Prasterone, also known as dehydroepiandrosterone (DHEA) and sold under the brand name Intrarosa among others, is a medication as well as over-the-counter dietary supplement which is used to correct DHEA deficiency due to adrenal insufficiency or old age, as a component of menopausal hormone therapy, to treat painful sexual intercourse due to vaginal atrophy, and to prepare the cervix for childbirth, among other uses. It is taken by mouth, by application to the skin, in through the vagina, or by injection into muscle. Side effects of prasterone in women include symptoms of masculinization like oily skin, acne, increased hair growth, voice changes, and increased sexual desire, headaches, insomnia, and others. The compound is a naturally occurring prohormone of androgens and estrogens and hence is an agonist of the androgen and estrogen receptors, the respective biological targets of androgens like testosterone and estrogens like estradiol. Prasterone also has a variety of activities of its own, including neurosteroid and other activities. DHEA, the active ingredient of prasterone, was discovered in 1934. An association between DHEA levels and aging was first reported in 1965. The compound started being used as a medication in the late 1970s and as a supplement in the early 1980s. The marketing of prasterone over-the-counter as a supplement is allowed in the United States but is banned in many other countries.
Medical uses
Deficiency DHEA and DHEA sulfate (DHEA-S) are produced by the adrenal glands. In people with adrenal insufficiency such as in Addison's disease, there may be deficiency of DHEA and DHEA-S. In addition, levels of these steroids decrease throughout life and are 70 to 80% lower in the elderly relative to levels in young adults. Prasterone can be used to increase DHEA and DHEA-S levels in adrenal insufficiency and older age. Although there is deficiency of these steroids in such individuals, clinical benefits of supplementation, if any, are uncertain, and there is insufficient evidence at present to support the use of prasterone for such purposes.
Menopause
Prasterone is sometimes used as an androgen in menopausal hormone therapy. In addition to prasterone itself, a long-lasting ester prodrug of prasterone, prasterone enanthate, is used in combination with estradiol valerate for the treatment of menopausal symptoms under the brand name Gynodian Depot. The current evidence of any benefit of DHEA supplementation to menopausal and postmenopausal women is inconclusive. Whereas prasterone (DHEA) supplementation in postmenopausal women can lead to an increase in E1, E2, testosterone, DHEA, and DHEAS serum levels, and a reduction in SHBG; still, the current evidence regarding the benefits of DHEA supplementation in postmenopausal women is inconclusive—while some studies suggest potential benefits, such as improved well-being, sexual function, and possibly decreased menopausal symptoms, these findings are not universally agreed upon. Moreover, the long-term safety data for DHEA supplementation is lacking, which is a significant concern. This is particularly relevant given that DHEA supplementation can lead to increased estrogenic availability, which could potentially have implications for conditions sensitive to hormonal levels.
Vaginal atrophy Prasterone, under the brand name Intrarosa, is approved in the United States in a vaginal insert formulation for the treatment of atrophic vaginitis. The mechanism of action of prasterone for this indication is unknown, though it may involve local metabolism of prasterone into androgens and estrogens.
Sexual desire Prasterone has been used orally at a dosage of 10 mg/day to increase sexual desire in women.
Childbirth
As the sodium salt of prasterone sulfate (brand names Astenile, Mylis, Teloin), an ester prodrug of prasterone, prasterone is used in Japan as an injection for the treatment of insufficient cervical ripening and cervical dilation during childbirth.
Available forms
Prasterone was previously marketed as a pharmaceutical medication under the brand name Diandrone in the form of a 10 mg oral tablet in the United Kingdom.
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![Prasterone: Testosterone levels following a single oral dose of 300 mg crystalline (non-micronized) or micronized prasterone (DHEA) in premenopausal women.[48]](https://upload.wikimedia.org/wikipedia/commons/thumb/e/ef/Testosterone_levels_following_a_single_oral_dose_of_300_mg_crystalline_or_micronized_DHEA_in_premenopausal_women.png/1280px-Testosterone_levels_following_a_single_oral_dose_of_300_mg_crystalline_or_micronized_DHEA_in_premenopausal_women.png?utm_source=en.wikipedia.org&utm_campaign=parser&utm_content=thumbnail)
![Prasterone: Estradiol and DHEA levels after a single intramuscular injection of Gynodian Depot (4 mg estradiol valerate, 200 mg prasterone enanthate) in women.[49][50][51]](https://upload.wikimedia.org/wikipedia/commons/thumb/d/dd/Estradiol_and_dehydroepiandrosterone_levels_after_a_single_intramuscular_injection_of_Gynodian_Depot_in_women.png/1280px-Estradiol_and_dehydroepiandrosterone_levels_after_a_single_intramuscular_injection_of_Gynodian_Depot_in_women.png?utm_source=en.wikipedia.org&utm_campaign=parser&utm_content=thumbnail)
