The Physiology and Pharmacology of Eicosanoids Flashcards
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
