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Androstenediol

Last Updated on May 19, 2021 by MyFormulary

Related Terms

  • 1,5alpha-Androsten-3,17-dione (1AD), 1,5alpha-androsten-3beta,17beta-diol, 19-norandrostenediol, 19-norandrostenedione, 3beta,17beta-androstenediol (AD), 4-androstenediol, 5-androstenediol, (Adiol), alpha-androstenediol, “Andro” prohormones, androstenediol 3-sulfate (ADIOLS), androstenediol glucuronide (3alpha-diol-G), androstenedione, beta-androstenediol, dehydroepiandrosterone, DHEA metabolite, methyl androstenediol.

Background

  • Testosterone prohormones, such as androstenediol, androstenedione, and dehydroepiandrosterone (DHEA), have been marketed as testosterone-enhancing and muscle-building nutritional supplements for the past decade. They have recently become more readily available in many countries through the Internet.
  • Androstenediol and other prohormones have been shown to increase androgen prohormone, testosterone, and estradiol levels in humans. However, despite promotional claims, studies have not demonstrated bodybuilding or sexually enhancing effects with prohormone supplements like androstenediol.
  • Research suggests that androstenediol may be less effective when taken by mouth.
  • Prohormone supplements, including androstenediol, are associated with potentially harmful side effects, including abnormal estrogen, testosterone and lipid levels, and the potential to contribute to cancerous cell growth.
  • Due to a lack of human benefit and the potential for negative health effects, the risk to benefit ratio of using androstenediol and other prohormone substances seems unfavorable. Prohormones are currently on the International Olympic Committee’s list of banned substances and are banned from many professional athletic sports. Moreover, some forms have been banned for over-the-counter sales by the U.S. Food and Drug Administration (FDA). Androstenediol is not currently listed on the FDA everything added to food in the United States (EAFUS) database, which contains ingredients added directly to food that the FDA has either approved as food additives or listed or affirmed as generally regarded as safe (GRAS).

Evidence Table

    Disclaimer

    These uses have been tested in humans or animals. Safety and effectiveness have not always been proven. Some of these conditions are potentially serious, and should be evaluated by a qualified healthcare provider.

    A A – A


    C C – C

*Key to grades:

Tradition

    Disclaimer

    The below uses are based on tradition, scientific theories, or limited research. They often have not been thoroughly tested in humans, and safety and effectiveness have not always been proven. Some of these conditions are potentially serious, and should be evaluated by a qualified healthcare provider. There may be other proposed uses that are not listed below.

Dosing

    Disclaimer

    The below doses are based on scientific research, publications, traditional use, or expert opinion. Many herbs and supplements have not been thoroughly tested, and safety and effectiveness may not be proven. Brands may be made differently, with variable ingredients, even within the same brand. The below doses may not apply to all products. You should read product labels, and discuss doses with a qualified healthcare provider before starting therapy.

  • Adults (18 years and older)

    • Research suggests that androstenediol may be less effective when taken by mouth.
    • An androstenediol-cyclodextrin complex that was placed under the tongue increased testosterone and estradiol levels in the blood.
  • Children (under 18 years old)

    • There is no proven safe or effective dose for androstenediol in children.

Safety

    Disclaimer

    The U.S. Food and Drug Administration does not strictly regulate herbs and supplements. There is no guarantee of strength, purity or safety of products, and effects may vary. You should always read product labels. If you have a medical condition, or are taking other drugs, herbs, or supplements, you should speak with a qualified healthcare provider before starting a new therapy. Consult a healthcare provider immediately if you experience side effects.

  • Allergies

    • Avoid in individuals with known allergy/hypersensitivity to androstenediol or any of its constituents.
  • Side Effects and Warnings

    • There is a lack of formal safety data on the effects of androstenediol in humans.
    • Sales of androstenediols and other pro-androgen hormones without a prescription are prohibited in the United States.
    • Avoid use in pregnant or lactating women due to a lack of available scientific evidence.
    • Avoid use in children due to a lack of available scientific evidence.
    • Avoid in individuals with estrogen- or testosterone-dependent cancers. Researchers have reported that androstenediol may enhance the growth of these cancers, and its androgenic effects were not blocked by two potent antiandrogens: hydroxyflutamide (Eulexin®) and bicalutamide (Casodex®).
    • Avoid in individuals in whom testosterone or estrogen supplementation is not recommended.
    • Use cautiously in men undergoing anti-androgen therapy or in individuals taking estrogenic or androgenic agents. Androstenediol has been shown to increase serum levels of androgen prohormone, testosterone, and estradiol.
    • Use cautiously in individuals with low serum levels of high density lipoprotein (HDL), as androstenediol may lower HDL levels.
    • There have been reports of prohormones containing prohibited substances, such as ephedrine, caffeine, or steroids, which were not listed on the product labels.
    • Achilles tendon ruptures have been linked to androstenediol use.
  • Pregnancy and Breastfeeding

    • Androstenediol is not recommended in pregnant or breastfeeding women due to a lack of available scientific evidence.
    • Some evidence suggests that androstenediol may be involved in modifying the maternal immune response during and after pregnancy.

Interactions

    Disclaimer

    Most herbs and supplements have not been thoroughly tested for interactions with other herbs, supplements, drugs, or foods. The interactions listed below are based on reports in scientific publications, laboratory experiments, or traditional use. You should always read product labels. If you have a medical condition, or are taking other drugs, herbs, or supplements, you should speak with a qualified healthcare provider before starting a new therapy.

  • Interactions with Drugs

    • Androstenediol may interact with androgens and estrogens, as it has been shown to increase levels of estradiol, testosterone, and many of its analogues.
    • Androstenediol may interact with cholesterol-lowering agents, as it has been shown to lower high-density lipoprotein (good cholesterol) levels.
    • Androstenediol may interact with anticancer agents. Androstenediol may stimulate the growth of breast cancer cells and exert androgenic activity on prostate cancer cells, but it may stop the growth in other cancer or tumor cells.
    • Andrenostenediol may also interact with hydrocortisone, aminoglutethimide-plus-hydrocortisone, antibiotics, antivirals, and immunosuppressants.
  • Interactions with Herbs and Dietary Supplements

    • Androstenediol may interact with androgens and phytoestrogens, as it has been shown to increase levels of estradiol, testosterone, and many of its analogues.
    • Androstenediol may interact with cholesterol-lowering agents, as it has been shown to lower high-density lipoprotein (good cholesterol) levels.
    • Androstenediol may interact with anticancer agents. Androstenediol may stimulate the growth of breast cancer cells and exert androgenic activity on prostate cancer cells, but it may stop the growth in other cancer or tumor cells.
    • Andrenostenediol may also interact with dehydroepiandrosterone (DHEA), antibacterials, antivirals, and immunosuppressants.

Attribution

  • This information is based on a systematic review of scientific literature edited and peer-reviewed by contributors to the Natural Standard Research Collaboration ().

Bibliography

    Disclaimer

    Natural Standard developed the above evidence-based information based on a thorough systematic review of the available scientific articles. For comprehensive information about alternative and complementary therapies on the professional level, go to . Selected references are listed below.

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    View Abstract
  • Ayotte, C, Levesque, JF, Cle, roux M, et al, A. Sport nutritional supplements: quality and doping controls. Can J Appl Physiol 2001;26 Suppl:S120-S129.
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  • Battista, V, Combs, J, and Warme, WJ. Asynchronous bilateral achilles tendon ruptures and androstenediol use. Am J Sports Med 2003;31(6):1007-1009.
    View Abstract
  • Broeder, CE. Oral andro-related prohormone supplementation: do the potential risks outweigh the benefits? Can J Appl Physiol 2003;28(1):102-116.
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  • Brown, GA and McKenzie, D. Acute resistance exercise does not change the hormonal response to sublingual androstenediol intake. Eur J Appl Physiol 2006;97(4):404-412.
    View Abstract
  • Brown, GA, Martini, ER, Roberts, BS, et al. Acute hormonal response to sublingual androstenediol intake in young men. J Appl Physiol 2002;92(1):142-146.
    View Abstract
  • Leszczynski, DE and Schafer, RM. Metabolic conversion of six steroid hormones by human plasma high-density lipoprotein. Biochim Biophys Acta 4-24-1991;1083(1):18-28.
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  • Miyamoto, H, Yeh, S, Lardy, H, et al. Delta5-androstenediol is a natural hormone with androgenic activity in human prostate cancer cells. Proc Natl Acad Sci USA 9-15-1998;95(19):11083-11088.
    View Abstract
  • Reed, MJ, Purohit, A, Woo, LW, et al. Steroid sulfatase: molecular biology, regulation, and inhibition. Endocr Rev 2005;26(2):171-202.
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  • Saudan, C, Baume, N, Robinson, N, et al. Testosterone and doping control. Br J Sports Med 2006;40 Suppl 1:i21-i24.
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  • Schmidt, M, Kreutz, M, Loffler, G, et al. Conversion of dehydroepiandrosterone to downstream steroid hormones in macrophages. J Endocrinol 2000;164(2):161-169.
    View Abstract
  • Shackleton, CH, Roitman, E, Phillips, A, et al. Androstanediol and 5-androstenediol profiling for detecting exogenously administered dihydrotestosterone, epitestosterone, and dehydroepiandrosterone: potential use in gas chromatography isotope ratio mass spectrometry. Steroids 1997;62(10):665-673.
    View Abstract
  • Tagawa, N, Hidaka, Y, Takano, T, et al. Serum concentrations of androstenediol and androstenediol sulfate, and their relation to cytokine production during and after normal pregnancy. Steroids 2004;69(10):675-680.
    View Abstract
  • Ziegenfuss, TN, Berardi, JM, and Lowery, LM. Effects of prohormone supplementation in humans: a review. Can J Appl Physiol 2002;27(6):628-646.
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