Chapter 76 - NSAIDS Flashcards
What are the products of the LOX cascades?
Leukotrienes, chemotactic factors
What are the products of the COX cascades?
Prostaglandins, thromboxanes, prostacyclin
What is the main COX enzymes involved in the production of inducible prostaglandins?
COX-2
Prostaglandins are required
for the normal function of which organs?
Brain, kidneys, GI, primary hemostatic system, reproductive system
Which NSAIDS is exclusively COX-1 inhibitor?
None, all of them have some degrees of dual-acting
Where has COX-3 been isolated in dogs?
Brain (inflammatory and pyretic effects identified)
What are COX-1-induced prostaglandins effects on the GI tract?
- Increase gastric mucous production
- Enhance local blood flow
- Play a role in gastric motility
What is the most common side effects of COX-2 selective NSAIDS?
Gastric ulceration (despite selectivity)
What pharmacologic properties of the drug promote the penetration of NSAIDS into gastric cells?
Weak acid -> more unionized form in acidic environment -> cross the membranes
Which COX enzymes mediate the prostaglandin and renin production/release by the juxtaglomerular apparatus?
Both COX-1 and COX-2 enzymes
How are NSAIDS metabolized in the liver?
By conjugation with glucuronic acid and glycin
How is idiosyncratic reaction to a drug defined?
Toxicity independent of the dose or duration of treatment
Which COX enzymes mediate the production of prostacyclin? Where is it produced? What are the effects of prostacyclin?
- COX-2
- Produced by epithelial cells
- Inhibits platelet aggregation and causes vasodilation
Which COX enzymes mediate the production of thromboxane A2? Where is it produced? What are the effects of thromboxane A2?
- COX-1
- Produced by platelets
- Increases platelet aggregation and causes vasoconstriction
How does aspirin affect platelet aggregation?
It reduces platelet aggregation by binding permanently thromboxane A2 and decreases its production by platelets
