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. It is also used in the treatment of prostate cancer. The medication is taken by mouth or by injection into muscle or fat once every 1 to 4 weeks.
Progynova (estradiol valerate) 1 mg oral tablets in the Chinese mainland
Side effects of estradiol valerate include breast tenderness, breast enlargement, nausea, headache, and fluid retention. It is an estrogen and hence is an agonist of the estrogen receptor, the biological target of estrogens like estradiol. It is an estrogen ester and a prodrug of estradiol in the body. Because of this, it is considered to be a natural and bioidentical form of estrogen.
Estradiol valerate was first described in 1940 and was introduced for medical use in 1954. Along with estradiol cypionate, it is one of the most widely used esters of estradiol. It is used in the United States, Canada, Europe, and throughout much of the rest of the world. It is available as a generic medication.
Medical uses
See also: Estradiol (medication) § Medical uses
The medical uses of It are the same as those of estradiol and other estrogens. Examples of indications for the medication include hormone therapy and hormonal contraception. In regard to the latter, It is available in combination with a progestin as a combined estradiol-containing oral contraceptive (with dienogest) and as a combined injectable contraceptive. Along with estradiol cypionate, estradiol undecylate, and estradiol benzoate, It is used as a form of high-dose estrogen therapy in feminizing hormone therapy for transgender women. It is also used as a form of high-dose estrogen therapy in the treatment of prostate cancer in men. Low-dose oral estradiol valerate (2–6 mg/day) has been used in the treatment of breast cancer in women who were previously treated with and benefited from but acquired resistance to aromatase inhibitors as well. Injectable estradiol valerate has been used to suppress sex drive in sex offenders.
Contraindications
See also: Estradiol (medication) § Contraindications
Contraindications of estrogens include coagulation problems, cardiovascular diseases, liver disease, and certain hormone-sensitive cancers such as breast cancer and endometrial cancer, among others.
Estradiol valerate is an estradiol ester, or a prodrug of estradiol. As such, it is an estrogen, or an agonist of the estrogen receptors. The affinity of estradiol valerate for the estrogen receptor is approximately 50 times lower than that of estradiol. In addition, estradiol valerate is rapidly cleaved into estradiol and is unable to reach target tissues in concentrations of significance, if at all. As such, estradiol valerate is essentially inactive in terms of estrogenic effect itself, acting solely as a prodrug to estradiol.
The molecular weight of estradiol valerate is about 131% of that of estradiol due to the presence of its C17β valerate ester, and hence estradiol valerate contains about 76% of the amount of estradiol of an equal dose of estradiol. Aside from dose adjustment to account for the difference in molecular weight, oral estradiol valerate is considered to be equivalent to oral estradiol. Because estradiol valerate is a prodrug of estradiol, it is considered to be a natural and bioidentical form of estrogen.
Description
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. In women, it is used in hormone therapy for menopausal symptoms and low estrogen levels, hormone therapy for transgender women, and in hormonal birth control. It is also used in the treatment of prostate cancer in men. The medication is taken by mouth or by injection into muscle or fat once every 1 to 4 weeks.
Chemical Properties White to off-white crystalline powder, odorless. Insoluble in water, easily soluble in ethanol, acetone, chloroform, slightly soluble in vegetable oil.
Uses It is a female hormone (estrogen).estradiol valerate injection It is used to reduce symptoms of menopause which are vaginal dryness, hot flashes, and others. The symptoms of menopause manifest because the body is making less estrogen; with It, these symptoms are brought to the lowest minimum. This medication therapy can also produce enough estrogen in women with ovarian failure, hypogonadism and can be used by men to treat prostate cancer (palliation only).
Indications
Estradiol valerate is commercially available as an intramuscular injection as the product Delestrogen and is indicated for the treatment of moderate to severe vasomotor symptoms and vulvovaginal atrophy due to menopause, for the treatment of hypoestrogenism due to hypogonadism, castration or primary ovarian failure, and for the treatment of advanced androgen-dependent carcinoma of the prostate (for palliation only). It is also available in combination with Dienogest as the commercially available product Natazia used for the prevention of pregnancy and for the treatment of heavy menstrual bleeding.
Definition ChEBI:It is a steroid ester. It is the parenterally-administered synthetic valerate ester of estradiol, a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females.
Therapeutic Function Estrogen
General Description It is a synthetic hormone that is extensively metabolized to estradiol and valeric acid before reaching the systemic circulation. It is well suited for treatment of the characteristic symptoms accompanying menopause in women.
estradiol valerate side effects As with all pharmaceutical medicines, some unwanted effects can occur from the use of estradiol valerate tablets 2mg.
Always consult a physician for medical advice before use.
Common side effects may include: bloating, vomiting, nausea, breast tenderness, headache, weight changes, and mood changes.
More severe side effects may include mental changes, breast lumps, vaginal bleeding, liver damage, increased thirst, and sudden vision loss.
Safety Profile Suspected carcinogen with carcinogenic and teratogenic data. Experimental reproductive effects. When heated to decomposition it emits acrid smoke and irritating fumes.
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
ATC code G03CA03 (WHO)
Bioavailability Oral: 3–5%
IM injection: 100%
Protein binding Estradiol: ~98% (to albumin and SHBGTooltip sex hormone-binding globulin)
Metabolism Cleavage via esterases in the liver, blood, and tissues
Metabolites Estradiol, valeric acid, and metabolites of estradiol
estradiol valerate half life
Elimination half-life Oral: 12–20 hours (as E2)
IM injection: 3.5 (1.2–7.2) days
Duration of action IM injection:
5 mg: 7–8 days
10 mg: 10–14 days
40 mg: 2–3 weeks
100 mg: 3–4 weeks
Excretion Urine (80%)
Melting point 144 to 145 °C (291 to 293 °F)
More Introduction:https://en.wikipedia.org/wiki/Estradiol_valerate
