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Estradiol levels after a single oral dose of 2 mg micronized estradiol or 2 mg estradiol valerate and with continuous oral administration of 2 mg/day micronized estradiol or 2 mg/day estradiol valerate (at steady state) in postmenopausal women. [109] Source was Wiegratz et al. (2001). [109]
Estradiol cypionate (Depo-Estradiol, Estradiol Cypionate) – 5 mg/mL (1 mg/mL and 3 mg/mL discontinued) 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.
Estradiol (E2) is a medication and naturally occurring steroid hormone. [11] [12] [13] It is an estrogen and is used mainly in menopausal hormone therapy and to treat low sex hormone levels in women.
Estrogen esters are essentially inactive themselves, with esters such as estradiol valerate and estradiol sulfate having about 2% of the affinity of estradiol for the estrogen receptor. [12] Likewise, the estrogen ether mestranol (ethinylestradiol 3-methyl ether) has about 1% of the affinity of estradiol for the estrogen receptor. [ 12 ]
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Estradiol decanoate, estradiol cyclooctyl acetate, estradiol 3-saccharinylmethyl ether, and EC508 (estradiol 17β-(1-(4-(aminosulfonyl)benzoyl)-L-proline)) are estradiol esters and novel oral forms of estradiol that have been developed with improved properties, such as greater bioavailability and reduced first-pass effect.
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