Dehydroepiandrosterone (DHEA)

Products

Vaginal suppositories containing dehydroepiandrosterone were registered in many countries in 2020 (Intrarosa). The active ingredient is referred to as prasterone in medications. Furthermore, an intramuscular injection solution containing the prodrug prasterone antate has been registered in many countries (Gynodian Depot). In the United States, dietary supplements (“dietary supplements”) containing dehydroepiandrosterone (DHEA) have been allowed to be sold freely since 1994, which contributed to the DHEA hype in the 1990s.

Structure and properties

Dehydroepiandrosterone (C19H28O2, Mr = 288.4 g/mol) is a natural steroid hormone. DHEA-S is the metabolite DHEA sulfate, which is formed in the body and is in equilibrium with DHEA.

Effects

DHEA (ATC A14AA07) has predominantly indirect androgenic and estrogenic effects. It is a natural and endogenous substance produced in the zona reticularis of the adrenal gland, the ovaries, and the brain, among others. It is a precursor hormone (prohormone) that is converted in the body into estrogens (estrone, estradiol) and androgens (androstenedione, androstenediol, testosterone), i.e. into female and male sex hormones. DHEA also binds directly to receptors in the central nervous system as a so-called neurosteroid.

Indications for use

Medical indications:

  • Local treatment of vulvovaginal atrophy in postmenopausal women (vaginal suppositories).
  • Hormonal replacement therapy due to natural or surgical menopause (injectable).

Other indications:

  • In some countries, DHEA is also explicitly approved for pain during sexual intercourse (dyspareunia).
  • DHEA was touted, especially in the 1990s, as an “anti-aging” drug, a fountain-of-youth hormone and a remedy for a wide variety of diseases. Due to the possible health risks, it should not be taken uncritically as an over-the-counter “dietary supplement” from our point of view.
  • Lupus erythematosus (in many countries no approval).

Dosage

According to the professional information. DHEA is administered topically and systemically. Vaginal suppositories are inserted intravaginally.

Abuse

DHEA can be abused as an anabolic steroid and as a doping agent and is prohibited both during and outside of athletic competition.

Contraindications

  • Hypersensitivity
  • Known, previous or suspected breast cancer.
  • Known or suspected estrogen-dependent malignant tumors (eg, endometrial cancer).
  • Untreated endometrial hyperplasia.
  • Unresolved genital bleeding
  • Previous or current venous thromboembolism (deep vein thrombosis, pulmonary embolism).
  • Existing or recent arterial thromboembolic disease (e.g., angina pectoris, myocardial infarction)
  • Known thrombophilic diseases
  • Acute liver disease or history of liver disease until results return to normal in liver function tests
  • Porphyria
  • Pregnancy

Full precautions can be found in the drug label.

Adverse effects

With vaginal use, the most common potential adverse effects include weight fluctuations, vaginal fluoride, and abnormal PAP smear results. With systemic therapy, other adverse effects occur.