Estrogen and Progestin Inhibitors Flashcards
MOA Clomiphene
partial agonist
block estrogen via negative feedback
fertility drug
AE Clomiphene
multiple births, hot flashes, ovary enlargment
Actions of SERM
Bone - agonist - suppress resorption
Endometrium - partial agonist - promote proliferation
Pituitary - inhibition - hot flashes
Breast - inhibition - inhibit proliferation
SERMs
Tamoxifen
Raloxifene
MOA Tamoxifen
Used for ER positive breast cancer
Agonist - bone
Partial agonist - endometrium
Antagonist - breast/HPG
AE Tomxifen
Hot flashes (HPG) Endometrial cancer (endometrium)
MOA Raloxifene
Used in cancer and postmenopausal bone loss
Agonist - bone
Antagonist - breast/uterus/HPG
AE Raloxifene
hot flashes (HPG no endometrium partial agonist = no cancer
MOA Danazole
Inhibit gonadal function
Used for endometriosis and breast fibrocystic disease
Mild adrenergic effects
MOA Anastrozole/Letrozole
Aromatase inhibitors
Used in breast cancer
AE Anastrozole/Letrozole
hot flashes (low estrogen) lethargy
Anti-Progesterone drugs
Mifepristone
Ulipristal
MOA Mifepristone
Abortifacient
<7 weeks gestation: 1st mifepristone, 2nd misoprostol 48h later
Mifepristone - block progeterone receptor
Misoprostol - induce contractions
MOA Ulipristal
Emergency contraceptive
up to 5 day contraceptive post intercourse
Other uses for anti-progesterones
contraceptive, anti-cancer, induce delivery after fetal death