Estrogens Flashcards
Locations of production of estrogens
Ovaries Testes adipose tissue (esp. obese) fetal adrenal cortex placenta
what’s the most potent estrogen?
17B-estradiol (E2)
what are the natural sources of weak estrogens and what is their putative effect?
DDT
bisphenol A
genistein
may lead to low birth rates
Growth promoting action of estrogen
formation of the endometrium and creation of progesterone receptors
anabolic effects of estrogens
closure of epiphyses, positive nitrogen balance
metabolic effects of estrogens
bone density
increase cognition (decreased hot flashes)
increased HDL, lowers LDL
increases serum and thyroid binding proteins
what are the two receptors for estrogen?
ERalpha and beta
what are the consequences of estrogen deficiency?
mood disorders, hot flashes, amenorrhea, failure to undergo puberty if congenital
what cancers are estrogen responsive?
breast, uterine, cervical
therapeutic uses for estrogens
acne, osteoporosis, prostate cancer, breast cancer (palliative only), OCP, HRT, mood swings, vasomotor disturbances (hot flashes), vaginal dryness/atrophy, CVD
failure of ovarian development (Turner’s, hypopituitarism)
dysmenorrhea
what was the first orally available estrogen drug? what is it used for today?
DES; palliation in inoperable breast and prostate cancer
what are the major drugs used today? how are they chemically modified? what is the zoonotic source?
estradiol-valerate or cypionate 17-esters
ethinyl estradiol & mestranol 17-alkylated
conjugated estrogens (Premarin) - horse derived
what are the advantages to the esters and the alkyls? to the conjugated?
esters are depot IM drugs (like the androgens)
alkyls are 10-20x more potent than endogenous estrogen (these are the OCPs)
conjugated estrogens are slightly less potent and are therefore used in post-menopausal HRT
route of delivery of estrogens
PO, IM, transdermal
major side effects of estrogens
thromboembolism, cancer (esp. breast, endometrial)
