Prostaglandins

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jgh7471
ID:
11033
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Prostaglandins
Updated:
2010-03-17 20:47:51
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Prostaglandins
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Prostaglandins Review
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  1. most abundant precursor to eicosanoids
    arachidonic acid

    found in membrane phospholipids
  2. what does 5,8,11,14- eicosatetraenoic acid lead to
    • 2 series prostaglandins
    • 4 series leukotrienes

    source: diet
  3. what does 5,8,11,14,17 eicosapentaenoic acid lead to
    5 series leukotrienes

    source: fish oils
  4. what does 8,11,14 eicosatrienoic acid lead to
    1 series prostaglandins

    source:
  5. meaning of the "letter" in naming prostaglandins and thromboxanes
    cyclopentane or oxetane ring substituents
  6. meaning of the "number" in maning prostaglandins and thromboxanes
    the number of double bonds on side chains
  7. meaning of "letters" in naming leukotrienes
    refer to adducts to arachidonic acid
  8. meaning of "numbers" in naming leukotrienes
    refer to number of double bonds in fatty acid
  9. most common prostaglandins
    1 and 2 series

    2 series more prevalent in most tissues
  10. in what tissues are prostaglandins stored
    they are not stored in tissues; their precursors are stored in nearly every tissue in the body
  11. the one tissue that does not store prostaglandins
    red blood cells
  12. tissues have different profiles of arachidonic acid metabolites
    true
  13. first step in synthesis of prostaglandins
    activation of phospholipase A2

    this cleaves arachidonic acid from esterified form in the cell membrane
  14. what converts prostaglandin H2 to thromboxane A2
    thromboxane synthase
  15. what converts prostaglandin H2 to prostaglandin I2
    prostacyclin synthase
  16. organ that rapidly degrades PGE and PGF
    lung

    PGE and PGF lose over 90% of activity after one pass through lung
  17. role of PGE2 and PGI2 in CV system
    vasodilators
  18. role of TXA2 in CV system
    vasoconstrictor
  19. role of PGI2 on platelets
    antiaggretory
  20. role of TXA2 on platelets
    proaggretory
  21. role of PGE and PGF 2alpha on uterine smooth muscle
    increase tone during pregnancy
  22. role of PGE on GI secretions
    inhibits gastric acid secretion

    stimulates mucus secretion (cytoprotective role)
  23. role of PGE2 and PGI2 in kidney
    • increase renal blood flow
    • - diuresis, natriuresis, kaliuresis
  24. role of TXA2 in kidney
    • decreases renal blood flow
    • decreases GFR (glomerular filtration rate)
  25. role of PGE2 and PGI2 on afferent neurons
    hyperalgesia (potentiate pain response)
  26. role of prostaglandins on the immune system
    modulate leukocyte activity (production of interleukins, adhesion molecules, TNF)
  27. role of prostaglandins in thrombosis
    a balance between PGI 2 and TXA2
  28. prostaglandins participating in parturition
    PGF2alpha, PGE2
  29. prostaglandins that regulate bronchial smooth muscle
    PGF2alpha, TXA2
  30. prostaglandins that regulate renal blood flow and salt excretion
    PGI2 and PGE2
  31. prostaglandins important for inflammation and immunity
    PGE2 and PGE1
  32. Alprostadil (PGE1)
    maintain patency of ductus arteriosus (countered by indomethacin to close ductus arteriosus)

    tx erectile dysfunction
  33. misoprostol (PGE1) indications
    prevent NSAID induced ulcers

    prevent renal transplant rejection

    used with RU-486 or methotrexate to terminate pregnancy
  34. misoprostol mechanism of action
    decrease gastric acid production

    immunosuppressive

    contracts pregnant uterus
  35. misoprostol side effects
    uterine contraction (contraindicated in pregnancy)
  36. dinoprostone
    leads to labor (ripening and dilation of the cervix)
  37. lubiprostone
    used for chronic constipation

    activates chloride channels (increases Cl into intestine lumen, Na and water follows)
  38. what synthesizes leukotrienes
    leukocytes
  39. effects of LTC4, LTD4, LTE4 (all leukotrienes)
    potent vasoconstrictors

    proinflammatory

    • bronchoconstrictors (involved with asthma)
    • -involved with Adult Respiratory Distress Syndrome (ARDS)
  40. zafirlukast and montelukast effects
    antagonize LTC4, LTD4, LTE4

    cys-LT1 receptor antagonists
  41. zafirlukast and montelukast uses
    • relax bronchiole smooth muscle in asthma pt
    • -not for acute asthma attack, the effects take about a week
    • decrease daytime asthma Sx
    • decrease nighttime awakening from asthma

    both completely metabolized by the liver CYP450 enzymes
  42. zafirlukast drug interactions
    warfarin
  43. montelukast drug interactions
    does not inhibit CYP 450 liver enzymes
  44. zileuton pharmacology
    5-lipoxygenase inhibitor

    leads to relaxation of bronchial smooth muscles
  45. zileuton uses
    Tx mild to moderate asthma

    rapidly absorbed

    half life of 2.5 hrs

    metabolized by liver P450 enzymes
  46. zileuton drug interactions
    increases serum concentrations of warfarin and theophylline

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