Estrogen and progestin inhibitors Flashcards
what is the MOA of clomephine?
PARTIAL AGONIST - blocks estrogen blocks / interrupts negative feedback
used to block negative effects
what is the therapeutic use of clomephine?
fertility drug
what are the main adverse effects of clomephine?
multiple births
hot flashes
if fertility issue is due to impaired gonadotropin release what can be used? what is the mechanism?
dose with clomephine during follicular phase - inhibit negative feedback
increase in LH and FSH
remove prior to day 14 - snaps pituitary back to positive feedback
what are SERMs?
selective estrogen receptor modulators
what is the effect of SERMs on bone?
suppress resorption
what is the effect of SERMs on endometrium?
proliferation
what is the effect of SERMs on the pituitary gland?
hot flashes
what is the effect of SERMs on breast tissue?
inhibit proliferation
what are the MOAs of tamoxifen on bone, endometrium, and breast/HPG axis?
bone - agonist
endometrium - partial agonist
breast/HPG axis - antagonist
what is the therapeutic use for tamoxifen?
ER positive breast cancer
what are the MOAs of raloxifene on bone and breast/uterus/HPG axis?
bone - agonist
breast/uterus/HPG axis - antagonist
what are the therapeutic uses for raloxifene?
cancer
postmenopausal bone loss
how do the side effects of tamoxifen differ from those of estrogen?
tamoxifen - increased hot flashes, decreased risk of breast cancer
what is the MOA of danazol?
inhibition of gonadal function through non-receptor based approach
what are the therapeutic uses for danazol?
endometriosis
breast fibrocystic disease
what are the adverse effects of danazol?
weight gain edema oily skin acne hirsutism hot flashes
what is the MOA of anastrazole?
aromatase inhibitor
what is the MOA of letrozole?
aromatase inhbitor
what is the therapeutic use for anastrazole and letrozole?
breast cancer
what are the adverse effects of anastrazole and letrozole?
GI
hot flashes
lethargy
what class of drug is mifepristone?
anti-progesterone (progesterone receptor modulator)
what is the MOA of mifepristone?
abortifacient antagonist of progesterone receptor
what class of drug is ulipristal?
anti-progesterone (progesterone receptor modulator)
what is the MOA of ulipristal?
antagonist of progesterone receptor
what is the clinical use of ulipristal?
emergency contraceptive up to 5 days after intercourse
what is the effect of progesterone on uterus smooth muscle?
decrease uterine contractions, decrease PG production
what is the effect of progesterone on the endometrium?
decrease uterine contractions
what is the general MOA for anti-progesterone (progesterone receptor modulator)?
- inhibit progesterone receptors
- uterine contractions
- lining of uterus is shed
- opens cervix
