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Flashcards in Female Sex Hormones Deck (61):
1

3 naturally occurring steroidal estrogens

estrone, estradiol, estriol

2

Nonsteroidal estrogenic compound

flavinoids (soybeans)

3

_____ is the major product of ovarian steroidgenesis

Estradiol/E2

4

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

graafian follicle

5

After ovulation, estrogens are produced by the ____

corpus lutem

6

During pregnancy estrogens are produced by the ____

fetoplacental unit

7

During menopause, estrogens are produced by ____

adrenal and hepatic conversion of precursors

8

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

Estrone/E1 and Estriol/E3

9

4 main female sex hormones

Progesterone, E1 estrone, E2 estradiol, E3 estriol

10

Product from which all sex hormones are derived is ____

pregnenolone (from cholesterol)

11

Two main male sex hormones

androstenedione and testosterone

12

_____ converts male sex hormones to estrogens.

aromatase

13

Functions of estrogen

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

14

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

T

15

Hematologic effects of estrogens

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

16

Metabolic effects of estrogens

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

17

Estrogen is a vasodilator/vasoconstrictor

vasodilator

18

How does estrogen decrease resorption of bone?

promotes apoptosis of osteoclasts

19

In a non pregnant state, progesterone is produced by____

LH stimulated corpus luteum

20

In a pregnant state, progesterone is produced by the ____

placenta

21

Functions of progesterone

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

22

4 types of steroid receptor ligands

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

23

MOA of pure agonist

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

24

MOA of mixed agonist/antagonist

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

25

MOA of pure agonist II

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

26

MOA of pure agonist I

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

27

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

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

28

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

receptor agonism

29

How does antiprogesterone RU486/mifepristone affect the pathway?

receptor antagonism

30

How does a selective ER modulator affect the pathway?

receptor modulation

31

How do aromatase inhibitors affect the pathway?

synthesis inhibition

32

3 indications of estrogen agonism

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

33

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

increases, decreases, decreases

34

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

increases, delays

35

ERT increases/decreases formation of angiotensin II.

decreases

36

ERT promotes/reverses acetylcholine induced vasoconstriction of the carotid.

reverses

37

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

T

38

T/F ERT increases bone loss and hip fractures.

F --> reduces

39

T/F ERT increases colon cancer risk.

F --> reduces

40

T/F ERT decreases thrombotic risk.

F --> increases

41

T/F ERT increases stroke of risk.

T

42

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

T

43

T/F ERT decreases risk of breast cancer.

F --> increases

44

T/F ERT increases risk of MI.

T

45

MOA of SERMs

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

46

Goal of SERM use

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

47

Tamoxifen MOA

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

48

Tamoxifen is a type ___ estrogen receptor modulator

IV

49

Tamoxifen is tumoristatic/tumoricidal

tumoristatic

50

Raloixifene MOA

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

51

Raloxifene is a type ____ estrogen receptor modulator

III

52

Raloxifene is tumoristatic/tumoricidal

tumoristatic

53

T/F tamoxifen increases risk of endometrial hyperplasia

T --> but raloxifene does not

54

anastrozole and exemestane MOA

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

55

Indications for progestin therapy

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

56

RU486 is a progesterone receptor type II _____

antagonist via a corepressor

57

Tx of hypogonadism

estrogens --> mestranol

58

Tx of ERT

estradiol cypionate

59

Tx of osteoporosis

raloxifene (SERM)

60

Tx of breast cancer

tamoxifen (SERM) and letrozole (aromatase inhibitor)

61

Tx of abortion

RU486