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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]
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]
[131] [132] Both oral estradiol valerate at 6 mg/day and intramuscular estradiol valerate at 10 mg every 10 days have been found to increase SHBG levels by 2.5- to 3-fold in transgender women. [ 133 ] [ 134 ] [ 135 ] For comparison, combined birth control pills containing ethinylestradiol and a progestin with minimal androgenic or ...
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.
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]
Estradiol is not produced in the gonads only; in particular, fat cells produce active precursors to estradiol, and will continue to do so even after menopause. [51] Estradiol is also produced in the brain and in arterial walls. In men, approximately 15 to 25% of circulating estradiol is produced in the testicles.
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