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Advanced Pharmacology > Week 1 Management of Pain > Flashcards

Week 1 Management of Pain Flashcards

1
Q

Opioid Considerations for Kidney Disease

What are the effects?

Avoid what meds?
Prefer what meds?

A

Decreased excretion leads to accumulation

Morphine, Codeine
Hydromorphone, Hydrocodone

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2
Q

Ketorolac*

How long can it be given?

A

LIMIT TO 5 DAYS THERAPY*

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3
Q

Afferent pathways =

CNS =

Efferent Pathways =

A

Sends signal to spinal cord

Discriminate & localized pain
Arouse and alert/activation “fight or flight”
Motivational factors

Module pain sensation

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4
Q

Nociceptive Pain*

A

Caused by damage to body tissue

Secondary to noxious stimuli

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5
Q

Opioid u - Agonist Pharmacologic Effects

GI, Biliary

A

Constipation
N/V
Increased biliary sphincter tone and pressure

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6
Q

Methylnaltrexone (Relistor)*

MOA
Elimination
Potential for

A

Acts on mu receptors in GI tract
Renally
GI perf

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7
Q

Fentanyl

Opioid conversion

A

0.1 IV

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8
Q

Tramadol*

MOA

A

Weak mu receptor binding
Inhibition of -> less resp depression and GI dysmotility

Morepinephrine and serotonin reuptake -> decreases seizure threshold

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9
Q

Disadvantages of Non-Opioids

____ effect of analgesia
SE of _____
Acute and chronic ____ ie APAP
Limited _____ availability

A

Ceiling
NSAIDS
Toxicities
Parenteral

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10
Q

Methadone*

Routes

A

PO

IV

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11
Q

Agonist/Antagonist Combo (Abuse deterrent)

Antagonists only act upon?
Examples

A

Manipulation of the product

Suboxone (buprenorphine/naloxone)
Embeda (morphine/naltrexone)

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12
Q

Opioid Dependent

A

Antagonist effect with withdrawal sx

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13
Q

Aspirin*

Onset
Peak 
Duration
Half Life
Emlimination
A 
15-20min
1-3 hr
3-6 hr
3 hr 
Urine and Liver
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14
Q

Opioid u - Agonist Pharmacologic Effects

Cardiovascular

A

Decreased myocardial O2 demand

Vasodilation and Hypotension

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15
Q

Class Wide Opioid Adverse Effects*

Constipation

  • Is very
  • Tx
A

Very common and persistence

Softener (docusate) + Stimulant (Senna, Bisacodyl)

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16
Q

Hydromorphone*

Half life
Excreted
Metabolites

A

Relatively short 2-3 hrs
NON-RENAL
NO METABOLITES

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17
Q

Tramadol*

Dosing

A

25-100mg q4-6 PRN

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18
Q

Salicylate Adverse Events (4)

A

GI irritation and bleeding (ulcers)

Dizziness, deafness, tinnitus (salicylism) with high doses

Reye’s Syndrome (liver disorder and encephalopathy) that occurs in children w viral infections

Asthmatics: increase risk of bronchospasm, urticaria, angioedema

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19
Q

COX Inhibition Chart*

Semiselective

A

Meloxicam, Diclofenac, Etodalac, indomethapiroxicam, piroxicam, nabumetone, sulindac

Increased affinity for COX2 but still retains for COX 1
Increased CV risk

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20
Q

Tramadol*

Routes

A

PO only

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21
Q

Ketorolac (Toradol)*

Is an _____
Routes
Indicated for what type of pain?

A

NSAID
PO, IV (the only parenterally available one)
Short term, moderate to severe*

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22
Q

Aspirin*

Properties

A

Analgesia
Anti-inflammatory
Anti-pyretic
Anti-platelet (prevents synthesis of Thromboxane A (vasoconstrictor and inducer of platelet aggregatio)

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23
Q

Codeine*

Used for what type of pain

A

Mild-moderate acute pain

is a weak agonist so low risk for abues

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24
Q

Methadone has ____ effects so caution w pts w hx of?*

A

Serotinergic

Seizures

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25
Q

Hydromorphone*

Dosing

A

2-4mg Q4-6 PO PRN

0.2-1mg Q2-3 IV PRN

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26
Q

Naltrexone (Vivitrol)*

Routes

A

IV, IM Depot

Hepatotoxic so used PO first!

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27
Q

Class Wide Opioid Adverse Effects*

Respiratory depression

  • Tolerance within __-__ days
  • increased risk for ____ insult
A

5-7

cardiac

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28
Q

Class Wide Opioid Adverse Effects*

Sedation
- Tolerance within?

A

days-weeks

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29
Q

Mepiridine

Opioid conversion

A

100, 300

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30
Q

Methadone*

Dosing

A
  1. 5mg Q8-12 PRN PO

2. 5 - 10mg Q8-12 PRN IV

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31
Q

Opioid Naive

A

Agonist activity with pain relief

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32
Q

Nalaxone (Narcan)*

What type of dosing may be required?

A

Repeated dosing

Bc half life of agonist and low systemic bioavailability dt extensive first pass

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33
Q

Morphine*

Routes

A

PO
PR (IV, IM, SQ)
Epidural, Intrathecal

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34
Q

Methadone*

Black Box Warning*

A

QTC - 500

(risk for fatal arrhythmias do EKG)*

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35
Q

Incomplete cross tolerance is likely due to subtle differences such as?

A

Affinity for opioid receptors
Converting between opioids when pain is controlled (can decrease by 25-50%) of equipotent dose
Moderate to severe pain: consider smaller dose reduction

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36
Q

Transmission: Ascending from

4)
3)
2)
1)

A

4) Brain stem, Midbrain, Cortex
3) Medulla
2) Spinal Cord
1) Peripheral pain receptors

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37
Q

Tramadol*

Metabolism
Excretion

A

CYP2D6

Renally and hepatically cleared - adjutment in dysfunction

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38
Q

Methylnaltrexone (Relistor)*

What is it used for?
What is it NOT used for?

A

OIC

NOT for acute reversal of toxic effects

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39
Q

NSAIDs General

Properties (4)
Interpatient _____
Potency and duration of action differ within group

A

Analgesic, Anti-inflammatory, Anti-pyretic, Anti-platelet (reversible)

Variability: may be used in combo with opioids

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40
Q

Black Boxed Warnings (NSAIDs) (3)*

A

1) Serious adverse cardiovascular thrombotic events (MI, Stroke)
2) GI, ulceration, bleeding, perforation
3) Tx of periop pain for CABG

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41
Q

Morphine

Opioid conversion

A

10, 30

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42
Q

Tx of Opioid Addiction (3)

A

1) Methadone
- used for detox, heavily regulated via clinics, 20-120 daily

2) Buprenorphine/Naloxone
- orally for dependence, prevents diversion if injected the nalaxone acts as antagonist

3) Naltrexone
- orally for opioid or alcohol abuse

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43
Q

How do Opioid Agonist Antagonists work

A

Stimulates one receptor while inhibiting another

(Pentazocine, butorphanol, nalbuphine)
Decreased abuse potential
Kappa agonist, mu partial agonist
Increased AE: anxiety, nightmares, hallucinations

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44
Q

Opioid Considerations for Liver Disease

What are the effects?

So what do you do with dosing?

A

Increased absorption dt decreased First pass metabolism

Decreased drug clearance

Use lower doses or administer less frequently

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45
Q

Patho of Pain (4) Steps

A

Stimulation
Transmission
Perception
Modulation

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46
Q

No tolerance Development (3)*

A

Miosis
Constipation
Seizures

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47
Q

Methodone*

Used for what type of pain?

A

Chronic

Controlled withdrawal (heroin, opioids)

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48
Q

Fentanyl

How and in what settings is it given in?

A

IV

ICU/Traumas - bc short half life -> doesn’t accumulate like morphine for and easily titrated

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49
Q

Ketorolac Adverse Events (2)*

A

Severe bleeding post op
Renal failure monitor: bleeding, liver enzymes, serum Cr

(very effective opiate sparing

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50
Q

COX Inhibition Chart*

Nonselective

A

Ibuprofen, Naproxen

Decreased CV risk
Increased GI risk

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51
Q

Opioid Antagonists

How do they work?
What are they used for? (3)

A

Compete with endogenous and exogenous opioids at mu receptors

Acute toxicity, Chronic dependence, Prevention and reversal of Opioid induced SE

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52
Q

Fentanyl*

Metabolism

A

Metabolized by CYP3A4

Preferred agent in liver failure

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53
Q

Immediate vs Controlled Release considerations

1) Why use controlled release?
2) Passing up controlled release means?
3) Immediate released used for?

A

1) Increases compliance, convenience, minimizes breakthrough pain
2) Real potential for abuse
3) mild-moderate or breakthrough pain

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54
Q

Meperidine*

Metabolites?
Has _____ effects
May still be used for?

A

Yes -> Normeperidine

Causes anxiety, seizure tremors (increased risk w renal dysfunction and prolonged use >48h, high cumulative doses

Serotinergic

Post-op shivering

55
Q

COX 1*

A

Cytoprotective Prostaglandins, Thromboxane

GI, Kidney, Lungs
Platelet Aggregation
Vasoconstriction

56
Q

NSAIDs: Adverse Events*

1) Cardio (3)
2) GI (4)
3) Respiratory (1)
4) Skin (1)
5) Renal (2)

A

1) Fluid retention, hypertension, edema
2) Irritation, ulcers, bleeding, perforation
3) Bronchospasm
4) Rash
5) Insufficiency or Failure (Don’t take with other nephrotoxic drugs diuretics furosemide, HCTZ, ace inhibitors)

57
Q

COX-2 Inhibitor Celecoxib*

Advantages over nonselective COX inhibitors (2)

A

Minimal GI effects*

Improved bleeding profile bc no effect on platelet aggregation

58
Q

Hydromorphone

Opioid conversion

59
Q

Acetaminophen*

Dose

A

Normal Adult

  • 325-650mg Q4 or 1000mg Q6 PRN
  • Max = 4 grams/day*

Liver impairment/Alcoholism
-Max = 2 grams/day*

60
Q

Salicylates Safety

Avoid use in recent ____

Contraindicated (3)

A

recent surgery (bleeding risk)

Active PUD (bleeding)
Hx of GI bleeding
Hypersensitivity to aspirin or NSAIDs (anaphylaxis)

61
Q

Hydrocodone*

Routes

62
Q

Opioid u-Agonist Pharmacologic effects

Immune System

A

Suppresses NK cells

63
Q

Methadone*

Elimination

A

Biphasic Renal Elimination - adjust for CrCL <30

Analgesia HL 8-12
Terminal HL 24-36

64
Q

Morphine*

Elimination
Metabolites (2)

A

Renally*

6 glucuronide (analgesia) 
3 glucoronide (myoclonus, confusion, hallucinations)
65
Q

Fentanyl*

Dosing

A

25-50mcg Q2-3

66
Q

Types of Pain (2)*

A

Nociceptive

Neuropathic/Functional

67
Q

Hydromorphone*

Routes

A

PO
PR (IV, IM, SQ)
Epidural

68
Q

Physical Dependence

A

Drug discontinued or reduced abruptly -> Rhinorrhea, lacrimation, hyperthermia, chills, myalgias, emesis, diarrhea, GI cramping, anxiety, agitation, hostility, sleepnessness

69
Q

Stimulation

Involves stimulation of:
Found within (2) structures:
Activated and sensitized by (3) impulses

Receptor activation leads to action potentials that are transmitted along ____ nerve fibers to the ____ ____

A

Free nerve endings (“Nociceptors”)
Somatic and Visceral structures
Mechanical, thermal, chemical impulses

Afferent, spinal cord

70
Q

Salicylates: Aspirin*

MOA

A

Irreversibly binds to COX1 and COX2 enzymes

71
Q

Codeine*

Metabolism

A

Converted to morphine and its active metabolites

CYP2D6 substrate metabolizer -> so genetic variant

72
Q

Benefits of Non-Opioids

Useful for \_\_-\_\_ pain
Widely \_\_\_\_ (OTC) 
May provide opiate \_\_\_ effect
When combined with opioids can provide \_\_\_\_ analgesia 
Relatively \_\_\_\_\_
Low incidence of \_\_\_\_/abuse
A 
Mild-Moderate 
Available
Sparing
Additive 
Inexpensive 
Addiction
73
Q

Hydrocodone*

Available as (2)

A

1) Immediate release
- APAP combo (Vicodin)
- Ibuprofen combo (Vicoprofen)

2) Extended release
- Zohydro, Hysingla

74
Q

NSAIDs: Safety cont…
Relative contraindication

  • Bleeding, GI events (risk in ____)
  • ____ with high blood loss
  • A____
  • ________ disease hx of (3)
  • Moderate to severe _____ impairment
  • De______
A 
Elderly 
Surgery 
Asthmatics 
Cardiovascular (MI, Stroke, HF) 
Renal 
Dehydration
75
Q

Patho of Pain

Regulated by ____ and _____ neurotransmitters in response to stimuli

Perception of Pain (3) systems

A

Excitatory and Inhibitory

Afferent Pathways
CNS
Efferent Pathways

76
Q

Acetaminophen*

Dosage forms

A

PO

PR (IV $$)

77
Q

Acetaminophen Toxicity*

US Black Box Warning:

Risk increased w (3)

A

May cause severe hepatotoxicity potentially requiring liver transplant or resulting in death from excessive intake >4/d in adults

Liver impairment
Alcohol Use
Intake of more than one source of Tylenol containing meds

78
Q

Opioid u - Agonist Pharmacologic Effects

CNS

A 
Analgesia 
Dysphoria, Euphoria 
Inhibition of cough reflex 
Miosis 
Respiratory Depression
79
Q

Codeine*

Combinations
Is a:

A

APA or ASA combos

Antitussive

80
Q

Oxymorphone

Opioid conversino

81
Q

Abuse Deterrents (3)

A

Physical/Chemical Barriers
Agonist/Antagonist Combos
Aversion

82
Q

Physical Chemical barriers (Abuse deterrent)

Effect on the drug?
Examples

A

Limits drug release upon manipulation of the product (chewing, crushing, cutting, grating, grinding)

Hysingla ER (hydrocodone)
Opana ER (oxymorphone) 
Exalgo (hydromorphone)
Oxycontin (oxycodone)
Oxecta (oxycodone)
83
Q

Morphine*

_____ release*

A

Histamine

Pruritus, Hypotension

84
Q

Hydrocodone

Opioid conversion

85
Q

Naltrexone (Vivitrol)*

What is it used for?
What is it NOT used for?

A

Opioid dependence

Not for acute reversal of toxic effects!

86
Q

Codeine*

Dosing

A

15-60mg Q4 PO PRN

87
Q

Methylnaltrexone (Relistor)*

Route

88
Q

Tramadol*

Drug interactions

A

CYP, Serotonin

89
Q

COX Inhibition Chart*

COX 2 Selective

A

Celecoxib

Increased CV risk
Decreased GI risk

90
Q

Acetaminophen (Tylenol): APAP*

MOA

A

Inhibits the synthesis of Prostaglandins in the CNS*

and works peripherally to block impulse generation

91
Q

Management of Pain

NonOpioids (4)
Opioids (4)
Adjunctive (3)

A

APAP, ASA, NSAIDs, COX-2 Inhibitors

Morphine, Oxycodone, Hydromorphone, Fentanyl

Antidepressants, Anticonvulsants, Antiarrhythmics

92
Q

Converting to and from analgesic patch

A

25mcg fentanyl patch -> 45-135 of PO morphine

Most have adequate response w 45-60mg

93
Q

Pain Severity vs. Therapy*

Mild pain range

Meds

A

1-3

APAP
ASA
NSAIDs
COX-2 Inhibitors

94
Q

Oxycodone

Opioid conversion

95
Q

Opioid u -Agonist Pharmacologic effects

Neuroendocrine

A

Inhibit luteinizing hormone

Stimulate ADH and prolactin

96
Q

Codeine*

Routes

97
Q

Opioid Considerations for the Elderly

1) Start doses lower by?
2) What med is preferred?
3) What meds are not preferred?
4) Potential for significant CNS SE such as?

A

1) 25-50%
2) Oxycodone dt short half life and no toxic metabolites /dilaudid doesn’t have metabolites either but is V potent
3) Those with active metabolites (meperidine, morphine, CNS stimulants)
4) Delirium

98
Q

Neuropathic/Functional*

Pain that is:
Described in terms of:
Result of:
Examples:

A

Disengaged from noxious stimuli
Chronic pain
Nerve damage (neuropathic) or abnormal
Postherpeutic neuralgia, Diabetic neuropathy, Fibromyalgia, IBS, tension headaches

99
Q

Fentanyl*

Potency

AE (2)

A

High potency, lipid soluble, RAPID ONSET

Bradycardia, Chest wall rigidity

100
Q

Classification of Opioid Agonists*

1) Phenanthrenes
2) Phenylpiperidines
3) Phenylheptanes

Helps with selection in cases of?

A

1) Levorphonal, Oxycodone, Codeine, Oxymorphone, Hydromorphone, Morphine, Hydrocodone
2) Fentanyl, Alfentanyl, Remifentanyl, Sufafentinal, Meperidine
3) Methadone

TRUE ALLERGIES

101
Q

Nalaxone (Narcan)*

What is it used for?

A

To reverse toxic effects of opioids (agonists and agonist/antagonists)

A COMPLETE REVERSAL AGENT (classic mu receptor antagonist)

May be used PO to prevent OIC

102
Q

Buprenorphine

Whats type of pain is it used for?

A

Partial Agonist

Chronic pain for those at high risk for abuse
- decreased abuse potential compared to morphine

103
Q

Chronic Pain Regimens*

Considerations for Long acting opioids*

A

Typically reserved for opioid tolerant patients
Ease of dosing
Long lasting analgesia

104
Q

Modulation

Initiation of ___ nociceptive system
Endogenous opiate system in CNS involves release of (3)
Descending system for control of pain transmission that can inhibit synaptic pain transmission at dorsal horn (endogenous _____, (3))

A

Anti
Enkaphalins, Dynorphins, B endorphins
Opioids, serotonin, norepinephrine, GABA

105
Q

Opioid u - Agonist Pharmacologic effects

Dermal

A

Flushing
Pruritis
Urticaria/Rash

106
Q

Class Wide Opioid Adverse Effects*

List some

A 
Fatigue
HA, Confusion, Delirium, Hallucinations, Nightmares, Mood changes, Increased ICP 
Bradycardia
GI effects, N/V
Urinary retention 
Sexual dysfunction 
ITCHING*
107
Q

Meperidine*

Routes

A

PO

PR (IV, IM, SQ)

108
Q

Opioid Diversion

A

The transfer of a controlled substance from a lawful to unlawful channel of distribution of use

Crushing, snorting, smoking, injecting, sharing

109
Q

Opioid Tolerance

A

Dose increase required to maintain similar analgesia

dt neuroadaption by body with chronic use/occurs as early as days of therapy

110
Q

Neuropathic Pain

Disengaged from (2)
____ excitability, enhanced sensory _____
Loss of ____ pain inhibition
____ of pain circuits (anatomically and biochemically)
Production of spontaneous nerve stimulation, autonomic neuronal pain stimulation, progressive increase in _____ of dorsal horn neurons

A

Noxious stimuli, Healing

Ectopic, transmission

Modulatory

Rewiring

Discharge

111
Q

Hydrocodone*

Metabolism

A

Converts to Hydromorphone via CYP2D6

112
Q

Incomplete cross tolerance

A

Pharmacologic tolerance develops to the opioid being used but may not exist w initial conversion to another opioid

113
Q

Pain Severity vs. Therapy*

Severe pain range

Meds

A

8-10

Opioids

114
Q

Aversion (Abuse deterrent)

What is it?
Examples

A

A substance added to a product to produce unpleasant effect if manipulated

Oxecta (oxycodone)

115
Q

IT IS A FARCE THAT NSAIDS are SAFE FOR ALL PATIENTS

A lot of _______

NSAIDs in a lot of ways drive ppl to _____

A

Cardiotoxicity

Dialysis

116
Q

Transmission

Afferent fibers synapse into various layers at the spinal cord’s ____ ____
Results in release of neurotransmitters (3)
Pain impulses are transmitted to the (2) via diff ascending pathways
From the ____ they are further passed to other CNS structures for processing

A

Dorsal Horn
Glutamate, Substance P, Calcitonin gene-related peptides
Brain stem, Thalamus
Thalamus

117
Q

Perception

A

The point at which pain becomes a conscious experience

118
Q

COX 2*

A

Inflammatory Prostaglandins, Prostacyclins

Inflammatory, Pain
Antiplatelet
Vasodilation

119
Q

Meperidine*

Metabolism

120
Q

COX-2 Inhibitor Celecoxib*

Disadvantages (3)

A 
Renal Dysfunction 
Avoid in pts with "sulfa-allergy" 
CARDIOVASCULAR EVENTS (eg rofecoxib Vioxx)
121
Q

COX Inhibition Chart*

Nonselective Irreversible

A

Aspirin

Decreased CV Risk
Increased GI Risk

122
Q

Salicylates

A

Aspirin*

Choline magnesium trisalicylate
Choline salicylate 
Diflunisal
Salsalate 
Sodium Salicylate
123
Q

Pain Severity vs. Therapy*

Moderate pain range

Meds

A

4-7

NSAIDS
Opiate + APAP
Tramadol

124
Q

Codeine

Opioid conversion

125
Q

Hydrocodone*

Used for what type of pain?

A

Moderate to severe pain in pts w limited opioid use

126
Q

Buprenorphine

Opioid conversion

A

0.3, 0.4 (sl)

127
Q

What drugs is not effected by liver disease?

What drug may be reduced?

A

Fentanyl

Codeine dt decreased conversion

128
Q

Morphine*

Dosing

A

15-30mg Q4 PO PRN

2-4mg Q4 IV PRN

129
Q

Aspirin

Diff than other NSAIDs that are ____
Used more for ____ effects

Once its inhibited its ____ which is why you can’t take it:

A

Reversible
Cardiovascular effects “suicide inhibitor”

Forever, 7 days before surgery (takes 7 days to make new platelets

130
Q

COX-2 Inhibitor (1)*

A

Celecoxib (Celebrex)

131
Q

Hydrocodone*

Dosing

A

5-10mg PO Q4-6 PRN

132
Q

Chronic Pain Regimens*

Consideration for Short acting opioid for breakthrough pain*

How do you calculate breakthrough pain meds?

When should you increase the long-acting dose?

A

Calculated by taking 10-15% of total dose and offer for every 2-4 hrs as needed

> /- 3 doses of breakthrough per day

133
Q

Opioid u - Agonist Pharmacologic effects

Genitourinary

A

Urinary retention
Prolongation of Labor
Increase bladder sphincter tone

134
Q

Fentanyl*

Routes

A 
IV
Transdermal 
Lozenge
Intranasal
Buccal 
Sublingual
Epidural

Advanced Pharmacology (14 decks)

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