How Do Estrogen Derivatives Work?

Reviewed on 1/6/2022

How do estrogen derivatives work?

Estrogen derivatives are medications used in the prevention and treatment of menopausal symptoms and various conditions associated with menopause, such as vaginal dryness and bone loss (osteoporosis). Estrogen derivatives are also used in the treatment of breast and prostate cancers.

Estrogens are a group of natural endogenous hormones in women and are present in smaller quantities in men. Estrogens are the primary hormones responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics. Estrogens also play an important role in male sexual function.

Estrogen derivatives supplement the deficiency in natural estrogens which get depleted with menopause in women. Estrogen derivatives relieve menopausal symptoms, prevent bone loss, and reduce the risk of cardiovascular disease in menopausal women.

Endogenous estrogens are of three major types, estradiol, estriol, and estrone. Estrogen derivatives are purified formulations of different types of estrogens derived from natural estrogens from pregnant mares or synthetic estrogen preparations. Estrogen derivatives bind to estrogen receptors in cells and have effects similar to estrogen.

Estrogen derivatives work by reducing elevated levels of reproductive hormones in postmenopausal women, which include gonadotropin-releasing hormone (GnRH) from the hypothalamus, and follicular stimulating hormone (FSH), and luteinizing hormone (LH) from the pituitary gland.

Estrogen derivatives may be combined with another class of medication known as selective estrogen receptor modulator (SERM). SERMs have estrogen-like effects on bone, increasing its density, but have antiestrogenic effects in the breast and uterus, which reduces the risk of endometrial hyperplasia (thickening) that estrogen can cause.


If menopause occurs in a woman younger than ___ years, it is considered to be premature. See Answer

How are estrogen derivatives used?

Estrogen derivatives may be administered through various routes including:

Oral tablets:

  • Intravenous (IV) injections into the vein
  • Intramuscular (IM) injections into the muscle
  • Vaginal creams, tablets, inserts, and rings
  • Transdermal skin patches
  • Topical emulsions or gels applied to the skin
  • The uses of estrogen derivatives include:


Off-label uses:

  • Uremic bleeding (bleeding due to high levels of blood urea)

Orphan designation:

What are the side effects of estrogen derivatives?

Side effects of estrogen derivatives may include the following:

Information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with travel medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.


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What are the names of estrogen derivative drugs?

Generic and brand names of estrogen derivative drugs include:


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