Reproductive Pharmacology (590-592) Flashcards
what is leuprolide
GnRH analog that acts as an agonist when pulsatile and an antagonist when continuous
what is leuprolide used to treat
infertility (given pulsatile); prostate cancer (continuous infusion with flutamide); uterine fibroids (continuous); precocious puberty (continuous)
what are the toxicities of leuprolide
antiandrogenic, nausea, vomiting
what are estrogens (ethinyl estradiol, diesthylstilbestrol and mestranol) used to treat
hypogonadism or ovarian failure, menstrual abnormalities, hormone replacement therapy in postmenopausal women, androgen-dependent prostate cancer
what are the toxicities of exogenous estrogens
increased risk of endometrial cancer, bleeding in postmenopausal women, DES in utero exposure causes vaginal clear cell adenocarcinoma, increased risk of thrombi, contraindicated in women with ER pos. breast cancer
name three selective estrogen receptor modulators (SERMs) and where they each work
clomiphene, tamoxifen and raloxifene
how/where does clomiphene work
estrogen receptor antagonist in hypothalamus; prevents feedback inhibition ==> increased LH and FSH
what is clomiphene used to treat
infertility due to anovulation (e.g. PCOS)
toxicities of clomiphene
hot flashes, multiple simultaneous pregnancies, ovarian enlargement, visual disturbances
how/where does tamoxifen work
estrogen receptor antagonist in breast tissues; estrogen receptor agonist in bone and uterus
what are the toxicities of tamoxifen
endometrial cancer, thromboemolism
what is tamoxifen used to treat
ER positive breast cancer
how/where does raloxifene work
estrogen receptor agonist in bone; estrogen receptor antagonist in uterus
what does raloxifene treat
treats osteoporosis by decreasing bone resorption
what is the toxicity associated with raloxifene
increased risk of thromboembolism
why is progesterone added to estrogen in hormone replacement therapy
unopposed estrogen causes
what are anastrozole and exemestane used for and what do they do
aromatase inhibitors used to treat postmenopausal women with breast cancer
how do progestins work
they bind progesterone receptors to decrease endometrial growth (by opposing estrogen) and increase vascularization of the endometrium
what are progestins used to treat
used in OCP’s, to treat endometrial cancer and to treat abnormal uterine bleeding
how does mifepristone (RU-486) work
competitive inhibitor of progestins and progesterone receptor
what is mifepristone used for
administered with misoprostol to terminate pregnancies
toxicities of mifepristone
heavy bleeding, nausea vomiting, anorexia, abdominal pain
how do oral contraceptives prevent ovulation
progestins and estrogens feedback negatively to decrease LH and FSH, preventing LH surge and thereby preventing ovulation
contraindications of oral contraceptives
smokers over the age of 35, history of thromboembolic disease or stroke, history of estrogen-dependent tumor
what is terbutaline and what does it do
beta-2 agonist that decreases frequency of uterine contractions during labor
what is danazol
synthetic androgen that acts as a partial agonist of androgen receptors (causes negative feedback on gonadotropins)
what is danazol used to treat
endometriosis and hereditary angioedema
what are the side effects of danazol
danazol has been largely replaced by leuprolide as a treatment for endometriosis because of side effects of weight gain, edema, acne, hirsutism, hepatotoxicity, decreased HDL, masculinization
what are testosterone and methyltestosterone used to treat
to treat secondary hypogonadism, stimulation of anabolism to promote recovery after burn or injury
