Prasterone, also known as dehydroepiandrosterone (DHEA).
Brand names Intrarosa and Gynodian Depot among others.
It is a medication as well as over-the-counter dietary supplement.
It 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 administered by mouth, or by application to the skin, through the vagina, or by injection into muscle.
Routes of administration- oral, vaginal insert, intramuscular injection, as prasterone enanthate, injection as prasterone sodium sulfate.
Bioavailability 50%.
Metabolism Hepatic.
Metabolites:
Androsterone
Etiocholanolone
DHEA sulfate
Androstenedione
Androstenediol
Testosterone
Dihydrotestosterone
Androstanediol
Estrone
Estradiol
Elimination half-life DHEA: 25 minutes, DHEA-S: 11 hours
Excretion Urine
Side effects in women include: symptoms of masculinization, acne, increased hair growth, voice changes, and increased sexual desire, headaches, insomnia, and others.
A naturally occurring prohormone of androgens and estrogens.
It is an agonist of the androgen and estrogen receptors, the respective biological targets of androgens like testosterone and estrogens like estradiol.
DHEA and DHEA sulfate are produced by the adrenal glands.
With adrenal insufficiency, there may be deficiency of DHEA and DHEA sulfate.
Levels of DHEA and DHEA sulfate steroids decrease throughout life and are 70 to 80% lower in the elderly relative to levels in young adults.
It can be used to increase DHEA and DHEA sulfate levels in adrenal insufficiency and older age.
But where there is a deficiency of these steroids, clinical benefits of supplementation, is uncertain.
It is sometimes used as an androgen in menopausal hormone therapy.
Approved in the United States in a vaginal insert formulation for the treatment of atrophic vaginitis.
As the sodium salt of prasterone sulfate 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.
It is produced naturally in the human body.
Not known to be associated with adverse effects, and it is not known whether prasterone is safe for long-term use.
Reported side effects include: acne, heart rhythm problems, liver problems, hair loss, and oily skin.
It may also alter the body’s regulation of blood sugar.
Some believe prasterone supplements might actually raise the risk of breast cancer, prostate cancer, heart disease, diabetes, and stroke, and it may stimulate tumor growth in types of cancer that are sensitive to hormones, such as some types of breast, uterine, and prostate cancer.
It may increase benign prostatic hyperplasia (BPH).
As a steroid hormone, high doses may cause aggressiveness, irritability, trouble sleeping, and the growth of body or facial hair on women.
It may stop menstruation.
It may lower the levels of HDL cholesterol), which could raise the risk of heart disease.
It may promote tamoxifen resistance in breast cancer.
With hormone replacement therapy patients may have more estrogen-related side effects when taking prasterone.
It may interfere with other medicines, and potential interactions between it and drugs are possible.
It is possibly unsafe for pregnancy, breastfeeding, hormone sensitive conditions, liver problems, diabetes, depression or mood disorders, polycystic ovarian syndrome (PCOS), or cholesterol problems.
Possess few or no side effects even at very high dosages.
It may cause masculinization and other androgenic side effects in women and gynecomastia and other estrogenic side effects in men.
It is metabolized into androgens and estrogens in the body.
It is transformed into androstenedione by 3β-hydroxysteroid dehydrogenase (3β-HSD) and into androstenediol by 17β-hydroxysteroid dehydrogenase.
Androstenedione and androstenediol can be converted into testosterone by 17β-HSD and 3β-HSD, respectively.
Subsequently, testosterone can be metabolized into dihydrotestosterone by 5α-reductase.
Androstenedione and testosterone can be converted into estrone and estradiol by aromatase, respectively.
Its transformation into androgens and estrogens is tissue-specific, occurring for instance in the liver, fat, vagina, prostate gland, skin, and hair follicles, among other tissues.
Prasterone supplementation dosages have ranged from 20 to 1,600 mg per day.
In people with adrenal insufficiency, oral dosages of 20 to 50 mg/day have been found to restore DHEA and DHEA-S levels to normal ranges.
Oral dosages of 100 to 200 mg/day prasterone have been found to result in supraphysiological levels of DHEA and DHEA-S.
At a high dosage of 1,600 mg/day orally for 4 weeks, treatment of postmenopausal women with prasterone has been found to increase serum levels of DHEA by 15-fold, and testosterone by 9-fold.
It can reliably increase testosterone levels in women, but not in men.
Available over-the-counter as a dietary supplement in the United States following the passage of the Dietary Supplement Health and Education Act of 1994.
In 2016, it was approved in an intravaginal gel formulation for the treatment of painful sexual intercourse due to vulvovaginal atrophy.
Marketed under the names DHEA and DHEA-S.
It is legal to sell in the United States as a dietary supplement.
It is a prohibited substance under the World Anti-Doping Code of the World Anti-Doping Agency.
In elderly men can induce a small but significant positive effect on body composition that is strictly dependent on prasterone conversion into its bioactive metabolites such as androgens or estrogens.
In middle-aged men, no significant effect of prasterone supplementation on lean body mass, strength, or testosterone levels was found in a randomized placebo-controlled trial.
Evidence exists sufficient to suggest that low serum levels of DHEA-S may be associated with coronary heart disease in men, but insufficient to determine whether prasterone supplementation would have any cardiovascular benefit.
There is some evidence of short-term benefit in those with systemic lupus.
Prasterone supplementation has not been found to be useful for memory function or a treatment for Alzheimer’s disease, but there is no evidence that it is effective.
In the short term clinical studies it improves mood.