Androderm - Androgel -Transdermal Testosterone Profile

Androderm/Androgel/Transdermal Testosterone Profile


Pharmaceutical Name: Testosterone
Molecular weight of base: 288.429
Chemical structure: 4-androstene-3-one,17beta-ol
Chemical Formula of base: C19 H28 O2
Active Life: depends on carrier of the transdermal
Anabolic/Androgenic Ratio: 100/100




Testosterone is responsible for the development and maintenance of male secondary sex characteristics. This includes it being a highly anabolic and androgenic hormone, therefore being capable of increasing users' muscle mass and strength/power when administered at larger than normal doses in the body. Transdermal testosterone compounds are those which are applied directly to the skin via creams or ointments, or else via a patch that it placed on and remains attached to the skin of the user for a period of time.

Testosterone is able to promote strength increases and muscular growth via numerous mechanisms. Of course first off testosterone promotes nitrogen retention in muscle therefore allowing the muscles to hold more protein and enabling repair and growth of those muscles. Secondly testosterone binds to the androgen receptor to promote receptor dependant mechanisms for muscular growth and fat loss (1). Testosterone also helps to increase the concentrations of androgen receptors in cells that are important for muscle growth and repair in muscle.

As mentioned, testosterone can play a role in promoting fat loss. Testosterone has the ability to bind to the androgen receptors in fat cells. This can enable the breakdown of body fat while and also deters new fat formation (2). Of course due to the fact that testosterone will encourage muscular growth, indirectly it will promote fat reduction because any excess calories are likely to be used in the muscle building process rather than being added as body fat.

Like most anabolic steroids, testosterone also increases red blood cell production. An increased number of red blood cells in the blood can improve endurance via better oxygenated blood as well as improving a user's ability to recuperate after strenuous physical activity. However it should be noted that there are other steroids and compounds out there that are far more adept at this function.

Among the other mechanisms that testosterone can help promote anabolism are via the increased production of insulin growth factor 1 it encourages, as well as suppressing the action of catabolic hormones in the body. In terms of performance enhancement, testosterone also offers numerous advantages. Namely it has the ability to increase the number of motor neurons in muscles and thereby improving muscular contraction. Like many other anabolic steroids testosterone also promotes glycogen synthesis (3). This will of course help to improve a user's endurance and strength by providing more fuel for intense workouts thus increasing endurance and strength, as glycogen is stored carbohydrates used as a fuel during exercise.

Transdermal delivery is one of the mechanisms by which testosterone, as well as other hormones and medications, can enter the blood stream of the user and thus produce the results desired. The obvious benefit of such a method is the lack of need for injections/needles, but as will be discussed later in this profile, this benefit may be overshadowed by the negative aspects of such a delivery mechanism.

Despite the limitations of the current commerically available transdermal testosterone products, new advancements in the delivery systems available for these types of compounds are being made to improve their delivery mechanisms (4, 5), with some "underground" steroid producers taking advantage of these. However it is often the case that these underground producers will not share the various ingredients that they incorporate into their products so an evaluation of their efficacy is impossible for the most part. Compounds including things such as DuroTak 87-2510, dodecylamine, span 80, propylene glycol, and octisalate, and countless others, have all been experimented with to help improve the topical delivery of compounds via active sites in the skin. However the majority of these go unused because of the lack of need in medicine for extremely high absorption rates for transdermal hormones. Massive doses are unneeded for therapeutic treatments, unfortunately for bodybuilders and strength athletes. As mentioned previously however, this has not prevented some underground steroid producers from exploiting these scientific findings.


Use/Dosing

Due to the frequent applications of transdermal creams and ointments the level of testosterone in the user is able to remain fairly stable throughout the administration of the compound. Gels and ointments may be applied from once or twice per day, to numerous times during a twenty-four hour period. Obviously the more frequent the application, the more stable the blood concentration of the hormone. Transdermal patches slowly release the hormone into the system of the user throughout its lifespan. Both methods have been demonstrated to provide more stable blood levels of the hormone then injectable versions. This is an obvious benefit when using it for hormone replacement therapy. When compared to the fact that when used in hormone replacement therapy many time testosterone enanthate and cypionate are administered only once every two to three weeks, with resulting fluctuating levels of plasma testosterone being quite large, with these levels often not being in the physiological range at least 50% of the time (6). It should be noted though that the peak plasma concentrations of the hormone delivered via most versions of transdermals never reach the same levels as those of even low doses of injectable testosterone compounds.

As with the other testosterone esters, the doses of the drug that are taken by users varies to a great degree depending on the experience and goals of the user. This also includes women administering testosterone. Women may find that transdermal testosterone is one of the most manageable of the testosterone products available along with possibly testosterone propionate, suspension or other non-estered compounds, due to the fact that it is fast acting and that the dosing and administration of the compound can be quickly altered if negative side effects become overly burdensome. With longer acting esters these adjustments are much more difficult to make rapidly and side effects could become more pronounced and/or exaggerated. For this reason, females who use testosterone may want to begin with transdermal testosterone when choosing which compound to use.

However unlike most injectable forms of testosterone, users will likely find that there is a limit to how much testosterone can be administered via the various transdermal methods. This is due to the absorption rates of the compounds and the practical restriction of how much of a product could conceivably be applied. Obviously users will not be able to use extremely large doses of testosterone via this method as they can with injectables, where some users can administer several grams of the hormone per week. However this delivery method may be suitable for those looking to run lower doses, or of course those simply looking to use replacement levels of testosterone.

Aside from the obvious dosing limitations of transdermal delivery, there is also the question of how to know exactly how much of the product in entering the system of the user and how to measure this. If one is consulting with a doctor during the use of the compound, frequent blood tests will likely be administered to determine exactly how much of the hormone is circulating in the system of the user. However, if the user is administering the product on their own without the supervision of a doctor, he or she will likely be left to their own devices to estimate how much the compound is being absorbed. This is obviously not an ideal protocol to follow as a user is unable to accurately measure the amount used no matter how experienced with anabolic steroids they are. Having said that however, most users determine whether they need to increase the amount of the product used by way of monitoring the side effects of testosterone, both negative and positive. For example libido, acne, hair growth, and other indicators can all be used to gauge the amount of testosterone being absorbed. Clearly experienced users would be far more adept at approximating their needs based on the response of the body.

In terms of application areas, low body fat areas are much more likely to result in a greater percentage of the hormone being absorbed then if one were to use areas that more body fat was stored (7). This is true of both transdermal gels/ointments and patches. Previous generations of transdermal delivery methods of testosterone once utilized scrotal site applications exclusively, however with the current delivery mechanisms in use this is no longer necessary.

Users should also apply transdermal gels by spreading them as thinly as possible, as this should also increase the rate of absorption. Heat has been demonstrated to positively affect the amount of testosterone that can be delivered via a transdermal patch as well (8). This is accomplished by applying a heat patch on top of the transdermal testosterone patch. This heat patch in turn slowly delivers a small amount of heat to the area for the duration of its application. In one study, the group using the heat patch experienced mean maximum serum testosterone concentrations of nearly one third greater then the group not using the heat patch with their treatment (8). This is quite a significant increase and one that users should take note of. However no such relationship between the application of transdermal gels/ointments and heat has been demonstrated.


Side Effects

Since transdermal testosterone is indeed simply another form of exogenous testosterone, the side effects associated with it are for the most part those commonly encountered with any type of testosterone compound. For more specific information about these, including those that may affect women, see the testosterone enanthate profile in this forum. In this section the side effects, and the characteristics of them, that are unique to transdermal testosterone alone will be dealt with.

For the most part, both the transdermal creams/ointments and patches are well tolerated by users. However the most common complaints with testosterone patches are difficulties with their adherence to the skin. With transdermal creams/ointments a small number of users reported some cases skin irritability/irritation (9, 10). It is thought that varying the areas to which the transdermal cream/ointment or patch is adhered to will lessen the severity or number of occurrences of skin irritation in users (11), however in some it is seemingly unavoidable.

As should be expected with any anabolic steroid, suppression of endogenous testosterone production will occur. Testicular atrophy is also likely to happen with such a compound (12). The usual protocol of post-cycle therapy and possibly the use of human chorionic gonadotropin during the cycle should be followed, but no special considerations need to be taken into account because of this.

A unique aspect of transdermal testosterone delivery is of course the fact that the hormone is absorbed through the skin of the user. This can in some cases cause difficulties that would never arise with the use of injectable compounds, namely accidental transfer to other persons (13). Obviously in the case of women and children this can cause serious physiological changes in some cases, but even other adult males would be wary of exogenous hormones entering their systems. Simple procedures such as washing one’s hands after applying gels and/or ointments or using rubber gloves to do so, ensuring that others do not come into contact with the areas of the skin that the gel/ointment was applied to, and that the gel/ointment is dried before the user could possibly come into contact with others should be followed. While these protocols will not completely ensure that no cross-contamination occurs, they can certainly limit the possibility.

Transdermal testosterone patches obviously have a far less greater risk of cross-contamination then transdermal gels (14). This difference is quite significant due to the two different delivery methods. Things such as sweating, vigorous activity and or rubbing of the skin surface, among others, can all alter the ability of gels to properly absorb. This is one of the benefits of using transdermal patches in comparison to gels and ointments.



References

1. Toth M., Zakar, T. Relative binding affinities of testosterone, 19-nortestosterone and their 5-alpha reduced derivatives to the androgen receptor and to other androgen-binding proteins: A suggested role of 5alpha-reductive steroid metabolism in the dissociation of "myotropic" and "androgenic" activities of 19-nortestosterone. J Steroid Biochem 17 (1982) 653-60

2. Sjogren J, Li M, Bjorntorp P. Androgen hormone binding to adipose tissue in rats. Biochim Biophys Acta. 1995 May 11;1244(1):117-20

3. Ramamani A, Aruldhas MM, Govindarajulu P. Differential response of rat skeletal muscle glycogen metabolism to testosterone and estradiol. Can J Physiol Pharmacol. 1999 Apr;77(4):300-4

4. Ainbinder D, Touitou E. Testosterone ethosomes for enhanced transdermal delivery. Drug Deliv. 2005 Sep-Oct;12(5):297-303.

5. Kuhnert B, Byrne M, Simoni M, Kopcke W, Gerss J, Lemmnitz G, Nieschlag E. Testosterone substitution with a new transdermal, hydroalcoholic gel applied to scrotal or non-scrotal skin: a multicentre trial. Eur J Endocrinol. 2005 Aug;153(2):317-26.

6. Gooren LJ, Bunck MC. Androgen replacement therapy: present and future. Drugs. 2004;64(17):1861-91.

7. Meikle AW, Matthias D, Hoffman AR. Transdermal testosterone gel: pharmacokinetics, efficacy of dosing and application site in hypogonadal men. BJU Int. 2004 Apr;93(6):789-95.

8. Shomaker TS, Zhang J, Ashburn MA. A pilot study assessing the impact of heat on the transdermal delivery of testosterone. J Clin Pharmacol. 2001 Jun;41(6):677-82.

9. Swerdloff RS, Wang C. Transdermal androgens: pharmacology and applicability to hypogonadal elderly men. J Endocrinol Invest. 2005;28(3 Suppl):112-6.

10. Wang C, Cunningham G, Dobs A, Iranmanesh A, Matsumoto AM, Snyder PJ, Weber T, Berman N, Hull L, Swerdloff RS.Long-term testosterone gel (AndroGel) treatment maintains beneficial effects on sexual function and mood, lean and fat mass, and bone mineral density in hypogonadal men. J Clin Endocrinol Metab. 2004 May;89(5):2085-98.

11. Murphy M, Carmichael AJ. Transdermal drug delivery systems and skin sensitivity reactions. Incidence and management. Am J Clin Dermatol. 2000 Nov-Dec;1(6):361-8.

12. Gray PB, Singh AB, Woodhouse LJ, Storer TW, Casaburi R, Dzekov J, Dzekov C, Sinha-Hikim I, Bhasin S. Dose-dependent effects of testosterone on sexual function, mood, and visuospatial cognition in older men. J Clin Endocrinol Metab. 2005 Jul;90(7):3838-46. Epub 2005 Apr 12.

13. Kunz GJ, Klein KO, Clemons RD, Gottschalk ME, and Kenneth Lee Jones. Virilization of Young Children After Topical Androgen Use by Their Parents. Pediatrics. 2004;114(1):282-284.

14. Mazer N, Fisher D, Fischer J, Cosgrove M, Bell D, Eilers B. Transfer of transdermally applied testosterone to clothing: a comparison of a testosterone patch versus a testosterone gel. J Sex Med. 2005 Mar;2(2):227-34.