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Pain (R) Flashcards

1
Q

cyclooxygenase enzymes

A

cox-1 and cox-2

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2
Q

COX-1: MOA & s/e

A

catalyzes synthesis of PGs used in normal body functions (eg. gastric cytoprotection)

“housekeeping” enzymes

blocking causes unwanted GI s/e

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3
Q

COX-2: example

A

acutely expressed as a part of the inflammatory response to cell damage

celecoxib(Celebrax)

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4
Q

NSAIDs are used for & MOA

A

-pain
-fever
-inflammation
-cardio-protection (ASA only)

block the synthesis of inflammatory prostaglandins by inhibiting cox enzyme from eliciting their actions

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5
Q

ASA: MOA

A

irreversible inhibitor (permanent) of COX-1 & COX-2

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6
Q

indomethacin

A

reversible inhibitor w/ greater affinity for COX-1

high risk for upper GI bleed/perf

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7
Q

coxibs: MOA & rx’ed for?

A

aka cox-2 inbibitors

selectively blocks COX-2 enzyme
spare the inhibition of COX-1

-pain
-fever
-inflammation

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8
Q

3 clinical efficacies of NSAIDs

A

-equal(analgesia & anti-inflammatory effects)

-therapeutic efficacy is based on pt’s response (associated with w/dose-dependent renal toxicity)

display “ceiling” effect

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9
Q

ceiling effect

A

higher doses do not provide any additional pain relief
-may inc the likelihood of s/e

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10
Q

non-selective NSAIDs

A

associated w/ GI toxicity if a pre-existing ulcer or dyspepsia, H. pylori infection & older age

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11
Q

managing GI s/e

A

-take w/ food or milk
-switch to diff NSAID w/ better safety profile
-COX-2 selective agent (celecoxin)
-gastroprotection (H2RA, PPI, misoprostol)

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12
Q

pts w/ increased risk of GI bleeding/ulcer that req a NSAID…rx

A

celecoxib (Celebrex)

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13
Q

if pt has a high risk of GI complications (hx of NSAID-related GI bleeding) additional drug class s/b Rx

A

PPI

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14
Q

risk of upper GI bleed: low

A
  • ibuprofen (lower than ALL tNSAIDs)
  • celecoxib (Celebrex)
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15
Q

risk of upper GI bleed: medium

A

-diclofenac
-etodolac
-meloxicam
-ketoptofen
-nabumetone
-naproxen

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16
Q

risk of upper GI bleed: high

A

-indomethacin, sulindac
-ketorolac (Toradol)
-piroxicam

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17
Q

preventative/therapeutic measures for: dyspepsia, abd pain, GI discomfort

A

combine NSAID w/ PPI or H2 blockers

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18
Q

preventative/therapeutic measures for: GI bleeding

A

-avoid NSAIDs w/ h/o NSAID-associated UGI bleeding

-add PPI/misoprostol

-celecoxib +/- PPI/misoprostol

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19
Q

NSAID black box warning (GI)

A

-inc risk: GI a/e including bleeding, ulceration, and perforation of the stomach or intestines, which can be fatal

-can occur at any time during use & w/o warning sxs

elderly at greater risk

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20
Q

preventative/therapeutic measures for: impaired renal fn

avoid?
BP meds?

A

-avoid NSAIDs
-use NSAIDs w/ caution when combined w/ meds that potential decease renal function (ACE inhibitors, beta-blockers)

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21
Q

preventative/therapeutic measures for: respiratory (aspirin-exacerbated resp disease)

A

use NSAIDs & ASA w/ caution in pts w/ asthma, esp w/ nasal polyps or recurrent sinusitis

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22
Q

NSAIDs & COXibs are associated w/

A

increased CV risk & bleeding risk

-fluid retention, HTN, edema
-rarely MI, stroke, CHR

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23
Q

cardiovascular: low risk from NSAIDs & COX

A

ibuprofen
naproxen

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24
Q

cardiovascular: high risk from NSAIDs & COX (name med)

A

diclofenac

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25
preventative/therapeutic measures for: cardiovascular complications (worsening HTN, MI) think: type of NSAID which conditions
-avoid COX-2 inhibitors/non-selective NSAIDs in pts at risk of CV events -avoid NSAIDs in pts w/ CHF -use NSAIDs w/ caution in pts w/ HTN [mean BP increase is 5mmHg]
26
preventative/therapeutic measures for: hepatic complications
avoid NSAIDs in pts w/ cirrhosis due to potential hematologic and renal complications
27
black box warning: cardiovascular for NSAIDs
inc risk of: CV thrombotic events myocardial infarction stroke (can be fatal)
28
preventative/therapeutic measures for: clotting problems contributing to significant bleeding
-avoid NSAIDs in pts w/ platelet defects or thrombocytopenia -avoid combining NSAIDs w/ anticoagulants [**risk of GI bleed increases 3-6x**] -if NSAIDs are nec in pts w/ an anticoagulant, expect an increase in INR [**INR inc up to 15%**] -avoid daily low-dose ASA if CV risk is low (<3% annual risk)
29
preventative/therapeutic measures for: prolonged pregnancy or labor
avoid NSAIDs toward the end of pregnancy (6-8wk before term)
30
STEPS
simplicity tolerability evidence price safety
31
if a pt fails therapy w/ an agent from one class of NSAIDs then
use of an agent from another class is reasonable
32
cox-2 selective agents have ideal indication for
-high risk GI bleed -high intolerance of non-selective NSAIDs -tx failure w/ non-selective agents
33
NSAIDs efficacy for neuropathic pain
minimal value
34
acetaminophen
-blocks PG synthesis in CNS -inhibits *peripheral pain* impulses does not interfere w/ COX-1 or COX-2 (no anti-inflammatory benefit) ***initial therapy for mild-moderate pain***
35
McNeil Consumer Healthcare reduced acetaminophen dose to
max 3,000mg daily and increased the dosing interval to q6
36
American Geriatric Society (AGS) Panel on Pharmacological Management of Persistent Pain in ***Older Persons*** recommend - how much acetaminophen?
less than 2g : -frail patients -80+ yo -consume alcohol
37
what's the dose for APAP when used for longer term duration (>7d) ?
3g/day w/ normal liver fn
38
what increases the risk of hepatotoxicity?
-heavy alcohol use -malnutrition -fasting -low body wt -advanced age -febrile illness -select liver disease -use of drugs w/ APAP ***dose: 2g/day or avoidance***
39
adjuvant analgesics
medications possessing analgesic properties but developed for purposes other than pain relief -anticonvulsants -antidepressants -lidocaine patches -corticosteroids -muscle relaxants
40
gabapentin or lidocaine patch
for post-herpetic neuralgia
41
1st line of therapy for diabetic peripheral neuropathy (DPN)
-amitriptyline ***avoid in elderly*** -duloxetine (SNRI; coexisting depression) -pregabalin (severe pain/insomnia)
42
TCAs
for **trigeminal neuralgia** (a condition that causes painful sensations similar to an electric shock on one side of the face)
43
opioids
most drugs are selective for mu receptor type mu-1: produces effects of analgesia mu-2: linked to sedation, reduced BP, itching, N, euphoria, dec resp, miosis (constricted pupils), dec bowel motility aka constipation
44
opioids are safe for
-acute, severe pain -mod-severe cancer pain -mod-severe chronic non-malignant & severe neuropathic [3rd/4th line) -mod-severe headaches [last resort: contraindication w/ triptans]
45
do opioids have a ceiling effect?
No
46
opioid treatment: intermittent pain
begin w/ short-acting morphine, oxycodone, hydrocodone -try one at a time -q4-6hr
47
opioid treatment: continuous pain
long-acting agents: -CR (controlled release) morphine -methadone -use short-acting agents to determine starting point -short-acting agents may be necessary for BTP
48
when does tolerance to most side effects occurs?
within first wk
49
recommendations for ongoing s/e sedation
-reduce dose by 25% & inc interval CNS stimulants: -**caffeine** 100-200mg POq6h -**methylphenidate** 5-10mg PO 1-3x/day -**dextroamphetamine** 5-10mg PO 1-3x/day -**modafinil**100-200mg PO daily
50
highest risk for respiratory depression
opioid naive risk is minimized in chronic users bc pts rapidly develop tolerance to this effect
51
for mild respiratory depression
decrease dose by 25%
52
for severe respiratory depression
naltrexone
53
antiemetic / prevention
hydroxyzine diphenhydramine ondansetrol
54
dose for hydroxyzine (1st generation histamine H1 antagonist)
25-100mg PO/IM q4-6 PRN
55
dose for diphenhydramine (Benadryl) antihistamine
25-50mg PO/IM q6 PRN
56
dose for ondansetron
4-8mg PO TID
57
antiemetic / treatment
prochlorperazine haloperidol metoclopramide granisetron ondansetron palonosetron if PRN unsuccessful may administer around-the-clock
58
CNS irritability: define & tx
usually abates soon after initiation of therapy -if confusion or delirium persists for more than 2wks: dicn't/alternate opioid dose reduction treat w/ BZD haloperidol
59
pruritis
more common w/ **parenteral** than oral opioids -do not confuse w/ true allergy tx: diphenhydramine (Benadryl) promethazine
60
constipation
-tolerance does not develop to this s/e -goal: 1 non-forced BM q1-2d
61
stimulant laxative
promote motility/peristalsis -senna -bisacodyl (Dulcolax) 17.2mg/day
62
stool softener
counteract drying & hardening effects of increased transit time docusate 100mg/day
63
peripheral opioids antagonists
does not affect analgesic response or promote withdrawal because it does not cross the BBB
64
allergenicity
true allergy to codeine (or related compound), the risk of cross-reactivity w/ another opioid can be reduced if an analgesic from a different chemical class is used
65
for severe, life-threatening reactions consider using
non-narcotic analgesics, such as NSAID agents or acetaminophen
66
cross allegenicity
pick drugs from another class
67
3 classes of opioids
-phenanthrenes -phenylpiperidines -phenylheptanones
68
phenanthrenes
morphine hydromorphone oxymorphone levorphanol codeine hydrocodone oxycodone
69
phenylpiperidine
meperidine fentanyl sufentanil alfentanil
70
phenylheptanones
(diphenylheptanes) methadone levomethadyl
71
FDA definition of opioid tolerance
for at least 1 wk s/he has been receiving oral -morphine 60mg/d -transdermal fentanyl 25mcg/hr -oxycodone 30mg/d -hydromorphone 8mg/d -oxymorphone 25mg/d
72
aberrant drug-related behavior
a behavior outside outside the boundaries of the agreed on treatment plan, est as early as possible in the doc-pt relationship
73
2 opioid antagonists
naloxone naltrexone
74
naloxone
(Narcan) tx of opioid agonist-induced respiratory depression and known/suspected overdose of opioid reverses both toxic and clinical effects of opioids
75
naltrexone
the adjuvant tx of alcoholism and nicotine dependence -used off-label for opiate agonist dependence and withdrawal -wt loss

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