Transdermal Testosterone

[Smokey729]

Transdermal Testosterone
(testosterone)
Transdermal Testosterone has been marketed heavily in the Hormone Replacement Therapy Market for the last decade. For over 50 years, testosterone therapy has been used for the treatment of hypogonadism. In recent years, there has been an increase in the use of testosterone therapy for men with late-onset hypogonadism, sometimes referred to as andropause. Testosterone therapy in older and hypogonadic men can significantly improve their sense of well-being, and lead to increases in muscle and bone mass, upper body strength, virility and libido (5). Oral delivery of unmodified testosterone is not really a viable option, due to its rapid first-pass metabolism, possible liver toxicity, and its relatively short half-life. Thus, injectable testosterone was used for a very long time as an effective hormone replacement method. Roughly a decade ago, alternatives to injectable and oral testosterone were developed. Originally, these alternative methods of application for testosterone meant shaving an area of the skins surface (*usually the scrotum... no, really) and attaching a testosterone patch with low, dry heat (again, no, really) like a hairdryer, which basically hot-glued the testosterone patch to the scrotum. I cant see, for the life of me, the logic employed by the doctor who thought this method was preferable to weekly or twice-monthly injections. Luckily, this painful procedure progressed to the point where its at now, and you can simply apply a self sticking patch or rub some testosterone gel anywhere on your body, and get the same effect. Recently, the BALCO scandal featured many references to the gel method. I think, for an adequate understanding of these types of products, were going to have to take a look at both the drug (testosterone) as well as the method of administration (transdermal delivery), and see how they work together, and how they compare with testosterone injections.






When some (nonscrotal) transdermal testosterone preparations have been examined, they showed that the plasma concentration of TS increased very rapidly, and reached the peak level within 3-6 hours of application of the experimental patch..(2) This is comparable with some of the better oral products out there, in my experience, an athlete would usually swallow a pill than have a patch hanging on them for a day, though.


Basically, you can expect all of the benefits of injectable testosterone with the transdermals (if the mg doses were the same, which they are not). What were dealing with here is Androderm, which is a patch containing 12.2mgs of testosterone, and androgel, which gives you about the same (you only get 10% of the total drug contained in the preparation... thus a hundred mgs of test in a gel form, would yield a 10mg amount in your body).


Heres a chart comparing a transdermal with an injectable, both using testosterone:






Steady-state pharmacokinetic profiles of T, BT, DHT, and E2 profiles during nightly applications of TTD systems (n = 27; , left panels) and biweekly IM injections of T enanthate (n = 29; X, right panels) measured at week 16. Dashed lines denote upper and lower limits of normal range based on morning serum samples (T, 306-1031 ng/dL; BT, 92-420 ng/dL; DHT, 28-85 ng/dL; E2, 0.9-3.6 ng/dL). Error bars denote SD.(1)


Not so great, huh? A mere 100mg shot of injectable testosterone provides much higher peak plasma concentrations of testosterone, even though the transdermal testosterone was more stable, with regards to blood plasma levels. So what are the advantages of transdermal application? Clearly, it provides a very stable blood level of the compound administered. I know it seems like Im killing you with charts, but take a look at this one:






Serum T concentrations (mean SE) before (day 0) and after transdermal T applications on days 1, 30, 90, and 180. Time 0 h was 0800 h, when blood sampling usually began. On day 90, the dose in the subjects applying T gel 50 or 100 was up- or down-titrated if their preapplication serum T levels were below or above the normal adult male range, respectively. In this and subsequent figures the dotted lines denote the adult male normal range, and the dashed lines and open symbols represent subjects whose T gel dose were adjusted.


So its consistent, ..but who cares? The levels of testosterone it give us are just enough to provide a slight boost, at a high (financial) cost. Wouldnt it be great if we could get this stuff dosed more highly? Or maybe even with clen, so we could apply it directly to fatty areas? Or with Tren? That would be great, huh? It would even have potential for first time needle-phobic steroid users to use items which were formerly only available as an injectable! Women could use a Tren product without leaving needle marks! In fact...with a little creativity, underground labs could even make transdermal products which would never get caught by customs (perhaps disguised as stickers or whatever).


Anyway...I guess thats not in the cards, though...


Lets move on...


One particularly successful transdermal testosterone delivery method involves the combination of DuroTak 87-2510 as an adhesive polymer. This is combined with 3% dodecylamine and 10% span 80. This, combined with testosterone creates a nice transdermal delivery system (4). Another experimental transdermal testosterone preparation contains occlusion, octisalate (OS), and propylene glycol (PG), called Solugel (which is a proprietary hydrogel containing PG 25% w/w) and Tegaderm (a semipermeable film dressing) on the permeation of TES was assessed. Occlusion had no effect on the permeation of TES, however, OS increased the flux of TES 2.9-fold. The concentration of PG which produced optimal TES flux was 20% v/v, and this concentration resulted in a 1.9-fold increase in TES permeation. By combining OS, PG, and occlusion, transdermal testosterone permeation through the skin was increased 8.7-fold, which was a synergistic enhancement, obviously, meaning the sum of the parts was far more than their individual totals (3). Why did I bother telling you all of the ingredients, which can easily be found at a chemical supply house, and bought legally? Certainly not so you could make your own transdermal preparations of testosterone (or Tren, or clen, or whatever)& that would be illegal. Even though you now know the ingredients, and could just make a gel with them and some testosterone (or tren, from Finaplex pellets), and create your own transdermal drug delivery product. That would be wrong&


References:



jcem.endojournals.org/content/vol84/issue10
In vitro and in vivo evaluation of a novel nonscrotal matrix-type transdermal delivery system of testosterone. Drug Dev Ind Pharm. 2005 Mar;31(3):257-61.
Synergistic enhancement of testosterone transdermal delivery. J Control Release. 2005 Apr 18;103(3):577-85.
The current status of therapy for symptomatic late-onset hypogonadism with transdermal testosterone gel. Eur Urol. 2005 Feb;47(2):137-46.
Effects of androgen substitution on lipid profile in the adult and aging hypogonadal male. Eur J Endocrinol. 2004 Oct;151(4):415-24. Review.
[Gruenewald, Matsumoto. J Am Geriatr Soc 2003;51:101; Morales. Aging Male 2004; in press].




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[Presser]

TESTOSTERONE GELS AND CREAMS

The only way to go, in my professional opinion, if physician and patient agree on a transdermal (TD) delivery system. Or TRT at all. As I have gained knowledge and experience, my position is now that TD’s are vastly superior to other modalities in TRT medicine. They are easy to apply, usually well absorbed, and rapidly establish stable serum androgen levels (by the end of the third day). I recommend all practitioners first try a testosterone gel for their TRT patients. Gels are better than creams, as I want the rapid T uptake into the dermal layer, which serves as reservoir for distribution throughout the day. Men do better on lower serum T levels on TD’s than IM.

The constant variability of serum androgens provided by T gels mimic the hormones of a young man; the stable daily level provided by T injections mimic the hormones of an old man; those of implantable pellets mimic the hormones of no one. Entropic hormone levels are part and parcel of the process of youth.
Much is made of the risk posed by accidental transferal of testosterone to others, such as children or sexual partners. Simply covering with a T-shirt has been shown to block transfer of the hormone. The testosterone sinks into the skin within an hour. One may shower, or even swim, without worry, usually after four hours. I remind my patients most of us have neither the time, nor the opportunity, for romance until evening (given the usual early morning application), and a quick shower is always nice for a gentleman to “freshen up” prior to same.

Gels and creams, like all transdermal delivery systems, provide a greater boost in DHT levels, compared to injectable testosterone preparations. As DHT is responsible for all the things of manhood--literally, AllThingsMale--the transdermals are better at treating sexual dysfunction than are injectables. However, issues of hair loss (which I treat with a compounded topical DHT blocking mixture) and possible prostate morbidity (a contentiously debatable point, to be sure, but resolved in the negative to my mind) then come into play. This might be a good time to mention I vehemently oppose adding finasteride or similar medication.

To end the debate on this topic, transdermal T gels/creams are more likely to elevate estrogen than injections, as long as the shots are properly administered once per week. That is because aromatase lives in the skin, along with higher concentrations of 5-AR, which converts T to E. Even so, the benefits of TD TRT outweigh the weekly convenience of shots.

Some have reported an increase in hair growth over the application area(s). All physicians who administer TRT must be prepared to disappoint their patients at this time by pointing out, sadly, this same effect cannot be achieved upon the scalp.

TESTOSTERONE INJECTION

I’ll start out by describing the drawbacks of IM testosterone. They are inconvenient for patients who do not wish to give themselves their own injections, as they must then make weekly trips to your office for same. Why IM test MUST be dosed weekly will be described in detail in another section. And this TRT modality represents hundreds of holes poked in their body over a lifetime. Some patients, as you well know, just hate shots (although I have noticed patients who had initially claimed this, but admitted, once they had come to enjoy the benefits of TRT, came to very much look forward to their shot day). And no doubt an invasive delivery system brings more risk than, for instance, a testosterone gel or cream (the best choice for TRT), although I have yet to hear of a single bad outcome from any of the tens of thousands of IM injections my patients have self-administered.

As a good and proper Osteopathic Physician, I am loath to introduce any substance to the body not absolutely necessary. Therefore the oil and preservative necessary to the injectable preparation are best avoided when possible, in my professional opinion.

When considering dosing of testosterone cypionate, it is important to remember that, due to the weight of the cypionate ester, a 100mg injection delivers, at best, 70mg of testosterone. This is important to keep in mind when comparing the effects of a 100mg weekly injection of test cyp to the 35mg total initial dose provided by Androgel/Testim 5gms QD over the same period.

HCG

Many practitioners consider this incredible hormone treatment of choice for hypogonadotropic (secondary) hypogonadism. Such certainly is intuitive, as supplementing with a LH analog indeed increases testosterone production in patients who do not concurrently suffer primary hypogonadism. But for some unexplained reason, while serum T levels may be adequately elevated, the patients simply do not report realization of the subjective benefits of TRT, when HCG is administered as sole TRT. You also run the risk of inducing LH insensitivity at higher dosages, and therefore may actually cause primary hypogonadism while attempting to treat secondary hypogonadism. HCG, especially at higher doses (defined as >500IU per shot), also dramatically increases aromatase activity, thus inappropriately elevating estrogens. Progesterone—a feminizing hormone in adult males—also elevates at those dosages. Personally, I recommend giving no more than 100IU of HCG per day, as starting dose. And please give it some time to work.

A real benefit of HCG is that it will prevent testicular atrophy. I do not think we should ignore the aesthetics of that consideration. Your patients will feel the same way.