Lecture 9 - Estrogen

Question 1

estrogen:

responsible for development of ____, ____ and ____ distribution

Answer 1

genetalia, breast;
fat

think growth for estrogen, secretion for progesterone

Question 2

estrogens:
ovary produces ____
placenta produces ___
adipose tissue produces ____

rank them in most to least potent

Answer 2

17beta-estradiol;
estriol;
estrone (via aromatization)

estradiol > estrone > estriol

Question 3

in the circulation, most of estrogen is (bound or unbound)?

when bound, it is bound to to ____ or ____

Answer 3

bound;

Sex Hormone binding globulin, albumin

Question 4

menstrual cycle:
order of phases?
_____ then _____ then _____ then _____

Answer 4

follicular phase, ovulation, luteal, menses

Question 5

menstrual cycle:
the follicular phase is characterized by increasing levels of _____, produced by the _____. this causes the endometrium to _____.

Answer 5

estrogen, developing follicule; grow (proliferative phase)

Question 6

ovulation:

an increase in _____ causes a ____ surge,

Answer 6

estrogen, LH

Question 7

luteal phase:

the _____ produces ____ and ____ . this causes the endometrium to ______

Answer 7

corpus luteum, estrogen, progesteron;

increase vascularity and secretions (secretory phase)

Question 8

when the ____ involutes, ____ and ____ levels fall. this causes _____

Answer 8

corpus luteum;
progesterone, estrogen;
menses

Question 9

at lower levels, estrogen _____ FSH and LH.

at higher levels, estrogen _____ FSH and LH

Answer 9

suppresses/inhibits;

stimulates

Question 10

if pregnancy occurs, _____ is produced from the syncitiotrophoblast of the placenta. this stimulates the ____ to produce ____ during the first trimester

Answer 10

HCG;
corpus luteum;
progesterone/estrogen

Question 11

estrogen synth:
in the ____ cell, cholesterol is converted to _____ by desmolase.

in the ____ cell, this is converted to estrone or estogen by _____

Answer 11

theca, androstenedione;

granulosa, aromatase

Question 12

most estrogens are metabolized in the _____. conjugated estrogens in the _____ can be hydrolyzed in the intestine and reabsorbed.

Answer 12

liver (high rate of first pass metabolism);

bile

Question 13

estrogen receptors are found in the ____. when bound, what do they do?

Answer 13

cytoplasm;

translocate to the nuclues–>bind transcription factors

Question 14

estrogens:
_____ the rate of resorption in bone.
____ HDL, ____ LDL;
_____ coagulability of blood

Answer 14

decrease;
increase, decrease;
increase

Question 15

estrogen uses:

hormone therapy in _____, _____, _____

Answer 15

post-menopausal women;
osteoporosis,
contraception

Question 16

estrogen side effects:
increased risk of ____ and ____ cancer;
uterine _____;
blood things: increased risk of ______

Answer 16

endometrial, breast;
bleeding;
thromboembolism

Question 17

things required for estrogen activity:
aromaticity in ____ ring;
____ at the 3 position;
17Beta ____ group

Answer 17

A;
hydroxyl;
OH

Question 18

ethinyl estradiol, mestranol, and quinestrol are _____-alkylated estrogens. this prevents conversion to ____ and enhances oral bioavailability/half life

Answer 18

17 alpha;

estrone

Question 19

estradiol valerate and cypionate are _____ that decrease the solubility and slows absorption. this ____ the action

Answer 19

esters;

prolongs

Question 20

what is a SERM

Answer 20

selective estrogen receptor modulators

Question 21

Diethyl-stilbestrol (DES) is associated with increased risk of ______ _____ in women exposed in utero. it is still used for _____, along with chlorotrianisene (both non-steroidal estrogens)

Answer 21

vaginal adenocarcinoma (clear cell);
prostate cancer

Question 22

tomxifen:
is a estrogen _____. used to treat _____ cancer;
increased risk of ______

Answer 22

partial agonist (ie agonist at bone, antagonist at breast);
ER+ breast;
thromboembolism (and endometrial cancer)

Question 23

raloxifene:
is a estrogen ______. mainly used to treat ____;
increased risk of _____

Answer 23

partial agonist (antagonist at uterus and breast, agonist at at bone);
osteoporosis;
thromboembolic events (not endometrial cancer)

Question 24

clomiphene:

is a _____ of estrogen receptors in the _____. this causes _____ release of LH and FSH, _____ ovulation

Answer 24

antagonist, hypothalamus;

increased, stimulating

Question 25

clomiphene:
used to treat infertility due to _____.
side effects = _____, ovarian _____, multiple simultaneous _____

Answer 25

anovulation (ie polycystic overian syndrome;

hot flashes, enlargement, pregnancies

Question 26

_____ is a pure estrogen receptor antagonist and is used for patients who are resistant to _____ with breast cancer

Answer 26

fulvestrant, tamoxifen

Question 27

anastrozole, letrozole, exemestane are all ____. used to treat _____

Answer 27

aromatase inhibitors (ie prevent peripheral conversion);
ER+ breast cancer