66: Estrogen & Progestin Inhibitors Flashcards
MOA and use of clomiphene
partial agonist to increase LH and FSH (block estrogen negative feedback) to induce ovulation
given during follicular phase
used as fertility drug
adverse effects clomiphene
- multiple births
- hot flashes
- ovary enlargement
- blurred vision
what is a partial agonist?
a drug that produces a lower max response as compared to the agonist (net response is lower than compared with natural - in this case less suppression via negative feedback)
SERMS selective estrogen receptor modulators
act differently in different tissue
bone =
endometrium =
pituitary =
breast =
bone = agonist
- suppress resorption
endometrium = partial agonist
- proliferation
pituitary and breast = antagonist
- hot flashes and inhibit proliferation
use tamoxifen
ER and breast CA
use raloxifene
CA
postmenopausal bone loss
adverse effects tamoxifen
hot flashes
endometrial CA
nausea/vomiting
adverse effects raloxifene
hot flashes
nausea/vomiting
SERMS (2)
tamoxifen
raloxifene
MOA danazole
inhibit gonadal functiion
use danazole
endometriosis
breast fibrocytic disease
adverse effects danazole
weight gain edema oily skin/ acne hirsutism hot flashes
MOA anastrozole and letrozole
aroamtase inhibitor
used to make estradiol
use anastrozole and letrozole
breast cancer
adverse effects are GI disturbances, hot flashes and lethargy
use mifepristone
abortion
antagonist MOA
less than 7 wks gestation : admin mifepristone then admin misoprostol 48 hrs later
