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Side effects of estradiol valerate include breast tenderness, breast enlargement, nausea, headache, and fluid retention. [15] [13] [14] Estradiol valerate is an estrogen and hence is an agonist of the estrogen receptor, the biological target of estrogens like estradiol. [5] [4] [16] It is an estrogen ester and a prodrug of estradiol in the body.
Estradiol, mainly as esters including estradiol valerate, estradiol cypionate, and estradiol enanthate, is also the exclusive estrogen used in combined injectable contraceptives. [6] As of 2021, more than 95% of prescriptions are for combined hormonal birth control forms containing the synthetic estrogen ethinylestradiol (EE). [7]
In 1966, oral estradiol valerate was introduced by Schering for medical use under the brand name Progynova. [32] [33] [213] [214] Esterification of estradiol, as in estradiol valerate, was believed to improve its metabolic stability with oral administration.
Estradiol valerate/hydroxyprogesterone caproate (EV/OHPC), sold under the brand names Gravibinon and Injectable No. 1 (or Chinese Injectable No. 1) among others, is a combined estrogen and progestogen medication which is used in the treatment of threatened miscarriage and other indications (e.g., as a means of pseudopregnancy) [1] [2] [3] and as a form of combined injectable birth control to ...
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.
Most combined oral contraceptives contain ethinylestradiol or its prodrug mestranol as the estrogen component, but a few contain estradiol or estradiol valerate. Ethinylestradiol is generally used in oral contraceptives instead of estradiol because it has superior oral pharmacokinetics (higher bioavailability and less interindividual ...
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