Estradiol cypionate

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

Estradiol Cypionate 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 cypionate 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 and organs such as 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 improve 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 cypionate is commercially available as Depo-Estradiol, an intramuscular depot injection used for the treatment of moderate to severe vasomotor symptoms associated with menopause and for the treatment of hypoestrogenism due to hypogonadism .

Estradiol cypionate
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Estradiol cypionate
Generic	Estradiol cypionate
Estradiol cypionate Other Names	Estradiol cypionate
Type
Formula	C₂₆H₃₆O₃
Weight	Average: 396.5622 Monoisotopic: 396.266445018
Protein binding	Estrogens circulate in the blood largely bound to sex hormone binding globulin (SHBG) and albumin .
Groups	Approved, Investigational, Vet approved
Therapeutic Class
Manufacturer
Available Country
Last Updated:	September 19, 2023 at 7:00 am

Uses

Estradiol cypionate is an estradiol prodrug used to treat vasomotor symptoms and hypoestrogenisms from hypogonadism.

Depo-Estradiol intramuscular depot injection is indicated for the treatment of moderate to severe vasomotor symptoms and hypoestrogenism due to hypogonadism.

Estradiol cypionate is also used to associated treatment for these conditions: Hypoestrogenism, Moderate Menopausal Vasomotor Symptoms, Severe Vasomotor Symptoms Associated With Menopause

How Estradiol cypionate 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.

Increases in the down-stream effects of ER binding reverses some of the symptoms of menopause and of hypoestrogenism, which are primarily caused by a loss of estrogenic activity.

Food Interaction

Exercise caution with grapefruit products. Grapefruit inhibits CYP3A4 metabolism, which may increase the serum concentration of estradiol cypionate.
Exercise caution with St. John's Wort. This herb induces the CYP3A4 metabolism of estradiol cypionate. Therefore it may reduce the serum concentration and effectiveness of estradiol cypionate.

Volume of Distribution

The distribution of exogenous estrogens is similar to that of endogenous estrogens. Estrogens are widely distributed in the body and are generally found in higher concentrations in the sex hormone target organs .

Elimination Route

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 .