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Estradiol can be taken by a variety of different routes of administration. [10] These include oral, buccal, sublingual, intranasal, transdermal (gels, creams, patches), vaginal (tablets, creams, rings, suppositories), rectal, by intramuscular or subcutaneous injection (in oil or aqueous), and as a subcutaneous implant. [10]
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]
Atypical (dual estrogen and nitrogen mustard alkylating antineoplastic): Estramustine phosphate sodium (Emcyt) – 140 mg; Oral estradiol valerate (except in combination with dienogest as an oral contraceptive) is not available in the U.S. and is used primarily in Europe. [2]
A review of selected studies reported a range of mean peak estradiol levels of 24 to 140 pg/mL occurring 1 to 12 hours after administration of 2 mg oral estradiol valerate. [4] A study found that, in accordance with their differences in molecular weights, oral estradiol produced higher levels of estradiol than oral estradiol valerate. [109]
Administering a vaginal tablet without an applicator. Intravaginal administration is a route of administration where the substance is applied inside the vagina . Pharmacologically , it has the potential advantage to result in effects primarily in the vagina or nearby structures (such as the vaginal portion of cervix ) with limited systemic ...
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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