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134 Cards in this Set
- Front
- Back
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What is the release of GnRH like?
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this is a pulsitile release
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What does GnRH stimulate?
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this stimulates the release of LH and FSH from the pituitary
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Where is GnRH released from?
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the hypothalamus
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What does tonic administration of GnRH cause?
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this downregulates GnRH receptors in the pituitary, and decreased gonadotropin release
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What is Gondorelin?
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this is a short acting GnRH agonist
used to stimulate FSH and LH production |
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What is Gondorelin given to treat?
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infertility
by pulsing Gondorelin this can induce ovulation in women with hypothalamic amenorrhea |
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What kind of drug is Leuprolide
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Long acting GnRH agonist
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What kind of drug is Goserelin
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Long acting GnRH agonist
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What kind of drug is Nafarelin
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Long acting GnRH agonist
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What does Leuprolide do?
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this causes an initial surge and then inhibition of gonadotropin release, by desensitizing the GnRH receptors
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What does goserelin do?
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this causes an initial surge and then inhibition of gonadotropin release, by desensitizing the GnRH receptors
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What does Nafarelin do?
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this causes an initial surge and then inhibition of gonadotropin release, by desensitizing the GnRH receptors
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How do long acting GnRH agonists affect postate cancer?
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reduces androgen production
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What two things are long acting GnRH agnosits like Leuoprolide used to treat?
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postate cancer
precocious puberty |
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What are the adverse effects in women of Leuprolide?
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Menopausal symptoms
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What are the adverse effects in men of Leuprolide
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Testicular atrophy
with postate tumors- may cause bone pain |
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How do you treat bone pain due to metastatic prostate tumors and Leuprolide?
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give an anti-androgen drug
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What is the contrainducation of Leuprolide use?
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Pregnancy/breast feeding
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What kind of drug is Cetrorelix?
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This is a GnRH antagonist
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What kind of drug is Ganirelix?
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GnRH antagonist
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What are the uses for GnRH antagonists Cetrorelix and Ganirelix?
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Suppresses LH and FSH, used in assisted reproductive technologies
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In the menstrual cycle, what suppresses FSH?
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increasing estrogen levels
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in the menstrual cycle, what suppresses LH?
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low levels of estrogen (negative feedback)
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In the menstrual cycle, how does estradiol affect LH secretion?
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high levels of estradiol enhance LH secretion, via a positive feedback
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What causes FSH release?
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GnRH
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What does FSH do in females?
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this causes development of ovarian follicles
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What does FSH do in men?
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stimulates spermatogenesis
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What is uFSH?
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this is a purified FSH preparation
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What is Follitropin alfa?
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this as recombinant FSH
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What is Menotropin?
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this is an FSH drug, but contains FSH and LH
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What causes LH secretion?
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GnRH
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What does LH do in women?
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required for progesterone synthesis in luteal cells
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What does LH do in men?
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causes testosterone synthesis in Leydig cells of testes
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What does human chorionic gonadotropin do?
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this is an LH agonist
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What does hCG do?
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this binds to LH receptor
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How is hCG's half life different than LH?
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it has a longer half life than LH
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What kind of drug is Lutropin?
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recombinant LH
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What are LH like drugs (hCG) used to treat in men?
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induce spermatogenesis, hCG is given to increase testosterone
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How long is the treatment of FSH (to stimulate spermatogenesis), after LH is given to increase testosterone production in men?
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many months
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What are is the typical order when givens FSH and LH?
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FSH is given first, and then hCG (or LH) in women
LH (hCG) then FSH in men |
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What are the main adverse effects of LH and FSH use?
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ovarian englargment, ovarian hyperstimulation syndrome
multiple births gynecomastia |
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What is the one bad adverse effect of LH and FSH?
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ovarian hyperstimulation syndrome
ovarian englargment, shock, hypovolemia, fluid in peritoneum |
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What regulates the production of estrogens in women?
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LH and FSH
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What regulates estrogen in pregnant women?
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fetal/placental unit
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What is estrogens effect on Ovaires
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prepares follicle cells for ovulation
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What is estrogens effect on uterus
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induces endometrial cell division and growth
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What is estrogens effect on puberty?
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this causes 2ndary female sex characteristics
and closing of epiphyses of long bones |
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What is estrogens effect on bone
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maintains bone mass
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What is estrogens effect on clotting
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synthesis of clotting proteins, increase in platelet adhesion
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What is estrogens effect on liver?
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causes synthesis of many liver proteins
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What is estrogens effect on blood fatty acid levels?
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increases HDL
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What do synthetic estrogens contain?
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Ethinyl Estradiol
Mestranol |
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What are Conjugated equine estrogens, synthetic conjugated estrogens, esterified estrogens, ans estropiapte in?
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these are conjugated estrogens used in hormone replacement therapy
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What is Diethylstillbestrol?
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this is a nonsteroidal estrogen with estrogenic activity
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What are synthetic estogens given for?
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primary hypogonadism
hormone replacement therapy oral contraceptives |
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how are the synthetic estrogens metabolized?
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heptaically
and undergo enterohepatic circulation* |
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What are the adverse effects of synthetic estrogens?
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migraine headaches
blood clots |
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What are the contrainducations of synthetic estrogen usage?
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estrogen dependent cancers
heart cancer clotting disorders |
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What is Tamoxifen?
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This is a Selective estrogen receptor modulator
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Where does Tamoxifen do what ?
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this is an agonist in uterus and bone
antagonist in breast |
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What does Tamoxifen treat?
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this is used to treat estrogen dependent breast cancer
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Does Tamoxifen treat hot flashes?
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no it does not
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What is the major adverse effect of Tamoxifen?
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increased risk of uterine cancer
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What is Toremifiene?
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this is selective estrogen receptor modulator, but it also increases HDL
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What is Raloxifene?
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this is a selective estrogen receptor modulator
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where does Raloxifene do what?
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this is an antagonist in breast and uterus (to reduce cancer odds)
and agonist in bone |
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What does Raloxifene treat?
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postmenopausal osteroporosis
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What kind of drug is Clomiphene?
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this is a SERM
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Where does Clomiphene do what?
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this is an antagonist in the hypothalamus
and agonist everywhere else |
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What does Clomiphene treat?
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this is used to stimulate LH and FSH secretion, by inhibiting negative feedback from estrogen
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What are the adverse effects of Clomiphene?
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multiple pregnancies
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What kind of drug is Fulvestrant?
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this is a pure estrogen receptor antagonist
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What kind of drug is Anastrozole?
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this is an aromatase inhibitor (prevents estrogen synthesis)
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What kind of drugs is letrozole?
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this is an aromatase inhibitor
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What kind of drug is Exemestane?
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this is an Irreversible aromatase inhibitor
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What are the uses of aromatase inhibitors like Anastrozole, Letrozole, and Exemestane?
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TX of breast cancer in postmenopausal women, or who's cancer has progressed while on tamoxifen (a selective estrogen receptor modulator, antagonistic in the breast)
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What are the side effects of Aromatase inhibitors?
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menopausal symptoms like hot flashes
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What causes progesterone synthesis?
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LH acting on the corpus luteum
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What is progesterones effect on uterus?
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turns uterus into secretory state, maintains pregnancy
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What is progesterones effect on endocervical glands?
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regulates cervix mucus composition (thick)
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What is progesterones effect on breasts?
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lobuloalveorlar development
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What is progesterones effect on body temp?
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this increases body temp
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What are the three Pregnanes?
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Progesterone
Medroxyprogesterone (provera) Meestrol acetate (megace) |
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What are the three Estranes?
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these are derived from testosterone
Norethindrone Norethindrone acetate Dienogest |
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What are the three Gonanes?
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Desogestrol
Norgestimate Norgestrel |
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What are Pregnanes, Estranes, and Gonanes used for?
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oral birth control
prevention of endometrial hyperplasia |
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What kind of drug is Mifepristone (RU 486)
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this blocks progestin binding to progesterone receptor
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What is Mifepristone used for?
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terminating pregnancy, because progesterones are required to maintain a pregnancy
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What kind of drug is Danazol?
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this is a weak progestin, androgen, and glucorticoid that suppresses ovarian function
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What is Danazol used to treat?
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endometriosis
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How do combination oral contraceptives affect ovulation?
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these inhibit ovulation, due to no LH surge
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How do combination oral contraceptives affect the endometirum and cervix?
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it causes decreased implantation
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What are the two most common forms of estrogen used in birth control pills?
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Ethinyl Estradiol or Mestranol
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What are the two most common progestins used in birth control pills?
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Levonorgestrel and norethindrone
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What is Drospirenone/Ethinyl Estradiol?
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this is Yaz
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What is special about Drospirenone/Ethinyl Estradiol?
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as this has a spironolacton (mineralcorticoid antagonist) it is FDA approved to reduce water retention and thus PMDD symptoms
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What are the progesterone only methods best used for?
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adolescents
this only decreases implantation |
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What are the common side effects of oral contraceptives?
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weight gain, nausea, edema, depression
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What are the cardiovascular complications of oral contraceptives?
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thromboembolic and blood clotting disroders- in women over 35 who smoke.
HTN MI |
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how long after stopping BC can it take for gonadotropins to return to normal levels?
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up to 3 months
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How do oral contraceptives affect cancer rates?
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these reduce the odds of endometrial and ovarian cancer by 50%
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What are the absolute contraindications for oral contraceptives
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thromboembolic disorders
estrogen dependent neoplasms |
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What are the relative contraindications of oral contraceptives
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Liver disease
adolesscents asthma migraines diabetes |
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What drugs interact with oral birth control?
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any that affect microsomal enzymes
(warfain, TCA's) |
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What are the main post menopausal problems that women have?
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Vasomotor- hot flashes
GU problems Osteoporosis (spinal compression fractures) Heart Disease |
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What are the main concernes of Hormone Replacement Therapy?
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Endometrial/Uterine cancer- (due to hyperplasia)
Breast cancer Gallbladder disease Clot formation |
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What MUST be given with estrogen only supplemention in menopause?
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MUST give progestins at the end of cycle to promote withdrawal bleeding- otherwise you get proliferation of endometrial tissue which causes cancer
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What HRT is given after a hysterectomy?
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Estrogen only- becasue you dont need to worry about proliferation
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Do you give HRT to girls who dont have ovary development?
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yes you do
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How does progesterone affect endometrial cancers?
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this produces remission in 1/3rd
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How does estrogen affect prostate cancer?
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this can cause remission in 50-80% of cases
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What is the rate limiting step of testosterone production, and what stimulates it?
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cholesterol to pregnenolone
stimulated by LH |
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Where in the body does 5alpha-reductase exist?
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this is in peripheral tissues
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What does 5alpha-reductase do?
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this turns testo into DHT
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What androgen has the best androgenic to anabolic ratio?
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Oxandrolone 1:13
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Why should androgens be avoided in the elderly?
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increased risk of prostate cancer
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Why should women be treated with androgens?
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female hypopituitarism
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What are the indications for treated both men and women with androgens?
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Tx of nephrosis
used in debilitated post op pts with negative nitrogen balance |
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What happens if you give pregnant women androgens?
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pseudohermaphroditism
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What happens to cholesterol levels in both sexes?
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decreases HDL, increases LDL
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How do estrogens treat prostate cancers?
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inhibit LH secretion
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What are long acting GnRH analogues and antagonists used for?
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treating precocious puberty and postate cancer
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What kind of hormones can Ketoconazole inhibit?
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androgen synthesis
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What kind of hormones does Spironolactone inhibit?*
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androgen synthesis- by inhibiting 17alpha hydroxylase activity
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What kind of drug is Flutamide?
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this is a androgen receptor antagonist
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What does Flutamide treat?
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prostate cancer
Topically- hirsutism/ baldness (prevents DHT formation) |
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What kind of drug s Bicalutamide?
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this is an androgen receptor antagonist
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What kind of drug is Nilutamide?
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this is a androgen receptor antagonist
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What kind of drug is Spironolactone?
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this is a mineralocorticoid antagonist- competes from androgen and estrogen receptors @ high doses
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What is spironolactone used to treat?
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hirsutism
precocious puberty |
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What kind of drug is Finasteride?
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a 5 alpha reductase inhibitor
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What kind of drug is Dutasteride?
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this is a 5 alpha reductase inhibitor
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What two things is Finasteride used to treat?
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BPH
male pattern baldness |
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What two things is Dutasteride used to treat?
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BPH
male pattern baldness |
