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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
Q

preventative/therapeutic measures for: cardiovascular complications (worsening HTN, MI)

think:
type of NSAID
which conditions

A

-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]

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26
Q

preventative/therapeutic measures for: hepatic complications

A

avoid NSAIDs in pts w/ cirrhosis due to potential hematologic and renal complications

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27
Q

black box warning: cardiovascular for NSAIDs

A

inc risk of:

CV thrombotic events
myocardial infarction
stroke

(can be fatal)

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28
Q

preventative/therapeutic measures for: clotting problems contributing to significant bleeding

A

-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)

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29
Q

preventative/therapeutic measures for: prolonged pregnancy or labor

A

avoid NSAIDs toward the end of pregnancy (6-8wk before term)

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30
Q

STEPS

A

simplicity
tolerability
evidence
price
safety

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31
Q

if a pt fails therapy w/ an agent from one class of NSAIDs then

A

use of an agent from another class is reasonable

32
Q

cox-2 selective agents have ideal indication for

A

-high risk GI bleed
-high intolerance of non-selective NSAIDs
-tx failure w/ non-selective agents

33
Q

NSAIDs efficacy for neuropathic pain

A

minimal value

34
Q

acetaminophen

A

-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
Q

McNeil Consumer Healthcare reduced acetaminophen dose to

A

max 3,000mg daily and increased the dosing interval to q6

36
Q

American Geriatric Society (AGS) Panel on Pharmacological Management of Persistent Pain in Older Persons recommend - how much acetaminophen?

A

less than 2g :

-frail patients
-80+ yo
-consume alcohol

37
Q

what’s the dose for APAP when used for longer term duration (>7d) ?

A

3g/day w/ normal liver fn

38
Q

what increases the risk of hepatotoxicity?

A

-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
Q

adjuvant analgesics

A

medications possessing analgesic properties but developed for purposes other than pain relief

-anticonvulsants
-antidepressants
-lidocaine patches
-corticosteroids
-muscle relaxants

40
Q

gabapentin or lidocaine patch

A

for post-herpetic neuralgia

41
Q

1st line of therapy for diabetic peripheral neuropathy (DPN)

A

-amitriptyline avoid in elderly

-duloxetine (SNRI; coexisting depression)

-pregabalin (severe pain/insomnia)

42
Q

TCAs

A

for trigeminal neuralgia

(a condition that causes painful sensations similar to an electric shock on one side of the face)

43
Q

opioids

A

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
Q

opioids are safe for

A

-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
Q

do opioids have a ceiling effect?

A

No

46
Q

opioid treatment: intermittent pain

A

begin w/ short-acting

morphine, oxycodone, hydrocodone
-try one at a time
-q4-6hr

47
Q

opioid treatment: continuous pain

A

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
Q

when does tolerance to most side effects occurs?

A

within first wk

49
Q

recommendations for ongoing s/e sedation

A

-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
-modafinil100-200mg PO daily

50
Q

highest risk for respiratory depression

A

opioid naive

risk is minimized in chronic users bc pts rapidly develop tolerance to this effect

51
Q

for mild respiratory depression

A

decrease dose by 25%

52
Q

for severe respiratory depression

A

naltrexone

53
Q

antiemetic / prevention

A

hydroxyzine
diphenhydramine
ondansetrol

54
Q

dose for hydroxyzine (1st generation histamine H1 antagonist)

A

25-100mg PO/IM q4-6 PRN

55
Q

dose for diphenhydramine (Benadryl) antihistamine

A

25-50mg PO/IM q6 PRN

56
Q

dose for ondansetron

A

4-8mg PO TID

57
Q

antiemetic / treatment

A

prochlorperazine
haloperidol
metoclopramide
granisetron
ondansetron
palonosetron

if PRN unsuccessful may administer around-the-clock

58
Q

CNS irritability: define & tx

A

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
Q

pruritis

A

more common w/ parenteral than oral opioids
-do not confuse w/ true allergy

tx:
diphenhydramine (Benadryl)
promethazine

60
Q

constipation

A

-tolerance does not develop to this s/e

-goal: 1 non-forced BM q1-2d

61
Q

stimulant laxative

A

promote motility/peristalsis

-senna
-bisacodyl (Dulcolax) 17.2mg/day

62
Q

stool softener

A

counteract drying & hardening effects of increased transit time

docusate 100mg/day

63
Q

peripheral opioids antagonists

A

does not affect analgesic response or promote withdrawal because it does not cross the BBB

64
Q

allergenicity

A

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
Q

for severe, life-threatening reactions consider using

A

non-narcotic analgesics, such as NSAID agents or acetaminophen

66
Q

cross allegenicity

A

pick drugs from another class

67
Q

3 classes of opioids

A

-phenanthrenes

-phenylpiperidines

-phenylheptanones

68
Q

phenanthrenes

A

morphine
hydromorphone
oxymorphone
levorphanol
codeine
hydrocodone
oxycodone

69
Q

phenylpiperidine

A

meperidine
fentanyl
sufentanil
alfentanil

70
Q

phenylheptanones

A

(diphenylheptanes)

methadone
levomethadyl

71
Q

FDA definition of opioid tolerance

A

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
Q

aberrant drug-related behavior

A

a behavior outside outside the boundaries of the agreed on treatment plan, est as early as possible in the doc-pt relationship

73
Q

2 opioid antagonists

A

naloxone
naltrexone

74
Q

naloxone

A

(Narcan)

tx of opioid agonist-induced respiratory depression and known/suspected overdose of opioid

reverses both toxic and clinical effects of opioids

75
Q

naltrexone

A

the adjuvant tx of alcoholism and nicotine dependence
-used off-label for opiate agonist dependence and withdrawal
-wt loss

Advanced Pharma (27 decks)

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