Estradiol Benzoate

Estradiol Benzoate Uses, Dosage, Side Effects, Food Interaction and all others data.

Estradiol Benzoate 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 Benzoate is not currently available in Canada or the US.

Estradiol Benzoate
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Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
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Trade Name	Estradiol Benzoate
Generic	Estradiol benzoate
Estradiol benzoate Other Names	benzoato de estradiol, Estradiol benzoate
Type
Formula	C₂₅H₂₈O₃
Weight	Average: 376.488 Monoisotopic: 376.203844762
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 Benzoate is an estrogen indicated in combination with progesterone for the treatment of irregular menstruation.

Estradiol Benzoate is not currently available in any FDA or Health Canada approved products.

Estradiol Benzoate is also used to associated treatment for these conditions: Menstrual Irregularities, Secondary Amenorrhea, Hypoestrogenism

How Estradiol Benzoate 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.