Estrogens

Question 1

Name the compound

Answer 1

Question 2

Name the compound

Answer 2

Question 3

Development and maintenance of female reproductive tissue (ovaries, uterus, breast, vagina)
Regulation in CNS (temp., mood)
Effects in peripheral tissues (bone, cardiovascular, liver)

Answer 3

Estrogens

Question 4

Development and maintenance of female reproductive tissue (uterus, breast)
Maintenance of pregnancy
Effects in other tissues (brain)

Answer 4

Progesterone

Question 5

Regulation of estrogen synthesis

Answer 5

Question 6

Granulosa cells produce ___________

Answer 6

estrogen

Question 7

Corpus luteum produces both ______ and _________

Answer 7

estrogen and progesterone

Question 8

Phase where estrogen suppresses the production of FSH

Answer 8

Early follicular phase

Question 9

Phase estrogen stimulates the surge of LH and FSH -> ovulation and formation of corpus luteum

Answer 9

Late follicular phase

Question 10

Phase estrogen and progesterone suppresses the production of LH and FSH

Answer 10

Luteal phase

Question 11

Biosynthesis of estrogens

Answer 11

Question 12

Metabolism and excretion

Answer 12

Question 13

Activity

Answer 13

Question 14

Ethinyl estradiol, Mestranol, and Quinestrol are examples of what estrogens

Answer 14

17 alpha-alkylated estrogens

Question 15

Estradiol valerate and estradiol cypionate are typically used for what clinical action

Answer 15

Slow absorption from the injection site (depot) prolongs the action

Question 16

Estrone sulfate and equilin sulfate are found it what substance? What are they classified as?

Answer 16

Usually collected from pregnant mares’ urine
Conjugated estrogens

Question 17

What is the estrogen?
Used in 1940-1970 to prevent miscarriage,
now used for advanced prostate cancer

Answer 17

Non-steroidal estrogen
Diethyl stilbestrol (DES)

Question 18

Postpartum breast engorgement, menopause symptoms, prostate cancer

Answer 18

Chlorotrianisene

Question 19

Partial estrogen agonists, mostly nonsteroidal estrogens

Answer 19

Selective estrogen receptor modulators (SERM)

Question 20

Prodrug; partial estrogen agonist
Antiestrogen actions: treatment and prevention of breast cancer
Estrogenic actions: weak estrogen agonist at endometrial cells, increases the risk for thromboembolic events, prevents osteoporosis

Answer 20

Tamoxifen

Question 21

Structurally similar to tamoxifen; SERM
Used to treat advanced breast cancer

Answer 21

Toremifene

Question 22

Structurally similar to toremifene, SERM, Estrogenic effects on the vaginal epithelium, Used to treat dyspareunia in post-menopausal women

Answer 22

Ospemifene

Question 23

SERM; partial estrogen agonist
Tissue-specific activities
Estrogen: Prevents osteoporosis in postmenopausal women
Decreases LDL levels in blood, increases the risk for blood clots
Antiestrogen: Decreases the risk for breast cancer, does not stimulate endometrial cells, may cause hot flashes

Answer 23

Raloxifene

Question 24

SERM; partial agonist
Increases secretion of FSH and LH by inhibiting negative estradiol feedback
Used to stimulate ovulation in women with oligomenorrhea or amenorrhea and ovulatory dysfunction; PCOS

Answer 24

Clomiphene

Question 25

SERD; pure estrogen receptor antagonist for the treatment of breast cancer

Answer 25

Fulvestrant (Faslodex)

Question 26

Block the biosynthesis of estrogens
Effective in some patients whose breast cancer is treatment resistant to tamoxifen
Ovulation induction, gynecomastia

Answer 26

Aromatase inhibitors:
Anastrozole, letrozole, and exemestane