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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 (Delestrogen, Estradiol Valerate) – 10 mg/mL, 20 mg/mL, 40 mg/mL Polyestradiol phosphate (Estradurin) was previously available in the U.S. but was discontinued. Combined with progestins
Major estradiol gel dispenser products include EstroGel and Elestrin while major estradiol gel packet products include DiviGel and Sandrena. Estradiol gels are administered daily. [ 186 ] [ 15 ] [ 10 ] [ 212 ] When estradiol is administered as a hydroalcoholic gel, it dries within 2 to 5 minutes following application to the skin. [ 194 ]
Vaginal tablets, including Vagifem which contains estradiol [6] Vaginal creams, including Premarin which is a compound cream [7] consisting primarily of conjugated estrogens isolated from mare's urine. Another vaginal cream is Ovesterin, which contains estriol.
SERMs are used for various estrogen-related diseases, including treatment of ovulatory dysfunction in the management of infertility treatment, prevention of postmenopausal osteoporosis, treatment and risk reduction of breast cancer, [4] and treatment of dyspareunia due to menopause.
[10] [4] Although relatively low, the oral bioavailability of EE is considerably higher than that of micronized estradiol (5%). [2] [10] Following a single 20 μg dose of EE in combination with 2 mg norethisterone acetate in postmenopausal women, EE concentrations have been found to reach a maximum of 50 pg/mL within an average of 1.5 hours. [7]