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Medicinal Chemistry > NSAIDs 2 > Flashcards

NSAIDs 2 Flashcards

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1
Q

What is the effect of COX2 in the peripheral injury site

A

Inflammation

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2
Q

What is the effect of COX2 in the Brain

A

Modulate pain perception
Promote fever (hypothalamus)

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3
Q

What is the effect of COX1 in the stomach

A

Protect mucosa

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4
Q

What is the effect of COX1 in the platelets

A

Aggregation

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5
Q

What is the effect of COX1 in the kidney

A

Vasodilation

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6
Q

Why most NSAIDs contain carboxylic acid?

A

They compete with arachidonic acid → need to be highly lipophilic and acidic

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7
Q

Why are acids good

A
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8
Q

Why are acids bad

A
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9
Q

Explain absorption of NSAIDs

A
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10
Q

Explain distribution of NSAIDs

A
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11
Q

Explain metabolism of NSAIDs

A
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12
Q

Explain excretion of NSAIDs

A
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13
Q

What are the GI side effects of NSAIDs

A
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14
Q

How can the GI side effects of NSAIDs be improved

A

NSAIDs taken with food or milk

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15
Q

Some NSAIDs have what CNS side effects

A

Dizziness and headache

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16
Q

NSAIDs side effects are mainly due to what

A

PGE inhibition, platelet aggregation inhibition

17
Q

When are NSAIDs prohibited to give

A

Before tooth extraction or surgery

18
Q

List the non selective cox inhibitors

A
19
Q

Salicylates promote what

A

Excretion of uric acid, useful in gout

20
Q

Salicylates inhibit what

A

Platelet aggregation, prevent heart attacks and stroke

21
Q

What are the side effects of salicylate related to GI

A
22
Q

What is the salicylates mechanism

A
23
Q

SAR of salicylates indicates what

A

That side effects mostly from the COOH function

24
Q

Salicylates are what

A
25
Q

Explain the SAR of salicylates

A
26
Q

Salicylates are contraindicated with what

A

Anticoagulants

27
Q

Explain the mechanism of the cox inhibition by aspirin

A
28
Q

Aspirin toxicity causes what

A
29
Q

What are the treatments of aspirin toxicity

A
30
Q

What are the two types of arylalkanoic acid

A
31
Q

List the arylacetic acids

A

Indomethacin
Diclofenac

32
Q

Explain the SAR of Arylacetic acid

A
33
Q

What is the most potent NSAIDs to day

A
34
Q

Explain the SAR of indomethacin

A
35
Q

What is the most widely used NSAIDs

A

Diclofenac

36
Q

What are the characters and properties of diclofenac

A
37
Q

Explain the potency of diclafenac

A
38
Q

What is special about diclofenac structure

A
39
Q

What are the 3 possible mechanism of action of diclofenac

A

Medicinal Chemistry (15 decks)

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