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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 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 ...
As unopposed estrogen therapy (using estrogen alone without progesterone) increases the risk of endometrial hyperplasia and endometrial cancer in women with intact uteruses, estradiol is usually combined with a progestogen like progesterone or medroxyprogesterone acetate to prevent the effects of estradiol on the endometrium.
An example pseudopregnancy regimen in women which has been used in clinical studies is intramuscular injections of 40 mg/week estradiol valerate and 250 mg/week hydroxyprogesterone caproate. [3] It has been found to result in estradiol levels of about 3,100 pg/mL at 3 months of therapy and 2,500 pg/mL at 6 months of therapy. [3]
Estradiol benzoate/estradiol valerate/hydroxyprogesterone caproate (EB/EV/OHPC), sold under the brand name Sin-Ol, is a combination medication of estradiol benzoate (EB), an estrogen, estradiol valerate (EV), an estrogen, and hydroxyprogesterone caproate (OHPC), a progestin, which was reportedly used as a combined injectable contraceptive in women in the early 1970s. [1]
Examples of estradiol injectables that may be used in menopausal hormone therapy include estradiol valerate and estradiol cypionate. [ 136 ] [ 137 ] In terms of injectable progestogens, injectable progesterone is associated with pain and injection site reactions as well as a short duration of action requiring very frequent injections, and is ...
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]
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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