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Summer Pharm - Exam 2 > Non-Opioid Analgesics - NSAIDs/APAP > Flashcards

Non-Opioid Analgesics - NSAIDs/APAP Flashcards

1
Q

major target for NSAIDs

A

COX 2

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2
Q

how is PG synthesis inhibited

A

inhibiting COX 1 AND COX 2

beneficial and risky

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3
Q

3 eicosanoids

A

PG

thromboxanes

LT

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4
Q

3 non selective COX inhibitors

A

ibuprofen

naproxen

ketorolac (toradol)

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5
Q

2 selective COX 2 inhibitors

A

celecoxib

APAP

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6
Q

harmful actions mediated by COX 2 eicosanoids that are mediated by NSAIDs

A

pain

inflammation

fever

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7
Q

beneficial actions of COX-1 eicosanoids that are diminished by NSAID use

A

kidney -> diuresis

secretions -> GI

platetelets -> pro -> clotting

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8
Q

inhibitory effects of NSAIDs on beneficial effects of COX 2 (5)

A

GI ulceration/bleeding

renal dysfxn

increased risk of thrombotic events

delayed labor

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9
Q

bad effects of NSAIDs are most critical in

A

elderly pt’s w. deteriorating renal fxn

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10
Q

2 main ways non opioid analgesics classified

A

selectivity → COX 1 vs COX 2

reversible vs irreversible inhibition

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11
Q

4 major groups of non opioid analgesics

A

NSAIDs

celecoxib

APAP

ASA

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12
Q

which non opioid analgesics are reversible

A

NSAIDs

celecoxib

APAP

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13
Q

which non opioid analgesic is irreversible

A

ASA

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14
Q

which non opioid analgesics inhibit COX 1 AND COX 2

A

NSAIDs → reversible

ASA → irreversible

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15
Q

celecoxib and APAP inhibit

A

COX 2

reversible

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16
Q

where does APAP inhibit COX 2

A

CNS

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17
Q

major dose dependent therapeutic uses of COX -2 inhibitors

A

analgesia

antipyretic

AI

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18
Q

which effect of COX-2 inhibitors requires the highest dose

A

anti-inflammatory

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19
Q

effect of COX-1 inhibitors that requires low daily dosing

A

antithrombotic

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20
Q

common s.e of COX inhibitors

A

GI ulceration → COX 1

increased bleeding risk → COX 1

delayed labor → COX 2

increased thrombotic events → COX 2

renal dysfxn → COX 1 and COX 2

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21
Q

which COX are found in the kidney

A

COX 1 AND COX 2

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22
Q

3 clinical uses of NSAIDs (NS COX inhibitors)

A

pain

antipyretic

anti-inflammatory

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23
Q

t/f: NSAIDs are as effective or superior to ASA and APAP for pain of inflammatory origin (muscle/dental/arthritis)

A

T!

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24
Q

what NSAID is available IM/IV for postop pain

A

ketorolac

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25
Q

which NSAID is available as a solution for pediatric fever

A

ibuprofen

APAP

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26
Q

t/f: NSAIDs are as effective or superior to ASA/APAP for antipyretic effects

A

T!

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27
Q

t/f: efficacies of NSAIDs/APAP/ASA are similar for anti-inflammatory effects

A

F!

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28
Q

is absorption of NSAIDs affected by food

A

no

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29
Q

NSAIDs are distributed to __ after repeated dosees

A

synovial fluid

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30
Q

metabolism/elimination of NSAIDs

A

metabolism: liver (CYP enzymes) →
elimination: renal

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31
Q

list NSAIDs in order of shortest to longest t½

A

ibuprofen

celecoxib

naproxen

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32
Q

3 relative contraindications for NSAIDs

A

PUD → interfere w. gastric cytoprotection via COX-1

antiplatelet/anticoagulant use

ASA/NSAID triad

HTN

DM

CKD

HF

33
Q

2 meds to manage mild dyspepsia

A

antacids

PPI (omeprazole)

34
Q

education for pt taking low dose ASA for cardioprotective effect who also needs to take NSAIDs for pain/inflammation

A

ASA

1 hr later -> NSAID

35
Q

is renal insufficiency caused by NSAIDs reversible

A

yes

36
Q

all __,

along with __ cause fluid retention

and should be used cautiously in pt’s w. __

A

NSAIDs

celecoxib

CVD

37
Q

what is the ASA/NSAID triad

A

hypersensitivity to ASA/NSAIDs

chronic rhinosinusitis w. nasal polyps

bronchial asthma

38
Q

why are GC better for asthmatics

A

decrease LT AND PGs

39
Q

why are NSAIDs bad for asthmatics

A

decrease PGs

increase LTs

40
Q

3 indications for celecoxib (selective COX 2 inhibitor)

A

inflammation

acute pain

primary dysmenorrhea

41
Q

2 inflammatory conditions French pointed out for celecoxib

A

RA

ankylosing spondylitis

42
Q

benefits of celecoxib outweigh risks in pt’s who can not tolerate NSAIDs due to __,

but risks outweigh benefits in pt’s w. __

A

GI s.e

CVD

43
Q

5 pt pops who might benefit from celecoxib

A

age > 65 yo

anticoag use

prior GI bleed

active PUD

concurrent use of oral GC

44
Q

besides celecoxib, 2 other safe options for pt’s at high risk for GI s.e w. NSAIDs

A

NSAID PLUS PPI

NSAID PLUS misoprostol

45
Q

what class of drug is misoprostol

A

PG analog

46
Q

does celecoxib alter platelet fxn or increase bleeding risk

A

no! → does not inhibit COX 1

47
Q

celecoxib increases the risk of (2)

A

ischemic CVD

HF

48
Q

how does celecoxib increase risk for ischemic CVD and HF

A

blocks COX 2 →

elevates bp

decreases renal fxn

49
Q

black box warning for celecoxib

A

adverse CV thrombotic events (similar risk to NS NSAIDs)

hypersensitivity rxn dt sulfa moiety

50
Q

GI risk: higher w. inhibition of COX 1 or COX 2

A

higher w. COX 1

51
Q

GI risk is lowest w. __

and highest w. __

A

lowest: ibuprofen (followed by celecoxib)
highest: naproxen

52
Q

CV risk: higher w. inhibition of COX 1 or COX 2

A

equal!

53
Q

renal risk: higher w. inhibition of COX 1 or COX 2

A

equal!

54
Q

alternative for pt w. HTN, DM, HF, CKD

A

APAP

tramadol

opioids

55
Q

t/f: APAP is less effective than NSAIDs for pain

A

F

56
Q

t/f: for antipyretic effects, APAP is effective or superior to ASA/NSAIDs

A

T!

57
Q

does APAP have anti-inflammatory action

A

no!

may have some use in OA

58
Q

why doesn’t APAP have anti inflammatory action

A

it inhibits central cytokine release, but not peripheral inflammation

59
Q

absorption rate of APAP is related to __

and is faster w. __

A

gastric emptying

liquid preps

60
Q

APAP is metabolized to (2)

A

sulfate

glucuronide

61
Q

a small % of APAP is metabolized to __

A

hepatotoxic metabolite

62
Q

ellimination/metabolism of APAP is unaffected by

A

renal fxn

63
Q

when you think elimination/metabolism of APAP, think phase

A

2

64
Q

t/f: APAP has few-no s.e when compared to NSAIDs

A

T!

bc it doesn’t work on peripheral COX 1 or COX 2

65
Q

major concern w. APAP

A

hepatotoxicity

66
Q

at what dose is risk of hepatotoxicity increased w. APAP

A

1000mg

67
Q

does 1000 mg of APAP provide greater analgesia

A

no!

68
Q

chronic ethanol induces __

and depletes protective __

A

CYP2E1

GSH

69
Q

be aware of APAP in __ products

A

opioid combo →

percocet

vicodin

70
Q

risk of APAP in opioid products

A

tolerance develops → need higher doses → hepatotoxicity

71
Q

tx for APAP overdose

A

N-acetylcysteine → replenishes GSH and inactivates Ac directly

72
Q

Phase 1 rxns

A

oxidation

hydrolysis

reduction

73
Q

phase 1 enzyme to know

A

CYP450

74
Q

inducing/inhibiting action of CYP450

A

significant

75
Q

saturability of CYP450

A

minimal

76
Q

phase II rxns

A

conjugations →

n-acetylation

glutathione

glucoronidation

sulfation

77
Q

phase II enzyme to know

A

transferase

78
Q

saturability of transferase

A

substantial

Summer Pharm - Exam 2 (12 decks)

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