Quiz 9 (and exam 4)

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Quiz 9 (and exam 4)
2012-04-17 02:04:34
Med Chem

SEX!!! (slides 1-41)
Show Answers:

  1. What is the starter molecule for all sex hormones?
  2. Primary male hormone?
  3. Primary female hormone?
  4. What enzyme converts testosterone to estradiol?
  5. This is a decapeptide released by the hypothalamus to stimulate the anterior pituitary gland to release LH and FSH?
  6. These are peptides that are closely related to estrogens, progesterone, and testosterone?
  7. _____ levels cause release of an ovum and development of follicular tissue into the CL and then progesterone secretion begins.
  8. What stimulates the development of ovarian follicles?
    LH and FSH
  9. How do we inhibit ovulation?
    increase estrogen and progesterone so that (-) feedback will decrease FSH and LH
  10. During pregnancy, this steroid maintains the CL and estrogen and progesterone production which prevents ovulation and menstruation?
  11. What can we use GnRH agonists for?
    • inducing ovulation
    • endometriosis
    • shrinking uterine fibroids
    • controlling excessive bleeding
    • precocious puberty
    • prostate cancer
    • testicular descent
  12. Non-standardized "bioidentical" steroid hormones?
    • yams
    • soy
  13. What is 17-beta-Estradiol converted to in the liver?
  14. What is estrone converted to in the liver?
  15. Which form of estradiol is excreted in the urine?
  16. Which two forms of estrogen are in equilibrium in the body and can be converted back and forth?
    17 Beta Estradiol and Estrone
  17. Transdermal Estradiol spray?
  18. Name the estradiol patches.
    • Climara
    • Vivelle
    • Fempatch
    • Alora
  19. Delestrogen generic name?
    estradiol valerate in oil
  20. DepoGen generic name?
    estradiol cypionate in oil
  21. What are the 2 prodrugs for injection as depot agents?
    • Estradiol valerate (Delestrogen)
    • Estradiol cypionate (DepoGen)
  22. This blocks the oxidation of the C17 beta hydroxyl group to a ketone which is a major pathway of metabolic inactivation? (keeps drugs from undergoing 1st pass, so we keep plasma levels high)
    ethinyl group (acetylene): triple bonded hydrogen
  23. Equine derived estrogen
  24. Non-steroidal estrogen that has had some controversy?
    Diethylstilbesterol derivatives
  25. Ethinyl estradiol
  26. What is Estinyl indicated for?
    • vasomotor symptoms of menopause
    • primary ovarian dysfunction
    • female castration
    • breast cancer
    • prostate cancer
    • atrophic vaginitis
    • female hypogonadism
  27. What is the advantage of HRT?
    helps prevent cardiovascular disease
  28. This is a non-steroidal estrogen that still has estrogenic activity?
  29. This drug is contraindicated in women of child bearing age due to risk of causing clear cell adenocarcinoma (CCA) of the vagina?
  30. What was DES historically prescribed for?
    preventing miscarriage
  31. This is a fairly new synthetic mixture of 10 different estrogens?
  32. This synthetic conjugated estrogen is indicated for menopause only?
  33. This drug is on the FDA safety monitoring list for possibly causing angioedema?
  34. This conjugated estrogen is indicated for treating menopause and osteoporosis?
  35. Name the 2 esterified estrogens indicated for treating osteoporosis?
    • Menest
    • Estratab
  36. Name the 2 estropipate salt estrogens used to treat osteoporosis?
    • Ortho-Est
    • Ogen
  37. What are the only 2 estrogens that are used in OCs?
    • Mestranol
    • Ethinyl Estradiol
  38. T/F: Progestin pill or mini pills have a slightly higher failure rate.
  39. Why do the progestin only pills (mini pills) have a higher failure rate?
    b/c they don't contain any estrogen (mestranol or ethinyl estradiol)
  40. Who should/can use the progestin-only pill (mini pill)?
    • women who are BF
    • hypertensive
    • family hx of breast cancer
    • smokers older than 35
  41. T/F: estrogens can cause blood clots and salt retention.
  42. Name the 2 SERMs.
    • Evista
    • Faslodex
  43. This SERM is not effective in treating hot flashes?
  44. this SERM is indicated for treating osteoporosis in pm women?
  45. This SERM can cause blood clotting problems, can cause hepatic failure and is metabolized by 3A4?
  46. This drug is an estrogen receptor antagonist that lacks estrogen activity in the breast and uterus, reduces bone resorption and turnover, and increases bone mineral density?
  47. What is Faslodex indicated for?
    txt of hormone receptor positive metastatic breast cancer in pm women w/ disease progression even after antiestrogen therapy
  48. This drug is administered once a month, has a half life of 40 days, is highly protein bound, and is met by 3A4?
  49. If a woman wants to take Faslodex, what precaution should she use?
    extra protection, but not oral (needs to be a barrier)
  50. This is a very greasy molecule that contains fluorine and could be toxic? (SERM)
  51. This is an estrogen receptor antagonist w/ equal binding to that of estradiol and this results in a DOWN regulation of estrogen receptors in breast cancer cells?
  52. This drug is a reversible inhibitor of the growth of tamoxifen-resistant cell lines?
  53. What is MegAce indicated for?
    AIDS wasting syndrome
  54. What is progestin and its analogs indicated for?
    • amenorrhea
    • abnormal uterine bleeding
    • endometriosis
    • infertility
    • AIDS wasting syndrome
  55. This is the primary endogenous substance of the CL?
  56. This promotes follicular maturation and ovulation, inhibits spontaneous uterine contractions, maintains pregnancy, increases the receptivity of embryo implantation, and makes the endometrium secretory?
  57. Which undergoes more enterohepatic recirculation, estrogen or progesterone?
  58. Too much Progestin = ?
    • increased appetite
    • weight gain
    • fatigue
    • hypomenorrhea
  59. Not enough progestin = ?
    • breakthrough bleeding
    • amenorrhea
    • hypermenorrhea
  60. When can you not take progestins?
    • impaired liver fxn
    • breast or prostate cancer
    • thromboembolic disease
  61. Diabetics should closely monitor glucose levels when taking what steroid?
  62. What is Crinone vaginal gel (ART) used for?
  63. This is an IU contraceptive device w/ barium sulfate and silicone oil?
  64. What is Prometrium used for?
    • amenorrhea
    • uterine bleeding
  65. Take this steroid hormone with food if upsets stomach?
  66. This progestin is good for the elderly, bulimic, anorexic, and patients with AIDS cachexia b/c it stimulates appetite?
  67. This drug is used for palliative txt of advanced breast or endometrial cancer or as an appetite stimulant in certain populations?
  68. Makena is an injection for what indication?
    preventing preterm birth (it slows down contractions)
  69. What are the 2 brand names of the progestin 17alpha-Hydroxyprogesterone Caproate?
    • Hylutin
    • Makena
  70. Hylutin is used for?
    • primary and secondary amenorrhea
    • dysfunctional uterine bleeding
  71. What is medroxyprogesterone acetate used for?
    • secondary amenorrhea
    • abnormal uterine bleeding due to hormone inmbalance
    • contraception
    • chemical castration in men who are creeps
  72. What are Prempro, Premphase and Combipatch used for?
    • treat moderate to severe vasomotor symptoms of menopause
    • vaginal atrophy
    • prevent osteoporosis
  73. Name the 3 combo products of estrogen + progestin.
    • Combipatch
    • Prempro
    • Premphase
  74. Where does the progestin starting material come from?
    mexican yam
  75. name the progestins used in birth control pills.
    • Norethidrone acetate
    • Norethidrone
    • Aygestin (also treats amenorrhea)
    • Norethynodrel
    • Norgesterel
    • Norgestimate
    • Levonorgestrel
    • Desogestrel
    • Etonogestrel
    • Ethynodiol Diacetate
  76. What is the newest moleculare entity progestin used as birth control w/ possibly less side effects?
  77. What are the monophasic OCs?
    • all tablets contain same amount of estrogen and progestins
    • could see breakthrough bleeding halfway through cycle
  78. What are the biphasic OCs?
    7-10 days one dose, then remainder of cycle gets a double dose of the progestin
  79. What is the triphasic OC?
    dose of progestin is increased in 3 phases over course of cycle while estrogen dose stays the same
  80. Do OCs cause an increase or a decrease in anticoagulation?
    both, depends on patient
  81. name the 2 progestin only (mini pills)
    • Micronor/ Nor QD (norethindrone only)
    • Ovrette (norgestrel only)
  82. What is the only OC approved by FDA to treat acne in women 15 or older?
    Ortho-tri cyclen
  83. This is an OC that is levonorgestrel and is 6 Silastic capsules that contain drug shot into the forearm?
  84. This implant OC can last up to 5 years, but eventually need to be surgically removed?
  85. This OC is an NME implant?
  86. Etonogestrel
  87. This is a 99% effective rod implant that is good for 3 years, is made of a biodegradable polymer inserted subdermally on upper arm?
  88. Name the 3 IUDs.
    • Progestasert
    • Mirena
    • NuvaRing
  89. Name the 2 IM depot OCs.
    • Depo-Provera
    • Lunelle
  90. T-shaped insert good for 1 year, contains 38 mg of progesterone and barium sulfate dispersed in silicone oil for slow release?
  91. T-shaped insert good for less than 5 years, contains 52 mg of levonorgestrel covered by a silicone membrane?
  92. A vaginal ring containing etonogestrel and ethinyl estradiol (progest and estrogen) that is new as of '06?
  93. Inject this drug IM once a month. contains medroxy and estradiol cypionate?
  94. Inject this drug IM every 3 months. contains only medroxy?
  95. Use this up to 5 days after an accident? Not an abortifactant.
  96. First skin patch for birth control?
  97. Spearmint flavored chewable tablet OC?
    Femcon FE
  98. Analog of spironolactone?
    Drospirenone (Yasmin)
  99. 91 day regimen OC, recommend a preg test once a month if using?
  100. Newest continuous OC that prevents menstruation?
  101. New postmenopausal product that might control hyperlipidemia and hot flashes?
  102. New 4-phasic OC that might mimic mother nature better?
  103. What can be used to treat female sexual dysfunction?
    • wellbutrin
    • ED drugs
    • alprostadil
    • estrogens
    • testosterone
    • apomorphine
    • moisturizers & lubes