Androstenedione information and Androstenedione side effects by Ray Sahelian, M.D.

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Twice a month we Email you a brief abstract of several new studies on various supplements and natural medicine topics and their practical interpretation by Ray Sahelian, M.D. We will mention research updates on androstenedione hormone and natural hormones as we come across them.

 

Androstenedione is a natural steroid hormone that was available over the counter as a supplement up to March 2004. There are still at least three other hormones available over the counter including melatonin, DHEA, and pregnenolone. The FDA has banned the sale of androstenedione as an over the counter supplement so you cannot legally buy androstenedione. However I still get emails from raw material suppliers trying to sell the following, so I'm not sure if they are still legal.

1, (5 alpha) Androstene -3,17 diol
1,(5 alpha)- Androstenedione
1,4- Androstadiene 3B, 17B dione
1,4-Androstadiene-3,17, diol
19 Nor Androstenediol
3,6 17 Androstenedione
4-Androstenediol
5-alpha-Androstanediol 
5-Androstenediol
5-Androstenedione
6-Bromoandrostenedione

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The metabolism of Androstenedione to testosterone
Basically, pregnenolone, the grandmother of all steroid hormones, is converted into DHEA, which is converted into androstenedione, which can then be converted into testosterone and estrogens. Hence, androstenedione side effects are likely to be similar to the side effects of DHEA, testosterone, or other androgens, and perhaps partially similar to estrogen side effects.
     Androstenedione is mostly made in the adrenal glands and testicles but can also be made in other parts of the body. Androstenedione is banned by the International Olympics Committee, professional tennis, the National Football League and the National Collegiate Athletics Association. Androstenedione remains legal in professional baseball, where McGwire's admission (a few years ago) to using it during the season when he hit a record 70 home runs boosted its popularity.

Does androstenedione have any benefits?
Some body builders report anecdotally that they notice increased strength on the days they work out when they use androstenedione. Others use it occasionally to boost sex drive or wellbeing. Those who are young and already have high levels of testosterone or androstenedione in their system are not likely to notice much of a sex boosting effect. Middle aged and older individuals may notice the benefits more easily. Androstenedione is potentially an alternative to DHEA or testosterone as a form of androgen replacement in aging men or women.

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Androstenedione Side effects
Androstenedione can have androgenic side effects that include acne, scalp hair loss, facial hair growth in women, aggressiveness, and irritability. Chronic use can also raise levels of estrogen, something that could lead to enlarged breasts and an increased risk of certain types of cancer. Prostate enlargement could be a concern in older men. Long-term androstenedione side effects with regular use for months or years are currently not fully known.

Future potential of Androstenedione
Doctors sometimes prescribe DHEA or testosterone to middle-aged and older men and women in order to increase libido and wellbeing, along with bone strength. Androstenedione, the father of testosterone, may be an alternative.

Summary
At this point, based on our limited knowledge of androstenedione, it is difficult to make any firm recommendations. If you are planning to take androstenedione, either for its body-building potential (which is not proven), or its sex boosting effects (which not everyone notices), limit your dosage to less than 20 mg, and take it only temporarily, that is, for a few days at a time. Have off periods of a few weeks or months between use in order to minimize any potential side effects. Androstenedione may be beneficial to those who are found to be deficient in testosterone. Andorstendione may perhaps be an alternative to testosterone replacement. Androstendione may still be available by prescription through compounding pharmacies.

Androstenedione Research update
Androstenediol administered sublingually with cyclodextrin bypasses first-pass hepatic catabolism and increases serum androstenedione, free testosterone, total testosterone, and estradiol concentrations.

Hepatotoxicity of androstenedione in pregnant rats.
Food Chem Toxicol. 2005 Feb;43(2):341-4.
Androstenedione, a naturally occurring steroid hormone, is a dietary supplement used to enhance athletic performance. Little is known, however, about the safety of androstenedione use by young adults including women of child bearing age. To test the possible hepatotoxic effects of androstenedione use, this study was undertaken using a rat model. Pregnant rats (six rats/dose) were exposed to androstenedione in corn oil by gastric intubation beginning 2weeks before mating and continuing through gestation day 19. On gestation day 20, blood and livers were collected from the pregnant rats for analysis of hepatotoxicity endpoints: serum alanine aminotransferase (ALT), aspartate aminotransferase (AST), lactate dehydrogenase (LDH), glutathione (GSH) and glutathione S-transferase (GST), total microsomal P450, nuclear DNA damage and lipid peroxidation. Under these experimental conditions, no significant differences were observed in any of these biomarkers over the concentration range examined.
       
A highly publicized study indicates that androstenedione may not live up to its hype. The study published in the June 2, 1999 issue of the Journal of the American Medical Association compared 300 mg of androstenedione with a dummy pill in 20 men ages 19 to 29 during an eight-week weightlifting program. Researchers found no difference in strength between the two groups of men.

Prohormones and sport.
J Steroid Biochem Mol Biol. 2002 Dec;83(1-5):245-51.
Several precursors of testosterone and nandrolone introduced on the nutritional supplement market as performance enhancing drugs are banned in sports. Until now they are legally sold without a prescription in the US. Results of excretion studies with related compounds including 7-keto-DHEA and 1-androstenediol are presented. The main metabolites of 7-keto-DHEA are 7-hydroxylated compounds. The commercial 1-androstenediol preparation was contaminated with several other anabolic steroids. Oxidation of 1-androstenediol to 1-androstenedione seems to be the major renal metabolic pathway. Additionally contaminated nutritional supplements containing banned substances not indicated on the label were administered. The results of the excretion studies indicate that after the intake of amounts substantially lower than the recommended dose athletes can fail a doping test for periods up to 120 h.

Since the FDA has banned the over the counter sale of androstenedione, two other steroid hormones now available without a prescription are DHEA and pregnenolone.

Androstenedione Emails
Q. I have noticed my 21-year-old's personality to have completely changed after several months of weightlifting and changing to a high protein diet. In addition to that, he takes Ripped Fuel, Creatine, Androstenedione and Xenadrine RFA-1 (ephedrine). He's aggressive, somewhat confused and has recently even broken up with his girlfriend of seven years, among other things. Just last week, I witnessed him pulling out his eyebrows and eating them. When I questioned him, he said, "It's protein." I do not know how he is taking these supplements or if he even takes them simultaneously. At one point, he was taking Human Growth Factor 1 as well. I spoke with our doctor about the changes in his behavior and she believes it's the changes he's made in his diet and the supplements. He says doctors don't know what they're talking about. He has definitely developed muscles (pumped up, if you will), but it seems like it's at the expense of his disposition. Have you heard of this happening to others?
     A. Yes, it’s most likely due to the androgens along with other stimulants.

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Q. You mention that androstenedione may still be available through a doctor/RX. I have been searching and can't see to find where or who may prescribe it and where to buy androstenedione. Can you be more specific?
     A. Androstenedione is available through compounding pharmacies, you can do an internet search for them and then you need a doctor's prescription to get it filled in order to buy the androstenedione. These are special pharmacies.