Womens Health Med Chem

Question 0

ER signaling

Answer 0

1) Bind to estrogen receptor
2) ER Transciption factor tether
3) growth factor phosphorylate ER
4) non genomic actions: cytoplasm proteins

Question 1

Estrogen

Answer 1

Female maturation
Endometrial effects
Metabolic bone resorption 
Adipose leptin
Blood coagulability 2,7,9,10

Question 2

Tamoxifen

Raloxifene, clomiphene

Answer 2

Blocks ER

Selective estrogen receptor modulator

SERM-ifen, iphene
Partial agonist antagonist

For breast cancer

Question 3

Major estrogens

Answer 3

Estriol, estrone, estradiol

Estradiol is major secretory product of the ovary

Question 4

Precursor for estrogen synthesis

Answer 4

Pregnenolone -> androstenedione ->

Aromatase to produce estrone and estradiol

Estrone is precursor for estriol

Question 5

Pulsatile GnRH

Answer 5

Endogenous

Question 6

Fertility

Answer 6

GnRH agonist (less multiple gestations)

Clomiphene: competitive inhibitor of endogenous estrogen and blocks negative feedback, stimulate ovulation

DC clomiphene if visual AE

Question 7

Contraception

Answer 7

Oral contraceptive: consistent high estrogen & progestin levels inhibit GnRH, inhibit FSH, LH (release and egg maturation), insufficient endometrial thickening, thick cervical mucus

Danazol: inhibits LH/FSH surge

Question 8

Endometriosis

Answer 8

Ketoconazole

Danazol: suppress ovarian function and midcycle LH/FSH surge

Synthetic androgen

Androgens cause atrophy

Question 9

Breast cancer

Answer 9

Fulvestrant - pure ER antagonist (if resistant to tamoxifen)
SERM

Anatrozole, letrozole Aromatase inhibitors (decrease estrogen production)
Exemestane: irreversible Aromatase inhibitor

Most breast cancer cells are ER+ and proliferate by estrogen

Block androgen conversion to estrogen

Question 10

GnRH

Answer 10

Stimulates release of FSH/LH

Question 11

FSH

Answer 11

Develops follicles, estrogen secretion, and induces expression of LH receptors

Question 12

LH

Answer 12

Regulates Aromatase ( production of 17B-estradiol from testosterone)

Surge LH= ovulation

Question 13

HPA negative feedback

Answer 13

Estrogen and progesterone on GnRH

Inhibin on FSH release

Question 14

GnRH neurons

Answer 14

Stimulated by NE neurons

Inhibited by opioid, dopamine, GABA

Question 15

Anterior pituitary

Answer 15

Stimulate production of hormones by peripheral endocrine/ liver

Question 16

Secretion of GnRH

Answer 16

Depends on gene KiSS and kisspeptin

High estrogen inhibits secretion of kisspeptin

Question 17

Estrogen metabolism

Answer 17

CYP 3A4

Rifampin, SJW

Question 18

Progesterone

Answer 18

Most important natural progestin produced by corpus luteum

Builds endometrium

Precursor to androgen and estrogen, adrenocorticoids

Elevate during pregnancy and peak in 3rd trimester, mimic pregnancy

Metabolized by liver

Question 19

Progestins

Answer 19

Most are 19-nortestosterone derivatives

Estrane 1st gen norethindrone

Drosperinone 4th gen derived from 17a-spironolactone
Minimize androgenic properties

Long term ovarian suppression
Thick cervical mucus

Question 20

Mifepristone

Answer 20

Binds to progesterone receptor and inhibits progesterone

Degrades corpus luteum

Question 21

Osphena

Answer 21

Treat painful interfourse

Estrogen agonist

Increases risk of endometrial cancer in women who use unopposed estrogen

Question 22

Aromatase inhibitor

Answer 22

Inhibit production of estrogen from testosterone

And block androstenedione to estrone