module 14 gonadal hormone inhibitors

Question 1

synthesis of progestins, androgens, and estrogens

Answer 1

cholesterol is the main precursor

- all are lipophilic

Question 2

progestines

Answer 2

17a hydroxyprogesterone
progesterone
-> converted to testosterone which is converted to estradiol

Question 3

Androgens

Answer 3

testosterone 
-> converted to estradiol 
Dehydroepiandrosterone DHEA
-> converted to Androstenedione
Androstenedione
-> converted to estrone

Question 4

estrogens

Answer 4

estradiol
-> converted to estriol
estrone
-> converted to estriol

Question 5

5a-reductase inhibitors meds

Answer 5

finasteride

dutasteride

Question 6

5a-reductase inhibitors MOA

Answer 6

competitive, selective inhibitors

inhibits testosterone -> dihydrotestosterone conversion

Question 7

dihydrotestosterone

Answer 7

binds to androgen Rc with 10-fold higher affinity than testosterone

Question 8

aromatase inhibitors

Answer 8

competitive inhibitors
- anastrazole
- letrozole
bind covalently: 
- exemestane
- formestane

Question 9

aromatase inhibitors MOA

Answer 9

inhibit androgen to estrogen conversion

• testosterone -> estradiol
• androstenedione -> estrone

Question 10

aromatase inhibitors use

Answer 10

breast canter that is hormone responsive (ER+)

Question 11

aromatase inhibitor AE

Answer 11

suppression of estrogen

• dec. bone density
• inc. risk osteoporosis/fx

Question 12

selective estrogen Rc modulators (SERM) meds

Answer 12

tamoxifen
raloxifene
clomiphene

Question 13

tamoxifen MOA

Answer 13

tissue specific agonist/antagonist effects

• inhibits growth of estrogen dependent breast tumors
• stimulatory in bones

Question 14

Tamoxifen AE

Answer 14

stimulates endometrial cancer

Question 15

raloxifene MOA

Answer 15

stimulates bone
- delay or prevent osteoporosis
inhibits breast and endometrium

Question 16

clomiphene MOA

Answer 16

induces ovulation

• Estrogen Rc antagonist in hypothalamus. anterior pituitary
• > inc. GnRH

Question 17

estrogen Rc antagonist med

Answer 17

fulvestrant

Question 18

fulvestrant MOA

Answer 18

pure antagonist

competitively inhibits ER in breast cancer cells

Question 19

fulvestrant use

Answer 19

breast cancer that is hormonally responsive

slows tumor growth

Question 20

androgen Rc antagonist meds

Answer 20

flutamide
bicalcutamide
spironolactone

Question 21

androgen Rc antagonist MOA

Answer 21

competitively inhibits binding of androgen to androgen Rc

Question 22

flutamide and bicalutamide use

Answer 22

prostate cancer

BPH

Question 23

spironolactone use

Answer 23

hirsutism

Question 24

progesterone Rc antagonist med

Answer 24

mifepristone (RU-486)

Question 25

mifepristone MOA

Answer 25

competitive inhibition of progesterone action

Question 26

mifepristone use

Answer 26

1st trimester termination of pregnancy

Question 27

GnRH agonists

Answer 27

leuprolide
goserelin
nafarelin

Question 28

GnRH Rc antagonist

Answer 28

cetrorelix

ganirelix