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In transgender women, estradiol valerate given by intramuscular injection is usually used at a dosage of 5 to 20 mg, but up to 30 to 40 mg, once every 2 weeks. [30] [31] [29] Estradiol valerate has also been used at a dose of 10 to 40 mg by intramuscular injection to limit bleeding in women with hemorrhage due to dysfunctional uterine bleeding.
With estradiol valerate, it is reported that a dose of 5 mg has a duration of 7 to 8 days, [274] 10 mg a duration of 10 to 14 days, [265] [282] 40 mg a duration of 2 to 3 weeks, and 100 mg a duration of 3 to 4 weeks. [282] High doses of estradiol valerate, such as 40 mg per week, can achieve pregnancy levels of estradiol. [283]
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.
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).
Estradiol: 25 μg/day b: 50 μg/day b: 100 μg/day b: Transdermal gel: Estradiol: 0.5 mg/day: 1–1.5 mg/day: 2–3 mg/day Vaginal: Estradiol: 25 μg/day – – Estriol: 30 μg/day: 0.5 mg 2x/week: 0.5 mg/day IM Tooltip Intramuscular or SC injection: Estradiol valerate – – 4 mg 1x/4 weeks Estradiol cypionate: 1 mg 1x/3–4 weeks: 3 mg 1x/3 ...
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]
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