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Testosterone is Your Friend
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Chapter 2: Androstenedione and Precursors ______________________________________________________
There are a variety of supposed testosterone precursors available including muira puama, homeopathic testosterone, Lepidium root, Tribulus terrestis, zinc formulations, tongkat ali (Longifolium), various herbal combinations, and other such concoctions scince has shown to be useless. Studies prove none of these have any value whatsoever and are simply well advertised scams. The only precursors that have any possible potential value are the androstenedione family.
Androstendedione and androstenediol are the direct pre-cursors of testosterone in mammals. These exist naturally in the 4- position structurally. There are also many analogs of these in-cluding 5- position, 19- position and nor- analogs. The only ones that have any science at all behind them are plain old, regular 4- positioned androstenedione or androstenediol. There has been an endless parade of junk science studies that purport to show how “dangerous” androstenedione is and how “ineffective” it is in raising testosterone in humans. In nearly every single one of these “studies” young men with naturally high testosterone are given huge overdoses of hundreds of milligrams of androstenedione. Even the few “studies” that used middle aged men, they were not hypogonadal and were still heavily overdosed. Since men cannot normally have high levels this overdose simply raises estrogen and estrone. Testosterone is not raised - just estrogens!!! Amazingly there have been no published studies on the responsible low-dose (i.e. 50 mg or less) use of androstenedione in hypogonadal men anywhere in the world, much less on testosterone deficient women. Women have ovaries rather than testicles and metabolize androstenedione (and androstenediol) into testosterone more efficiently than men. It may well be possible for women to take oral androstenedione to raise their testosterone, but we will need studies to see if their blood levels of androstenedione go up too much and if any excess estrone and estradiol are formed as by-products. Since one third of American women are castrated without cause and their testosterone levels are cut in half, this would certainly be much needed research.
The University of Ontario was about the only institution in the world to even address this issue (Canadian Journal of Applied Physiology v. 27, 2002, pp. 628-45). They pointed out that sublingual administration of the androstenedione family is far more effective in hypogonadal men. It is very difficult to solubilize androstenedione and it must be complexed in cyclodextrin sus-pension to dissolve under the tongue. They referred to Blacquier et al back in 1967 (Acta Endocrinologica v. 55, pp.697-704) who found that androstenediol was almost three times as effective in transforming into testosterone than androstenedione. If this is true we should be studying androstenediol rather than androstenedione primarily in both men and women. They also referred to Horton et al back in 1955 (Journal of Clinical Investigation v. 45, pp. 301-13) who was one of the only researchers in the world to show that women transform the androstenedione family into testosterone more efficiently than men. They found that about 60% of plasma testosterone is derived from androstenedione biologically in women, while only about 37% is derived in men. They referred to Mahesh et al back in 1962 (Acta Endocrinologica v. 41, pp. 400-6) where women were given completely irresponsible 100 mg doses of oral androstenedione and then 100 mg of DHEA! They also found orally administered androstenedione family hormones were very poorly absorbed by either sex, and intravenously administration was far more effective. Of course, injecting people with anything is always a poor idea unless absolutely necessary in a medical emergency. We must always remember that women only make about 300 mcg (less than one third of one milligram) of testosterone daily and a general rule is to get about 150 mcg into their blood if they are proven to be deficient.
While this is the best review ever published on testosterone prohormones, they still just didn’t comprehend that high dose oral supplementation, especially in young men, is completely irrational and merely produces estrogens. They continually referred to previous studies where healthy men with normally high testosterone levels were given irrational amounts of oral androstenedione. Again, men only produce about 6-8 mg a day of testosterone and men with normal levels should not take any at all. King et al in 1999 gave healthy young men 300 mg of oral androstenedione. Of course their estradiol and estrone levels rose dramatically, but not their testosterone. Wallace et al gave middle aged men both 100 mg of DHEA and 100 mg of androstenedione, but did not even test them to see if they were deficient in either hormone! Leder et al in 2000 gave healthy men 300 mg of androstenedione and got huge rises in both estradiol and estrone, but not testosterone. Earnest et al in 2000 gave men either 200 mg of androstenedione or androstenediol who were not low in testosterone. At least Earnest found out that the androstenediol was more effective than the androstenedione. Ballantyne et al gave healthy men 200 mg of oral androstenedione with the usual bad effects. Brown et al in 2000 gave men 300 mg of oral androstenedione and got estrogens. The list goes on. There has not been one single study giving hypogonadal middle aged or elderly men a reasonable 50 mg oral dose of any of the androstenedione prohormones, much less using the more promising androstenediol, much less using this sublingually in suspension. These completely unscientific “studies” will now be used to ban all the andro-stenedione family and make mere possession a felony punishable by five years in federal prison under the Steroid Hormone Act.
When androstenedione first became available in the marketplace in the mid-1990’s many older men successfully used this to raise testosterone levels by simply taking an inexpensive 50 mg tablet. At the time this seemed like a practical and effective means of raising testosterone without seeing a doctor to get a prescription. It should be mentioned that unreputable companies tried to promote supposedly transdermal androstenedione creams which were claimed to penetrate the skin and bypass the liver to make it more effective. These were plain and simple frauds, yet you still see them offered from time to time. Androstenedione and androstenediol are not metabolized into testosterone very effectively whether taken orally, or used transdermally. Injections are more effective but very ill advised. If you used, for example, a ridiculous 5 grams of 10% androstenedione cream (which would be 500 mg of actual androstenedione), you would only be getting about 50 mg of actual hormone into your bloodstream (a 10% absorption rate is reasonably expected here). With an 8% conversion rate you would be getting a mere 4 mg of actual testosterone in your body. That means at best that 500 mg of androstenedione would end up as a mere 4 mg of available testosterone in your blood - ideally and theoretically that is. We simply don’t know what would happen with women. Since women only produce about 300 mcg (one third of one mg) of testosterone a day it would be reasonable to experiment with using a half gram of 10% androstenedione cream on women who are low in testosterone. This might not work at all, however. Again, the research on women is ignored.
One possible answer here that has gotten almost no attention or research is to use the sublingual route especially with androstenediol rather than androstenedione. It is very difficult to dissolve any of the androstenedione family unfortunately. This can be done by cyclodextrin suspension, but only in a laboratory and not at home. Research into low dose sublingual administration of androstenediol for both men and women might turn out to be very beneficial.
One problem is that some men simply don’t metabolize oral supplemental androstenedione into testosterone and they just make estrogens from it. The biggest problem is, that after a period of time, the androstenedione is no longer effective and will not make testosterone. No matter how you choose to raise your testo-sterone you must monitor your estrone and estradiol before you start. Then you should monitor your levels every 6 months to make sure you aren’t raising your estrogens. Even if androstenedione does work for a man, and even if he is willing to monitor his estradiol and estrone every six months, it will simply stop working after a while. Obviously this just isn’t the long term answer.
Another concern is that young body builders with diminished intelligence were reading articles and advertisements in the body building magazines. They would then take very large doses of androstenedione up to several hundred milligrams per day. Since they already had high, youthful levels of testosterone they were simply raising their estradiol and estrone levels dangerously and not making any testosterone at all. Worse, they were putting themselves at risk for various forms of cancer and other serious conditions. This made the politicians jump on the legislative bandwagon to ban over the counter sales of androstenedione without a prescription. House Bill 207, Senate Bill 502, etc. are not anti-andro bills at all, but rather anti- supplement bills that will open the door to take away your rights to buy all natural hormones and supplements. There is no doubt androstenedione (as happened with the natural plant stimulant ephedrine) will soon be felony classified as an illegal drug. Then, all the natural hormones such as DHEA, melatonin, pregnenolone and progesterone will also be classified as dangerous drugs with long prison sentences for mere possession as is true in Canada and other countries.
One answer to this for both men and women is to find a medical doctor who is well educated in testosterone therapy. You can talk to your local compounding pharmacist and ask him which doctors are writing prescriptions for transdermal testosterone. Then ask him if he will make up a sublingual testosterone solution for you. The problem here is the doctor will want 1) an office visit, 2) an expensive blood test, 3) a second office visit, and 4) an expensive compounded testosterone product from the compounding pharmacist. Often the doctor won’t even make the prescription refillable. Later he’ll want more office visits and blood tests to continue your therapy. This is obviously the road to the poor house.
There are Internet sites selling both sublingual testosterone tablets and aqueous suspensions of natural testosterone. In the U.S. it is perfectly legal for you under U.S. Code 21, Section 331 to order (use registered mail) or personally import drugs from foreign countries for your own use. The problem is when you go to these Internet sites you’ll probably be confused by the array of scams such as homeopathic transdermal testosterone cream and the endless variety of dangerous weightlifter steroids offered.
The bottom line here is that androstenedione and andro-stenediol cannot be recommended long term for men since 1) the conversion is so poor, 2) the effects are temporary, 3) some men don’t convert to testosterone at all, 4) the risks of estrogen forma-tion are high, 5) it will soon be illegal, and 6) constant blood or saliva monitoring is necessary. For women we simply do not know what happens when they take oral androstenedione family pro-hormones, use transdermal cream, or use them sublingually. This would be most interesting to investigate. One study at King’s College in London (Clinical Chemistry v. 49, 2003, pp. 167-9) gave women a toxic 100 mg of oral androstenedione, which drove their testosterone levels through the roof! Five milligrams would have been a reasonable investigative dose, but only in women pro-ven to be deficient in testosterone, which these women were not at all.
If you merely add a hydrogen atom to androstenedione you get testosterone. If you merely remove a hydrogen atom from androstenediol you also get testosterone. Both of these are the direct biological precursors in mammals.
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