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[23] [24] Other common esters of estradiol in use include estradiol cypionate, estradiol enantate, and estradiol acetate, the former two of which are C17β esters of estradiol similarly to estradiol valerate and the latter of which is the C3 acetate ester of estradiol.
As such, estradiol valerate is regarded as essentially inactive in terms of estrogenic effect itself, acting solely as a prodrug to estradiol, [4] and estradiol cypionate is described as a prodrug of estradiol similarly. [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.
[1] [10] It has been said that, via intramuscular injection, the duration of estradiol benzoate (with an ester of length 1 carbon plus a benzene ring) is 2 to 3 days, of estradiol dipropionate (with two esters each of length 2 carbons) is 1 to 2 weeks, of estradiol valerate (ester of 5 carbons) is 1 to 3 weeks, and of estradiol cypionate (ester ...
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]
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]
A variety of C17β and/or C3 ester prodrugs of estradiol, such as estradiol acetate, estradiol benzoate, estradiol cypionate, estradiol dipropionate, estradiol enantate, estradiol undecylate, estradiol valerate, and polyestradiol phosphate (an estradiol ester in polymeric form), among many others, have been developed and introduced for medical ...
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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