Estradiol benzoate
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
Main articles : Estradiol ( medication ) § Medical uses , and High-dose estrogen The medical uses of estradiol benzoate are the same as those of estradiol and other estrogens . [ 8 ] [ 12 ] Estradiol benzoate is used in hormone therapy for the treatment of menopausal symptoms such as hot flashes and vaginal atrophy and in the treatment of hypoestrogenism and delayed puberty due to hypogonadism or other causes in women . [ 8 ] [ 12 ] It is also used in hormone therapy for transgender women . [ 13 ] [ 28 ] [ 29 ] Aside from hormone therapy , estradiol benzoate is used in the treatment of gynecological disorders such as menstrual disorders , dysfunctional uterine bleeding , and breast engorgement . [ 8 ] [ 12 ] In addition , it is used as a form of high-dose estrogen therapy in the palliative treatment of prostate cancer in men . [ 8 ] Estradiol benzoate has a relatively short duration of action , and is administered by intramuscular injection usually two to three times per week . [ 8 ] [ 12 ] It is used in the treatment of menopausal symptoms at a dosage of 1 to 1.66 mg initially and 0.33 to 1 mg for maintenance two times per week , and in the treatment of hypoestrogenism and delayed puberty at a dosage of 1.66 mg two to three times per week . [ 8 ] [ 30 ] The dosage used in hormone therapy for transgender women is 0.5 to 1.5 mg two to three times per week . [ 13 ] In the treatment of prostate cancer , estradiol benzoate is used at a dosage of 1.66 mg three times per week ( for a total of 5 mg per week ) . [ 8 ]
Estradiol benzoate (EB), sold under the brand name Progynon-B among others, is an estrogen medication which is used in hormone therapy for menopausal symptoms and low estrogen levels in women, in hormone therapy for transgender women, and in the treatment of gynecological disorders. It is also used in the treatment of prostate cancer in men. Estradiol benzoate is used in veterinary medicine as well. When used clinically, the medication is given by injection into muscle usually two to three times per week. Side effects of estradiol benzoate include breast tenderness, breast enlargement, nausea, headache, and fluid retention. Estradiol benzoate 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 benzoate was discovered in 1933 and was introduced for medical use that same year. It was the first estradiol ester to be discovered or marketed, and was one of the first estrogens to be used in medicine. Along with estradiol dipropionate, estradiol benzoate was among the most widely used esters of estradiol for many years following its introduction. However, in the 1950s, longer-acting estradiol esters that necessitated less frequent injections, such as estradiol valerate and estradiol cypionate, were developed, and have since largely superseded estradiol benzoate.