Estradiol (medication)
Estradiol is also available in the U.S. in combination with progestogens for the treatment of menopausal symptoms and as a combined hormonal contraceptive:Estradiol and estradiol esters are also available in custom preparations from compounding pharmacies in the U.S. This includes subcutaneous pellet implants, which are not available in the United States as FDA-approved pharmaceutical drugs. In addition, topical creams that contain estradiol are generally regulated as cosmetics rather than as drugs in the U.S. and hence are also sold over-the-counter and may be purchased without a prescription on the Internet.
Pharmacokinetics of estradiol
Estradiol has been assessed for use by rectal administration in a number of studies. Uses of estradiol by this route have included treatment of menopausal symptoms in postmenopausal women. Rectal administration of estradiol is described as qualitatively and quantitatively similar to vaginal administration of estradiol. The use of estradiol by the rectal route considerably bypasses the liver and hence the first-pass metabolism that occurs with oral estradiol, similarly to other parenteral routes of estradiol such as vaginal and transdermal administration. Irritation of the intestines does not usually occur with rectal estradiol. The use of estradiol by the rectal route is not well-accepted by all individuals, and due to its inconvenience, it has been said that rectal administration of estradiol has gained no practical clinical importance.