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Estradiol cypionate is of about 46% higher molecular weight than estradiol due to the presence of its C17β cypionate ester, and contains about 69% of the amount of estradiol by weight. [ 59 ] [ 22 ] [ 25 ] Because estradiol cypionate is a prodrug of estradiol, it is considered to be a natural and bioidentical form of estrogen.
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 an intramuscular injection of 10 mg estradiol valerate in oil, Climacteron (150 mg testosterone enanthate, 1 mg estradiol benzoate, 7.5 mg estradiol dienanthate in oil), and control group in 20, 11, and 11 ovariectomized women, respectively. [128] Assays were performed using RIA. [128] Source was Sherwin et al. (1987). [128]
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 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: 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 ...
Estradiol valerate/cyproterone acetate (Femilar) was introduced for use as a birth control pill in Finland in 1993, but was never marketed elsewhere. [235] Subsequently, estradiol valerate/dienogest (Natazia, Qlaira) was marketed as a birth control pill in 2008 [236] and estradiol/nomegestrol acetate (Naemis, Zoely) was introduced in 2012. [128]
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]
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