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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 cypionate is and has been available as an oil solution for intramuscular injection provided in vials and ampoules at concentrations of 1, 3, and 5 mg/mL (and containing 5, 10, 15, 25, or 50 mg estradiol cypionate total).
EC/MPA is available in the form of a microcrystalline aqueous suspension of 5 mg EC and 25 mg MPA given in a 0.5 mL aqueous solution for intramuscular injection once per month. [10] It is provided in the form of single-dose vials and ampoules. [10] The particle sizes of the formulation are 93% within a range of 5 to 16 μm. [11]
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 ...
Simplified curves of estradiol levels after intramuscular injection of different 5 mg estradiol benzoate, 5 mg estradiol valerate, 5 mg estradiol cypionate, or 10 mg estradiol enanthate in oil solution in women. [4] Source: Garza-Flores (1994). [4]
Given by subcutaneous injection in mice, estradiol is about 10-fold more potent than estrone and about 100-fold more potent than estriol. [ 166 ] Estrogens have antigonadotropic effects at sufficiently high concentrations via activation of the ER and hence can suppress the hypothalamic–pituitary–gonadal axis .
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