Sex hormone pharmacology

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  1. Parent steroid of estrogens; androgens; proestins; mineralcorticoids; and glucocorticoids
  2. Form of estrogen produced in ovaries. Stronger or weaker?
    E2; estradiol stronger
  3. Form of estrogen produced in adipose tissue. Stronger or weaker?
    E1; estrone weaker
  4. Receptor responsible for estrogen mediated cell signaling.
    Estrogen response element
  5. Another level of regulation of estrogen; tamoxifen is an example of this.
    Selective Estrogen receptor modifier
  6. Enzyme important in synthesis of dihydrotestosterone
    5 alpha reductase
  7. Effect of circulating estrogen levels on LH and FSH
  8. Estrogen preparations 4 types
    conjugated equine estrogens; ethinyl estradio; transdermal estradiol; estradio cypionate/valerate
  9. isolated from pregnant mares; for HRT
    conjugated equine estrogens (premarin and prempro)
  10. oral contraceptives; modification makes it orally active
    ethinyl estradiol
  11. HRT contraception; patch
    transdermal estradiol
  12. intramuscular HRT for estrogen
    estradio cypionate and valerate
  13. metabolism of estrogen
    hepatic; inducers of CYP450 increase elimination
  14. enterohepatic cycling
    conjugated estrogens excretedinto bile; reconstitued by bacteria; and reabsorbed by the GI
  15. uses of estrogen/estrogen preparations
    HRT post ovisectomy and postmenopausal; contracption; acne; dysmenorrhea; endometriosis
  16. progestin preparations
    progesterone esters; synthetic analogues (norgestrel; levonorgestrel; norethindrone; desogestrel); drospirenone
  17. use for intramuscular injectsion in Depo-provera and HRT
    Medroxyprogesterone acetate
  18. Used in combination contraceptive and postcoital contraceptive; high androgenic activity
    Norgestrel and levorgestrel (poscoital); high androgenic activity
  19. Used in combination contraceptive and postcoital contraceptive; moderate androgenic activity
  20. Used in combination contraceptive and postcoital contraceptive; lowest androgenic activity; but not used because of this side effect
    desogestrel; dvt
  21. Use in some oral contraceptives; has both antialdosterone and antiandrogenic effects
  22. Uses of progesterone
    dysmenorrhea; endometriosis; uterine bleeding; oral contraceptives; HRT to decrease endometrial cancer
  23. MOA of oral contraceptives
    1. inhibit LH surge at the pituitary 2. endometrial atrasia 3. increase thickness of cervical mucus (progesterone)
  24. Components of oral contraceptives
    ethinyl estradio and progesterone analogue
  25. How triphasic compare to di and mono phasic preparations
    Estrogen remains the same; progesterone levels increase incrimentally. Less hormone exposurein triphasic preparations.
  26. Monophasic therapies; durgs and dosages.
    Contains EE and drospirenone. Drugs: Yasmin and Yaz. Anti aldosterone and antil-androgen due to drospirenone.
  27. What are the extened time pills
    Lybrel (1 year); seasonale (84 days + 7days free); seasonique (84 days + 7 day of EE)
  28. Common side effects of contraceptive use
    N/V weight gain; breast tenderness; edema. Breast cancer; gall stones; serum binding protein elevated; increases coagulation (infarction; DVT; stroke)
  29. Adverse effects of contraceptive use
    Hirsutism; glucose intolerance; HDL decrease and IDL increase; depression
  30. 4 general Contra indications to contraceptive use
    Breast cancer/liver tumor; DVT/PE/CVA/IHD; smokers >35; <6wks postpartum and breast feeding
  31. Formulation (2) and use for progestin only contraception
    Norgestrel and norethindrone; prenant women where estrogen is contraindicated
  32. Three options of morning after contraception.
    Levonorgestrel (plan B); ulipristal acetate (progesteron receptor modulator); IUD inseration.
  33. Three non-oral contraceptives
    Injection (lunelle); vaginal ring (nuva ring); contraceptive patch (ortho Evera)
  34. Three non-oral progesteron only
    IUD (levonorgestrel); implant (etonorgestrel); IM injection of medroxyprogesterone acetate
  35. Estrogen sx associated with menopause
    osteoporosis; vasomotor sx; urogenital atrophy; vaginitis
  36. Selective estrogen receptor modulator for treating osteoperosis
    Raloxifene; antagonist in uterus and breast; agonist in bone and lipid (decreases LDL).
  37. Regiments available for estrogen replacement therapy
    cyclic therapy (estrogen then methylprogesterone) and continuous (conjugated estrogen and medroxyprogesterone)
  38. Conclusion on HRT
    Risks outweigh benifits.
  39. Two drugs that acts on hypo pituitary axis to decrease LH surge
    Luprolide (GnRH agonist; downregulates GnRH receptors) and Ganirelix (GnRH receptor antagonist)
  40. FSH and LH analogues
    Urofollitropin (FSH); placental hCG (LH); menotropins (hMG->FSH&LH). Ovarian hyperstimulation syndrome.
  41. DopaR agonist; treat hyper prolactinemia and parkinson's
  42. Three androgen preparations
    testosterone; metyltestosterone; oxandrolone and nandrolone
  43. Uses of androgen preparation
    hypogonadism; revers protein loss in trauma; buff up
  44. Adverse effects of androgen use
    masculination; acne; sleep apnea; erythrocytosis; gynecomastia; azoospermia; lower HDL; increase aggressivness; hepatic enzyme elevation
  45. anti androgens (4)
    finasteride; flutamide; spironolactone; ketoconazole
  46. androgen receptor antagonists
    fluamide and spironolactone (also aldosterone antagonist)
  47. MOA of ketoconazole; uses
    decreases androgen prouction; also antifungal drug
  48. selective estrogen recptor modulators (4)
    tamoxifen; toremifene; raloxifene; clomiphene
  49. antagonis at breast; agonist at endometrium; treat breast cancer; worry about endometrial cancer
    Mechanism of action and use of tamoxifen and toremifene
  50. agonist at bone antagonist in breast and endometrial cancer
    raloxifene MOA and uses
  51. stimulate ovulation; inihibit negative feed back of LH/FSH at hypo and stimulates GnRH release
    clomiphene MOA and uses
  52. decreases estrogen synthesis (3)
    Danazole letrozole anastrozole
  53. decrease estrogen receptors (sequesteres it)
  54. competative progesterone antagonist; uses?
    mifeprestone (induce abortion)
  55. non-steroidal estrogen; not used much
Card Set:
Sex hormone pharmacology
2012-12-15 17:21:10

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