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Flashcards in NSAIDS Deck (74)
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1

Which 3 symptoms do NSAIDS treat?

inflammation
fever
pain

2

What are the 3 classes of NSAIDS?

1) Aspirin and Salicylic Acids
2) Non-selective and traditional NSAIDS
3) COX-2 specific inhibitors

3

What is the shared mechanism of all NSAIDS?

inhibiting activity of cylooxygenase enzymes

prevent conversion of arachadonic acid to prostaglandins and thromboxane

4

COX-1 is associated with _____________________ while COX-2 is associated with _____________________.

1: regulating homeostasis
2: inflammatory response

5

How do NSAIDS prevent conversion of arachadonic acid into prostaglandins and thromboxane?

prevent binding of arachadonic acid to active site

6

What are 2 aspirin specific indications?

1) Stroke/MI prevention
2) inhibition of platelet activaion

7

Other than inflammation, pain, fever, what are some lesser known indications of NSAIDS?

promote closure of patent ductus arteriosus
cancer prevention

8

True or False: all NSAIDS act as competitive COX enzyme inhibitors?

FALSE; aspirin is non-competitive (covalently modifies enzyme permanently)

9

What is aspirin's mechanism of action?

irreversible non-competitive COX inhibitor

10

Which Cox enzyme is inducible?

2 (induced in response to pro-inflammatory stimuli)

11

Where is Cox1 located? Cox2?

1: ubiquitously
2: induced in macs, monocytes (low level constitutive expression in kidney and endothelium)

12

What 3 housekeeping functions does COX-1 perform?

1) platelet regulation
2) kidney function
3) stomach acid/mucous production

13

What 3 effects do prostaglandins produced by Cox-2 have on the body?

1) increased vasodilation (increased blood flow)
2) increased migration of phagocytes
3) increased vascular permeability (increased edema)

14

True or false: PGs generate pain response

FALSE; they increase response to painful stimuli (decrease activation threshold for pain stimuli)

15

How do NSAIDS impair fever generation?

Fever: caused by IL-1 and TNF being produced in periphery and go to CNS to induce COX2 to make PGE2 which causes fever

NSAIDS inhibit COX2

16

What 5 housekeeping functions is COX1 responsible for?

1) GI tract (cytoprotective for stomach lining)
2) cardiovascular system (regulates BP)
3) Kidney (PGs promote vasodilation, GFR, maintain normal renal blood flow)
4) Female reproduction (PGs cause too many cramps, helps birth)
5) Control of ductus arteriosus (PGs keep this open)

17

What is aspirin's mechanism of action?

irreversibly inhibits COX-1 by acetylating the enzyme within its active site

(also inhibits COX-3 but much less potently)

18

What is the predominant COX in the stomach?

COX-1

19

What do PGs do in the stomach?

1) inhibit gastric acid section
2) increase gastric bicarb production
3) increase gastric mucous production
4) increase vasodilation

20

Platelets only express ______ and produce ____________.

COX-1
Thromboxane

21

Endothelial cells express __________ and produce _______________

COX-1 and 2
PGI2

22

True or false: endothelial cells produce thromboxane

FALSE; lack TXA2 synthase

23

Which PG promotes platelet aggregation? Which one inhibits it?

Thromboxane promotes

PGI2 (prostacyclin) inhibits platelet agg

24

Can NSAIDS delay or promote labor?

DELAY (because prostaglandins are needed in labor)

25

When is it appropriate to give NSAIDS to an infant?

in cases where ductus does not close spontaneously (after 12-24 hours)

PGs keep it open so you want to block those

26

Rank these 3 drugs with their specificity for COX1 inhibition?
ibuprofen, naproxen, aspirin

strongest to least
aspirin>naproxen>ibuprofen

27

Is aspirin an acid or a base?

weak acid (rapidly absorbed in stomach)

28

True or false: both aspirin and salicylic acid inhibit COX1 and 2 and are anti-inflammatory

true

29

Where is aspirin metabolized?

serum (rapidly to salicylic acid and acetic acid)

30

True or false: aspirin is equally potent inhibitor of Cox1 and 2

FALSE (more potent for 1)