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Estradiol: 150 μg/day: 300 μg/day: 600 μg/day Transdermal patch: 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 ...
Estradiol levels with 50 to 100 μg/day transdermal estradiol patches applied to the forearm and to the scrotum in a crossover study in 2 men with prostate cancer. [14] In 35 men treated continuously with one 100 μg/day estradiol patch scrotally, the mean estradiol level was ~500 pg/mL (range ~125–1,200 pg/mL).
Available transdermal estradiol patches in the United States [1] [2] [a]; Brand name Dose (µg/day) DOA (d) Size [b] [c] (cm 2) Levels (pg/mL) Intro. Alora [3] [4]: 25, 50, 75, 100 3–4
A dosage of two to six 100 μg/day transdermal estradiol patches can achieve mean levels of estradiol in the area of 200 to 400 pg/mL and can be used as a form of high-dose estrogen therapy, for instance to suppress testosterone levels in the treatment of prostate cancer in men and in feminizing hormone therapy for transgender women.
Estradiol is an estrogen, or an agonist of the nuclear estrogen receptors (ERs), the estrogen receptor alpha (ERα) and the estrogen receptor beta (ERβ). [1] [2] [6] In one study, the EC 50 Tooltip half-maximal effective concentration value of estradiol for the human ERα was 50 pM (0.05 nM) and for the human ERβ was 200 pM (0.2 nM).
A dosage of 1 mg/day oral estradiol valerate has been found to produce approximate circulating concentrations of 50 pg/mL estradiol and 160 pg/mL estrone, while a dosage of 2 mg/day results in circulating levels of 60 pg/mL estradiol and 300 pg/mL estrone. [108]
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