Estradiol valerate
Route/form Estrogen Dosage
Oral Estradiol 1-2 mg 3x/day
Oral Conjugated estrogens 1.25-2.5 mg 3x/day
Oral Ethinylestradiol 0.15-3 mg/day
Oral Ethinylestradiol sulfonate 1-2 mg 1x/week
Oral Diethylstilbestrol 1-3 mg/day
Oral Dienestrol 5 mg/day
Oral Hexestrol 5 mg/day
Oral Fosfestrol 100-480 mg 1-3x/day
Oral Chlorotrianisene 12-48 mg/day
Oral Quadrosilan 900 mg/day
Oral Estramustine phosphate 140-1400 mg/day
Transdermal patch Estradiol 2-6x 100 μg/day Scrotal : 1x 100 μg/day
IM or SC injection Estradiol benzoate 1.66 mg 3x/week
IM or SC injection Estradiol dipropionate 5 mg 1x/week
IM or SC injection Estradiol valerate 10-40 mg 1x/1-2 weeks
IM or SC injection Estradiol undecylate 100 mg 1x/4 weeks
IM or SC injection Polyestradiol phosphate Alone : 160-320 mg 1x/4 weeks With oral EE : 40-80 mg 1x/4 weeks
IM or SC injection Estrone 2-4 mg 2-3x/week
IV injection Fosfestrol 300-1200 mg 1-7x/week
IV injection Estramustine phosphate 240-450 mg/day
Medical uses
See also : Estradiol ( medication ) § Medical uses The medical uses of estradiol valerate are the same as those of estradiol and other estrogens . Examples of indications for the medication include hormone therapy and hormonal contraception . In regard to the latter , estradiol valerate is available in combination with a progestin as a combined estradiol-containing oral contraceptive ( with dienogest ) [ 23 ] and as a combined injectable contraceptive . [ 24 ] [ 25 ] [ 26 ] Along with estradiol cypionate , estradiol undecylate , and estradiol benzoate , estradiol valerate is used as a form of high-dose estrogen therapy in feminizing hormone therapy for transgender women . [ 27 ] [ 28 ] [ 29 ] [ 30 ] It is also used as a form of high-dose estrogen therapy in the treatment of prostate cancer in men . [ 10 ] Low-dose oral estradiol valerate ( 2–6 mg/day ) has been used in the treatment of breast cancer in women who were previously treated with and benefited from but acquired resistance to aromatase inhibitors as well . [ 31 ] [ 31 ] [ 32 ] In the United States , the approved indications of estradiol valerate injections include the treatment of moderate to severe hot flashes and vaginal atrophy associated with menopause in women , the treatment of hypoestrogenism due to hypogonadism , castration , or primary ovarian failure in women , and the palliative treatment of advanced prostate cancer in men . [ 10 ] Elsewhere in the world , oral estradiol valerate is similarly approved for the treatment of symptoms associated with menopause or hypoestrogenism due to castration in women . [ 11 ] Such symptoms may include hot flashes , outbreaks of sweat , sleep disturbances , depressive moods , irritability , headaches , and dizziness . [ 11 ] Estradiol valerate by intramuscular injection is usually used at a dosage of 10 to 20 mg every 4 weeks in the treatment of menopausal symptoms and hypoestrogenism due to hypogonadism , castration , or primary ovarian failure in women . [ 10 ] In the past , it was used at even higher doses of 10 to 40 every 1 to 4 weeks for estrogen replacement . [ 33 ] 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 . [ 10 ] 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 . [ 28 ] [ 29 ] [ 27 ] 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 . [ 34 ] :318 [ 35 ] :60
Estradiol valerate (EV), sold for use by mouth under the brand name Progynova and for use by injection under the brand names Delestrogen and Progynon Depot among others, is an estrogen medication. In women, it is used in hormone therapy for menopausal symptoms and low estrogen levels, hormone therapy for transgender women, and in hormonal birth control. It is also used in the treatment of prostate cancer in men. The medication is taken by mouth or by injection into muscle once every 1 to 4 weeks. Side effects of estradiol valerate include breast tenderness, breast enlargement, nausea, headache, and fluid retention. Estradiol valerate is a synthetic estrogen and hence is an agonist of the estrogen receptor, the biological target of estrogens like estradiol. It is an estrogen ester and a prodrug of estradiol in the body. Because of this, it is considered to be a natural and bioidentical form of estrogen. Estradiol valerate was first described in 1940 and was introduced for medical use in 1954. Along with estradiol cypionate, it is one of the most widely used esters of estradiol. Estradiol valerate is used in the United States, Canada, Europe, and throughout much of the rest of the world. It is available as a generic medication.