Estrogen and Progestin Inhibitors Flashcards
MOA of clomiphene
estrogen receptor partial agonist - blocks estrogen negative feedback
use of clomiphene
fertility drug
adverse effects of clomiphene
- multiple births
- hot flashes
- ovary enlargement
- blurry vision
fxnal consequences of SERM use
bone - suppress resoprtion
endometrium - proliferation
pituitary - hot flashes
breast - inhibit proliferation
Tamoxifen MOA
- agonist: bone
- partial agonist: endometrium
- antagonist: breast/HPG axis
what is Tamoxifen used for
ER+ Breast CA
adverse effects of tamoxifen
- hot flashes
- endometrial CA
- nausea, vomiting
what drugs are SERM
tamoxifen
raloxifene
MOA of raloxifene
agonist: bone
antagonist: breast/uterus/HPG axis
use for raloxifene
CA
postmenopausal bone loss
SE of raloxifene
- hot flashes
- N&V
what drug inhibit estrogen by inhibit gonadal function
danazol
what is danazol used for
- endometriosis
- breast fibrocystic disease
SE of danazol
- weight gain
- edema
- oily skin
- acne
- hirsutism
- hot flashes
danazol metabolite (ethisterone) has mild androgenic effects
which drug inhibits estrogen by inhibiting aromatase
anastrazole
letrozole
what is anastrazole and letrozole used for
breast cancer
SE of anastrazole and letrozole
- GI distrubance
- hot flashes
- lethargy
what drug is an antiprogesterone (progesterone receptor modulator)?
Abortifacient
e.g. Mifepristone
what drug is an antiprogesterone (progesterone receptor modulator) that acts as a partial agonist?
Emergency contraceptive
Ulipristal
dosing for mifepristone?
less than 7 weeks gestation:
1st dose of mifepristone
2nd dose of misoprostol 48 hours later
Ulipristal can be used as an emergency contraceptive up to ___ days after intercourse
5
MOA of antiprogesterones
- inhibit progesterone receptors
- uterine contractions
- lining of uterus is shed
- opens cervix
Anti-progesterones other potential clinical uses:
1: disrupt ovulation
Tx 2 and 3 cancer
Induce delivery after 4
induce 5 at end of 3rd trimester
- contraceptive
- breast
- endometrial
- fetal death
- labor