Estradiol dienantate
Estradiol dienantate Uses, Dosage, Side Effects, Food Interaction and all others data.
Estradiol Dienanthate is a pro-drug ester of Estradiol, a naturally occurring hormone that circulates endogenously within the human body. Estradiol is the most potent form of all mammalian estrogenic steroids and acts as the major female sex hormone. As a pro-drug of estradiol, estradiol benzoate therefore has the same downstream effects within the body through binding to the Estrogen Receptor (ER) including ERα and ERβ subtypes, which are located in various tissues including in the breasts, uterus, ovaries, skin, prostate, bone, fat, and brain.
Estradiol is commonly produced with an ester side-chain as endogenous estradiol has very low oral bioavailability on its own (2-10%). First-pass metabolism by the gut and the liver quickly degrades the estradiol molecule before it gets a chance to enter systemic circulation and exert its estrogenic effects . Esterification of estradiol aims to improves absorption and bioavailability after oral administration (such as with Estradiol valerate) or to sustain release from depot intramuscular injections (such as with Estradiol Cypionate) through improved lipophilicity. Following absorption, the esters are cleaved, resulting in the release of endogenous estradiol, or 17β-estradiol. Ester pro-drugs of estradiol are therefore considered to be bioidentical forms of estrogen .
Estradiol dienantate is not currently available in any commercially available products in Canada or the US.
Trade Name | Estradiol dienantate |
Generic | Estradiol dienanthate |
Estradiol dienanthate Other Names | Estradiol dienantate |
Type | |
Formula | C32H48O4 |
Weight | Average: 496.732 Monoisotopic: 496.355260026 |
Protein binding | Estrogens circulate in the blood largely (>95%) bound to sex hormone binding globulin (SHBG) and to albumin. |
Groups | Approved, Investigational, Vet approved |
Therapeutic Class | |
Manufacturer | |
Available Country | |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Estradiol dienantate is an estrogen used in some combined hormonal oral contraceptives.
Estradiol dienantate is not currently available in any FDA or Health Canada approved products.
Estradiol dienantate is also used to associated treatment for these conditions: Pregnant State
How Estradiol dienantate works
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.
Food Interaction
No interactions found.Elimination Route
Estradiol, estrone and estriol are excreted in the urine along with glucuronide and sulfate conjugates.
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