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Pharm Exam 4 > Acetaminophen and NSAIDs > Flashcards

Acetaminophen and NSAIDs Flashcards

1
Q

Takes Arachidonic Acid out of the phospholipid membrane.

A

Phospholipase A2

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2
Q

Converts AA to Prostaglandins

A

Cyclooxygenase

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3
Q

COX1 makes:

A

Prostaglandin E2
Thromboxane
Prostacycline

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4
Q

What does PGE2 control?

A

Renal perfusion/GFR

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5
Q

What does Prostacycline control?

A

Gastric acid secretion

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6
Q

COX 2 makes prostaglandins that control what?

A

Pain, inflammation, and fever.

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7
Q

COX 2 makes __________ prostaglandins

A

pro-inflammatory

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8
Q

What do NSAIDs inhibit?

A

COX pathways.

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9
Q

These are anti-pyretic, analgesic, and anti-inflammatory.

A

NSAIDs

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10
Q

Act by inhibiting cyclooxygenase enzymes, causing decreased prostaglandin synthesis.

A

NSAIDs.

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11
Q

Prevent AA from binding to COX so that no prostaglandins are made.

A

NSAIDs

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12
Q

4 types of NSAIDs

A

Aspirin
Ibuprofen
Naproxen
Indomethacin

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13
Q

Aspirin is AKA

A

Acetylsalicyclic acid

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14
Q

NSAIDs that are propionic acids

A

Ibuprofen

Naproxen

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15
Q

Motrin and Advil are:

A

Ibuprofen

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16
Q

Aleve is:

A

Naproxen

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17
Q

Used for fever, mild-to-moderate pain, dental pain, headache, and it has the lowest risk of GI bleeding.

A

Ibuprofen (Motrin and Advil)

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18
Q

NSAID that’s an acetic acid derivative.

A

Indomethacin

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19
Q

Why does the heart make prostaglandins?

A

To keep the vessels supplying the heart open, so more blood can get to the heart.

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20
Q

How do NSAIDs affect the heart?

A

Fewer prostaglandins are made, so less blood travels through the heart.

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21
Q

Action of PGE2 on nociceptive nerve endings.

A

PGE2 sensitizes nociceptive nerve endings to painful stimuli.

Primes nociceptors to sense pain.

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22
Q

How do NSAIDs cause analgesia?

A

They prevent PGE2 from being made, so nociceptors are not primed to sense pain.

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23
Q

T/F: No single NSAID has superior analgesic efficacy over another.

A

TRUE

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24
Q

Pyresis

A

Fever

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25
Q

Pyrogen definition

A

Fever promoting agent

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26
Q

How does PGE2 cause fever in people?

A

It increases the set point for the thermoregulatory center in the brain, and body temperature doesn’t get regulated until it’s pretty high.

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27
Q

How do NSAIDs lower temperature in patients with a fever?

A

They decrease the amount of PGE2 made, so that it cannot reset the hypothalamic thermoregulatory center “set point.”

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28
Q

An inducible isoform that is induced by pro-inflammatory stimuli in migratory cells and inflamed tissues.

A

COX-2

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29
Q

Analgesic doses of NSAIDs are ____ and have a ______.

A

small; ceiling.

30
Q

Anti-inflammatory doses of NSAIDs are ______ and don’t have a _______.

A

high; ceiling.

31
Q

Do NSAIDs have high or low first pass metabolism?

32
Q

NSAIDs are weak _____ that are rapidly absorbed in the acidic environment of the stomach.

33
Q

Why do NSAIDs slow the clearance of drugs in the kidney?

A

Bc they inhibit PGE2, thus slowing renal perfusion rate.

34
Q

How do COX1 and COX2 increase GFR in the kidney?

A

By making prostaglandins, which vasodilate the arteries, and increase the amount of blood going to the kidney.

35
Q

Role of PGE2 in the GI mucosa.

A

Gastric protection:

Mucus secretion
Bicarbonate secretion
Increased mucosal blood flow.

36
Q

What does inhibition of COX-1 by NSAIDs do in the GI?

A

Peptic ulcers

GI bleeding

37
Q

Which COX is found in the GI?

38
Q

Role of PGE2 in the kidney.

A

1) Arteriolar dilation to increase GFR/Renal Perfusion.

2) Increases Na and water excretion.

39
Q

Which COX are found in the kidney?

A

COX 1 and COX 2

40
Q

What does inhibition of Cyclooxygenase by NSAIDs cause in the kidney?

A

1) Na and Water retention.
2) Hypertension
3) Hemodynamic acute kidney injury.

41
Q

Which cyclooxygenases are found in the heart?

A

COX 1 and COX 2

42
Q

What does PGI2 (Prostacyclin) by COX 2 do in the heart?

A

1) Vasodilation of heart arteries

2) Inhibits platelet aggregation

43
Q

What does Thromboxane A2 by COX-1 do in the heart?

A

1) Causes platelet aggregation

2) Vasoconstriction

44
Q

What happens if COX 1 and 2 are inhibited in the heart?

A

Stroke and MI

45
Q

Role of PGE2 in the stomach.

A

Inhibits gastric acid secretion.

46
Q

Role of PGI2 in the stomach.

A

Causes mucus and bicarbonate secretion.

47
Q

What do NSAIDs inhibit in the stomach?

A

PGE2 and PGI2 by inhibiting COX-1 activity.

48
Q

NSAIDs ______ stomach acid secretion and ________ mucus production, thus ________ the adverse effects and toxicities in the GI.

A

increase; decrease, increasing

49
Q

Which prostaglandin is found in the heart?

50
Q

Which cyclooxygenase makes PGI2 in the heart?

51
Q

PGI2 is called what?

A

Prostacyclin

52
Q

COX __ makes _____ in the heart.

53
Q

T/F: Cardiovascular toxicity with NSAIDs is due to inhibition of cardioprotective PGI2, which is generated by COX-2.

54
Q

NSAID that selectively inhibits COX-2

55
Q

T/F: NSAIDs are contraindicated in pregnancy.

56
Q

_______ is preferred if analgesic or antipyretic effects are needed during pregnancy.

A

Acetaminophen (Tylenol)

57
Q

Why should NSAIDs be avoided in the third trimester?

A

Can cause premature closure of the ductus arteriosus.

58
Q

These NSAIDs have important cardiovascular effects that include increased risk for MI, stroke, heart failure, and hypertension.

A

Celecoxib (COX-2 inhibitor)

59
Q

These cyclooxygenase inhibitors are preferred bc they have fewer symptomatic gastric and duodenal ulcers and a decrease in GI symptoms.

A

COX-2 Inhibitors

60
Q

COX-2 selective inhibitor.

61
Q

This COX inhibitor has a lower incidence of gastroduodenal ulcers compared to nonselective NSAIDs.

62
Q

Higher doses of this drug are clearly associated with an increased cardiovascular risk.

63
Q

T/F: In patients taking routine NSAIDs for 10 days or fewer to alleviate pain, most patients are not at any increased risk of developing adverse CV, GI, renal, or respiratory adverse effects.

64
Q

This NSAID is used as an anti-platelet.

65
Q

Common doses of aspirin

A

81-325 mg once a day

66
Q

Which cyclooxygenase does Aspirin inhibit?

67
Q

Platelets make this cyclooxygenase.

68
Q

Aspirin irreversibly inhibits COX-___, preventing ____ synthesis.

This antiplatelet effect lasts 8-10 days (the life of the platelet).

69
Q

How does Aspirin inhibit COX-1?

A

By acetylating it.

70
Q

This NSAID is prescribed as secondary prevention of heart attack and stroke.

71
Q

This NSAID is for fever and pain, but not anti-inflammatory.

A

Acetaminophen (Tylenol)

72
Q

Acetaminophen MOA

A

Centrally acting:

1) It raises the pain threshold.
2) It inhibits endogenous pyrogens of the heat-regulating centers in the brain.

Pharm Exam 4 (9 decks)

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