Esterified

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

Esterified contain a mixture of estrogenic substances; the principle component is estrone. Preparations contain 75% to 85% sodium estrone sulfate and 6% to 15% sodium equilin sulfate such that the total is not <90%. Esterified are a man-made mixture of estrogens that are used to treat symptoms of menopause such as hot flashes, vaginal dryness, vaginal burning or irritation, or other hormonal changes in the vagina. It is being also for the prevention and treatment of osteoporosis.

Estrogens are responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics. Estradiol is the principle intracellular human estrogen and is more potent than estrone and estriol at the receptor level; it is the primary estrogen secreted prior to menopause.

Esterified
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	Esterified
Generic	Esterified estrogens
Esterified estrogens Other Names	Esterified estrogens, Estrogens, esterified, Estrogens,esterified
Type
Protein binding	Approximately 95-98% of estradiol is bound loosely to albumin or tightly to sex hormone binding globulin.
Groups	Approved
Therapeutic Class
Manufacturer
Available Country
Last Updated:	September 19, 2023 at 7:00 am

Uses

Esterified is a female hormone used to treat conditions related to estrogen deficiency and moderate to severe vasomotor menopausal symptoms in women.

Esterified are indicated to replace estrogen in women with ovarian failure or other conditions that cause a lack of natural estrogen in the body. It is also indicated for the treatment of symptoms of breast cancer in both men and women. In men it can be used for the treatment of advanced prostate cancer. It is also indicated for the treatment of menopausal symptoms.

Esterified is also used to associated treatment for these conditions: Advanced Prostate Carcinoma, Hypogonadism, Metastatic Breast Cancer, Premature Ovarian Failure (POF), Moderate Menopausal Vasomotor Symptoms, Moderate Vulvovaginal atrophy, Severe Vasomotor Symptoms Associated With Menopause, Severe menopausal vulvovaginal atrophy

How Esterified works

Estrogens modulate the pituitary secretion of gonadotropins, luteinizing hormone, and follicle-stimulating hormone through a negative feedback system; estrogen replacement reduces elevated levels of these hormones.

Toxicity

LD50 IP 325 mg/Kg (rat). LD50 IV 1740 mg/Kg (mouse). LD50 oral >5000 mg/Kg (rat).

Food Interaction

Avoid grapefruit products. Grapefruit inhibits CYP3A metabolism, which may increase the serum concentration of esterified estrogens.
Avoid St. John's Wort. This herb induces CYP3A metabolism and may reduce serum levels of esterified estrogens.

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 concentration in the sex hormone target organs.

Elimination Route

Readily absorbed after oral administration. High concentrations of estrone are achieved with oral administration, whereas higher concentrations of estradiol are generally achieved after percutaneous absorption. Although vaginal products (such as gel, rings, etc.) are administered locally, they achieve high serum concentrations.

Half Life

Half-life varies, it is in the range 1-2 hr.

Clearance

There is variation in the clearance rate depends on each estrogen individual: estradiol-17β: 580 L/day/m2 estrone: 4050 L/day/m2 estriol: 1110 L/day/m2