NSAIDs

Question 1

Aspirin is unique among the NSAIDs for its ability to ______.

Answer 1

decrease clotting

Question 2

Celecoxib is unique among the NSAIDs because it ______.

Answer 2

doesn’t have any gastric side effects

Question 3

The COX1 pathway in platelets turns arachidonic acid into ______.

Answer 3

thromboxane

Question 4

Eicosanoids are ________.

Answer 4

signaling molecules made from oxidizing 20-carbon fatty acids

Question 5

List some of the effects of prostaglandins from the COX 1 pathway.

Answer 5

• GI: decreased acid production and increased mucous/bicarb secretion; increase smooth muscle contractions
• Platelets (TXA2): pro-aggregatory effect
• Kidneys: increased renal blood flow

Question 6

On vascular endothelial cells, prostaglandins work to _________.

Answer 6

cause vasodilation and anti-clotting

Question 7

COX1 is ___________, while COX2 is ________.

Answer 7

constitutively functioning; dependent of stimuli for induction

Question 8

Acetaminophen does not function in the periphery, only in the ______. Thus it is not an anti-inflammatory.

Answer 8

CNS (on COX2, to be specific)

Question 9

Glucocorticoids inhibit _____ and stimulate ______, thus leading to a strong anti-inflammatory effect.

Answer 9

COX; annexins (which inhibit phospholipase A, the enzyme that makes arachidonic acid)

Question 10

Ketorolac is ________, as is Celebrex.

Answer 10

prescription only

Question 11

The antiplatelet effect of aspirin is ______, while the antiplatelet effect of other NSAIDs is _______.

Answer 11

4 - 7 days; 2 days

Question 12

If you have to recommend a tNSAID, for GI patients ______ is better, while for cardio patients ______ is better.

Answer 12

ibuprofen; naproxen

Question 13

Celecoxib (Celebrex) is a ________ inhibitor.

Answer 13

selective COX2

Question 14

Celecoxib is great for _________.

Answer 14

patients who cannot tolerate high doses of NSAIDs due to GI tract

Question 15

Selective COX2 inhibitors have ________ effect on platelets.

Answer 15

no (because platelets are mediated by COX1)

Question 16

What is inhibited by NSAIDs to induce analgesia?

Answer 16

Inhibition of COX-2 at site of inflammation

Question 17

The antipyretic effect of NSAIDs is mediated by ______.

Answer 17

inhibition of COX-2 in the hypothalamus

Question 18

The anti-inflammatory effect of NSAIDs occurs through _______.

Answer 18

inhibition of COX-2 at sites of inflammation

Question 19

NSAIDs inhibit thrombogenesis by ______.

Answer 19

inhibiting COX-1 in platelets

Question 20

Which isoform of COX is present in the stomach, and what does it do?

Answer 20

COX-1, and it produces PGE which decreases acid/pepsin secretions and increase mucous/bicarb secretions

Question 21

Which isoform of COX is present in the kidneys?

Answer 21

Both!

Question 22

Inhibiting ______ leads to bleeding problems, while inhibiting ______ leads to thrombosis.

Answer 22

COX-1 in platelets; COX-2 in vascular endothelial cells

Question 23

The traditional NSAIDs are _______ and include the following drugs: _________.

Answer 23

reversible inhibitors of COX-1 and COX-2; ibuprofen, ketorolac, and naproxen

Question 24

Acetaminophen does not _________, but does inhibit ______.

Answer 24

COX-1 or COX-2 in the peripheral system; COX-2 in the CNS, leading to antipyretic effect and analgesia

Question 25

Celecoxib (Celebrex) is a ________.

Answer 25

selective reversible inhibitor of COX-2

Question 26

Aspirin (acetyl salicylic acid) is an _________.

Answer 26

irreversible inhibitor of COX-1 and COX-2

Question 27

________ mediates platelet aggregation.

Answer 27

Thromboxane A2 (produced by the COX-1 pathway)

Question 28

In the kidneys, NSAIDs cause _______.

Answer 28

vasoconstriction and fluid retention

Question 29

Celebrex is great for __________.

Answer 29

patients at risk of GI bleeds (still has renal risk)

Question 30

Recommended maximum doses of acetaminophen are ______ for those without liver disease and ______ for those with.

Answer 30

4000 mg / day; 2000 mg/day (because alcohol induces CYP2E1)

Question 31

Low-dose aspirin is essentially ______.

Answer 31

platelet COX-1 selective, thus it is antithrombotic

Question 32

In the kidneys, PGE2 and PGI2 ________.

Answer 32

increase renal blood flow

Question 33

In vascular smooth muscle, PGE2 and PGI2 lead to _______ while TXA2 leads to _______.

Answer 33

vasodilation; vasoconstriction

Question 34

The anti-thrombotic enzyme on vascular endothelial cells is ______.

Answer 34

COX-2

Question 35

Leukotrienes lead to _________.

Answer 35

vasoconstriction, bronchoconstriction, vascular permeability, and chemotaxis for phagocytic cells

Question 36

The lowest GI-risk NSAID is _______ and the highest is ______.

Answer 36

ibuprofen; naproxen

Question 37

The lowest CV-risk NSAID is ________ and the highest is _______.

Answer 37

naproxen; ibuprofen

Question 38

Aspirin overdose first leads to _____ and then _______.

Answer 38

respiratory alkalosis; metabolic acidosis

Question 39

Acetylsalicylic acid is rapidly hydrolyzed by _____.

Answer 39

esterases