pharma II test IV gonadal hormones

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pharma II test IV gonadal hormones
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2013-05-01 23:18:02
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pharma II test IV gonadal hormones
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  1. 3 GnRH antagonists (physiologic)
    • cetrorelix - cetrotide
    • ganirelix - antagon
    • abarelix - plenaxis
  2. inhin moa
    acts on the anterior piruitary gland to inhibit the release of FSH
  3. activin moa
    acts to stimulate the release of FSH
  4. where is aromatase synthesized
    ovary and placenta
  5. after menopause where does the majority of circulating estrogen come from
    • adipose tissue
    • a little comes from adrenal cortex
  6. common precursor to testosterone & estrogen synthesis
    antiproliferative effect on female endometrium
    promotes endometrial lining to secrete
    required for maintenance of pregnancy
    progestins
  7. general mechanisme of hormones
    • in the plasma progestins, androgens and estrogens bind to sex hormone binding globulin (SHBG) and albumin
    • the unbound fraction diffuses into cells and bind to the nuclear hormone receptor subfamily
  8. 3 main AE of estrogens
    • endometrial hyperplasia & carcinom
    • breast cancer
    • N/V
  9. 2 indications of estorgen postmenopausal therapy
    • hot flushes
    • sleep disturbances
  10. what do you need to watch out for with vaginal estrogens
    100% absorbed because they bypass first pass effect. watch for overdosing
  11. major progestin in humans and purpose
    • progesterone - acts prior to gestation to prepare the uterus for implantatoin of a fertilized ovum
    • T 1/2
  12. therapeutic uses of progestins
    • postmenopausal hormone therapy to counteract the AE's of estrogen
    • dysmenorrhea
    • endometriosis
  13. SERM
    used to treat estrogen (+) breast cancer
    AE - hot flushes, endometrial cancer
    tamoxifen - nolvadex
  14. SERM
    does not activate estrogen receptor in the endometrium
    ind - approved for osteoporosis
    raloxifene - evista
  15. anti-estrogen
    luteolytic property
    ind - abortificant
            emergency post-coital contraceptive
                  single dose 600mg
    miefpristone - RU486
  16. aromatase inhibitors 4
    ind - breast cancer
    precocious pregnancy
    • anastrozole
    • letrozole
    • fadrozole
    • exemestane
  17. aromatase inhibitor
    ind-treat breast cancer in tamoxifen resistant individuals
    moa - pure estrogen receptor antagonist
    fulvestrant - faslodex
  18. ovulation inducer
    moa - partial agonist at estrogen receptors
    AE - hot flushes, multiple pregnancy
    CI - enlarged ovaries
    clomiphene - clomid
  19. estrogen & progesterone
    ind - treats endometriosis, fibrocystic disease of the breast
    moa - suppress pituitary ovarian axis
    AE - weight gain, edema, decreased breast size, acne, hot flushes, changes in libido
    caution in hepatic disease
    danazol
  20. 3 layers of the prostate and makeup
    • glands or epithelial tissue
    •   androgen dependent - 25% of BPH
    • smooth muscle tissue - 75% of prostate
    •   a1-adrenergic receptors
    • capsule shell
    •   a1-adrenergic receptors
  21. 5a-reductase ihibitor
    moderately effective in reducing BPH <50g
    peak onset in 6 mo
    pregnancy catergory X
    AE - sexual dysfunction
    finasteride - propecia
  22. 5a-reductase inhibitor
    inhibits both type I & II
    faster and more complete decrease in DHT
    dutasteride - avodart
  23. antiandrogen
    receptor inhibitor
    used to treat prostatic carcinoma
    flutamide
  24. antiandrogen
    receptor inhibitor
    used to treat hirsutism
    • cyproterone
    • spironolactone - aldactone
  25. antiandrogen
    receptor inhibitor
    ind - prostate cancer
    • bicalutimide - casodex
    • nilutamide - nilandron

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