NSAIDs

Question 1

what does antipyretic mean?

Answer 1

anti fever

Question 2

Describe the biosynthetic pathway of prostaglandins and the specific enzymes involved at each step

Answer 2

AA–>cyclooxygenase (PGG) via COX1 and 2 –> PG E2, D2, or F2a via endoperoxide isomerase

Question 3

Describe the biosynthetic pathway of Prostacyclin and the specific enzymes involved at each step

Answer 3

AA–>PGG via COX1 and 2–>PGI2 (enzyme?)

Question 4

Describe the biosynthetic pathway of Thromboxane and the specific enzymes involved at each step

Answer 4

AA–>PGG via COX1 and 2–>TXA (enzyme?)

Question 5

Describe the biosynthetic pathway of Leukotriene and the specific enzymes involved at each step

Answer 5

AA–>5-HPETE via 5’-lipoxygenase–>LTA4 (leukotriene A4)–> LTB4 or LTC4/D4/E4

Question 6

LT stands for

Answer 6

leukotriene

Question 7

AA stands for

Answer 7

arachadonic acid

Question 8

COX1 and COX2 stand for

Answer 8

cyclooxygenase 1 and 2. these are ezymes

Question 9

Is COX1 constitutively expressed or induced and what does this mean?

Answer 9

constitutively expressed. It has baseline levels of activity at all times and is located ubiquitously. It is constitutively expressed for ‘housekeeping functions’

Question 10

Is COX2 constitutively expressed or induced and what does this mean?

Answer 10

induced. it is upregulated for specialized functions and is only located in inflamed or activated tissues.

Question 11

what induces COX2

Answer 11

cytokines, shear stress, growth factors

Question 12

T or F. COX1 and 2 are both inhibited by NSAIDs?

Answer 12

T.

‘nuff said

Question 13

What do steroids inhibit?

Answer 13

phospholipases (as in phospholipase A2 that leads to arachadonic acid)

Question 14

What does COX1 do to the GI tract?

Answer 14

think protection.

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

Question 15

What does COX1 do to platelets?

Answer 15

pro-aggregatory effect (TXA2)

Question 16

What does COX1 do to the kidneys?

Answer 16

increases renal blood flow (makes for a healthy kidney)

promotes diuresis

Question 17

What does COX1 do to vascular smooth muscle?

Answer 17

vasodilation and vasoconstriction

Question 18

What does COX1 do to the bone?

Answer 18

stimulates bone formation and resorption.

Question 19

What does COX2 do to areas of pain and inflammation?

Answer 19

enhance edema
enhance leukocyte infiltration via vasodilation
potentiation of bradykinin pain producing activity

Question 20

What does COX2 do to hypothalmus/fever?

Answer 20

↑ Heat generation

↓ Heat loss

Question 21

What does COX2 do to the kidneys?

Answer 21

maintenance of renal blood flow to adapt to stress

Question 22

What does COX2 do to endothelial cells?

Answer 22

Vasodilation

anti-aggregatory platelet effects

Question 23

What does COX2 do to uterine smooth muscle?

Answer 23

labor contractions near partuition

Question 24

What does COX2 do to ductus arteriosus?

Answer 24

maintains it via vasodilatory effects

Question 25

COX1 is pro-aggregatory for platelets while COX2 is antiaggregatory, T or F?

Answer 25

T

Question 26

What are the prostaglandin effects on vascular smooth muscle?

Answer 26

PGE2-vasodilation | TXA2-vasoconstriction

Question 27

What are the prostaglandin effects on platelets?

Answer 27

pro-aggretory (TXA2 although PGI2 seems to be anti-aggregatory)

Question 28

What are the prostaglandin effects on GI tract smooth muscle and secretory cells?

Answer 28

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

Question 29

What are the prostaglandin effects on kidney cells?

Answer 29

PGE2/PGI2 increase RBF, promote diuresis

Question 30

What are the prostaglandin effects on uterine cells?

Answer 30

PGE2/PGI2 induce contractions near partuition

Question 31

What are the prostaglandin effects on inflammatory cells?

Answer 31

PGE2/PGI2 potentiate pain, edema, fever

Question 32

what might being some side effects of inhibiting COX1 (given what it is responsible for)

Answer 32

GI ulceration prolonged bleeding acute renal failure

Question 33

what might being some side effects of inhibiting COX2 (given what it is responsible for)

Answer 33

``` acute renal failure thrombotic events (COX2 selective agents) prolonged gestation ```

Question 34

COX1 acts on what areas of the body?

Answer 34

GI tract, Bone, Kidney, Vascular smooth muscle, Bone Go By Kids Vice Principal

Question 35

COX2 acts on what areas of the body?

Answer 35

areas of pain/inflammation, hypothalamus/fever, kidneys, endothelial cells, uterine smooth muscle, ductus arteriosus

Question 36

What does LBT4 do that is critical for the immune response?

Answer 36

enhanced chemotaxis of neutrophils.

Question 37

What do LTC4/D4/E4 do to pulmonary/vascular SM?

Answer 37

think hypersensitivity immune response processes (like asthma) increased vascular permeability bronchoconstriction vasoconstriction

Question 38

TXA2 will ______ SM while PGI2 will ______ it.

Answer 38

vasoconstrict | vasodilate

Question 39

TXA2 will ______ platelets while PGI2 will ______ them.

Answer 39

aggregate | disaggregate

Question 40

general way to think of TXA2 compared to PGI2

Answer 40

TXA2- close and plug things up | PGI2- open things up and don't let them clot

Question 41

How does Aspirin act on COX1 and 2?

Answer 41

1 and 2 irreversible

Question 42

How does Acetominophen act on COX1 and 2?

Answer 42

CNS COX2 inhibitor

Question 43

How do tNSAIDs act on COX1 and 2?

Answer 43

1 and 2 reversible

Question 44

How do COX2 selective inhibitors act on COX1 and 2? what is an example?

Answer 44

2 reversible | celecoxib

Question 45

What are the Therapeutic Uses of Aspirin?

Answer 45

Analgesic, Antipyretic, Anti-inflammatory, Anti-thrombotic

Question 46

What are the Therapeutic Uses of tNSAIDs?

Answer 46

Analgesic, Antipyretic, Anti-inflammatory,

Question 47

What are the therapeutic uses of COX2 selective inhibitors?

Answer 47

Analgesic, Antipyretic

Question 48

What are the therapeutic uses of acetaminophen?

Answer 48

analgesic, antipyretic

Question 49

Memorize chart to get LO #8

Answer 49

just do it