Prostaglandins & Drugs

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  1. What are the 3 lipoxygenase enzymes and their major sites of action?
    5-lipoxygenase = white cells = leukotrienes (most important clinically)

    12-lipoxygenase = platlets

    15-lipoxygenase = macrophages & epithelial cells
  2. What is the path of leukotriene formation via 5-lipoxygenase? what do they collectively form? What is the physiologic manifestation?
    Arachodonic acid > 5-HPETE > LTA4 > LTB4

    or LTA4 > LTC4 > LTD4 > LTE4 (via LTC4 synthase)

    All these for slow-reacting substance (SRS) of anaphylaxis and cause bronchospams
  3. What are the leukotriene receptors and where are they found?
    • BTL: LTB4 in neutrophils, lung, spleen
    • cysTL1: LTD4 & LTE4 in smooth muscle especially in lung
    • cystTL2: LTC4 in endothelium & smooth muscle

    ALL activate PLC (phospholipase C)
  4. zileuton
    inhibits 5-lipoxygenase
  5. zafirlukast & monteleukast
    • cysTL1 blockers
    • once a day dosage
    • use for persistent asthma
  6. Aspirin
    • inhibits both COX 1 and 2
    • via acetylation
  7. Indomethacin & sulindac
    COX-1 inhibitor
  8. Ibuprofen & meclofenamate
    Cox 1 &2 inhibitor
  9. Nabumetone
    partially selective COX 2 inhibitor
  10. Celecoxib, Valdecoxib, Rofecoxib (vioxx)
    • selective COX 2 inhibitors
    • latter 2 were found to have increased risk of MI & stroke
  11. What is the pathway for prostaglandins?
  12. what is the prostaglandin pathway for vasculature?
  13. what is the prostaglandin pathway for asthma?
  14. what is the prostaglandin pathway for uterus?
  15. what is the prostaglandin pathway for gastric secretion?
  16. what is the prostaglandin pathway for platlets?
  17. Alprostadil
    • PGEI
    • treat peripheral vascular disease
    • keeps ductus arteriosus patent in infants
    • PGI along with PGE2 keep ductus open in fetus
  18. Indomethacin
    closes ductus (unknown how)
  19. Steroids
    • great for asthma
    • inhibits PLA-2
    • therefore inhibits the production of arachodonic acid
  20. Dinoprostone (PGE2) & carboprost
    • induce labor and abortions
    • works through PLC path
    • provide contractions
  21. Aspirin
    • reduce production of thromboxane A2 by platlet
    • this inhibits platlet aggregation

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Prostaglandins & Drugs
2011-09-21 03:04:58

Prostaglandin Drugs
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