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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 higher dosage of estradiol gel containing 1.5 mg estradiol per daily application has been found to produce mean estradiol levels of 40 to 100 pg/mL and estrone levels of 90 pg/mL, while 3 mg per day has been found to result in respective mean estradiol and estrone levels of 60 to 140 pg/mL and 45 to 155 pg/mL. [15]
Estradiol: 25 mg 1x/6 months: 50 mg 1x/6 months: 100 mg 1x/6 months Footnotes: a = No longer used or recommended, due to health concerns. b = As a single patch ...
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 valerate: Progynova: Estrogen: Oral: 2–10 mg/day Progynova: Estrogen: Sublingual: 1–8 mg/day Delestrogen [c] Estrogen: IM, SC: 2–10 mg/wk or 5–20 mg every 2 wks Estradiol cypionate: Depo-Estradiol: Estrogen: IM, SC: 2–10 mg/wk or 5–20 mg every 2 wks Estradiol dipropionate: Agofollin: Estrogen: IM, SC: 2–10 mg/wk or 5 ...
The use of high-dose estrogen therapy in breast cancer has mostly been superseded by antiestrogen therapy due to the improved safety profile of the latter. [17] High-dose estrogen therapy was the standard of care for the palliative treatment of breast cancer in women up to the late 1970s or early 1980s. [18
Estradiol cypionate (EC), sold under the brand name Depo-Estradiol 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 trans women, and in hormonal birth control for women. [14] [8] [15] [16] It is given by injection into muscle once every 1 to ...
Relugolix is a selective antagonist of the gonadotropin-releasing hormone receptor (GnRHR), with a half-maximal inhibitory concentration (IC 50) of 0.12 nM. [1] [8] [9] A dosage of relugolix of 40 mg once per day has been found to suppress estradiol levels to postmenopausal levels (<20 pg/mL) within 24 hours in premenopausal women. [1]
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