Pharmacologic inhibition of prostaglandin synthesis Flashcards

1
Q

Prostaglandins modulate this, the detection of stimuli associated to perception of pain

A

Nociception

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2
Q

Prostaglandins are ligands to this

A

GPCR

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3
Q

Prostaglandins are derived from this

A

Membrane lipids

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4
Q

Prostaglandin that maintains a patent ductus arteriosus during pregnancy

A

PGE2

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5
Q

2 prostaglandins that stimulate mucus secretion and decrease acid production in the GI

A

PGE2 and PGI2

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6
Q

Enzyme that converts membrane phospholipids to arachidonic acid

A

Phospholipase A2

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7
Q

Enzyme that converts arachidonic acid to leukotrienes

A

5-lipoxygenase

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8
Q

Enzyme that converts arachidonic acid to prostaglandin G

A

COX1/2

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9
Q

Enzyme that converts prostaglandin G to prostaglandin H2

A

Peroxidase

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10
Q

In the prostaglandin synthesis pathway, what reaction does phospholipase A2 catalyze?

A

Membrane phospholipids to arachidonic acid

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11
Q

In the prostaglandin synthesis pathway, what reaction does 5-lipoxygenase catalyze?

A

Arachidonic acid to leukotrienes

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12
Q

In the prostaglandin synthesis pathway, what reaction does COX1/2 catalyze?

A

Arachidonic acid to Prostaglandin G

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13
Q

In the prostaglandin synthesis pathway, what reaction does peroxidase catalyze?

A

Prostaglandin G to Prostaglandin H2

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14
Q

NSAIDs inhibit this enzyme

A

Cyclooxygenase enzymes involved in prostaglandin and thromoxane synthesis

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15
Q

Cyclooxygenase enzyme that is mostly constitutive expressed

A

COX-1

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16
Q

Cyclooxygenase enzyme that has inducible expression

A

COX-2

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17
Q

Does COX-1 have inducible or constitutive expression?

A

Mostly constitutive

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18
Q

Does COX-2 have inducible or constitutive expression?

A

Inducible

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19
Q

Therapeutic prostaglandin inhibition has this effect on hypothalamus set point temperature

A

Decreases, lowers fever

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20
Q

Therapeutic prostaglandin inhibition has this effect on peripheral pain receptor activation

A

Blocks it, induces analgesia

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21
Q

Therapeutic prostaglandin inhibition has this effect on inflammation

A

Blocks inflammatory vasodilation, decreasing inflammation

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22
Q

Therapeutic prostaglandin inhibition blocks production of this molecule, thus decreasing platelet aggregation

A

Thromboxane A2

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23
Q

Prostaglandin that promotes platelet adhesion and clot formation

A

Thromboxane A2

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24
Q

What is the MOA for non-aspirin (traditional) NSAIDs

A

Reversible inhibitors of COX-1 and COX-2

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25
All NSAIDs except this are associated with increased risk of cardiovascular effects
Naproxen
26
Naproxen is this exception to NSAIDs
Is not associated with increased risk of cardiovascular effects
27
Naproxen is the only NSAID that is not associated with increased risk of this
cardiovascular effects
28
These are reversible inhibitors of COX-1 and COX-2
Non-aspirin (traditional) NSAIDs
29
Inhibition of constitutive prostaglandins reduces these in the GI
Cyto-protective prostaglandins
30
Inhibition of constitutive prostaglandins reduces prostaglandins that control this blood flow
Renal
31
This irreversibly inhibits COX-1 and COX-2 prostaglandin H2 synthesis and function
Aspirin (acetylsalicyclic acid)
32
What is the MOA of aspirin (acetylsalicylic acid)?
Irreversibly inhibits COX-1 and COX-2 prostaglandin H2 synthesis and function (acetylates serine in COX, blocks substrate processing)
33
Acetylsalicylic acid is another name for this drug
Aspirin
34
Aspirin irreversibly inhibits COX-1 and COX-2 synthesis and function of this
Prostaglandin H2
35
Aspirin acetylates this in COX, blocking substrate processing
Serine
36
This acetylates serine in COX, blocking substrate processing
Aspirin (acetylsalicyclic acid)
37
Samter's triad is another name for this
Aspirin-exacerbated respiratory disease (AERD)
38
Aspirin-exacerbated respiratory disease (AERD) is associated with this triad of conditions
Asthma, nasal polyposis, and rhinitis
39
Samter's triad of asthma, nasal polyposis and rhinitis are associated with increased sensitivity to this
Aspirin
40
Toxicity to this drug can cause signs of intoxication (nausea, vomiting, dizziness) and tinnitus/decreased hearing
Aspirin
41
Tinnitus and decreased hearing can occur with use of this drug
Aspirin
42
What is salicylism?
Nausea, vomiting, dizziness, tinnitus/decreased hearing that are toxicities to aspirin
43
All NSAIDs have block box warning of increased risk of these adverse effects
Cardiovascular and GI
44
This type of drug can induce premature closure of ductus arteriosus
NSAID
45
NSAIDs can induce premature closure of this
Ductus arteriosus
46
COX-2 inhibitor that is used in patients at high risk for GI ulceration
Celecoxib (Celebrex)
47
What is Celecoxib (Celebrex)?
COX-2 inhibitor that is limited to use in patients at high risk for GI ulceration
48
Celecoxib (Celebrex) inhibits this
COX-2
49
Celecoxib (Celebrex) is limited to NSAID indication in patients at high risk for this
GI ulceration
50
Drug whose use is limited to NSAID indication in patients at high risk for GI ulceration
Celecoxib (Celebrex)
51
Drug that is a COX-2 inhibitor
Celecoxib (Celebrex)
52
Proposed MOA of this is central inhibition of COX1/2
Acetaminophen
53
Acetaminophen limited effect on this explains lack of anti-inflammatory action
Peripheral COX enzyme
54
Does Acetaminophen have anti-inflammatory action?
No Has limited effect on peripheral COX enzyme
55
Does Acetaminophen have an effect on platelet aggregation?
No
56
What is the proposed MOA of Acetaminophen?
Central inhibition of COX1/2
57
Overdose of this can deplete glutathione, resulting in free NAPQI that damages the liver
Acetaminophen
58
Acetaminophen overdose can deplete this, resulting in free NAPQI that damages the liver
Glutathione
59
Acetaminophen overdose can deplete glutathione, resulting in this that damages the liver
NAPQI
60
Glutathione precursor that is an antidote to Acetaminophen overdose
N-acetylcysteine (NAC)
61
N-acetylcysteine (NAC) is a precursor to this
Glutathione
62
N-acetylcysteine (NAC) is an antidote used in overdose of this
Acetaminophen
63
N-acetylcysteine (NAC) antidote is most effective when used in this timeframe of acetaminophen overdose
within 10 hours
64
What is the cumulative daily dosing limit of Acetaminophen?
4g/day Lowered with existing liver disease or with alcohol use
65
Only prostaglandin synthesis inhibitor that is used to reduce fever and pain only, not inflammation
Acetaminophen
66
Prostaglandin synthesis inhibitor that is very toxic to children, and triggers leukotriene-triggered asthma in some patients
Aspirin