Lecture 9 - Estrogen Flashcards
estrogen:
responsible for development of ____, ____ and ____ distribution
genetalia, breast;
fat
think growth for estrogen, secretion for progesterone
estrogens:
ovary produces ____
placenta produces ___
adipose tissue produces ____
rank them in most to least potent
17beta-estradiol;
estriol;
estrone (via aromatization)
estradiol > estrone > estriol
in the circulation, most of estrogen is (bound or unbound)?
when bound, it is bound to to ____ or ____
bound;
Sex Hormone binding globulin, albumin
menstrual cycle:
order of phases?
_____ then _____ then _____ then _____
follicular phase, ovulation, luteal, menses
menstrual cycle:
the follicular phase is characterized by increasing levels of _____, produced by the _____. this causes the endometrium to _____.
estrogen, developing follicule; grow (proliferative phase)
ovulation:
an increase in _____ causes a ____ surge,
estrogen, LH
luteal phase:
the _____ produces ____ and ____ . this causes the endometrium to ______
corpus luteum, estrogen, progesteron;
increase vascularity and secretions (secretory phase)
when the ____ involutes, ____ and ____ levels fall. this causes _____
corpus luteum;
progesterone, estrogen;
menses
at lower levels, estrogen _____ FSH and LH.
at higher levels, estrogen _____ FSH and LH
suppresses/inhibits;
stimulates
if pregnancy occurs, _____ is produced from the syncitiotrophoblast of the placenta. this stimulates the ____ to produce ____ during the first trimester
HCG;
corpus luteum;
progesterone/estrogen
estrogen synth:
in the ____ cell, cholesterol is converted to _____ by desmolase.
in the ____ cell, this is converted to estrone or estogen by _____
theca, androstenedione;
granulosa, aromatase
most estrogens are metabolized in the _____. conjugated estrogens in the _____ can be hydrolyzed in the intestine and reabsorbed.
liver (high rate of first pass metabolism);
bile
estrogen receptors are found in the ____. when bound, what do they do?
cytoplasm;
translocate to the nuclues–>bind transcription factors
estrogens:
_____ the rate of resorption in bone.
____ HDL, ____ LDL;
_____ coagulability of blood
decrease;
increase, decrease;
increase
estrogen uses:
hormone therapy in _____, _____, _____
post-menopausal women;
osteoporosis,
contraception
estrogen side effects:
increased risk of ____ and ____ cancer;
uterine _____;
blood things: increased risk of ______
endometrial, breast;
bleeding;
thromboembolism
things required for estrogen activity:
aromaticity in ____ ring;
____ at the 3 position;
17Beta ____ group
A;
hydroxyl;
OH
ethinyl estradiol, mestranol, and quinestrol are _____-alkylated estrogens. this prevents conversion to ____ and enhances oral bioavailability/half life
17 alpha;
estrone
estradiol valerate and cypionate are _____ that decrease the solubility and slows absorption. this ____ the action
esters;
prolongs
what is a SERM
selective estrogen receptor modulators
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)
vaginal adenocarcinoma (clear cell); prostate cancer
tomxifen:
is a estrogen _____. used to treat _____ cancer;
increased risk of ______
partial agonist (ie agonist at bone, antagonist at breast); ER+ breast; thromboembolism (and endometrial cancer)
raloxifene:
is a estrogen ______. mainly used to treat ____;
increased risk of _____
partial agonist (antagonist at uterus and breast, agonist at at bone); osteoporosis; thromboembolic events (not endometrial cancer)
clomiphene:
is a _____ of estrogen receptors in the _____. this causes _____ release of LH and FSH, _____ ovulation
antagonist, hypothalamus;
increased, stimulating
clomiphene:
used to treat infertility due to _____.
side effects = _____, ovarian _____, multiple simultaneous _____
anovulation (ie polycystic overian syndrome;
hot flashes, enlargement, pregnancies
_____ is a pure estrogen receptor antagonist and is used for patients who are resistant to _____ with breast cancer
fulvestrant, tamoxifen
anastrozole, letrozole, exemestane are all ____. used to treat _____
aromatase inhibitors (ie prevent peripheral conversion); ER+ breast cancer