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A study that used high- to very-high-dose oral estradiol to treat postmenopausal women with estrogen receptor-positive breast cancer found that mean steady-state estradiol levels in the 6 mg/day group were about 300 pg/mL and in the 30 mg/day group were about 2,400 pg/mL. [37]
100 mg 1x/6 months Footnotes: a = No longer used or recommended, due to health concerns. b = As a single patch applied once or twice per week (worn for 3–4 days or 7 days), depending on the formulation.
The total endometrial proliferation dose of sublingual estradiol in women is 60 to 140 mg per cycle or 14 days and of sublingual estradiol benzoate in women is 60 to 180 mg per cycle or 14 days. [75]: 310 Both sublingual estradiol and sublingual estradiol benzoate have a persistence of estrogenic effect after a dose of only one day.
2–10 mg/day Various: Estrogen: Sublingual: 1–8 mg/day Climara [c] Estrogen: TD patch: 25–400 μg/day Divigel [c] Estrogen: TD gel: 0.5–5 mg/day Various: Estrogen: SC implant: 50–200 mg every 6–24 mos Estradiol valerate: Progynova: Estrogen: Oral: 2–10 mg/day Progynova: Estrogen: Sublingual: 1–8 mg/day Delestrogen [c] Estrogen ...
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]
Trough estradiol levels and MADRS Tooltip Montgomery–Åsberg Depression Rating Scale scores with 1 mg sublingual micronized estradiol 3 to 8 times per day (3 to 8 mg/day total; mean 4.8 mg/day total) in women with postpartum depression. [8] Blood was drawn specifically in the mornings before the first dose of sublingual estradiol for the day. [8]
Average number of moderate-to-severe hot flashes per week with placebo and different doses of oral estradiol in menopausal women [40] [41]. Estradiol is used in menopausal hormone therapy to prevent and treat moderate to severe menopausal symptoms such as hot flashes, vaginal dryness and atrophy, and osteoporosis (bone loss). [11]
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).
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