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80 Cards in this Set
- Front
- Back
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what is the funciton of FSH
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stimulates gametogenesis, need with LH for proper ovarian sterogenesis
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what are FSH analogs used for?
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to treat hypogonadotropic hypogonadism (infertility), stimulate ovarian follicle development in women and spermatogenesis in men
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what is a side effect of FSH analog use?
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overstimulation and hyperstimulation - mutliple births, gynecomastia in men, ovarian enlargemnt, ascites, hypovolemia
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what are menotropins?
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purified FSH extract isolated from urine of menopausal women - contains little LH
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what is urofollitropin?
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pruified FSH extracted from the urine of menopausal women that contains almost no LH, more pure than menotropins
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what are follitropin alpha?
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recombinant FSH - produced in bacterial cells. Costs WAY more thanmenotropins
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what is the action of LH?
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responsible for regulation of gonadal steroid hormone produciton; males stimulates leydig cells to produce testosterone; females works with FSH to stumulate follicular development and produce progesterone and androgen by the corpus letuem
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what are the uses for LH?
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treat hypogonadotropic hypogonadism or as part of invitro fertilization
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what are the side effects of LH analogs?
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headache, depression, edema, precocious puberty, gynecomastia, autoAb against HCG - rare
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what are the preparations for LH?
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HCG - almost identical structure to LH; extracted and purifed from human placenta
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what are the metabolic effects of estrogen?
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increased bone mass due to decreased PTH activity- promotes death of osteoclasts and positively affects osteoblast funciton
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what are the side effects of exogenous estrogen?
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thromboembolic events - increased clotting factors, increase HTN, angina, MI; cancer - breat, endometrial and uterine
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what is the major side effect of diethylstilbestrol?
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vaginal tumors in the female offspring of women who were on it
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what is micronized estradiol?
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a preparation of estrogen for oral use
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what is the transdermal estradiol patch?
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a preparation of estrogen that releases estradiol over several days
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what is ethinyl estradiol and mestranol?
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17-substituted versions of estrogen that have improved oral bioavailability
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what are sulfate conjugated esters?
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conjugated ester isolated from pregnant mare's urine
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what should be given to all non-hysterectomized women in addition to exogenous estrogen?
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progestin - to protect the endometrium
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what kind of dose is given for hormone replacement therapy?
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smaller dose than for contraception
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what are the risks of HRT?
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increased incidence of breast cancer, HTN
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What is a major cause for noncompliance with SERMs?
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they can precipitate hotflashes
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what is clomiphene?
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anti-estrogen: weak estrogenic activity and intermediate antagonist activity
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what is the M.O. of clomiphene?
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inhibits normal feedback of estradiol on secretion of GnRH and LH/FSH - increases LH/FSH in the ovaries
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what is clomiphene used for?
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stimulation of ovulation due to increased LH/FSH levels
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what are the side effects of clomiphene?
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multiple births, flushing
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what is tamoxifen?
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Selective estrogen recetpor modifer (SERM)
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What is raloxifene?
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Selective estrogen recetpor modifer (SERM)
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what is termifene?
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Selective estrogen recetpor modifer (SERM)
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what is the M.O. of SERMs?
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compete with estradiol for estrogen receptor binding
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What is the action of SERMs?
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estrogenic effect that is more pronounced in bone; antiestrogenic effects that is more pronounced in breast
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what are the uses for SERMs?
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for estrogen dependent breast cancer and osteoporosis
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What are the side effects of SERMs?
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nausea, vomiting, hot flashes
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What is unique about tamoxifen?
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it has an increased risk of endometrial cancer
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what is fulvestrant?
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an estradiol analog that is a competitive inhibitor of the estrogen receptor - binding causes degradation of the receptor
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what is fulvestrant used for?
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estrogen dependent breast cancer - good alternative to SERMs if they have failed
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in what situation do you see a better outcome with anatrozole and letrozole than with SERMs?
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advanced breast cancer
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what is anatrozole?
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aromatse inihbitor
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what is letrozole?
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aromatse inihbitor
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what are anatrozole and letrozole used for?
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estrogen dependent breast cancer when SERMs have failed - better outcome for advanced breast cancer than seen with SERMs
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what are the side effects of fulvestrant?
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pain at the injection site (given IM - monthly), hot flashes, diarrhea
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what are the side effects of anatrozole and letrozole?
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hot flashes and diarrhea - but less than with SERMs
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what is the funciton of combination progestin and estrogen production for birth control?
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inhibit both FSH and LH = no ovulation; inhibit implantation and produce mucus secretion that is impermeable to sperm
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what are the preparations for combo progestin/estrogen for birth control?
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ethinyl estradiol with norgestrel, norethindrone, desogestrel or drospirenone
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what is the action of progestin only birth control?
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thinned endometrium and thicker mucus - DOSEN'T consistantly inhibit ovulation = high failure rate
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what is progestin only birth control called?
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mini pills
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what is plan B?
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post coital contraceptive - high dose progestin given 2 days in 2 doses separated by 12 hours, must be given within 72 hours!!
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What is DES used for?
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post coital contraceptive - high dose synthetic estrogen; not used much
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what is the goal of multiphase birth control?
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to decreased overall dose of progestin and estrogen
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what are the adverse effects of birth control?
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nausea, diarrhea, exacerbation of acne and hirsuitism, breakthrough bleeding
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what is out of whack if there is breakthrough bleeding during the first 1- 9 days of the cycle?
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estrogen dose is insufficient
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what is out of whack if there is breakthrough bleeding during days 10-12 of the cycle?
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progestin dose is insufficient
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what are the major complications of birth control?
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thromboembolic events, small increase in BP, cancer - breast, endometrial, uterine, migranes
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what are the health benefits of birth control?
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improved cycle regularity, decreased bleeding, decreased dymenorrhea, decreased incidence of ovarian cancer and PID, increased bone density mass
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what is milfepristone?
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anti-progestin - receptor antagonist
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what is milfepristone used for?
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post -coital contraceptive through the first 49 days of pregnancy - only available directly in clinic
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what is metabolism of milfepristone?
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highly plasma protein bound, metabolized by the liver - P450s
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what are the side effects of milfepristone?
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cramping, nausea, vomiting, diarrhea, dizziness
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what is the major endogenous androgen?
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testosterone
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what is dihydrotestosterone?
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active metabolite of testosterone, formed by 5-reductase
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what is produced by the cyclization (aromatization) of testosterone?
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estradiol
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what are the maturational effects of testosterone?
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penile and scrotal growth, secondary sex characteristics, male pattern baldness (mainly DHT), oily skin, thickiening of vocal cords
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what are the anabolic effects of teststorone?
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promote body growth in both sexes, increase protein syntehsis, decreas protein breakdown, incrases RBC produciton but stimulating EPO
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what are the adverse effects of exogenous testosterone?
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masculinization, feminization (paradoxical in men), edema due to mineralocorticoid effects, hepatoxicity - increased risk of hepatic tumors, aggressiveness
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what is testosterone used for?
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replacement therapy - testicular failure - started at puberty. If started eariler can close long bones; impotense in hypogonadal males; ovarian suppression, hereditary angioneurotic edema
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what is danazol used for?
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ovarian suppression due to its weak androgenic activity and for endometriosis due to its suppresssion of LH and FSH
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Wha are 17 substituted androgens used for?
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hereditary angioneurotic edema - increases the expression o fthe inhibitors that are lost in the complement cascade due to the disease
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what is testosterone cypionate?
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preparation of testosterone that is an ester = concentrates in fate and releases over prolonged time
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what is testosterone enanthate?
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preparation of testosterone that is an ester = concentrates in fate and releases over prolonged time
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what is testosterone transdermal system?
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patch placed on scrotum - CAN IRRITATE SCROTUM!!!!!!!
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what is methyltestosterone?
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17 substituted androgen - orally active
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what is fluoxymesterone?
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17 substituted androgen - orally active
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what is the adverse effect of 17 substituted androgens?
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higher incidence of hepatoxocitiy and chance of liver failure
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what is cyproterone?
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strong anti androgen, weak progestinal activity
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what is crypterone used for?
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to treat hirsuitisum
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what are flutamide, bicalutamide and nilutamide?
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competitive inhibitors of testosterone and DTH receptors
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what are flutamide, bicalutamide and nilutamide used for?
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prostate cancer
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what are the side effects of flutamide, bicalutamide and niutamide?
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hot flashes, decreased libido and impotence
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what is finasteride?
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competitive inhibitor of 5alpha reductase
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what is finasteride used for?
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BPH and male pattern baldness, used off label as prostate cancer prophylaxis
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what are the side effects of finasteride?
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decreased libido and impotence
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