The Physiology and Pharmacology of Eicosanoids Flashcards

1
Q

What does phospholipase A2 do?

A

Cleaves Arachidonic acid from the cell membrane

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2
Q

What is derived from Arachidonic acid?

A

PG2 series each is a different physiologic mediator

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3
Q

What do prostaglandins work on (PG2)?

A

G protein receptors

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4
Q

What are imposters of prostaglandins?

A

Long-chain fatty acids (less pro-inflammatory)

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5
Q

What is a normal substrate for prostaglandins?

A

C20:4 Omega-6 FA

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6
Q

What does constitutive mean?

A

Levels fluctuates very little

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7
Q

What does inducible mean?

A

A stimulus to increase levels

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8
Q

Is COX-1 inducible or constitutive?

A

Constitutive

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9
Q

Is COX-2 inducible or constitutive?

A

Both

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10
Q

Is COX-3 constitutive or inducible?

A

Constitutive

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11
Q

What is a byproduct of COX and what can it cause?

A

Superoxide, inflammation

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12
Q

Where do antipyresis drugs work on COX-1/2?

A

In the CNS

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13
Q

Where do analgesic drugs work on COX-1 and 2?

A

COX-1 peripheral

COX-2/3 central

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14
Q

Aspirin 3 doses and usage?

A

Antiplatelet 81 mg/day
Antipyresis 325-650 mg every 4-6 hrs
Anti-inflammatory 3.2-6.0 g/day

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15
Q

How does aspirin affect the cox enzymes?

A

Irreversibly acetylates and inactivates COX-1 and COX-2

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16
Q

Why do you not administer aspirin to children and neonates?

A

Reyes Syndrome: causes fatty liver and encephalopathy; uncouples oxidative phosphorylation

17
Q

When do you not administer aspirin?

A

Triad of nasal polyps asthma and aspirin allergy

18
Q

How does ibuprofen work?

A

Inhibits COX-1 and COX-2

19
Q

What is Indomethacin?

A

Very effective anti-inflammatory agent; short term use due to side effects (headache)

20
Q

What does naproxen inhibit?

A

COX-1 and COX-2 enzymes

21
Q

What can naproxen cause?

A

sudden death/MI in patients

22
Q

What is the most effective analgesic?

A

Ketorolac; pure COX-1 inhibition

23
Q

What are the side effects of ketorolac?

A

Major and significant risk for gastric injury; 5 day treatment course only

24
Q

What does Tylenol-acetaminophen do?

A

Inhibit COX-3; not anti-inflammatory toxic to liver

25
Q

What do non-selective COX inhibitors inhibit?

A

Thromboxane (COX-1 path) and Prostacyclin (COX-2 path)

26
Q

What does selective COX-2 inhibitor affect?

A

Prostacyclin formation but leaves thromboxane intact

27
Q

What does thromboxane cause in the GI tract?

A

Gastric mucin formation