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Pharmacology > Week 12-Analgesics > Flashcards

Week 12-Analgesics Flashcards

1
Q

What are the non-opioid analgesics?

A

NSAIDs

acetaminophen

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2
Q

What are the adjuvant analgesics?

A

anticonvulsants (gabapentin)
TCAs
SSRIs
SNRIs

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3
Q

What are the opiate analgesics?

A

codeine

morphine

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4
Q

What are the opioid analgesics?

A 
propoxyphene
tramadol
hydromorphone
oxycodone
fentanyl
meperidine
methadone
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5
Q

What is the MOA of NSAIDs

A

inhibition of cyclooxygenase (COX)

*most are non selective for COX 1 and 2

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6
Q

COX 1 is _______

A

city protective

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7
Q

COX 2 is ______

A

inflammatory

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8
Q

What level of pain are NSAIDs given?

A

mild to moderate

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9
Q

What is the ceiling effect associated with NSAIDs?

A

addition drug gives no additional analgesia, only increased side effects

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10
Q

What are the NSAID class side effects? (4)

A

GI upset
GI irritation/ ulceration
edema
renal impairment

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11
Q

What are the non Opioid NSAID classes? (6)

A 
salicylic acid derivative
propionic acids
acetic acids
fenamates
oxicame
cox-2 inhibitors
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12
Q

what are the NSAID salicylic acid derivatives?

A

aspirin and salsalate

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13
Q

What are the NSAID propionic acids?

A

ibuprofen
ketoprofen
naproxen

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14
Q

What are the acetic acid NSAIDs?

A

keterolac
diclofenac
etodolac
indomethacin

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15
Q

What is a oxicam NSAID?

A

meloxicam

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16
Q

What is a COX 2 inhibitor NSAID?

A

Celecoxib (Celebrex)

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17
Q

If one NSAID fails then _____

A

try another

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18
Q

Why do NSAID combinations with dual MOAs work in synergy?

A

efficacy > sum of the individual components

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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

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20
Q

What is the maximum dose of acetaminophen daily?

A

4 grams daily- soon to be 3g daily per FDA?

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21
Q

What is the maximum dose of aspirin?

A

4 grand daily but higher for anti-inflammatory

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22
Q

What is the maximum dose of ibuprofen?

A

3.2 grams daily

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23
Q

What NSAID is a weak anti-inflammatory agent and contraindicated with less than 16 years old?

A

salicylic acids- aspirin

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24
Q

What are salicylic acids (aspirin) contraindicated if less than 16 years of age?

A

Risk of Reyes Syndrome

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25
Q

What is the max daily dose of salicylic acid for anti-inflammatory?

A

3.6-5.4 grams daily

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26
Q

What NSAID is anti-inflammatory, anitypyretic and analgesic?

A

propionic acids-ibuprofen

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27
Q

What is the max dose of ibuprofen for fever/pain/dysmenorrhea?

A

max 1.2 grams daily

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28
Q

What is the only commonly available injectable NSAID used for moderate to severe pain?

A

keterolac (Toradol)

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29
Q

When is keterolac (Toradol) useful?

A

post- op pain

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30
Q

Why is keterolac (toradol) only used for 5 days?

A

increased risk of GI bleed

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31
Q

What is the usual dose of keterolac (toradol)?

A

30mg IVP q6h (max 120md/daily)

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32
Q

When should keterolac (toradol) dose be reduced to 15mg?

A

pts >65 years
body weight less than 50kg
“moderately” elevated serum creat (>2mg/dL)

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33
Q

What NSAID is for mild to moderate pain that is little used anymore?

A

fenamates-Mefenamic acid (Ponstel)

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34
Q

What NSAID should you avoid alcohol due to enhancing mucosal irritation?

A

fenamates-Mefenamic acid (Ponstel)

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35
Q

What NSAID is mainly used for acute & chronic RA and OA?

A

Oxicams- Piroxicam (Feldene) & Meloxicam

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36
Q

What is the advantage of oxicams?

A

long half life (45-50 hours)

allows daily dosing

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37
Q

When should the dose of oxicams be reduced?

A

with hepatic dysfunction

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38
Q

What is the only remaining selective COX 2 inhibitor?

A

celecoxib (Celebrex)

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39
Q

What COX- 2 inhibitor was “voluntarily” removed in 2004? why?

A

Rofecoxib (Vioxx) due to increased number of “cardiac events” AMIs

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40
Q

When is celecoxib (Celebrex), a selective COX 2 inhibitor useful?

A

in non-cardiac patients (orthopedics)

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41
Q

What is a NON NSAID, Non-opioid analgesic that is an antipyretic agents with little anti-inflammatory activity?

A

acetaminophen (Tylenol)

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42
Q

What is the result of acetaminophen overdose?

A

hepatic failure

avoid in pts with alcoholic liver disease

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43
Q

What is the MOA of acetaminophen?

A

inhibits both COX isoenzymes

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44
Q

What is the result of Acetaminophen’s COX inhibition being more pronounced in the brain?

A

inhibits hypothalamic heat-regulating center

explaining its anti-pyretic activity

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45
Q

What is the acetaminophen adjustment for renal impairment?

A

CrCl 10-50: administer every 6 hours
CrCl <10: administer every 8 hours
*metabolites accumulate

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46
Q

What is the injection form of acetaminophen?

A

Afirmed

100mg/100mL (post op x 4 doses)

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47
Q

What is the dose of Afirmed in adults/adolescent greater than 50kg?

A

1000mg every 6 hours

max 4 grams/daily

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48
Q

What is the dose of Afirmed in adults/adolescents less than 50kg?

A

15mg/kg every 6 hours OR 12.5mg/kg every 4 hours

max 75mg/kg/daily

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49
Q

What is the child dosing of acetaminophen?

A

10-15mg/kg/dose every 4-6 hours

MAX 5 doses a day

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50
Q

What is the treatment for acetaminophen toxicity?

A

N-acetylcysteine (Mucomyst) oral loading dose 140mg/kg

IV therapy: N-acetylcystine (Acetadote)

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51
Q

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?

A

resulted in more than a 2 fold increase risk of offspring ADHD

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52
Q

What duration of acetaminophen use during pregnancy was associated with a decrease in ADHD use?

A

use for less than 8 days

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53
Q

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)

A

No significant difference in pain scores 2 hours post dose.

54
Q

What is the classic analgesic receptor?

A

mu

55
Q

What is the basis of mixed agonist-antagonist agents?

A

opioid receptors

56
Q

What is a natural agent from opium?

A

opiates

codeine and morphine

57
Q

What are modifications of natural opiates or synthetics?

A

opioids

58
Q

What are the mixed opioid agonist-antagonists?

A

buprenorphine
butorphanol
pentazocine
Nalbuphine (nubain)

59
Q

What mixed opioid agonist-antagonists is still used?

A

Nalbuphine (nubain)
more effective in feamles
ceiling effect on respiratory depression
use in labor and delivery

60
Q

What is “endogenous morphine” that is derived from small endogenous peptide hormones?

A

endorphins

61
Q

What accounts for the variability of response to pain?

A

endorphins

62
Q

What are the opiate/opioid side effects?

A 
nausea
itching
sedation &amp; cognitive impairment
respiratory distress
meiosis (pinpoint pupils)
decreased GI peristalsis
63
Q

What should be done for opiate/opioid decreased peristalsis?

A

constipation and impaction need to anticipate and prophylaxis!
tolerance does NOT develop

64
Q

How can opioid induced constipation be prevented?

A

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
Q

What are the opioids for mild to moderate pain?

A

tramadol (ultram)
codeine (Tylenol #2-4)
Hydrocodone (Vicodin, lortab and Norco)

66
Q

What is significant about tramadol (ultram)? (4)

A

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
Q

When was tramadol (ultram) reclassified as a controlled substance? (C-III)

A

in 2014, less abuse potential

68
Q

What is a naturally occurring opiate with weak analgesic effects and an antitussive?

A

codeine

69
Q

60 mg of codeine produces less analgesics than what?

A

650mg of aspirin

70
Q

What metabolizes codeine to morphine?

A

CYP2D6

71
Q

What CYP2D6 inhibitors decrease codeines effect?

A 
antiemetic phenothiazines (thorazine, compazine and phenergen)
haloperidol, fluoxetine and paroxetine
72
Q

What percentage of the populations lacks the CYP2D6 enzyme?

A

10%

73
Q

What medication if only available PO with acetaminophen C-III?

A

hydrocodone

Norco, lortab and Vicodin

74
Q

What medication has better pain relief and longer duration compared to codeine?

A

hydrocodone

75
Q

Hydrocodone is metabolized by _____ to ______.

A

CYP2D6; hydromorphone (Dilaudid)

76
Q

What percentage of unintentional overdoses involve combination products, most commonly hydrocodone?

A

63%

77
Q

What are the opioids for moderate to severe pain (C-II)?

A 
morphine
hydromorphone (dilaudid)
oxycodone
Meperidine
Methadone
Fentanyl
78
Q

What is a prototype pure mu receptor agonist

A

morphine

79
Q

What are the 2 active metabolites that are both really eliminated of morphine?

A

morphine-3-glucuronide (M3G) is a neurotoxin AND

M6G has analgesia 2-4x that of morphine

80
Q

What is the result of morphine induced histamine release?

A

hypotension

pruritus

81
Q

What medication has a significant first-pass effect? (concentration is greatly reduced before it reaches systemic circulation)?

A

morphine

82
Q

What is the parenteral to oral dose ratio of morphine?

A

1:3

83
Q

What is the infection dose of morphine sulfate?

A

2mg/mL

84
Q

What are the dosage forms of morphine sulfate? (5)

A 
injection
immediate release (MSIR)
SR Capsules (Kadian)
CR tabs (MS Contin)
Oral Solution (Roxanol)
85
Q

What medication is 5-7x more potent than morphine that can result in iatrogenic overdoses?

A

hydromorphone (dilaudid)

86
Q

What are the improved side effect profiles of hydromorphone (dilaudid)?

A

less histamine release

no active opioid metabolites (good in really impaired)

87
Q

What is the recent sustained release product and dosages?

A

Exalgo

8, 12, 16, and 32mg CR tabs

88
Q

What hydromorphone medication was recalled by the FDA for alcohol destroying the time release mechanism resulting in overdoses?

A

SR Palladone

89
Q

What is the dosage form of hydromorphone (dilaudid) injection?

A

2mg/mL

90
Q

What is more potent with fewer side effects than morphine?

A

oxycodone (oxycontin)

less histamine release, pruiritis and nausea)

91
Q

Oxycodone is metabolized by _______ to _____.

A

CYP2D6; oxymorphone (also active)

92
Q

When is oxycodone useful?

A

in patients with CYP2D6 deficiency or if on inhibitors (phenothiazine antiemetics, fluoxetine and paroxetine)

useful in non responders to codeine & hydrocodone

93
Q

What are the dosage form of oxycodone?

A 
oxycodone IR
Roxicodone
Oxycodone CR (OxyContin)
with acetaminophen (Percocet)
with aspirin (Percodan)
94
Q

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?

A

Meperidine (Demerol)

95
Q

What is Meperidine (Demerol) metabolized to?

A

active normeperidine (neurotoxic)

96
Q

What is significant about the active normeperidine metabolite of Meperidine (demerol)?

A

long metabolite half life that accumulates
euphoria, irritability, delirium, tremors and seizures
toxicity is NOT reversed by opiate antagonists
metabolite is really eliminated

97
Q

What is Meperidine (Demerol) contraindicated?

A

in patients on MAOIs (serotonin syndrome)

98
Q

When can Meperidine (Demerol) be used according to American Pain Society (APS)?

A

in patients with serious opiate allergies

useful in controlling post anesthesia shivering

99
Q

What medication has unique pharmacology-racemic mix of L & D isomers?

A

Methadone (Dolophine)

100
Q

What does the L isomer of Methadone (Dolophine) do?

A

opioid activity

101
Q

What does the D isomer of Methadone (Dolophine) do?

A

NMDA antagonist & NE/Serotonin reuptake inhibitor)

102
Q

What can Methadone (Dolophine) also be useful for?

A

neuropathic pain

103
Q

What medication has the longest & variable half life (12-190 hours; usually 24h)

A

Methadone (Dolophine)

104
Q

What medication is useful entreatment of opiate addiction?

A

Methadone (Dolophine)

dosed every 24h

105
Q

How long does analgesia last with Methadone (Dolophine)?

A

4-8 hours

therefore dose every 6-8 hours for analgesia

106
Q

What medication is 100x more potent than morphine and is therefore dosed in mcg?

A

Fentanyl

107
Q

What medication is extremely lipophilic, rapid onset and short duration of (30-60minutes)?

A

fentanyl

108
Q

Why is Fentanyl a safe option in renal failure?

A

No active metabolites

109
Q

What medication has fewer adverse effects than morphine or dilaudid with minimal histamine release and little hypotensive effect?

A

fentanyl

110
Q

What are the dosage forms of fentanyl?

A

injection
lozenge (Actiq)
Transdermal (Duragesic)

111
Q

What medication is not usually used in opiate naive patients?

A

Duragesic

112
Q

What needs to monitor when giving duragesic?

A

respiratory rate for the first 24 hours

113
Q

How often does Duragesic need to be replaced?

A

every 72 hours
DONT ADD
look for multiple patched when admitting out patients

114
Q

When is fentanyl (Actiq and fentora) used?

A

only for long standing chronic (cancer) pain?

115
Q

What medication is a pure mu receptor ANTAGONIST?

A

naloxone (narcan)

116
Q

What medication if used to reverse sedation and respiratory depression and reverses analgesia?

A

naloxone (narcan)

117
Q

What is the dose of naloxone?

A

dilute 0.4mg to less than 10mL saline (0.9%NaCl)

administer slow IVP (1ml every 1-2 minutes)

118
Q

When should you stop administering naloxone?

A

monitor respiratory rate and stop when it increases

119
Q

What is the first thing to be done with equianalgesic dosing?

A

convert all doses to oral morphine equivalents

120
Q

What should be done for every 12 hour dosing?

A

Divide by 2
round down to SR
provide that dose as MS Contin every 12 hours ATC

121
Q

What should be done for every 8 hour dosing?

A

divide by 3
round down to SR
provide that dose as MC contin every 8 hours around the clock

122
Q

What can be done to provide “breakthrough” pain with equianalgesic dosing?

A

provide 20-25% (divided by 4 or 6) as IR every 4-6 hours PRN

123
Q

What is the oral equiananalgesic dose of morphine 10mg parenteral?

A

30mg PO

124
Q

What is the oral equianalgesic dose of hydromorphone 1.5mg parenteral?

A

7.5mg PO

125
Q

What are the recommendations of the CBC Opioid-Prescribing Guidelines?

A
  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
Q

How can you obtain morphine milligram equivalents (MME)?

A

multiple the total daily opioid dose by the conversion factor to obtain equivalent TTD of morphine in mg

127
Q

What medications are used for medication assisted therapy (MAT)?

A

buprenorphine
naltexone
methadone

128
Q

What MAT is a partial opioid antagonist to help with withdrawal symptoms that can be started with opioids in the pts system?

A

buprenorphine

129
Q

What MAT is a opioid antagonist that may precipitate withdrawal symptoms that cannot be given unless opioid free for 7-14 days before use?

A

naltrexone

130
Q

What is the IM form of naltrexone?

A

Vivitrol

131
Q

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 ?

A

Methadone

Pharmacology (17 decks)

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