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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
Hydromorphone* Dosing
2-4mg Q4-6 PO PRN | 0.2-1mg Q2-3 IV PRN
26
Naltrexone (Vivitrol)* Routes
IV, IM Depot Hepatotoxic so used PO first!
27
Class Wide Opioid Adverse Effects* Respiratory depression - Tolerance within __-__ days - increased risk for ____ insult
5-7 | cardiac
28
Class Wide Opioid Adverse Effects* Sedation - Tolerance within?
days-weeks
29
Mepiridine Opioid conversion
100, 300
30
Methadone* Dosing
2. 5mg Q8-12 PRN PO | 2. 5 - 10mg Q8-12 PRN IV
31
Opioid Naive
Agonist activity with pain relief
32
Nalaxone (Narcan)* What type of dosing may be required?
Repeated dosing Bc half life of agonist and low systemic bioavailability dt extensive first pass
33
Morphine* Routes
PO PR (IV, IM, SQ) Epidural, Intrathecal
34
Methadone* Black Box Warning*
QTC - 500 (risk for fatal arrhythmias do EKG)*
35
Incomplete cross tolerance is likely due to subtle differences such as?
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
36
Transmission: Ascending from 4) 3) 2) 1)
4) Brain stem, Midbrain, Cortex 3) Medulla 2) Spinal Cord 1) Peripheral pain receptors
37
Tramadol* Metabolism Excretion
CYP2D6 Renally and hepatically cleared - adjutment in dysfunction
38
Methylnaltrexone (Relistor)* What is it used for? What is it NOT used for?
OIC NOT for acute reversal of toxic effects
39
NSAIDs General Properties (4) Interpatient _____ Potency and duration of action differ within group
Analgesic, Anti-inflammatory, Anti-pyretic, Anti-platelet (reversible) Variability: may be used in combo with opioids
40
Black Boxed Warnings (NSAIDs) (3)*
1) Serious adverse cardiovascular thrombotic events (MI, Stroke) 2) GI, ulceration, bleeding, perforation 3) Tx of periop pain for CABG
41
Morphine Opioid conversion
10, 30
42
Tx of Opioid Addiction (3)
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
43
How do Opioid Agonist Antagonists work
Stimulates one receptor while inhibiting another (Pentazocine, butorphanol, nalbuphine) Decreased abuse potential Kappa agonist, mu partial agonist Increased AE: anxiety, nightmares, hallucinations
44
Opioid Considerations for Liver Disease What are the effects? So what do you do with dosing?
Increased absorption dt decreased First pass metabolism Decreased drug clearance Use lower doses or administer less frequently
45
Patho of Pain (4) Steps
Stimulation Transmission Perception Modulation
46
No tolerance Development (3)*
Miosis Constipation Seizures
47
Methodone* Used for what type of pain?
Chronic Controlled withdrawal (heroin, opioids)
48
Fentanyl How and in what settings is it given in?
IV ICU/Traumas - bc short half life -> doesn't accumulate like morphine for and easily titrated
49
Ketorolac Adverse Events (2)*
Severe bleeding post op Renal failure monitor: bleeding, liver enzymes, serum Cr (very effective opiate sparing
50
COX Inhibition Chart* Nonselective
Ibuprofen, Naproxen Decreased CV risk Increased GI risk
51
Opioid Antagonists How do they work? What are they used for? (3)
Compete with endogenous and exogenous opioids at mu receptors Acute toxicity, Chronic dependence, Prevention and reversal of Opioid induced SE
52
Fentanyl* Metabolism
Metabolized by CYP3A4 | Preferred agent in liver failure
53
Immediate vs Controlled Release considerations 1) Why use controlled release? 2) Passing up controlled release means? 3) Immediate released used for?
1) Increases compliance, convenience, minimizes breakthrough pain 2) Real potential for abuse 3) mild-moderate or breakthrough pain
54
Meperidine* Metabolites? Has _____ effects May still be used for?
Yes -> Normeperidine Causes anxiety, seizure tremors (increased risk w renal dysfunction and prolonged use >48h, high cumulative doses Serotinergic Post-op shivering
55
COX 1*
Cytoprotective Prostaglandins, Thromboxane GI, Kidney, Lungs Platelet Aggregation Vasoconstriction
56
NSAIDs: Adverse Events* 1) Cardio (3) 2) GI (4) 3) Respiratory (1) 4) Skin (1) 5) Renal (2)
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
COX-2 Inhibitor Celecoxib* Advantages over nonselective COX inhibitors (2)
Minimal GI effects* Improved bleeding profile bc no effect on platelet aggregation
58
Hydromorphone Opioid conversion
1.5, 7.5
59
Acetaminophen* Dose
Normal Adult - 325-650mg Q4 or 1000mg Q6 PRN - Max = 4 grams/day* Liver impairment/Alcoholism -Max = 2 grams/day*
60
Salicylates Safety Avoid use in recent ____ Contraindicated (3)
recent surgery (bleeding risk) Active PUD (bleeding) Hx of GI bleeding Hypersensitivity to aspirin or NSAIDs (anaphylaxis)
61
Hydrocodone* Routes
PO only
62
Opioid u-Agonist Pharmacologic effects Immune System
Suppresses NK cells
63
Methadone* Elimination
Biphasic Renal Elimination - adjust for CrCL <30 Analgesia HL 8-12 Terminal HL 24-36
64
Morphine* Elimination Metabolites (2)
Renally* ``` 6 glucuronide (analgesia) 3 glucoronide (myoclonus, confusion, hallucinations) ```
65
Fentanyl* Dosing
25-50mcg Q2-3
66
Types of Pain (2)*
Nociceptive Neuropathic/Functional
67
Hydromorphone* Routes
PO PR (IV, IM, SQ) Epidural
68
Physical Dependence
Drug discontinued or reduced abruptly -> Rhinorrhea, lacrimation, hyperthermia, chills, myalgias, emesis, diarrhea, GI cramping, anxiety, agitation, hostility, sleepnessness
69
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 ____ ____
Free nerve endings ("Nociceptors") Somatic and Visceral structures Mechanical, thermal, chemical impulses Afferent, spinal cord
70
Salicylates: Aspirin* MOA
Irreversibly binds to COX1 and COX2 enzymes
71
Codeine* Metabolism
Converted to morphine and its active metabolites CYP2D6 substrate metabolizer -> so genetic variant
72
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 ```
``` Mild-Moderate Available Sparing Additive Inexpensive Addiction ```
73
Hydrocodone* Available as (2)
1) Immediate release - APAP combo (Vicodin) - Ibuprofen combo (Vicoprofen) 2) Extended release - Zohydro, Hysingla
74
NSAIDs: Safety cont... Relative contraindication - Bleeding, GI events (risk in ____) - ____ with high blood loss - A____ - ________ disease hx of (3) - Moderate to severe _____ impairment - De______
``` Elderly Surgery Asthmatics Cardiovascular (MI, Stroke, HF) Renal Dehydration ```
75
Patho of Pain Regulated by ____ and _____ neurotransmitters in response to stimuli Perception of Pain (3) systems
Excitatory and Inhibitory Afferent Pathways CNS Efferent Pathways
76
Acetaminophen* Dosage forms
PO | PR (IV $$)
77
Acetaminophen Toxicity* US Black Box Warning: Risk increased w (3)
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
Opioid u - Agonist Pharmacologic Effects CNS
``` Analgesia Dysphoria, Euphoria Inhibition of cough reflex Miosis Respiratory Depression ```
79
Codeine* Combinations Is a:
APA or ASA combos Antitussive
80
Oxymorphone Opioid conversino
1, 10
81
Abuse Deterrents (3)
Physical/Chemical Barriers Agonist/Antagonist Combos Aversion
82
Physical Chemical barriers (Abuse deterrent) Effect on the drug? Examples
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
Morphine* _____ release*
Histamine Pruritus, Hypotension
84
Hydrocodone Opioid conversion
30 PO
85
Naltrexone (Vivitrol)* What is it used for? What is it NOT used for?
Opioid dependence Not for acute reversal of toxic effects!
86
Codeine* Dosing
15-60mg Q4 PO PRN
87
Methylnaltrexone (Relistor)* Route
SQ only
88
Tramadol* Drug interactions
CYP, Serotonin
89
COX Inhibition Chart* COX 2 Selective
Celecoxib Increased CV risk Decreased GI risk
90
Acetaminophen (Tylenol): APAP* MOA
Inhibits the synthesis of Prostaglandins in the CNS* | and works peripherally to block impulse generation
91
Management of Pain NonOpioids (4) Opioids (4) Adjunctive (3)
APAP, ASA, NSAIDs, COX-2 Inhibitors Morphine, Oxycodone, Hydromorphone, Fentanyl Antidepressants, Anticonvulsants, Antiarrhythmics
92
Converting to and from analgesic patch
25mcg fentanyl patch -> 45-135 of PO morphine Most have adequate response w 45-60mg
93
Pain Severity vs. Therapy* Mild pain range Meds
1-3 APAP ASA NSAIDs COX-2 Inhibitors
94
Oxycodone Opioid conversion
20 PO
95
Opioid u -Agonist Pharmacologic effects Neuroendocrine
Inhibit luteinizing hormone | Stimulate ADH and prolactin
96
Codeine* Routes
PO only
97
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?
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
Neuropathic/Functional* Pain that is: Described in terms of: Result of: Examples:
Disengaged from noxious stimuli Chronic pain Nerve damage (neuropathic) or abnormal Postherpeutic neuralgia, Diabetic neuropathy, Fibromyalgia, IBS, tension headaches
99
Fentanyl* **Potency** AE (2)
High potency, lipid soluble, RAPID ONSET Bradycardia, Chest wall rigidity
100
Classification of Opioid Agonists* 1) Phenanthrenes 2) Phenylpiperidines 3) Phenylheptanes Helps with selection in cases of?
1) Levorphonal, Oxycodone, Codeine, Oxymorphone, Hydromorphone, Morphine, Hydrocodone 2) Fentanyl, Alfentanyl, Remifentanyl, Sufafentinal, Meperidine 3) Methadone TRUE ALLERGIES
101
Nalaxone (Narcan)* What is it used for?
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
Buprenorphine Whats type of pain is it used for?
Partial Agonist Chronic pain for those at high risk for abuse - decreased abuse potential compared to morphine
103
Chronic Pain Regimens* Considerations for Long acting opioids*
Typically reserved for opioid tolerant patients Ease of dosing Long lasting analgesia
104
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))
Anti Enkaphalins, Dynorphins, B endorphins Opioids, serotonin, norepinephrine, GABA
105
Opioid u - Agonist Pharmacologic effects Dermal
Flushing Pruritis Urticaria/Rash
106
Class Wide Opioid Adverse Effects* List some
``` Fatigue HA, Confusion, Delirium, Hallucinations, Nightmares, Mood changes, Increased ICP Bradycardia GI effects, N/V Urinary retention Sexual dysfunction ITCHING* ```
107
Meperidine* Routes
PO | PR (IV, IM, SQ)
108
Opioid Diversion
The transfer of a controlled substance from a lawful to unlawful channel of distribution of use Crushing, snorting, smoking, injecting, sharing
109
Opioid Tolerance
Dose increase required to maintain similar analgesia dt neuroadaption by body with chronic use/occurs as early as days of therapy
110
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
Noxious stimuli, Healing Ectopic, transmission Modulatory Rewiring Discharge
111
Hydrocodone* Metabolism
Converts to Hydromorphone via CYP2D6
112
Incomplete cross tolerance
Pharmacologic tolerance develops to the opioid being used but may not exist w initial conversion to another opioid
113
Pain Severity vs. Therapy* Severe pain range Meds
8-10 Opioids
114
Aversion (Abuse deterrent) What is it? Examples
A substance added to a product to produce unpleasant effect if manipulated Oxecta (oxycodone)
115
IT IS A FARCE THAT NSAIDS are SAFE FOR ALL PATIENTS A lot of _______ NSAIDs in a lot of ways drive ppl to _____
Cardiotoxicity Dialysis
116
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
Dorsal Horn Glutamate, Substance P, Calcitonin gene-related peptides Brain stem, Thalamus Thalamus
117
Perception
The point at which pain becomes a conscious experience
118
COX 2*
Inflammatory Prostaglandins, Prostacyclins Inflammatory, Pain Antiplatelet Vasodilation
119
Meperidine* Metabolism
Renal
120
COX-2 Inhibitor Celecoxib* Disadvantages (3)
``` Renal Dysfunction Avoid in pts with "sulfa-allergy" CARDIOVASCULAR EVENTS (eg rofecoxib Vioxx) ```
121
COX Inhibition Chart* Nonselective Irreversible
Aspirin Decreased CV Risk Increased GI Risk
122
Salicylates
Aspirin* ``` Choline magnesium trisalicylate Choline salicylate Diflunisal Salsalate Sodium Salicylate ```
123
Pain Severity vs. Therapy* Moderate pain range Meds
4-7 NSAIDS Opiate + APAP Tramadol
124
Codeine Opioid conversion
100, 200
125
Hydrocodone* Used for what type of pain?
Moderate to severe pain in pts w limited opioid use
126
Buprenorphine Opioid conversion
0.3, 0.4 (sl)
127
What drugs is not effected by liver disease? What drug may be reduced?
Fentanyl Codeine dt decreased conversion
128
Morphine* Dosing
15-30mg Q4 PO PRN | 2-4mg Q4 IV PRN
129
Aspirin Diff than other NSAIDs that are ____ Used more for ____ effects Once its inhibited its ____ which is why you can't take it:
Reversible Cardiovascular effects "suicide inhibitor" Forever, 7 days before surgery (takes 7 days to make new platelets
130
COX-2 Inhibitor (1)*
Celecoxib (Celebrex)
131
Hydrocodone* Dosing
5-10mg PO Q4-6 PRN
132
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?
Calculated by taking 10-15% of total dose and offer for every 2-4 hrs as needed >/- 3 doses of breakthrough per day
133
Opioid u - Agonist Pharmacologic effects Genitourinary
Urinary retention Prolongation of Labor Increase bladder sphincter tone
134
Fentanyl* Routes
``` IV Transdermal Lozenge Intranasal Buccal Sublingual Epidural ```

Advanced Pharmacology (14 decks)

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