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Estradiol valerate is usually used in the treatment of advanced prostate cancer in men at a dosage of 30 mg or more every 1 to 2 weeks by intramuscular injection. [13] 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.
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]
Due to its estrogenic activity, estradiol has antigonadotropic effects and can inhibit fertility and suppress sex hormone production in both women and men. [25] [26] Estradiol differs from non-bioidentical estrogens like conjugated estrogens and ethinylestradiol in various ways, with implications for tolerability and safety. [11]
An example pseudopregnancy regimen in women which has been used in clinical studies is intramuscular injections of 40 mg/week estradiol valerate and 250 mg/week hydroxyprogesterone caproate. [3] It has been found to result in estradiol levels of about 3,100 pg/mL at 3 months of therapy and 2,500 pg/mL at 6 months of therapy. [3]
Due to its estrogenic activity, estradiol has antigonadotropic effects and can inhibit fertility and suppress sex hormone production in both women and men. [4] [5] Estradiol differs from non-bioidentical estrogens like conjugated estrogens and ethinylestradiol in various ways, with implications for tolerability and safety. [1]
Estradiol levels after a short intravenous infusion of 20 mg estradiol in aqueous solution or an intramuscular injection of an equimolar dose of estradiol benzoate, estradiol valerate, or estradiol undecylate in oil solution in women. [6] [7] Sources: Geppert (1975) and Leyendecker et al. (1975). [6] [7]