Flashcards in Sex Steroids Deck (11):
What are the uses of estrogens?
- most common in oral contraceptives
- second most common is postmenopausal hot flashes and baginal atrophy
- also used in replacement therapy for hypogonadism and osteoporosis
What are side effects of estrogen use?
- most common: nausea and breast tenderness
- endometrial hyperplasia, endometrial carcinoma, edema, weight gain, breast carcinoma, hyper pigmentation, thrombosis, myocardial infarction
Name estrogenic drugs
17 ethanol estradiol
Conjugated estrogens (Premarin)
What is a potential complication of diethylatilboesterol in pregnancy?
Has been associated with cervical and vaginal carcinoma in the daughters of women who took the drug during pregnancy
Name the drugs considered SERMS
SERMS: mixed agonist antagonists of estrogen
Tamoxifen - antagonist to estrogen receptors in breast, estrogen agonist in uterus and bone
Raloxifene (evista) - agonist activity in bone, antagonist activity in breast and endometrium (used to treat osteoporosis)
Clomiphene (clomid) - partial estrogen receptor agonist in hypothalamus. Stimulates ovulation - used to treat female infertility
Use and MOA of tamoxifen
Used to treat estrogen sensitive breast cancer in post-menopausal women. MOA: antagonist to estrogen receptors in the breast but agonist to receptors in bone and uterus. Prevents endogenous estrogens from stimulating tumor growth.
Use and MOA of raloxifene
Used to treat and prevent osteoporosis. MOA: has agonist activity in bone and antagonist in breast and endometrial tissue. Binds to estrogen receptors and induces expression of gene that maintains bone density.
Use and MOA of clomiphene
Used to treat female infertility by stimulating ovulation. MOA: partial estrogen receptor agonist in the hypothalamus. Interferes with the negative feedback mechanism by binding to estrogen receptors and makes hypothalamus sense a lack of estrogen. This results in release of more gonadotropins and GnRH which stimulate ovulation.
What are the uses and side effects of progesterone drugs?
Oral contraceptives, replacement therapy, treatment of dysfunctional uterine bleeding, dysmennorhea, and endometriosis
Side effects: weight gain, edema, depression, increased clotting (leading to possible thrombophlebitis or pulmonary embolism)
What is the use and MOA of mifepristone?
Works to terminate pregnancy by breaking down the uterine lining