Female Sex Hormones

Question 1

3 naturally occurring steroidal estrogens

Answer 1

estrone, estradiol, estriol

Question 2

Nonsteroidal estrogenic compound

Answer 2

flavinoids (soybeans)

Question 3

_____ is the major product of ovarian steroidgenesis

Answer 3

Estradiol/E2

Question 4

During first part of menstrual cycle estrogens are produced by theca and granulosa cell of _____

Answer 4

graafian follicle

Question 5

After ovulation, estrogens are produced by the ____

Answer 5

corpus lutem

Question 6

During pregnancy estrogens are produced by the ____

Answer 6

fetoplacental unit

Question 7

During menopause, estrogens are produced by ____

Answer 7

adrenal and hepatic conversion of precursors

Question 8

____ and _____ are formed in the liver from estradiol or in peripheral tissues from andostendione.

Answer 8

Estrone/E1 and Estriol/E3

Question 9

4 main female sex hormones

Answer 9

Progesterone, E1 estrone, E2 estradiol, E3 estriol

Question 10

Product from which all sex hormones are derived is ____

Answer 10

pregnenolone (from cholesterol)

Question 11

Two main male sex hormones

Answer 11

androstenedione and testosterone

Question 12

_____ converts male sex hormones to estrogens.

Answer 12

aromatase

Question 13

Functions of estrogen

Answer 13

female maturation, endometrial proliferation during follicular phase, hematologic effect, metabolic effect

Question 14

T/F estrogen is an important modulator of bone growth and fusion of ephiphyses

Answer 14

T

Question 15

Hematologic effects of estrogens

Answer 15

increases coagulability of blood in extrinsic pathway (increased II, VII, IX, X and decreases antithrombin III) + increase in HDL, increased TAG –> unclear what the net effect is

Question 16

Metabolic effects of estrogens

Answer 16

increased production of leptin, tbg, fibrinogen, transferrin, cbg, shbg

Question 17

Estrogen is a vasodilator/vasoconstrictor

Answer 17

vasodilator

Question 18

How does estrogen decrease resorption of bone?

Answer 18

promotes apoptosis of osteoclasts

Question 19

In a non pregnant state, progesterone is produced by____

Answer 19

LH stimulated corpus luteum

Question 20

In a pregnant state, progesterone is produced by the ____

Answer 20

placenta

Question 21

Functions of progesterone

Answer 21

progestational profile of the endometrium/preparation for implantation, renders uterus refractory to oxytocin until onset of labor

Question 22

4 types of steroid receptor ligands

Answer 22

pure agonist, mixed agonist/antagonist, pure antagonist I, pure antagonist II

Question 23

MOA of pure agonist

Answer 23

agonist binds to receptor –> complex binds to HRE –> recruits coactivator –>gene transcription

Question 24

MOA of mixed agonist/antagonist

Answer 24

Ligand binds to receptor –> complex binds HRE –> differential recruitment of co-activator/repressor –> abrogated gene transcription (type III-IV antagonist)

Question 25

MOA of pure agonist II

Answer 25

ligand binds to receptor --> complex binds to HRE --> recruits co-repressor --> 0 gene transcription

Question 26

MOA of pure agonist I

Answer 26

ligand binds to receptor --> complex does not bind HRE --> no gene transcription

Question 27

T/F estrogen can have a genomic or a non-genomic resposne

Answer 27

T --> i.e. binding to blood vessels will vasodilate without a genomic response

Question 28

How do natural and synthetic estrogens/progestins affect the pathway?

Answer 28

receptor agonism

Question 29

How does antiprogesterone RU486/mifepristone affect the pathway?

Answer 29

receptor antagonism

Question 30

How does a selective ER modulator affect the pathway?

Answer 30

receptor modulation

Question 31

How do aromatase inhibitors affect the pathway?

Answer 31

synthesis inhibition

Question 32

3 indications of estrogen agonism

Answer 32

primary hypogonadism/secondary estrogen deficiency, suppression of ovulation, post-menopausal estrogen replacement

Question 33

ERT increases/decreases HDL, increases/decreases LDL and increases/decreases oxidation of HDL/LDL.

Answer 33

increases, decreases, decreases

Question 34

ERT increases/decreases the thickness of externa and media layers of the carotid but speeds up/delays intimal thickening.

Answer 34

increases, delays

Question 35

ERT increases/decreases formation of angiotensin II.

Answer 35

decreases

Question 36

ERT promotes/reverses acetylcholine induced vasoconstriction of the carotid.

Answer 36

reverses

Question 37

T/F ERT relieves hot flashes, night sweats, vaginal dryness, and vaginal atrophy.

Answer 37

T

Question 38

T/F ERT increases bone loss and hip fractures.

Answer 38

F --> reduces

Question 39

T/F ERT increases colon cancer risk.

Answer 39

F --> reduces

Question 40

T/F ERT decreases thrombotic risk.

Answer 40

F --> increases

Question 41

T/F ERT increases stroke of risk.

Answer 41

T

Question 42

T/F ERT increases incidence of ovarian/endometrial cancer.

Answer 42

T

Question 43

T/F ERT decreases risk of breast cancer.

Answer 43

F --> increases

Question 44

T/F ERT increases risk of MI.

Answer 44

T

Question 45

MOA of SERMs

Answer 45

bind to ER --> complex binds to ERE in nucleus- -> conformational state dependent recruitment of coactivator/repressor --> tissue specific agonism/antagonism

Question 46

Goal of SERM use

Answer 46

maintain good effects of ERT on bone, eliminate bad effects on endometrium and breast

Question 47

Tamoxifen MOA

Answer 47

suppresses E2 dependent growth of breast cancer (antagonist); agonist in uterus, bone

Question 48

Tamoxifen is a type ___ estrogen receptor modulator

Answer 48

IV

Question 49

Tamoxifen is tumoristatic/tumoricidal

Answer 49

tumoristatic

Question 50

Raloixifene MOA

Answer 50

suppresses E2 dependent growth of breast AND uterine tissue; agonist in bone; lowers LDL

Question 51

Raloxifene is a type ____ estrogen receptor modulator

Answer 51

III

Question 52

Raloxifene is tumoristatic/tumoricidal

Answer 52

tumoristatic

Question 53

T/F tamoxifen increases risk of endometrial hyperplasia

Answer 53

T --> but raloxifene does not

Question 54

anastrozole and exemestane MOA

Answer 54

inhibit action of aromatase--> tx of ER+ tumors

Question 55

Indications for progestin therapy

Answer 55

replacement therapy, contraception/ivf, endometriosis, dysfunctional uterine bleeding

Question 56

RU486 is a progesterone receptor type II _____

Answer 56

antagonist via a corepressor

Question 57

Tx of hypogonadism

Answer 57

estrogens --> mestranol

Question 58

Tx of ERT

Answer 58

estradiol cypionate

Question 59

Tx of osteoporosis

Answer 59

raloxifene (SERM)

Question 60

Tx of breast cancer

Answer 60

tamoxifen (SERM) and letrozole (aromatase inhibitor)

Question 61

Tx of abortion

Answer 61

RU486