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Estradiol is an estrogen, or an agonist of the nuclear estrogen receptors (ERs), the estrogen receptor alpha (ERα) and the estrogen receptor beta (ERβ). [1] [2] [6] In one study, the EC 50 Tooltip half-maximal effective concentration value of estradiol for the human ERα was 50 pM (0.05 nM) and for the human ERβ was 200 pM (0.2 nM).
For purposes of comparison with normal physiological circumstances, menstrual cycle circulating levels of estradiol in premenopausal women are 40 pg/mL in the early follicular phase, 250 pg/mL at the middle of the cycle, and 100 pg/mL during the mid-luteal phase. [163] Mean integrated levels of circulating estradiol in premenopausal women ...
Estradiol levels with 50 to 100 μg/day transdermal estradiol patches applied to the forearm and to the scrotum in a crossover study in 2 men with prostate cancer. [14] In 35 men treated continuously with one 100 μg/day estradiol patch scrotally, the mean estradiol level was ~500 pg/mL (range ~125–1,200 pg/mL).
Estradiol levels with rectal administration of estradiol in women after a single 1 mg dose 3 hours post-dose, with 0.5 mg/day 6 hours after the last dose, and with 1 mg/day 6 hours after the last dose. [261] [72] [242] [70] Estradiol has been assessed for use by rectal administration in a number of studies.
Mean estradiol levels during 1 to 8 mg/day oral estradiol therapy alone or in combination with 100 to 200 mg/day spironolactone in transgender women. [ 3 ] Percent change in estradiol (E2), estrone (E1), LH, and FSH levels over a 24-hour period following a single dose of 2 mg oral estradiol in women.
During the reproductive years of human females, levels of estradiol are somewhat higher than that of estrone, except during the early follicular phase of the menstrual cycle; thus, estradiol may be considered the predominant estrogen during human female reproductive years in terms of absolute serum levels and estrogenic activity.
Trough estradiol levels and MADRS Tooltip Montgomery–Åsberg Depression Rating Scale scores with 1 mg sublingual micronized estradiol 3 to 8 times per day (3 to 8 mg/day total; mean 4.8 mg/day total) in women with postpartum depression. [8] Blood was drawn specifically in the mornings before the first dose of sublingual estradiol for the day. [8]
The Women's Health Initiative (WHI) is an ongoing study of over 27,000 women that began in 1991, with the most recent analyses suggesting that, when initiated within 10 years of menopause, HRT reduces all-cause mortality and risks of coronary disease, osteoporosis, and dementia; after 10 years the beneficial effects on mortality and coronary ...
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