Flashcards in Reproductive Pharmacology Deck (19):
GnRH analog that can be used as antagonist or agonist
Leuprolide (pulsatile--agonist, continuous--antagonist) downregulates GnRH receptor in pituitary --> decreased FSH/LH
Uses of leuprolide? Toxicities?
infertility (pulsatile), prostate cancer (continuous use with flutamide), uterine fibroids (continous), precocious puberty (continuous); Has anti-androgen effects
What are risks of estrogen use?
increased risk of endometrial cancer, bleeding in postmenopausal women, clear cell adenocarcinoma of vagina (DES exposure in utero), increased risk of thrombi
What are some SERMS?
clomiphene, tamoxifen, raloxifene
Antagonist at estrogen receptors in hypothalamus
Clomiphene; SERM that prevents normal feedback inhibition and increases release of LH and FSH from pituitary to stimulate ovulation; use to treat infertility due to anovulation (PCOS)
Antagonist of estrogen receptors at breast tissue
Tamoxifen; SERM that is also agonist at uterus/bone. Ass w/ endometrial cancer, thromboembolic events; Primarily used to treat ER+ breast cancer
Antagonist of estrogen receptors at uterus
Raloxifene: SERM that is agonist on bone also; increases risk of thromboembolic events; decrease resorption of bone-->used to treat osteoporosis
What are risks of unopposed estrogen therapy?
increased risk of endometrial cancer (thats why you add progesterone); possibly increased cardiovascular risk
aromatase inhibitors used in post-menopausal women with breast cancer (decrease conversion of androgens to estrogens)
bind progesterone receptors to decrease growth and increase vascularization of endometrium---used in OCPs and treatment of endometrial cancer, abnormal bleeding
competitive inhibitor of progestins at progresterone receptor--used to terminate pregnancy; administered with misoprostol (PGE1)
B2 agonist that relaxes the uterus, used to decrease contraction frequency in women during labor
synthetic androgen used in endometriosis and hereditary angioedema; androgen effects and decreased HDL levels/hepatotoxic
What effects to testosterone have on serum lipids?
Increase LDL and decrease HDL
5 alpha reductase inhibitor (blocks conversion of testoterone to DHT), used in BPH and promotes hair growth at the cost of gynecomastia and decreased sexual performance
competitive inhibitor of testosterone receptor used in Prostate Ca
Used in treatment of PCOS to prevent hirsutism
Ketoconazole (inhibits 17,20 desmolase; steroid synthesis), Spironolactone (inhibits steroid binding, 17 alpha hydroxylase, 17,20 desmolase); both cause gynecomastia and amenorrhea
alpha1 antagonist used to treat BPH by inhibiting smooth muscle contraction; selective for alpha1A,D receptors found only on prostate