979-32-8CCCCC(=O)O[C@H]1CC[C@H]2[C@@H]3CCc4cc(O)ccc4[C@H]3CC[C@]12CRSEPBGGWRJCQGY-RBRWEJTLSA-NEstradiol valerate is a steroid ester.
Breast Feeding; Lactation; Milk, Human; Estrogens; Hormones
FDA approved drugs -> Active ingredient
FDA approved drugs -> Active ingredient
Pharmaceuticals
Danger
H302 (29.7%): Harmful if swallowed [Warning Acute toxicity, oral]
P203, P261, P264, P270, P271, P280, P301+P317, P302+P352, P304+P340, P317, P318, P321, P330, P362+P364, P405, and P501 (click each P-code to see the statement)
Aggregated GHS information provided per 64 reports by companies from 11 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.
Drug Induced Liver Injury Rank (DILIrank 2.0)
Estradiol valerate
vLess-DILI-concern
2
Adverse reactions
DOI:10.1016/j.drudis.2016.02.015
Estrogen mediates its effects across the body through potent agonism of the Estrogen Receptor (ER), which is located in various tissues including in the breasts, uterus, ovaries, skin, prostate, bone, fat, and brain. Estradiol binds to both subtypes of the Estrogen Receptor: Estrogen Receptor Alpha (ERα) and Estrogen Receptor Beta (ERβ). Estradiol also acts as a potent agonist of G Protein-coupled Estrogen Receptor (GPER), which has recently been recognized as a major mediator of estradiol's rapid cellular effects.
Estradiol enters target cells freely (e.g., female organs, breasts, hypothalamus, pituitary) and interacts with a target cell receptor. When the estrogen receptor has bound its ligand it can enter the nucleus of the target cell, and regulate gene transcription which leads to formation of messenger RNA. The mRNA interacts with ribosomes to produce specific proteins that express the effect of estradiol upon the target cell. Estrogens increase the hepatic synthesis of sex hormone binding globulin (SHBG), thyroid-binding globulin (TBG), and other serum proteins and suppress follicle-stimulating hormone (FSH) from the anterior pituitary. Increases in the down-stream effects of ER binding reverses some of the symptoms of menopause, which are primarily caused by a loss of estrogenic activity.
ESTRADIOL VALERATE
Estrogen Receptor Agonists [MoA]; Estrogen [EPC]; Estradiol Congeners [CS]
Compounds that interact with ESTROGEN RECEPTORS in target tissues to bring about the effects similar to those of ESTRADIOL. Estrogens stimulate the female reproductive organs, and the development of secondary female SEX CHARACTERISTICS. Estrogenic chemicals include natural, synthetic, steroidal, or non-steroidal compounds.
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979-32-8DTXSID8023004CHEMBL1511CHEBI:31561White to off-white crystalline powder, odorless. Insoluble in water, easily soluble in ethanol, acetone, chloroform, slightly soluble in vegetable oil.
IM Injection: When conjugated with aryl and alkyl groups for parenteral administration, the rate of absorption of oily preparations is slowed with a prolonged duration of action, such that a single intramuscular injection of estradiol valerate or estradiol cypionate is absorbed over several weeks. Natazia: After oral administration of estradiol valerate, cleavage to 17β-estradiol and valeric acid takes place during absorption by the intestinal mucosa or in the course of the first liver passage. This gives rise to estradiol and its metabolites, estrone and other metabolites. Maximum serum estradiol concentrations of 73.3 pg/mL are reached at a median of approximately 6 hours (range: 1.5–12 hours) and the area under the estradiol concentration curve [AUC(0–24h)] was 1301 pg·h/mL after single ingestion of a tablet containing 3 mg estradiol valerate under fasted condition on Day 1 of the 28-day sequential regimen.
Estradiol, estrone and estriol are excreted in the urine along with glucuronide and sulfate conjugates.
개요Estradiol 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.
용도Estradiol valerate is a female hormone (estrogen). 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 estradiol valerate, 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).
일반 설명Estradiol valerate 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.
정의ChEBI: Estradiol valerate 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.