Estrogen and Progesterone Flashcards
(37 cards)
Which estrogen in the major circulating one in pre-menopausal women?
17-beta-estradiol (E2)
Which estrogen is the main one in post-menopausal women? And where is it produced in the body?
Estrone (E1); produced in the adipose tissue from adrenal androgens
What is the metabolic product of estrone and estradiol?
Estriol
In response to which hormone, does follicular cells decrease production of estradiol and begin producing progesterone?
Luteinizing Hormone
Which hormones does the corpus luteum produce?
Estradiol and progesterone
Which hormone can cause endometrial hyperplasia and increase risk of endometrial cancer?
Estrogen
What is the effect of estrogen on bones?
Maintain density by decreasing resorption; promote closure of epiphyses (termination of bone growth)
What is the effect of estrogen on cardiovascular system?
Increases HDL and decreases LDL; increase blood coagulation through enhanced hepatic production of clotting factors
What is the mechanism of estrogen action?
- binding to nuclear receptors (inactive form)
- binding causes dissociation of co-repressor, dimerization of receptor, and binding to ERE (estrogen response elements)
- coactivators recruited and transcription and protein synthesis follows
Definition of menopause
cessation for 12 months
Define perimenopause
period before menopause which symptoms such as hot flashes and night sweats first begin
What were the findings of Womens’ Health Initiative?
E+P or E alone increased risk of CV disease and decreased risk of fracture in post-menopausal women
What risks are associated with HRT therapy in post-menopausal women?
CHD; venous thromboembolism; non-fatal stroke; breast cancer (but not E alone); Endometrial cancer (if used E alone); gall bladder disease; cognitive decline and dementia
What is Premarin?
Conjugated equine estrogens: mix of estrogens but mainly estrone
What are the benefits of transdermal route administration of estrogen?
Avoids first pass metabolism so you’re not getting as much effects of clotting factors. This lowers risk of VTE.
What is Estring?
Vaginal ring containing 17-beta-estradiol which is sustained release for 90 days.
What is vagifem?
Estradiol hemihydrate tablets inserted vaginally daily then 2x/week for maintenance.
What is the mechanism of SERM?
Selective estrogen receptor modifiers bind to nuclear estrogen receptors and competitively inhibit the binding of estrogen. Can either produce antagonistic effect or agonistic effect depending on tissue.
Which drugs are considered SERM?
Tamoxifen, Raloxifene, Clomiphene
Tamoxifen is used as first line therapy for breast cancer in pre-menopausal women or post-menopausal women?
Pre-menopausal women. Post-menopausal, it is 2nd line therapy.
In which tissue is tamoxifen agonistic and which tissue is it antagonistic?
Agonist in uterus and bone. Antagonist in breast cancer.
Tamoxifen is used as adjunct therapy in early stage breast cancer or advanced stage?
Early stage; in adjunct to surgery or chemo
In which tissue is raloxifene agonistic and which tissue is it antagonistic?
Agonist at bone and antagonist at uterus and breast
Uses of raloxifene?
- Preventing invasive breast cancer in women at high risk
- Post-menopausal osteoporosis (vertebral fracture, not hip)
