Repro Pharm Flashcards
Leuprolide mech
GnRH analog
Agonist if pulsatile
antagonist if continuous (downregulates GnRH receptor in pituitary -> decreased FSH/LH -> low T/E in M/F
Leuprolide clinical use
Pulsatile - Infertility
Continuous - prostate cancer (+ flutamide), uterine fibroids, precocious puberty
Leuprolide tox
Antiandrogen, n/v
Methyltestosterone/testosterone mech.
Agonist at androgen receptors
Methyltestosterone use
Treats hypogonadism, promotes secondary sex characteristics, stimulation of anabolism to promote recovery after burn or injury
Methyltestosterone tox
masculinization in females, reduces intratesticular T in males by inhibiting release of LH (via negative feedback), gonadal atrophy, premature closure of epiphyseal plates, Increased LH, decreased HDL
Antiandrogens
Finasteride, Flutamide, Ketoconazole, Spironolactone
Finasteride
5a reductase inhibitor (decreased conversion of T to DHT). Useful in BPH. Also promotes hair growth (treats male pattern baldness (to treat use something that encourages female breast growth)). Side Effects: impotence, decreased sexual function, gynecomastia.
Flutamide
A nonsteroidal competitive inhibitor of androgens at the T receptor. Use - prostate cancer
Ketoconazole
Inhibits steroid synthesis (inhibits 17,20-desmolase)
Spironolactone
Inhibits steroid binding
Ketoconazole, Spironolactone
treat PCOS to prevent hirsutism. Side effects = gynecomastia & amenorrhea
Estrogens
ethinyl estradiol, DES, mestranol
Estrogen mech
Bind E receptors
Estrogens Use
Hypogonadism or ovarian failure, menstrual abnormalities, HRT in postmenopausal women; use in men with androgen dependent prostrate cancer.
Estrogen Tox
increased risk of endometrial cancer, bleeding in postmenopausal women, clear cell adenocarcinoma of vagina in females exposed to DES in utero, increased risk of thrombi