DD5 - NSAIDS

Question 1

Cox1 and 2.

Which one is constitutively expressed ? Induced?

Answer 1

Cox 1: constitutively

Cox2: induced

Question 2

Effects of Cox 1 on GI tract

Answer 2

think protective effects

• ↓ acid/pepsin secretion
• ↑ mucous/bicarbonate production
• ↑ contractions of smooth muscle

Question 3

Effects of COX1 on platelets

Answer 3

[TXA2]

• Pro-aggregatory effect

Question 4

Effects of COX1 on kidneys

Answer 4

• ↑ Renal blood flow (makes for healthy kidney)

* Promote diuresis

Question 5

Effects of COX1 on vascular smooth muscle

Answer 5

[PGI2, PGE2] - vasodilation

[TXA2] - vasoconstriction

Question 6

Effects of COX1 on Bone

Answer 6

PGE2- Stimulates bone formation and resorption

Question 7

Effects of COX2 on areas of pain/inflammation

Answer 7

• Enhance edema formation
  
  • Enhance leukocyte infiltration via vasodilation
  • Potentiation of bradykinin pain-producing activity

Question 8

Effects of COX2 on hypothalamus/fever

Answer 8

• ↑ Heat generation

* ↓ Heat loss

Question 9

Effects of COX2 on kidneys

Answer 9

• Renal adaptation to stress via maintenance of RBF

* Present constitutively, but most important in elderly

Question 10

Effects of COX2 on endothelial cells

Answer 10

• Vasodilation

* Anti-aggregatory platelet effects

Question 11

Effects of COX2 on uterine smooth muscles

Answer 11

[PGE2, PGF2]

• Labor contractions near parturition

Question 12

Effects of COX2 ductus arteriosus

Answer 12

[PGE2]

• Maintenance of patent ductus arteriosus via vasodilatory effects

Question 13

Prostaglandin effects on:

vascular smooth muscle

Answer 13

PGE2 causes vasodilation,

TXA2 causes vasoconstriction

Question 14

Prostaglandin effects on:

platelets

Answer 14

TXA2 pro-aggregatory

Question 15

Prostaglandin effects on:

GI tract smooth muscle and secretory cells

Answer 15

PGE2/PGI2 inhibit HCl secretion, increase mucous secretion, increase SM contraction

Question 16

Prostaglandin effects on:

kidney cells

Answer 16

GE2/PGI2 increase RBF, promotes diuresis

Question 17

Prostaglandin effects on:

uterine cells

Answer 17

PGE2/PGF2 induces contractions near parturition

Question 18

Prostaglandin effects on:

inflammatory cells

Answer 18

PGE2/PGI2 potentiate pain, edema, fever

Question 19

Side effects:

inhibit cox-1

Answer 19

GI ulceration,
prolonged bleeding time,
and acute renal failure

Question 20

Side effects:

inhibit cox-2

Answer 20

acute renal failure, thrombotic events (COX-2 selective agents), and prolonged gestation

Question 21

Describe the differences between LTB4 and LTC4/LTD4/LTE4 on inflammatory cell function and pulmonary / vascular smooth muscle.

Answer 21

• LTB4: Enhanced chemotaxis of neutrophils, aggregation, and transmigration through the endothelium
○ *critical for immune response

• LTC4/LTD4/LTE4: Increased vascular permeability, bronchoconstriction, vasoconstriction
○ Important role in asthma, psoriasis, and various hypersensitivity processes.

Question 22

4 types of NSAIDS

Answer 22

Aspirin
Acetaminophen
tNSAIDs
COX-2 Selective inhibitors (celecoxib)

Question 23

Aspirin Effect on COX-1&2

Answer 23

1&2 Irreversible

Question 24

Acetaminophen Effect on COX-1&2

Answer 24

CNS Cox2 inhibitor

Question 25

tNSAIDs Effect on COX-1&2

Answer 25

1&2 Reversible

Question 26

COX-2 selective inhibitors | (celecoxib) Effect on COX-1&2

Answer 26

2 Reversible

Question 27

Aspirin therapeutic uses

Answer 27

AG, AP, AI, AT *only one that is AT

Question 28

Acetaminophen

Answer 28

AG, AP *only one that is not AI

Question 29

tNSAIDs

Answer 29

AG, AP,AI

Question 30

Celecoxib (cox2 selective inhibitor)

Answer 30

Ag, AP, AI

Question 31

Which one, COX1 or 2 is Pro thrombic?

Answer 31

Cox1 - likes to clot - good for you usually

Question 32

Which one, COX1 or 2 is Anti thrombic?

Answer 32

Cox2

Question 33

Aspirin at low or high doses is antithrombotic? why?

Answer 33

low: aspirin (ASA) concentrates in the hepatic portal vein → concentration differential between endothelial surface and platelets → selective inhibitory effect on platelet COX1 and endothelial COX2 → preferential inhib effect on Cox1 → block the pro-clotting COX1 = antithrombotic effect

Question 34

Aspirin and acetominophen are metabolized via which phase I or II?

Answer 34

Phase 2