Estrogens

Question 1

What does estrogen do in the body?

Answer 1

development and maintenance of female reproductive tissues; regulation in CNs; effects in peripheral tissues

Question 2

What does progesterone do in the body?

Answer 2

Development and maintenance of female reproductive tissues; maintenance of pregnancy; effects in other tissues (brain)

Question 3

Most potent estrogen in humans

Answer 3

17beta-estradiol

Question 4

Where is 17b-estradiol produced?

Answer 4

mostly in the ovaries in premenopausal women; synthesized most in the placenta during pregnancy

Question 5

Estrogen and progesterone are produced by

Answer 5

granulosa cells and the corpus luteum

Question 6

Early follicular phase

Answer 6

estrogen suppresses the production of FSH

Question 7

Late follicular phase

Answer 7

Estrogen and progesterone stimulate the surge of LH and FSH -> ovulation and formation of the corpus luteum

Question 8

Luteal phase

Answer 8

Estrogen and progesterone suppresses the production of LH and FSH

Question 9

What happens if pregnancy does not occur?

Answer 9

corpus luteum degenerates; production of estrogen and progesterone by corpus luteum declines

Question 10

What happens if pregnancy occurs?

Answer 10

fertilized egg/embryo secretes hCG; hCG acts like LH to stimulate corpus luteum to produce progesterone during the first trimester; higher progesterone levels support maintenance of the endometrium

Question 11

Estron and estriol are synthesized

Answer 11

in the liver and in peripheral tissues

Question 12

Natural estrogens

Answer 12

17beta-estradiol
Estrone
Estriol

Question 13

Synthetic estrogens

Answer 13

Drugs with estrogenic activities

Question 14

Phytoestrogens

Answer 14

Estrogen-mimetic compounds in plants (flavonoids)

Question 15

Environmental estrogens

Answer 15

Compounds used in the manufacture of plastics (bisphenols, alkyphenols, phthalate phenols)

Question 16

Metabolism and excretion of estrogen

Answer 16

Metabolized in the liver mostly and excreted to the bile and to the urine

Question 17

Physiologic effects of estrogen

Answer 17

Female maturation, endometrial effects, metabolic and CV effects, blood coagulation, CNS/mood

Question 18

Clinical uses of estrogens

Answer 18

Postmenopausal hormone therapy in post-menopausal women, osteoporosis

Question 19

Adverse effects of estrogens

Answer 19

Uterine bleeding, endometrial carcinoma, breast cancer, thromboembolism, nausea, headache, fluid retention, weight gain

Question 20

17alpha-alkylated estrogens

Answer 20

Mestranol;
Quinestrol;
Ethinyl estradiol

Question 21

17alpha-alkylation prevents

Answer 21

conversion to estron -> enhances oral bioavailability and increases the half life

Question 22

Estrogenic esters

Answer 22

Estradiol valerate

Estradiol cypionate

Question 23

Esterification decreases

Answer 23

solubility and slows the absorption -> prolongs the action

Question 24

Conjugated estrogens

Answer 24

Estrone sulfate

Equilin sulfate

Question 25

Where do you get conjugated estrogens from

Answer 25

collected from pregnant mare urine

Question 26

Non-steroidal estrogens

Answer 26

Diethyl stilbestrol | Chlorotrianisene

Question 27

Diethyl stilbestrol

Answer 27

used in advanced prostate cancer

Question 28

Chlorotrianisene

Answer 28

postpartum breast engorgement; menopause symptoms; prostate cancer

Question 29

Selective estrogen receptor modulators (SERM)

Answer 29

Tamoxifen Toremifene Raloxifene Clomiphene

Question 30

Tamoxifen

Answer 30

partial estrogen agonist; antiestrogen and estrogenic actions; treatment of breast cancer; prevents breast cancer in high risk women

Question 31

Raloxifene

Answer 31

SERM; partial estrogen agonist; prevents osteoporosis; decreases LDL levels; increases risk for blood clots; does not stimulate endometrial cells; may cause hot flashes

Question 32

Clomiphene

Answer 32

SERM; partial estrogen agonist; increases secretion of FSH and LH by inhibiting negative estradiol feedback; used to sitmulate ovulation in women with oligomenorhea or amenorrhea and ovulatory dysfunction; polycystic ovary syndrome

Question 33

Fulvestrant

Answer 33

selective estrogen receptor downregulator; pure estrogen receptor antagonist

Question 34

Aromatase inhibitors

Answer 34

Anastrozole, Letrozole, Exemestane