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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.
Estradiol (E2) is a medication and naturally occurring steroid hormone. [11] [12] [13] It is an estrogen and is used mainly in menopausal hormone therapy and to treat low sex hormone levels in women.
Estradiol, mainly as esters including estradiol valerate, estradiol cypionate, and estradiol enanthate, is also the exclusive estrogen used in combined injectable contraceptives. [6] As of 2021, more than 95% of prescriptions are for combined hormonal birth control forms containing the synthetic estrogen ethinylestradiol (EE). [7]
Estrogen plus other progestogens <5 years ≥5 years: 1.70 (1.50–1.91) 2.02 (1.81–2.26) Footnotes: a = Oral estrogen plus progesterone was not analyzed because there was a low number of women who used this therapy. Sources: See template.
Atypical (dual estrogen and nitrogen mustard alkylating antineoplastic): Estramustine phosphate sodium (Emcyt) – 140 mg; Oral estradiol valerate (except in combination with dienogest as an oral contraceptive) is not available in the U.S. and is used primarily in Europe. [2]
Femilar, which is an estradiol-containing birth control pill, contains 1 to 2 mg estradiol valerate and 1 to 2 mg CPA, and has been approved for use in Finland since 1993. [5] CPA alone has been found to suppress ovulation in 3 of 5 women at a dose of 0.5 mg/day and in 5 of 5 women at a dose of 1 mg/day.
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).
[15] [16] [27] Along with estradiol valerate, estradiol undecylate, and estradiol benzoate, estradiol cypionate is used as a form of high-dose estrogen therapy in feminizing hormone therapy for transgender women. [28] [17] [29] [30] The medication has been used to induce puberty in girls with delayed puberty due to hypogonadism. [31] [25]