Testoderm — testosterone

Testoderm and Testoderm TTS are testosterone delivery systems that utilize a “patch” to deliver the hormone transdermally. Both products were designed to deliver an approximate 5 mg dose of testosterone to the body over a 24-hour period, after which point the patch is replaced with a fresh one. Testoderm is an older matrix-type skin patch, which uses no penetration enhancers, so it must be applied on the scrotum, where the skin is much more permeable to testosterone. Testoderm TTS is a newer reservoir-type skin patch containing an alcoholic gel of testosterone, which can be placed on the arm, back, or upper buttocks. Testoderm and Testoderm TTS are designed to mimic the natural circadian rhythm of testosterone release in healthy young men, higher during the first 12 hours and lower during the next 12 hours of each day. The clinical significance of this, if any, is not known.

Brand name Testoderm, Testoderm TTS
Androgenic 100
Anabolic 100
Standard Standard
Chemical Names 4-androsten-3-one-17beta-ol
17beta-hydroxy-androst-4-en-3-one
Estrogenic Activity moderate
Progestational Activity low

Testoderm History

Testoderm was developed in the United States by Alza Corporation, and introduced for sale in 1998. The drug is FDA-approved for testosterone replacement therapy in men with a deficiency or absence of endogenous testosterone. The Testoderm system itself did not make use of any penetration enhancers, and consequently is applied to an area of shaved scrotal skin, which is about 5 times more permeable to testosterone than normal body skin. Lacking an integrated adhesive, Alza soon released an updated version of Testoderm called simply Testoderm With Adhesive. Testoderm was an effective androgen replacement product, but did have the slight disadvantage of elevating DHT levels in many patients due to the prominence of 5-alpha reductase in the scrotum.

Testoderm was ultimately the first testosterone patch to be developed for commercial sale. While it was deemed a success initially, it was soon obsolete next to the newer and less intrusive Androderm patch (FDA approved in 1995). Alza released Testoderm TTS in 1998, in an effort to retain its share of the male androgen replacement market. The new updated patch can be placed on three types of skin (back, arms,and upper buttocks), and has the advantage of causing less skin irritation next to Androderm. It also does not require that the patient rotate application sites each day. Since its approval in the U.S., Testoderm TTS has also been approved in select markets abroad, although not widely.

How is Testoderm Supplied

Testoderm, Testoderm With Adhesive, and Testoderm TTS transdermal testosterone systems are available in select human drug markets. Each comes in the form of a transdermal patch system, which delivers approximately 5 mg of testosterone each.

Structural Characteristics of Testoderm

Testoderm is a matrix-type transdermal drug delivery system that contains testosterone (free) enclosed in a skin-applied patch. Testoderm TTS is reservoir-type transdermal drug delivery system that contains testosterone (free) enclosed in a skin-applied adhesive patch. Both are designed to provide steady but varying levels of testosterone transdermally during each 24-hour period of application.

Testoderm Side Effects (Estrogenic)

Testosterone is readily aromatized in the body to estradiol (estrogen). The aromatase (estrogen synthetase) enzyme is responsible for this metabolism of testosterone. Elevated estrogen levels can cause side effects such as increased water retention, body fat gain, and gynecomastia. Testosterone is considered a moderately estrogenic steroid. Exceeding therapeutic doses will increase the likelihood of estrogenic side effects. In such cases, an anti-estrogen such as clomiphene citrate or tamoxifen citrate is commonly applied to prevent estrogenic side effects. One may alternately use an aromatase inhibitor like Arimidex (anastrozole), which more efficiently controls estrogen by preventing its synthesis. Aromatase inhibitors can be quite expensive in comparison to anti-estrogens, however, and may also have negative effects on blood lipids.

Testoderm Side Effects (Androgenic)

Testosterone is the primary male androgen, responsible for maintaining secondary male sexual characteristics. Exceeding therapeutic doses is likely to produce androgenic side effects including oily skin, acne, and body/facial hair growth. Men with a genetic predisposition for hair loss (androgenetic alopecia) may notice accelerated male pattern balding. Women are warned of the potential virilizing effects of anabolic/androgenic steroids, especially with a strong androgen such as testosterone. These may include deepening of the voice, menstrual irregularities, changes in skin texture, facial hair growth, and clitoral enlargement.

In androgen-responsive target tissues such as the skin, scalp, and prostate, the high relative androgenicity of testosterone is dependant on its reduction to dihydrotestosterone (DHT). The 5-alpha reductase enzyme is responsible for this metabolism of testosterone. The concurrent use of a 5-alpha reductase inhibitor such as finasteride or dutasteride will interfere with site-specific potentiation of testosterone action, lowering the tendency of testosterone drugs to produce androgenic side effects. It is important to remember that anabolic and androgenic effects are both mediated via the cytosolic androgen receptor. Complete separation of testosterone’s anabolic and androgenic properties is not possible, even with total 5-alpha reductase inhibition.

Testoderm Side Effects (Hepatotoxicity)

Testosterone does not have hepatotoxic effects; liver toxicity is unlikely. One study examined the potential for hepatotoxicity with high doses of testosterone by administering 400 mg of the hormone per day (2,800 mg per week) to a group of male subjects. The steroid was taken orally so that higher peak concentrations would be reached in hepatic tissues compared to intramuscular injections. The hormone was given daily for 20 days, and produced no significant changes in liver enzyme values including serum albumin, bilirubin, alanine-amino-transferase, and alkaline phosphatases.

Testoderm Side Effects (Cardiovascular)

Anabolic/androgenic steroids can have deleterious effects on serum cholesterol. This includes a tendency to reduce HDL (good) cholesterol values and increase LDL (bad) cholesterol values, which may shift the HDL to LDL balance in a direction that favors greater risk of arteriosclerosis. The relative impact of an anabolic/androgenic steroid on serum lipids is dependant on the dose, route of administration (oral vs. injectable), type of steroid (aromatizable or non-aromatizable), and level of resistance to hepatic metabolism. Anabolic/androgenic steroids may also adversely affect blood pressure and triglycerides, reduce endothelial relaxation, and support left ventricular hypertrophy, all potentially increasing the risk of cardiovascular disease and myocardial infarction. Therapeutic doses of testosterone used to correct insufficient androgen production in otherwise healthy aging men are unlikely to increase atherogenic risk, and may actually reduce the risk of cardiovascular mortality.

To help reduce cardiovascular strain it is advised to maintain an active cardiovascular exercise program and minimize the intake of saturated fats, cholesterol, and simple carbohydrates at all times during active AAS administration. Supplementing with fish oils (4 grams per day) and a natural cholesterol/antioxidant formula such as Lipid Stabil or a product with comparable ingredients is also recommended.

Testoderm Side Effects (Testosterone Suppression)

All anabolic/androgenic steroids when taken in doses sufficient to promote muscle gain are expected to suppress endogenous testosterone production. Testosterone is the primary male androgen, and offers strong negative feedback on endogenous testosterone production. Testosterone-based drugs will, likewise, have a strong effect on the hypothalamic regulation of natural steroid hormones. Without the intervention of testosterone-stimulating substances, testosterone levels should return to normal within 1-4 months of drug secession. Note that prolonged hypogonadotrophic hypogonadism can develop secondary to steroid abuse, necessitating medical intervention.

Testoderm Administration (General)

Testoderm is applied daily (in the morning) to intact, clean, shaven dry skin of the scrotum. Testoderm TTS is applied daily (in the morning) to intact, clean, dry skin of the back, arms, or upper buttocks. Many OTC ointments will significantly reduce the penetration of testosterone when applied to the skin before use, and should be avoided.

Testoderm Administration (Men)

To treat androgen insufficiency, the prescribing guidelines for Testoderm and Testoderm TTS recommend the application of one patch daily, which delivers approximately 5 mg of testosterone systemically. For physique- or performance-enhancing purposes, higher doses would be necessary to achieve supraphysiological levels of testosterone. This would require at least three or four patches per day, delivering approximately 15-20 mg of testosterone. This level is sufficient for most users to notice gains in muscle size and strength, although this is not a very realistic idea in a practical sense. Lower doses may be used, but typically when accompanied by other anabolic/androgenic steroids. Testosterone is ultimately very versatile, and can be combined with many other anabolic/androgenic steroids to tailor the desired effect.

Testoderm Administration (Women)

Testoderm and Testoderm TTS are not FDA-approved for use in women. Testosterone is not recommended for women for physique- or performance-enhancing purposes due to its strong androgenic nature and tendency to produce virilizing side effects.

Testoderm Availability

Given their high relative price and low delivery of testosterone, Testoderm and Testoderm TTS are not commonly traded on the black market. Counterfeits have not yet been reported.

References

Wlliam Llewellyn (2011) - Anabolics

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