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Testosterone is Your Friend
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Chapter 5: Various Delivery Systems
This is going to be a long and well cited chapter for very good reasons. It must be shown conclusively that generally me-dical doctors - even in the most respected clinics, hospitals and universities - know almost nothing about supplemental testosterone (or any other hormones). Nearly all of the very few doctors who actually administer testosterone are doing it bass ackwards and don’t have a clue as to what they’re doing. Yes, this also includes the pricey life extension clinics. We’re going to see what they are doing wrong. We’re going to see why we shouldn’t take unnatural esters either orally or by injections. We’re going to see that low doses of plain natural testosterone administered transdermally or sublingually are the most practical , safest, most effective and least expensive ways to use it. (DMSO delivery is not allowed by law and hasn’t been studied in clinics). Let’s look at some studies on the various delivery systems to see what works, what doesn’t work, and why.
You will also see why patches technically do work, but are a very overpriced promotion of the pharmaceutical corporations. Subcutaneously implanted time release pellets are natural testosterone, but are very expensive and have to be implanted surgically under the skin by a doctor. This is simply impractical and unnecessary. Even the new prescription hydroalcoholic gels sold in the chain pharmacies are weak and very overpriced. Most of the compounding pharmacists will try to vastly overcharge you for a transdermal cream that contains a mere two dollars worth (about 25 cents worth in the case of women) of actual natural testosterone. Finding a doctor who will even write a prescription for transdermal or sublingual testosterone from a compounding pharmacist can be very difficult. In 2004 we can hope that the Mexican Internet pharmacies will start legally selling transdermal testosterone (and estriol) creams by mail. Meanwhile you can choose to make your own from testosterone suspensions as discussed earlier. If you take natural testosterone by mouth it will basically be broken down as it passes through the liver. If you take large amounts (i.e. 120 mg for men) orally of an ester salt like cyprionate or undecanoate only a very small per cent of it will be absorbed and much unwanted toxic metabolites will be produced with serious side effects resulting.
At the University of Munster in 2002 (European Journal of Endocrinology v. 146, pp. 505-11) hypogonadal men were given 120 mg a day of oral undecanoate. This shows how poorly oral testosterone salts are absorbed to give them literally 3,000% (thirty times) what they need. Men only make 6 to 8 mg a day and need only 3-5 mg as a daily supplement. Of course their estrogen levels went off the scale. Even though these men were given the wrong type of testosterone in the wrong way they still got impressive benefits, albeit with side effects. If they had used natural testosterone in natural ways they would have gotten better benefits and no side effects from estrogen excess.
You can use natural sublingual testosterone in very small 3-5 mg per drop doses for men, and 0.15-0.30 milligrams (150-300 micrograms) per drop for women, but this is almost unknown. A compounding pharmacist should be able to make this upon request in a vegetable oil solution. (Testosterone does not taste good at all however.) At UCLA in Torrance in 1996 (Journal of Clinical Endocrinology and Metabolism v. 81, pp. 3654-62) hypogonadal men aged 19 to 60 were given sublingual testosterone. Unfortunately, they were given 15 mg doses which made their testosterone go up about 500% and their estradiol almost 400%. At least their FSH and LH levels fell - which is usually desirable for men. Obviously the sublingual route is very effective for a mere 15 mg to put the men completely out of range like that. Even with this overdosing the men got dramatic short term benefits such as increased lean muscle mass (but not less body fat), more strength, better bone metabolism and better blood parameters. If they had given these men proper 3-5 mg doses the results would have been better and there would have been no side effects. We can still learn important lessons with such excessive doses in that sublingual route is very effective and very practical, and using low amounts will not aromatise into estradiol or estrone. The real value of this kind of hard to find study is that the sublingual route is the most effective natural legal means we have as regards actual absorption.
If you can obtain liquid testosterone in water (the usual means of injectable) you can do this yourself if you’re careful. Evaporate the solution to dryness. For every gram of testosterone powder you have 333 X 3 mg, 250 X 4 mg or 200 X 5 mg doses. Just add 333, 250 or 200 drops of vegetable oil respectively and stir. Put one drop under your tongue everyday in the morning for three months and test for testosterone, estradiol and estrone. Always do this before noon to follow the natural cycle. This does not taste good. Your doctor and compounding pharmacist may or may not be willing to do this for you.
Injections of ester salts like propionate or enanthate are absolutely the worst possible means of delivery. Anyone who advises this is demonstrating their complete lack of knowledge. You will find very expensive so-called life extension doctors giving such injections because they are quacks. The problem here is that you get a huge rise in testosterone way over the normal range which falls daily until you are back to your subnormal levels by the next injection. In addition your estrone and estradiol levels go up grossly exceeding your normal ranges.
While patches are technically transdermal and do use natural testosterone they are very expensive, completely un-necessary and cause skin irritation from being left on day after day.
The most practical and effective means of delivery - aside from sublingual - is the transdermal route using natural, unsalted testosterone in either a cream or a gel. Again, DMSO solutions cannot be studied or used legally, but you can make your own.
Unfortunately you cannot buy a testosterone nasal spray. This would be a very effective, convenient and inexpensive way to put this right in a mucous membrane. The FDA will not allow doctors to prescribe this, pharmaceutical companies to make this, or compounding pharmacists to formulate this. If you had 99% USP natural testosterone you could make a 1% suspension (not solution) in 90% water with 10% ethanol and keep it refrigerated. Some nasal pumps deliver 100 mg of spray with each pump, so each pump would deliver 1 mg in the nasal mucosa. Three pumps therefore would deliver 3 mg most all of which would be absorbed. Researchers at the U. of Rhode Island in 1998 developed such a simple nasal delivery with excellent effectiveness but it is not approved for use even by prescription.
Again, you cannot legally buy transdermal testosterone in DMSO (dimethylsulfoxide), but you can add DMSO to your cream or gel yourself to make it more effective. If you took 100 g of 3% cream for men and added 100 g of DMSO you would then still use the usual quarter gram daily since it is so much more effective transdermally. A woman would add 100 g of DMSO to 100 g of 0.3% cream and still use the usual quarter gram. This would at least double the effectiveness of your cream or gel. DMSO is inexpensive, safe and readily available on the Internet. The very most effective natural delivery system is sublingual testosterone in DMSO solution.
Some very good work was done by SmithKline Beecham pharmaceuticals in 1996 (Journal of Clinical Pharmacology v. 36, pp.732-9). They did use expensive patches which they referred to as “delivery systems” because that is what they produce for profit. You should understand that a year’s worth of patches is only about 7 grams of testosterone at a cost of about $10. They charge over $1,300 a year for the patches so the profit margin is quite obvious. They used 2.5 mg, 5.0 mg and 7.5 mg of actually delivered testosterone in hypogonadal men aged 35 to 56. They did not say how many mg are contained in the Androderm® patch and what per cent of that actually went into the blood. The 2.5 mg delivered dose barely raised their levels to low normal. The 5 mg dose brought up the levels by about 50% into normal desired range. The 7.5 mg put the men unnecessarily into the high normal range This was a very thorough and well done study where they clearly distinguished between bound and bioavailable levels and compared them. They also pointed out that testosterone applied directly to the scrotum results in 5-alpha reductase activity which converts this into high levels of undesirable DHT. The point here is that when 5 mg actually enter the bloodstream this is a practical dose to start with and will work for some men, but too high for others. Women only need 150 to 300 mcg (micrograms) delivered as they utilize this more efficiently than men.
SmithKline Beechum did another study in 1998 (Journal of Clinical Pharmacology v. 38, pp. 54-90). Here they just used the 5 mg delivered dose since it was the most practical and effective. Again, they used the patches on thin skin such as the back. Here they reveal that the 5 mg delivered patch contains 24.4 mg of testosterone, so only about 20% goes into the blood while it is applied. DHT and estradiol did not go up with such normal doses. The only drawback here is the high cost of the patches, whereas creams and gels are inexpensive.
At UCLA in Torrance in 2000 (Journal of Clinical Endocrinology and Metabolism v. 85, pp. 964-9) the researchers used a 1% gel on hypogonadal men aged 26 to 59 years old. The problem here is that they applied 10 grams (!) a day which is 100 mg of hormone. The blood levels went up a dangerous 500% and the DHT and estradiol levels also rose dangerously. What is wrong with these people? They should add a permeation enhancer to their gel since they only claimed a 10% delivery. Applying, say, 20 mg and delivering 5 mg into the blood would have given good results. They noted that the average male production is only 6-7 mg a day. Imagine slathering ten grams of gel on your body every day! If they had done the equivalent with women they would have used one gram of gel with 10 mg of testosterone and caused severe androgenocity. You wonder how educated people can do such things. One revelation was that it is better to use four different sites for application rather than one single site for better penetration.
These very same researchers published another study in the same journal (p. 4500-10) where they even compared the 5 mg delivered patch. They still couldn’t figure out that applying 100 mg of testosterone was completely irresponsible. At least this time they did try a 5 gram gel as well as their usual 10 gram dose. They still didn’t figure it out.
Incredibly these same people did a third study in the same journal (p. 2839-53) wasting 15 more pages. In this study they cut the dose down to 5 grams of gel (50 mg of testosterone). They found that men increased lean muscle mass and strength, had better blood parameters, decreased fat mass, improved their mood, enhanced their sexual activity and generally benefited dramatically from the treatment. They claim their hydroalcoholic gel only delivers less than 12% of the contained testosterone, so they should find a permeation enhancer to improve such poor performance.
More studies on the Androderm® patches were done at the famous Karolinska Institute in Sweden in 1997 (Clinical Endocrinology v. 47, pp. 727-37). The men aged 21 to 65 were given the 5 mg delivered patches and raised their testosterone immediately to desired youthful levels without raising estradiol or DHT. They also lowered FSH and LH which is a desirable benefit in aging men. The men were first subjected to testosterone enanthate injections of over 200 mg every three weeks which produced the usual terrible results. Intramuscular (i.m.) injections gave extreme peaks of 42 nmol and extreme lows of only 7 nmol (normal is about 24 nmol). The patches, on the other hand, produced excellent results with the exception of skin irritation in some men. The usual physical and psychological benefits were achieved including curing gynecomastia (male breast growth), weight loss, increased libido, less depression and improved mood.
At the well known Johns Hopkins Center in Baltimore in 2001 (Journal of Clinical Endocrinology & Metabolism, v. 86, pp. 1026-33) a more professional study was done with 70 references. The transdermal patches were used with excellent results. Hypo-gonadal men aged 21 to 65 were first given the intramuscular injections of enanthate ester. This, as usual, resulted in extreme fluctuations with over range and then under range values between the injections. This also resulted in extreme fluctuations with very high estradiol levels. The men using the patches very much improved their vital testosterone to estrogen ratios. They found that that low testosterone was correlated with higher BMI (body mass index) generally, and higher testosterone with lower BMI. Low testosterone is very correlated with obesity in other words. There were many of the usual benefits associated with raising their levels to youthful ones. Intelligent, professional studies like this using natural testosterone to produce normal levels will change medicine and demonstrate the proper use of supplemental hormones.
Other doctors walk in perpetual darkness it seems. Surprisingly, at the Karolinska Institute in 1995 (Journal of Steroid Biochemistry v. 55, pp. 121-7) healthy young men with naturally high testosterone were given weekly injections of 250 mg of testosterone enanthate. The rationale for this egregious behavior was to help determine how to detect illegal steroid use in professional athletes. Estrone and estradiol levels went through the roof and stayed there for the entire nine month period. Testosterone went way over normal levels in these young healthy men. LH (luteinizing hormone) almost disappeared and the testosterone to LH ratio went up one thousand (i.e. 1,000) times! There is no point in wasting any more time on such complete lack of professionalism other than to demonstrate how callous some doctors can be to the very health and well being of their patients.
To show you how some doctors do not want to advance, learn, grow or improve medical practice we just have to look at a 2001 review with a full 43 references from Massachusetts General Hospital in Boston. Here, after reviewing much of the vast body of worldwide published literature on the many proven benefits of testosterone they still call this “controversial”. They were insightful enough to admit that oral and injected routes are very inferior to the transdermal delivery method as the safest and most effective means of supplementation. Yet, their conclusion was, “In summary, the potential benefit of testosterone in the aging male is still controversial and awaits the results of large, randomized, placebo-conrolled studies.” They go on to say, “Testosterone therapy has the potential to cause a number of adverse events and is classified as a Schedule III controlled substance.” There are no adverse events whatsoever when natural testosterone is used transdermally in proper amounts. Some people just hate progress obviously.
More incompetence comes from the University of Munster in 2002 (Journal of Andrology v. 23, pp. 419-25) where unfortun-ate men were injected with 1,000 mg (yes, that is one whole gram) of testosterone undecanoate esters every six weeks for over three years. Testosterone levels would go to dangerous heights and then fall again to subnormal levels. Estradiol levels went off the charts. They claimed “no statistically significant changes in prostate volume” occurred, but the average prostate size almost doubled due to the extreme estradiol and estrone levels. These misguided souls concluded, “injections of TU at intervals of up to 3 months offer an excellent alternative for substitution therapy of male hypo-gonadism.” A mental institution might be an appropriate place for such practicioners.
A revealing study was done at Koln University in Germany in 1999 (Metabolism Clinics and Experiments v. 48, pp. 590-6). Here hypogonadal men were given four different delivery systems: 1) 100 mg oral mesterolone, 2) 160 mg oral undecanoate ester, 3) 250 mg i.m injected enanthate ester every second day, and 4) a 1,200 mg crystalline (s.c.) subcuteaneous implant. In 1999 at a major European university this is how incompetent top physicians are. Mesterolone is a dangerous, toxic anabolic steroid, and 25 mg is the normal dose. Huge oral doses of esters are toxic and raise estradiol levels. Such dangerous injections of esters every two days have severe side effects. A crystalline implant of 1,200 mg delivers far too much testosterone too quickly. After poisoning these poor men four different ways they said their total cholesterol, LDL, and triglycerides rose while HDL fell. Words fail me here.
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