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Androstenediol

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Related terms
Background
Evidencetable
Tradition
Dosing
Safety
Interactions
Attribution
Bibliography

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

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. GRADE *


Androgen prohormones are widely promoted for their effects on building lean body mass, reducing body fat, and enhancing physical endurance. Androstenediol and other prohormones have been shown to increase testosterone and estradiol levels in humans. However, significant improvements in muscle mass and athletic performance have not been observed in human studies.
C
* Key to grades

A: Strong scientific evidence for this use
B: Good scientific evidence for this use
C: Unclear scientific evidence for this use
D: Fair scientific evidence for this use (it may not work)
F: Strong scientific evidence against this use (it likley does not work)


Tradition / Theory

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.

  • Body fat reducer, hemophilia, hormone imbalances (testosterone), immunostimulation, mood enhancement, neuroprotection, sexual activity enhancement.

Dosing

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

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

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 (www.naturalstandard.com).

Bibliography
  1. Ando, S, De Amicis, F, Rago, V, et al. Breast cancer: from estrogen to androgen receptor. Mol Cell Endocrinol 7-31-2002;193(1-2):121-128.
  2. 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.
  3. Battista, V, Combs, J, and Warme, WJ. Asynchronous bilateral achilles tendon ruptures and androstenediol use. Am J Sports Med 2003;31(6):1007-1009.
  4. Broeder, CE. Oral andro-related prohormone supplementation: do the potential risks outweigh the benefits? Can J Appl Physiol 2003;28(1):102-116.
  5. 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.
  6. 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.
  7. 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.
  8. Loria, RM. Immune up-regulation and tumor apoptosis by androstene steroids. Steroids 2002;67(12):953-966.
  9. 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.
  10. Reed, MJ, Purohit, A, Woo, LW, et al. Steroid sulfatase: molecular biology, regulation, and inhibition. Endocr Rev 2005;26(2):171-202.
  11. Saudan, C, Baume, N, Robinson, N, et al. Testosterone and doping control. Br J Sports Med 2006;40 Suppl 1:i21-i24.
  12. Schmidt, M, Kreutz, M, Loffler, G, et al. Conversion of dehydroepiandrosterone to downstream steroid hormones in macrophages. J Endocrinol 2000;164(2):161-169.
  13. 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.
  14. 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.
  15. Ziegenfuss, TN, Berardi, JM, and Lowery, LM. Effects of prohormone supplementation in humans: a review. Can J Appl Physiol 2002;27(6):628-646.

Copyright © 2011 Natural Standard (www.naturalstandard.com)


The information in this monograph is intended for informational purposes only, and is meant to help users better understand health concerns. Information is based on review of scientific research data, historical practice patterns, and clinical experience. This information should not be interpreted as specific medical advice. Users should consult with a qualified healthcare provider for specific questions regarding therapies, diagnosis and/or health conditions, prior to making therapeutic decisions.


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