PHRM 825 Exam 2 - Estrogens (drugs)

Estrogenic esters

estradiol valerate, estradiol cypoinate

esterification decreases solubility and slows the absorption

estradiol valerate, estradiol cypoinate

slow absorption from the injection site (depot) prolongs the action → less frequent injections

estrogenic esters

conjugates estrogens

estrone sulfate, equilin sulfate

non-steroidal estrogens

diethyl stilbestrol, chlorotrianisene

used in advanced prostate cancer, increased risk of vagina adenocarcinoma in women exposed in utero

diethyl stilbestrol

used to prevent miscarriage

diethyl stilbestrol

postpartum breast engorgement, menopause symptoms, prostate cancer

chlorotrianisene

partial estrogen agonist, prodrug

tamoxifen

antiestrogen actions: treat and prevent breast cancer

tamoxifen

estrogenic actions: increase risk of thromboembolic events, prevents osteoporosis

tamoxifen

SERM, treat advanced breast cancer

toremifene

SERM, estrogenic effects on the vaginal epithelium, treat dyspareunia (post-menopausal)

ospemifene

SERM, partial estrogen agonist

raloxifene, clomiphene

estrogen actions: prevents osteoporosis (postmenopausal), decrease LDL, increase risk of blood clot

raloxifene

antiestrogen actions: decrease risk of breast cancer, no endometrial cell stimulation, hot flashes

rolxifene

increases secretion of FSH and LH (no negative feedback of estradiol)

clomiphene

stimulates ovulation in women and PCOS

clomiphene

SERD, estrogen antagonist, treats bread cancer

fulvestrant

used if become resistant to tamoxifen

fulvestrant, aromatase inhibitors

aromatase inhibitors

anastrozole, letrozole, exemestane

block of biosynthesis of estrogens

aromatase inhibitors

ovulation induction, gynecomastia

aromatase inhibitors