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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.
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]
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]
Estradiol valerate/megestrol acetate; Estradiol valerate/methenmadinone caproate (Lutofollin) Polyestradiol phosphate/medroxyprogesterone acetate; Additional preparations listed at Combined injectable birth control § Research; For other indications: Estradiol valerate/gestonorone caproate (SH-834, SH-8.0834)
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]
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 cypionate (Depo-Estradiol, Estradiol Cypionate) – 5 mg/mL (1 mg/mL and 3 mg/mL discontinued) Estradiol valerate (Delestrogen, Estradiol Valerate) – 10 mg/mL, 20 mg/mL, 40 mg/mL; Polyestradiol phosphate (Estradurin) was previously available in the U.S. but was discontinued.
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).