NSAIDs Flashcards

1
Q

what does antipyretic mean?

A

anti fever

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2
Q

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

A

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

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3
Q

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

A

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

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4
Q

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

A

AA–>PGG via COX1 and 2–>TXA (enzyme?)

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5
Q

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

A

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

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6
Q

LT stands for

A

leukotriene

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7
Q

AA stands for

A

arachadonic acid

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8
Q

COX1 and COX2 stand for

A

cyclooxygenase 1 and 2. these are ezymes

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9
Q

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

A

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

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10
Q

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

A

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

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11
Q

what induces COX2

A

cytokines, shear stress, growth factors

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12
Q

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

A

T.

‘nuff said

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13
Q

What do steroids inhibit?

A

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

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14
Q

What does COX1 do to the GI tract?

A

think protection.

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

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15
Q

What does COX1 do to platelets?

A

pro-aggregatory effect (TXA2)

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16
Q

What does COX1 do to the kidneys?

A

increases renal blood flow (makes for a healthy kidney)

promotes diuresis

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17
Q

What does COX1 do to vascular smooth muscle?

A

vasodilation and vasoconstriction

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18
Q

What does COX1 do to the bone?

A

stimulates bone formation and resorption.

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19
Q

What does COX2 do to areas of pain and inflammation?

A

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

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20
Q

What does COX2 do to hypothalmus/fever?

A

↑ Heat generation

↓ Heat loss

21
Q

What does COX2 do to the kidneys?

A

maintenance of renal blood flow to adapt to stress

22
Q

What does COX2 do to endothelial cells?

A

Vasodilation

anti-aggregatory platelet effects

23
Q

What does COX2 do to uterine smooth muscle?

A

labor contractions near partuition

24
Q

What does COX2 do to ductus arteriosus?

A

maintains it via vasodilatory effects

25
Q

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

A

T

26
Q

What are the prostaglandin effects on vascular smooth muscle?

A

PGE2-vasodilation

TXA2-vasoconstriction

27
Q

What are the prostaglandin effects on platelets?

A

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

28
Q

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

A

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

29
Q

What are the prostaglandin effects on kidney cells?

A

PGE2/PGI2 increase RBF, promote diuresis

30
Q

What are the prostaglandin effects on uterine cells?

A

PGE2/PGI2 induce contractions near partuition

31
Q

What are the prostaglandin effects on inflammatory cells?

A

PGE2/PGI2 potentiate pain, edema, fever

32
Q

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

A

GI ulceration
prolonged bleeding
acute renal failure

33
Q

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

A
acute renal failure
thrombotic events (COX2 selective agents)
prolonged gestation
34
Q

COX1 acts on what areas of the body?

A

GI tract, Bone, Kidney, Vascular smooth muscle, Bone

Go By Kids Vice Principal

35
Q

COX2 acts on what areas of the body?

A

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

36
Q

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

A

enhanced chemotaxis of neutrophils.

37
Q

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

A

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

38
Q

TXA2 will ______ SM while PGI2 will ______ it.

A

vasoconstrict

vasodilate

39
Q

TXA2 will ______ platelets while PGI2 will ______ them.

A

aggregate

disaggregate

40
Q

general way to think of TXA2 compared to PGI2

A

TXA2- close and plug things up

PGI2- open things up and don’t let them clot

41
Q

How does Aspirin act on COX1 and 2?

A

1 and 2 irreversible

42
Q

How does Acetominophen act on COX1 and 2?

A

CNS COX2 inhibitor

43
Q

How do tNSAIDs act on COX1 and 2?

A

1 and 2 reversible

44
Q

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

A

2 reversible

celecoxib

45
Q

What are the Therapeutic Uses of Aspirin?

A

Analgesic, Antipyretic, Anti-inflammatory, Anti-thrombotic

46
Q

What are the Therapeutic Uses of tNSAIDs?

A

Analgesic, Antipyretic, Anti-inflammatory,

47
Q

What are the therapeutic uses of COX2 selective inhibitors?

A

Analgesic, Antipyretic

48
Q

What are the therapeutic uses of acetaminophen?

A

analgesic, antipyretic

49
Q

Memorize chart to get LO #8

A

just do it