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Flashcards in NSAIDS Deck (35)
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1

what pathways do NSAIDs block?

Cyclooxygenase 1 and 2 (and thus prostanoids)

2

what do eicosanoids bind to?

prostaglandins, thrombaxanes, leukotrienes

3

enzyme expression seen with Cox-1

TXA2 in platelets

4

enzyme expression seen with Cox-2

PGE/TXA2 in activated macrophages

5

For COX-1 and COX-2: which is constitutively expressed and which is induced?

COX-1 is constitutive
COX-2 is induce by stress

6

Major side effect of inhibition of COX-1

GI related problems
Prostaglandins regulate stomach acids- inhibition can cause bloody stools, stomach bleeding, anemia...

7

Major difference between aspirin and other NSAIDs

aspirin is an irreversible inhibitor

8

NSAID uses

analgesia, anti-pyretic
only at high doses is it anti-inflammatory

9

one potential good side effect of NSAIDs, now being researched?

cancer prevention

10

common NSAID side effects

GI- pain, nausea, diarrhea, ulcers, perforation
Renal- insufficiency, failure, low efficacy of HTN Rx
MI !!! black box warning

11

can you use NSAIDs in pregnancy

No- prostaglandins involved in uterin fxn
prolonged gestation, post-partum hemorrhage

12

what is acetylsalicylic acid and why is it special?

aspirin
non-selective for COX-1 and and COX-2
Irreversible- acetylates serine- kills enzyme

13

contraindication of aspirin

use in children- Reye's syndrome

14

antipyretic effect of aspirin

only works at low doses
high doses can induce pyretic effect

15

therapeutics of aspirin

cardioprotective- decreases platelet aggregation for 4-7 days
decrease MI risk (only in at-risk individuals)

16

where is aspirin secreted

proximal tubule and glomerular filtration
need to adjust dose in renal failure

17

how to prevent GI problems (drug)

co-formulation with misoprostol (or other proton-pump inhibitor)

18

aspirin hypersensitivity

induced effect- neoantigen formation
common in people with nasal polyps
cross sensitivity with NSAIDs

19

side effects with toxic doses of aspirin

tinnitus
respiratory and metabolic acidosis

20

only NSAIDs for IV use

ibuprofen and ketorolac

21

half-life of ibuprofen

2 hours

22

max daily dose of ibuprofen

2400mg

23

half life of naproxen

14 hours

24

patients have more GI effects on ibuprofen or naproxen?

naproxen

25

half life of celebrex

11 hours

26

which pathway does celebrex inhibit

cox-2

27

side effect not seen with celebrex that is seen with other NSAIDs

GI problems

28

who is contraindicated for celebrex

CAD or cerebrovascular disease
sulfa allergies

29

what does a COX-2 inhibitor prevent

vasodilation, inhibition of platelet aggregation (i.e. celebrex causes more platelet aggregation)

30

when is misoprostol contraindicated

used to induce labor- don't use in early pregnancy- causes termination