by on April 20, 2012
Brand Names:Climera, Delestrogen, Estrace and Vivelle
Generic name:estradiol
Pregnancy Category:C
Half-life:13 hours

What is Estradiol?

Estradiol is a prescription form of the female sex hormone, estrogen. This medication is sold under various brand names, including Climera, Delestrogen, Estrace and Vivelle. A type of steroid, estradiol is derived from cholesterol that is produced by the liver. Although estradiol is considered predominantly female, men also make small amounts of the hormone in their adrenal cortex and testes. The estradiol prescribed by your doctor is a synthesized form of estrogen that is produced in a medical laboratory.

Estradiol has various effects on the human body:

  • It regulates the development of secondary sex characteristics in women and it has control over the reproductive system.
  • It regulates the menstrual cycle.
  • Estrogen has control over some aspects of the metabolism – it stimulates the development of bones which plays an important role in the prophylaxis of osteoporosis. Estradiol reduces the level of cholesterol in blood and slightly increases that of triglycerides. It can influence the carbohydrate metabolism in patients with diabetes. Another important feature of estradiol is that it increases the concentration of the proteins that take part in blood clotting.


Estradiol medications are available in a wide variety of forms, all of which must be prescribed and monitored by a doctor. Oral estradiol tablets, such as Estrace, are usually taken once per day; Estrace is also available as a vaginal cream. In addition to vaginal creams, estradiol comes as a topical cream that is designed for non-vaginal use. Estradiol is also available in the form of a weekly transdermal patch, such as Climera Vivelle. In some cases, doctors may prescribe an injectable form of estradiol, known as Delestrogen.

Estradiol Uses

Estradiol is an estrogen replacement therapy that is intended to relieve symptoms that are associated with menopause, including vaginal itching, hot flashes, vaginal inflammation, mood swings and vaginal dryness. It is also prescribed as an estrogen replacement for women with ovarian failure or to prevent osteoporosis in postmenopausal women.

  • It is used for the treatment of delayed sexual development and conditions connected with the absence of normal menstrual flow.
  • As a replacement therapy after surgical removal of the ovaries.
  • Replacement therapy during menopause. Menopausal women are at higher risk of osteoporosis, heart diseases and depression due to the lack of endogenous estradiol production. Estradiol alleviates the symptoms connected with menopause such as hot flashes, vaginal dryness and mood swings.
  • It is a part of the contraceptive pills.
  • Sometimes it is used in the in vitro programs

Some doctors may occasionally prescribe estradiol medications as part of a comprehensive breast cancer treatment plan for women and, less frequently, to treat advanced forms of prostate cancer in men.

How does estradiol work?

Estradiol works by binding to estrogen receptors, entering the nucleus of the target cell and influencing the activity of certain estrogen-regulated genes.


Estradiol is available in a number of formulations – tablets, injection solutions (for intramuscular administration), vaginal globules, vaginal rings, creams and transdermal preparations. A lot of companies produce estradiol-containing medicines. Among them are Bayer, Novartis, Novo Nordisk, Pfizer, Sandoz, Warner Chilcott etc.

There is a great variety of brand medicines containing estradiol or some of its derivates. Here are some of them:

  • Oral forms – Estrofem, Estrace, Femtrace
  • Injection solutions –Progynon depot, Delestrogen
  • Vaginal globules – Vagifem
  • Vaginal rings- Estring
  • Vaginal creams – Estrace
  • Transdermal preparations – Climara, Estraderm

Precautions when taking medicines containing estradiol or its derivates

You should not use them if:

  • you have had deep veins thrombosis(blood clots) or pulmonary embolism
  • you have or have had breast cancer, uterine cancer or any other hormone-dependent tumor.
  • You have condition known as endometrial hyperplasia
  • you have or have had abnormal vaginal bleeding
  • you are suffering from heart diseases such as heart coronary disease or you have had a heart attack
  • you have liver dysfunction
  • you are suffering from porphyria
  • you are allergic to any of the ingredients of the medicine.

You should check your breasts regularly for lumps. Estradiol is a prescription medicine. Do not hesitate to discuss any questions you may have with your doctor. Ruling out a number of diseases and risk factors including some types of cancer is necessary before starting the therapy as well as regular check-ups.