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
Pyrogen definition
Fever promoting agent
26
How does PGE2 cause fever in people?
It increases the set point for the thermoregulatory center in the brain, and body temperature doesn't get regulated until it's pretty high.
27
How do NSAIDs lower temperature in patients with a fever?
They decrease the amount of PGE2 made, so that it cannot reset the hypothalamic thermoregulatory center "set point."
28
An inducible isoform that is induced by pro-inflammatory stimuli in migratory cells and inflamed tissues.
COX-2
29
Analgesic doses of NSAIDs are ____ and have a ______.
small; ceiling.
30
Anti-inflammatory doses of NSAIDs are ______ and don't have a _______.
high; ceiling.
31
Do NSAIDs have high or low first pass metabolism?
Low
32
NSAIDs are weak _____ that are rapidly absorbed in the acidic environment of the stomach.
acids.
33
Why do NSAIDs slow the clearance of drugs in the kidney?
Bc they inhibit PGE2, thus slowing renal perfusion rate.
34
How do COX1 and COX2 increase GFR in the kidney?
By making prostaglandins, which vasodilate the arteries, and increase the amount of blood going to the kidney.
35
Role of PGE2 in the GI mucosa.
Gastric protection: Mucus secretion Bicarbonate secretion Increased mucosal blood flow.
36
What does inhibition of COX-1 by NSAIDs do in the GI?
Peptic ulcers | GI bleeding
37
Which COX is found in the GI?
COX 1
38
Role of PGE2 in the kidney.
1) Arteriolar dilation to increase GFR/Renal Perfusion. | 2) Increases Na and water excretion.
39
Which COX are found in the kidney?
COX 1 and COX 2
40
What does inhibition of Cyclooxygenase by NSAIDs cause in the kidney?
1) Na and Water retention. 2) Hypertension 3) Hemodynamic acute kidney injury.
41
Which cyclooxygenases are found in the heart?
COX 1 and COX 2
42
What does PGI2 (Prostacyclin) by COX 2 do in the heart?
1) Vasodilation of heart arteries | 2) Inhibits platelet aggregation
43
What does Thromboxane A2 by COX-1 do in the heart?
1) Causes platelet aggregation | 2) Vasoconstriction
44
What happens if COX 1 and 2 are inhibited in the heart?
Stroke and MI
45
Role of PGE2 in the stomach.
Inhibits gastric acid secretion.
46
Role of PGI2 in the stomach.
Causes mucus and bicarbonate secretion.
47
What do NSAIDs inhibit in the stomach?
PGE2 and PGI2 by inhibiting COX-1 activity.
48
NSAIDs ______ stomach acid secretion and ________ mucus production, thus ________ the adverse effects and toxicities in the GI.
increase; decrease, increasing
49
Which prostaglandin is found in the heart?
PGI2
50
Which cyclooxygenase makes PGI2 in the heart?
COX-2
51
PGI2 is called what?
Prostacyclin
52
COX __ makes _____ in the heart.
2; PGI2
53
T/F: Cardiovascular toxicity with NSAIDs is due to inhibition of cardioprotective PGI2, which is generated by COX-2.
TRUE
54
NSAID that selectively inhibits COX-2
Celecoxib
55
T/F: NSAIDs are contraindicated in pregnancy.
True
56
_______ is preferred if analgesic or antipyretic effects are needed during pregnancy.
Acetaminophen (Tylenol)
57
Why should NSAIDs be avoided in the third trimester?
Can cause premature closure of the ductus arteriosus.
58
These NSAIDs have important cardiovascular effects that include increased risk for MI, stroke, heart failure, and hypertension.
Celecoxib (COX-2 inhibitor)
59
These cyclooxygenase inhibitors are preferred bc they have fewer symptomatic gastric and duodenal ulcers and a decrease in GI symptoms.
COX-2 Inhibitors
60
COX-2 selective inhibitor.
Celecoxib
61
This COX inhibitor has a lower incidence of gastroduodenal ulcers compared to nonselective NSAIDs.
Celecoxib
62
Higher doses of this drug are clearly associated with an increased cardiovascular risk.
Celecoxib
63
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.
True
64
This NSAID is used as an anti-platelet.
Aspirin
65
Common doses of aspirin
81-325 mg once a day
66
Which cyclooxygenase does Aspirin inhibit?
COX-1
67
Platelets make this cyclooxygenase.
COX-1
68
Aspirin irreversibly inhibits COX-___, preventing ____ synthesis. This antiplatelet effect lasts 8-10 days (the life of the platelet).
1; TXA2
69
How does Aspirin inhibit COX-1?
By acetylating it.
70
This NSAID is prescribed as secondary prevention of heart attack and stroke.
Aspirin
71
This NSAID is for fever and pain, but not anti-inflammatory.
Acetaminophen (Tylenol)
72
Acetaminophen MOA
Centrally acting: 1) It raises the pain threshold. 2) It inhibits endogenous pyrogens of the heat-regulating centers in the brain.