Estrogens Flashcards
What is the function of estrogens?
Development and maintenance of female reproductive tissues.
Regulation in CNS (temperature, mood)
Progesterone functions to
Maintain female reproductive tissues
Maintain pregnancy
What is 17b-estradiol?
Most potent estrogen
Produced in ovaries and placenta during pregnancy
Estrogen and progesterone are produced by the ________cells in the corpus luteum
Granulosa
In the early follicular phase, _________ suppresses FSH production
Estrogen
Late in the follicular phase, _______and ________ Stimulate the surge of LH and FSH
Estrogen
Progesterone
The corpus luteum produces_______
Estrogen and Progesterone
hCG acts like _____ to stimulate the corpus luteum to produce__________ during the first trimester.
LH
Progesterone
What is the precursor for estrogen synthesis?
DHEA==> Androstenedione=====(Via 17b-Hydroxysteroid dehydrogenase)====>Testosterone===(Aromatase)===>17B-Estradiol
Estrone and estriol are synthesized in the______ and ______
Liver and peripheral tissues
17B-Estradiol is synthesized _________
In the Ovaries mostly
How are estrogens metabolized?
In the liver and excreted via bile
Main effects of estrogens?
Osteoporosis
Increased blood coagulation
Mood changes
Growth of axillary and pubic hair
Stromal development and ductal growth in the breast
Development of endometrial lining during menstrual cycles
Prolonged exposure leads to hyperplasia of the endometrium and abnormal bleeding.
Clinical uses of estrogens include:
Postmenopausal hormone therapy
Osteoporosis
Hormonal contraception
What are the adverse effects of Estrogen use?
Uterine bleeding Endometrial carcinoma Breast cancer Thromboembolism Weight gain
Name 3 17a-Alkylated estrogens
Ethinyl estradiol
Mestanol
Quinestrol
17a-alkylation increases halflife and oral bioavailability
Esterification of estrogens__________
Decreases solubility and slows absorption
Give 2 examples of estrogenic esters
Estradiol valerate
Estradiol cypionate
Give two examples of conjugated estrogens
Estrone Sulfate
Equilin Sulfate
Name two Non-Steroidal estrogens
Diethyl stilbestrol
Chlorotrianisene
Diethyl Stilbestrol is used for_______
Prevent miscarriage (1940-1970)
Used to treat advanced prostate cancer
(Increased risk of vaginal adenocarcinoma)
Chlorotrianisene is used for_______
Postpartum breast engorgement
Menopause symptoms
Prostate cancer
How do Selective Estrogen Receptor Modulators (SERMs) work?
Partial estrogen agonists- Block action of stronger estrogens
Tamoxifen is a ________and used in the treatment of ______
SERM
Breast cancer also prevents breast cancer in high risk patients.
Prevents osteoporosis
Tamoxifen is a _____drug
Pro
Toremifene
Very similar structure and function to Tamoxifen
Raloxifene and Badoxifen
Are SERMs used to prevent osteoporosis in postmenopausal women
Decrease LDL levels
Decreases breast cancer risk
Stimulates endometrial cells.
Clomiphene works by increasing________and _______ secretion by inhibiting __________ negative feedback
FSH
LH
Estradiol
Clomiphene (SERM) is used for________?
Stimulating Ovulation in women with Oligomenorrhea or amenorrhea and ovulary dysfunction (from polycystic ovary syndrome)
Fluvestrant is a__________
Selective estrogen receptor downregulator (SERD). Pure estrogen receptor antagonist. Used in patients resistant to Tamoxifen
Aromatase inhibitors work by________
Blocking biosynthesis of estrogens. They are effective in patients whose breast cancer is resistant to Tamoxifen.
Name 3 Aromatase inhibitors
Anast(rozole)
Let(rozole)
Exemestane
