Estrogen and progestin inhibitors

Question 1

what is the MOA of clomephine?

Answer 1

PARTIAL AGONIST - blocks estrogen blocks / interrupts negative feedback

used to block negative effects

Question 2

what is the therapeutic use of clomephine?

Answer 2

fertility drug

Question 3

what are the main adverse effects of clomephine?

Answer 3

multiple births

hot flashes

Question 4

if fertility issue is due to impaired gonadotropin release what can be used? what is the mechanism?

Answer 4

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

Question 5

what are SERMs?

Answer 5

selective estrogen receptor modulators

Question 6

what is the effect of SERMs on bone?

Answer 6

suppress resorption

Question 7

what is the effect of SERMs on endometrium?

Answer 7

proliferation

Question 8

what is the effect of SERMs on the pituitary gland?

Answer 8

hot flashes

Question 9

what is the effect of SERMs on breast tissue?

Answer 9

inhibit proliferation

Question 10

what are the MOAs of tamoxifen on bone, endometrium, and breast/HPG axis?

Answer 10

bone - agonist
endometrium - partial agonist
breast/HPG axis - antagonist

Question 11

what is the therapeutic use for tamoxifen?

Answer 11

ER positive breast cancer

Question 12

what are the MOAs of raloxifene on bone and breast/uterus/HPG axis?

Answer 12

bone - agonist

breast/uterus/HPG axis - antagonist

Question 13

what are the therapeutic uses for raloxifene?

Answer 13

cancer

postmenopausal bone loss

Question 14

how do the side effects of tamoxifen differ from those of estrogen?

Answer 14

tamoxifen - increased hot flashes, decreased risk of breast cancer

Question 15

what is the MOA of danazol?

Answer 15

inhibition of gonadal function through non-receptor based approach

Question 16

what are the therapeutic uses for danazol?

Answer 16

endometriosis

breast fibrocystic disease

Question 17

what are the adverse effects of danazol?

Answer 17

weight gain 
edema 
oily skin 
acne 
hirsutism 
hot flashes

Question 18

what is the MOA of anastrazole?

Answer 18

aromatase inhibitor

Question 19

what is the MOA of letrozole?

Answer 19

aromatase inhbitor

Question 20

what is the therapeutic use for anastrazole and letrozole?

Answer 20

breast cancer

Question 21

what are the adverse effects of anastrazole and letrozole?

Answer 21

GI
hot flashes
lethargy

Question 22

what class of drug is mifepristone?

Answer 22

anti-progesterone (progesterone receptor modulator)

Question 23

what is the MOA of mifepristone?

Answer 23

abortifacient antagonist of progesterone receptor

Question 24

what class of drug is ulipristal?

Answer 24

anti-progesterone (progesterone receptor modulator)

Question 25

what is the MOA of ulipristal?

Answer 25

antagonist of progesterone receptor

Question 26

what is the clinical use of ulipristal?

Answer 26

emergency contraceptive up to 5 days after intercourse

Question 27

what is the effect of progesterone on uterus smooth muscle?

Answer 27

decrease uterine contractions, decrease PG production

Question 28

what is the effect of progesterone on the endometrium?

Answer 28

decrease uterine contractions

Question 29

what is the general MOA for anti-progesterone (progesterone receptor modulator)?

Answer 29

1. inhibit progesterone receptors
2. uterine contractions
3. lining of uterus is shed
4. opens cervix