disease
43
What is the MOA of acetaminophen?
inhibits both COX isoenzymes
44
What is the result of Acetaminophen's COX inhibition being more pronounced in the brain?
inhibits hypothalamic heat-regulating center
| explaining its anti-pyretic activity
45
What is the acetaminophen adjustment for renal impairment?
CrCl 10-50: administer every 6 hours
CrCl <10: administer every 8 hours
*metabolites accumulate
46
What is the injection form of acetaminophen?
Afirmed
| 100mg/100mL (post op x 4 doses)
47
What is the dose of Afirmed in adults/adolescent greater than 50kg?
1000mg every 6 hours
| max 4 grams/daily
48
What is the dose of Afirmed in adults/adolescents less than 50kg?
15mg/kg every 6 hours OR 12.5mg/kg every 4 hours
| max 75mg/kg/daily
49
What is the child dosing of acetaminophen?
10-15mg/kg/dose every 4-6 hours
| MAX 5 doses a day
50
What is the treatment for acetaminophen toxicity?
N-acetylcysteine (Mucomyst) oral loading dose 140mg/kg
IV therapy: N-acetylcystine (Acetadote)
51
According to a study in Norway 114, 744 children born between 1999-2009 with history go long-term acetaminophen use during pregnancy was associated with what?
resulted in more than a 2 fold increase risk of offspring ADHD
52
What duration of acetaminophen use during pregnancy was associated with a decrease in ADHD use?
use for less than 8 days
53
According to JAMA study of single dose opioid vs non opioid for upper extremity pain in the ED what was the different among ibuprofen vs (oxycodone, hydrocodone and codeine)
No significant difference in pain scores 2 hours post dose.
54
What is the classic analgesic receptor?
mu
55
What is the basis of mixed agonist-antagonist agents?
opioid receptors
56
What is a natural agent from opium?
opiates
| codeine and morphine
57
What are modifications of natural opiates or synthetics?
opioids
58
What are the mixed opioid agonist-antagonists?
buprenorphine
butorphanol
pentazocine
Nalbuphine (nubain)
59
What mixed opioid agonist-antagonists is still used?
Nalbuphine (nubain)
more effective in feamles
ceiling effect on respiratory depression
use in labor and delivery
60
What is "endogenous morphine" that is derived from small endogenous peptide hormones?
endorphins
61
What accounts for the variability of response to pain?
endorphins
62
What are the opiate/opioid side effects?
```
nausea
itching
sedation & cognitive impairment
respiratory distress
meiosis (pinpoint pupils)
decreased GI peristalsis
```
63
What should be done for opiate/opioid decreased peristalsis?
constipation and impaction need to anticipate and prophylaxis!
tolerance does NOT develop
64
How can opioid induced constipation be prevented?
100mg of docusate sodium and 17.2mg of sennosides twice a day
OR
10mg biscadoyl at bedtime as needed if no BM in previous 24 hours; repeat in the morning if still no BM
65
What are the opioids for mild to moderate pain?
tramadol (ultram)
codeine (Tylenol #2-4)
Hydrocodone (Vicodin, lortab and Norco)
66
What is significant about tramadol (ultram)? (4)
weak opioid analgesic, useful for chronic pain
limit use for acute pain (increase dosage over weeks, increases N/V)
dual mechanism of action (weakly binds mu and inhibitors NE and serotonin reuptake)
useful for neuropathic pain
67
When was tramadol (ultram) reclassified as a controlled substance? (C-III)
in 2014, less abuse potential
68
What is a naturally occurring opiate with weak analgesic effects and an antitussive?
codeine
69
60 mg of codeine produces less analgesics than what?
650mg of aspirin
70
What metabolizes codeine to morphine?
CYP2D6
71
What CYP2D6 inhibitors decrease codeines effect?
```
antiemetic phenothiazines (thorazine, compazine and phenergen)
haloperidol, fluoxetine and paroxetine
```
72
What percentage of the populations lacks the CYP2D6 enzyme?
10%
73
What medication if only available PO with acetaminophen C-III?
hydrocodone
| Norco, lortab and Vicodin
74
What medication has better pain relief and longer duration compared to codeine?
hydrocodone
75
Hydrocodone is metabolized by _____ to ______.
CYP2D6; hydromorphone (Dilaudid)
76
What percentage of unintentional overdoses involve combination products, most commonly hydrocodone?
63%
77
What are the opioids for moderate to severe pain (C-II)?
```
morphine
hydromorphone (dilaudid)
oxycodone
Meperidine
Methadone
Fentanyl
```
78
What is a prototype pure mu receptor agonist
morphine
79
What are the 2 active metabolites that are both really eliminated of morphine?
morphine-3-glucuronide (M3G) is a neurotoxin AND
| M6G has analgesia 2-4x that of morphine
80
What is the result of morphine induced histamine release?
hypotension
| pruritus
81
What medication has a significant first-pass effect? (concentration is greatly reduced before it reaches systemic circulation)?
morphine
82
What is the parenteral to oral dose ratio of morphine?
1:3
83
What is the infection dose of morphine sulfate?
2mg/mL
84
What are the dosage forms of morphine sulfate? (5)
```
injection
immediate release (MSIR)
SR Capsules (Kadian)
CR tabs (MS Contin)
Oral Solution (Roxanol)
```
85
What medication is 5-7x more potent than morphine that can result in iatrogenic overdoses?
hydromorphone (dilaudid)
86
What are the improved side effect profiles of hydromorphone (dilaudid)?
less histamine release
| no active opioid metabolites (good in really impaired)
87
What is the recent sustained release product and dosages?
Exalgo
| 8, 12, 16, and 32mg CR tabs
88
What hydromorphone medication was recalled by the FDA for alcohol destroying the time release mechanism resulting in overdoses?
SR Palladone
89
What is the dosage form of hydromorphone (dilaudid) injection?
2mg/mL
90
What is more potent with fewer side effects than morphine?
oxycodone (oxycontin)
| less histamine release, pruiritis and nausea)
91
Oxycodone is metabolized by _______ to _____.
CYP2D6; oxymorphone (also active)
92
When is oxycodone useful?
in patients with CYP2D6 deficiency or if on inhibitors (phenothiazine antiemetics, fluoxetine and paroxetine)
useful in non responders to codeine & hydrocodone
93
What are the dosage form of oxycodone?
```
oxycodone IR
Roxicodone
Oxycodone CR (OxyContin)
with acetaminophen (Percocet)
with aspirin (Percodan)
```
94
What is not recommended as a first line agent, more lipophilic and therefore has a more rapid onset with shorter duration of 2-3 hours?
Meperidine (Demerol)
95
What is Meperidine (Demerol) metabolized to?
active normeperidine (neurotoxic)
96
What is significant about the active normeperidine metabolite of Meperidine (demerol)?
long metabolite half life that accumulates
euphoria, irritability, delirium, tremors and seizures
toxicity is NOT reversed by opiate antagonists
metabolite is really eliminated
97
What is Meperidine (Demerol) contraindicated?
in patients on MAOIs (serotonin syndrome)
98
When can Meperidine (Demerol) be used according to American Pain Society (APS)?
in patients with serious opiate allergies
| useful in controlling post anesthesia shivering
99
What medication has unique pharmacology-racemic mix of L & D isomers?
Methadone (Dolophine)
100
What does the L isomer of Methadone (Dolophine) do?
opioid activity
101
What does the D isomer of Methadone (Dolophine) do?
NMDA antagonist & NE/Serotonin reuptake inhibitor)
102
What can Methadone (Dolophine) also be useful for?
neuropathic pain
103
What medication has the longest & variable half life (12-190 hours; usually 24h)
Methadone (Dolophine)
104
What medication is useful entreatment of opiate addiction?
Methadone (Dolophine)
| dosed every 24h
105
How long does analgesia last with Methadone (Dolophine)?
4-8 hours
therefore dose every 6-8 hours for analgesia
106
What medication is 100x more potent than morphine and is therefore dosed in mcg?
Fentanyl
107
What medication is extremely lipophilic, rapid onset and short duration of (30-60minutes)?
fentanyl
108
Why is Fentanyl a safe option in renal failure?
No active metabolites
109
What medication has fewer adverse effects than morphine or dilaudid with minimal histamine release and little hypotensive effect?
fentanyl
110
What are the dosage forms of fentanyl?
injection
lozenge (Actiq)
Transdermal (Duragesic)
111
What medication is not usually used in opiate naive patients?
Duragesic
112
What needs to monitor when giving duragesic?
respiratory rate for the first 24 hours
113
How often does Duragesic need to be replaced?
every 72 hours
DONT ADD
**look for multiple patched when admitting out patients**
114
When is fentanyl (Actiq and fentora) used?
only for long standing chronic (cancer) pain?
115
What medication is a pure mu receptor ANTAGONIST?
naloxone (narcan)
116
What medication if used to reverse sedation and respiratory depression and reverses analgesia?
naloxone (narcan)
117
What is the dose of naloxone?
dilute 0.4mg to less than 10mL saline (0.9%NaCl)
| administer slow IVP (1ml every 1-2 minutes)
118
When should you stop administering naloxone?
monitor respiratory rate and stop when it increases
119
What is the first thing to be done with equianalgesic dosing?
convert all doses to oral morphine equivalents
120
What should be done for every 12 hour dosing?
Divide by 2
round down to SR
provide that dose as MS Contin every 12 hours ATC
121
What should be done for every 8 hour dosing?
divide by 3
round down to SR
provide that dose as MC contin every 8 hours around the clock
122
What can be done to provide "breakthrough" pain with equianalgesic dosing?
provide 20-25% (divided by 4 or 6) as IR every 4-6 hours PRN
123
What is the oral equiananalgesic dose of morphine 10mg parenteral?
30mg PO
124
What is the oral equianalgesic dose of hydromorphone 1.5mg parenteral?
7.5mg PO
125
What are the recommendations of the CBC Opioid-Prescribing Guidelines?
1. nonpharmacologic therapy and non opioid are preferred for chronic pain
2. When starting, prescribe immediate-release opioids
3. Prescribe lowest effective dose
4. For acute pain use the lowest effective IR dose for 3-7 days
5. evaluate benefits and harm within 1-4 weeks of starting and again every 3 months or more frequently
6. incorporate strategies to mitigate risk: offer naloxone for h/o of OD, SA, doses greater than 50MME per day or benzos
7. Monitor controlled substance use with PDMP
8. Urine D/S before staying new and annually
9. avoid prescribing with Benzes
10. Offer or arrange evidence-based treatment (MAT) for patients with opioid use disorder
126
How can you obtain morphine milligram equivalents (MME)?
multiple the total daily opioid dose by the conversion factor to obtain equivalent TTD of morphine in mg
127
What medications are used for medication assisted therapy (MAT)?
buprenorphine
naltexone
methadone
128
What MAT is a partial opioid antagonist to help with withdrawal symptoms that can be started with opioids in the pts system?
buprenorphine
129
What MAT is a opioid antagonist that may precipitate withdrawal symptoms that cannot be given unless opioid free for 7-14 days before use?
naltrexone
130
What is the IM form of naltrexone?
Vivitrol
131
What MAP is a long-acting opioid agonist that transfers opioid addiction to longer half-life allowing for a taper and therefore requires daily dosing ?
Methadone
