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Pronunciation | /ˌɛstrəˈdaɪoʊl ˈvæləreɪt/ ES-trə-DY-ohl VAL-ə-rayt[1] |
Trade names | Delestrogen, Progynon Depot, Progynova, many others |
Other names | EV; E2V; Oestradiol valerate; Estradiol pentanoate; Estradiol valerianate |
Routes of administration | By mouth, sublingual, intramuscular injection,[2] subcutaneous injection |
Drug class | Estrogen; Estrogen ester |
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Pharmacokinetic data | |
Bioavailability | Oral: 3–5%[4][5] IM injection: 100%[6][4] |
Protein binding | Estradiol: ~98% (to albumin and SHBG )[7][8] |
Metabolism | Cleavage via esterases in the liver, blood, and tissues[4] |
Metabolites | Estradiol, valeric acid, and metabolites of estradiol[4] |
Elimination half-life | Oral: 12–20 hours (as E2)[4][7] IM injection: 3.5 (1.2–7.2) days[9] |
Duration of action | IM injection: • 5 mg: 7–8 days[10] • 10 mg: 10–14 days[11][12] • 40 mg: 2–3 weeks[11] • 100 mg: 3–4 weeks[11] |
Excretion | Urine (80%)[4] |
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ECHA InfoCard | 100.012.327 |
Chemical and physical data | |
Formula | C23H32O3 |
Molar mass | 356.506 g·mol−1 |
3D model (JSmol) | |
Melting point | 144 to 145 °C (291 to 293 °F) |
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Estradiol valerate (EV), sold for use by mouth under the brand name Progynova and for use by injection under the brand names Delestrogen and Progynon Depot among others, is an estrogen medication. It is used in hormone therapy for menopausal symptoms and low estrogen levels, hormone therapy for transgender people, and in hormonal birth control.[5][4][13][14] It is also used in the treatment of prostate cancer.[13] The medication is taken by mouth or by injection into muscle or fat once every 1 to 4 weeks.[13][14]
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.[16][5][4] Because of this, it is considered to be a natural and bioidentical form of estrogen.[16][17][4][18]
Estradiol valerate was first described in 1940 and was introduced for medical use in 1954.[19][20][21] Along with estradiol cypionate, it is one of the most widely used esters of estradiol.[22] Estradiol valerate is used in the United States, Canada, Europe, and throughout much of the rest of the world.[23][24] It is available as a generic medication.[25]
pmid7169965
was invoked but never defined (see the help page).pmid22257576
was invoked but never defined (see the help page).pmid7389356
was invoked but never defined (see the help page).Lauritzen-1988
was invoked but never defined (see the help page).Delestrogen-Label
was invoked but never defined (see the help page).Progynova-Label
was invoked but never defined (see the help page).Ghosh-2010
was invoked but never defined (see the help page).Natural estrogens considered here include: [...] Esters of 17β-estradiol, such as estradiol valerate, estradiol benzoate and estradiol cypionate. Esterification aims at either better absorption after oral administration or a sustained release from the depot after intramuscular administration. During absorption, the esters are cleaved by endogenous esterases and the pharmacologically active 17β-estradiol is released; therefore, the esters are considered as natural estrogens.
Kleemann-2014
was invoked but never defined (see the help page).Publishing2013
was invoked but never defined (see the help page).Duetsch-1969
was invoked but never defined (see the help page).Yen-1991
was invoked but never defined (see the help page).Elks-2014
was invoked but never defined (see the help page).© MMXXIII Rich X Search. We shall prevail. All rights reserved. Rich X Search