Esterified Estrogens
Esterified Estrogens Uses, Dosage, Side Effects, Food Interaction and all others data.
Esterified Estrogens 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 Estrogens 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.
| Trade Name | Esterified Estrogens |
| Generic | Esterified estrogens |
| Esterified estrogens Other Names | Esterified estrogens, Estrogens, esterified, Estrogens,esterified |
| Weight | 0.3mg, 0.625mg, 1.25mg, 2.5mg |
| Type | Oral tablet |
| 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 | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Esterified Estrogens is a female hormone used to treat conditions related to estrogen deficiency and moderate to severe vasomotor menopausal symptoms in women.
Esterified Estrogens 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 Estrogens 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 Estrogens 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
Elimination Route
Mainly urinary as estradiol, estrone, estriol, and their glucuronide and sulfate conjugates.
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