The Physiology and Pharmacology of Eicosanoids Flashcards
(27 cards)
What does phospholipase A2 do?
Cleaves Arachidonic acid from the cell membrane
What is derived from Arachidonic acid?
PG2 series each is a different physiologic mediator
What do prostaglandins work on (PG2)?
G protein receptors
What are imposters of prostaglandins?
Long-chain fatty acids (less pro-inflammatory)
What is a normal substrate for prostaglandins?
C20:4 Omega-6 FA
What does constitutive mean?
Levels fluctuates very little
What does inducible mean?
A stimulus to increase levels
Is COX-1 inducible or constitutive?
Constitutive
Is COX-2 inducible or constitutive?
Both
Is COX-3 constitutive or inducible?
Constitutive
What is a byproduct of COX and what can it cause?
Superoxide, inflammation
Where do antipyresis drugs work on COX-1/2?
In the CNS
Where do analgesic drugs work on COX-1 and 2?
COX-1 peripheral
COX-2/3 central
Aspirin 3 doses and usage?
Antiplatelet 81 mg/day
Antipyresis 325-650 mg every 4-6 hrs
Anti-inflammatory 3.2-6.0 g/day
How does aspirin affect the cox enzymes?
Irreversibly acetylates and inactivates COX-1 and COX-2
Why do you not administer aspirin to children and neonates?
Reyes Syndrome: causes fatty liver and encephalopathy; uncouples oxidative phosphorylation
When do you not administer aspirin?
Triad of nasal polyps asthma and aspirin allergy
How does ibuprofen work?
Inhibits COX-1 and COX-2
What is Indomethacin?
Very effective anti-inflammatory agent; short term use due to side effects (headache)
What does naproxen inhibit?
COX-1 and COX-2 enzymes
What can naproxen cause?
sudden death/MI in patients
What is the most effective analgesic?
Ketorolac; pure COX-1 inhibition
What are the side effects of ketorolac?
Major and significant risk for gastric injury; 5 day treatment course only
What does Tylenol-acetaminophen do?
Inhibit COX-3; not anti-inflammatory toxic to liver
