Standard Testosterone (Standard)
Chemical Names 4-androsten-3-one-17beta-ol, 17beta-hydroxy-androst-4-en-3-one
Estrogenic Activity moderate
Progestational Activity low
Androderm is a testosterone delivery system that utilizes an adhesive “patch” to deliver the hormone transdermally. The testosterone itself is dissolved in an alcoholic gel similar to AndroGel®, except here the gel is contained in a protected external drug reservoir. This design provides approximately double the hormone bioavailability of AndroGel®, and also severely limits the transfer of testosterone to other people during rigorous skin-to-skin contact. The patches come in two strengths, 2.5 mg and 5 mg, indicating the amount of testosterone each is to supply systemically over a 24-hour period (they contain 12.2 and 24.3mg of testosterone respectively). Androderm® was 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.
Androderm® was developed in the United States by TheraTech (Salt Lake City). It was approved for sale as a prescription agent by the Food and Drug Administration in September 1995, and is indicated for testosterone replacement therapy in men with a deficiency or absence of endogenous testosterone. This includes cases of primary hypogonadism, which may be caused by cryptorchidism, bilateral torsion, orchitis, vanishing testis syndrome, orchiectomy, Klinefelter’s syndrome, chemotherapy, or alcohol/heavy metal toxicity. It is also prescribed to treat hypogonadotrophic hypogonadism, including patients with luteinizing hormone or luteinizing hormone-releasing hormone (LHRH) deficiency caused by tumors, injury, or radiation. Primary hypogonadism is usually characterized by low testosterone and high gonadotropin (LH/FSH) levels, while hypogonadotrophic hypogonadism is usually associated with low testosterone and low to normal gonadotropin levels. Watson currently sells this product in the United States under the Androderm® brand name. In Europe, the ATMOS® brand from Astra is most commonly found.
TheraTech’s transdermal testosterone system is available in select human drug markets, where it is commonly sold as Androderm® or ATMOS®. It is produced in two strengths, one containing 12.2mg of testosterone, and one containing 24.3mg of testosterone. These are intended to deliver approximately 2.5 mg and 5 mg of testosterone systemically to the patient over a 24-hour period.
Androderm® is a transdermal drug delivery system that contains an alcoholic gel of testosterone (free) enclosed in an adhesive patch with a protected drug reservoir. It is designed to provide steady but varying levels of testosterone transdermally during each 24-hour period of application.
Figure 1. Mean serum testosterone concentrations (ng/dL) measured during single-dose applications of two Androderm 2.5 mg systems applied at night to the back. The figures reflect the greatest response in a study comparing four different sites of application (abdomen, back, thigh and upper arm) in 34 hypogonadal men. Source: Androderm® prescribing information. Watson Pharma, Inc.
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.
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.421
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.422
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.
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.
The above side effects are not inclusive. For more detailed discussion of potential side effects, see the Steroid Side Effects section of this book.
Androderm® is applied daily (before bed) to intact, clean, dry skin of the back, upper arms, thighs, and/or abdomen. The site(s) of application should be rotated so that no patch is reapplied to the same area in less than 7 days. Lower bioavailability may be noticed in some areas of the body, such as the chest and calves. Androderm should not be applied to the scrotum. It should also not be applied over a bony area of the body, or any part of the body that could be subject to prolonged pressure during sleep or sitting. Application to these sites has been associated with burn-like blister reactions. Skin irritation causes approximately 1 in 20 patients to discontinue treatment. Irritation may be ameliorated by treatment of the affected area with over-the-counter topical hydrocortisone cream applied after the patch is removed. A small amount of prescription 0.1% triamcinolone acetonide cream may also be applied to the center of each patch before application, which should reduce irritation and not significantly alter the transdermal absorption of testosterone. Many OTC ointments will significantly reduce the penetration of testosterone when applied to the skin before use, and should be avoided.
To treat androgen insufficiency, the prescribing guidelines for Androderm® recommend two 2.5 mg patches or one 5 mg patch per day. Morning serum testosterone levels are later measured, at which point the physician may adjust upwards or downwards if necessary. 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 5 mg or eight 2.5 mg 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.
Androderm® is 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.
Transdermal testosterone patches are manufactured in many countries worldwide, and remain widely available. Common trade names include Androderm® and ATMOS®. Given the high sophistication and low black market value, counterfeits have not yet been reported.
421. Enzyme induction by oral testosterone. Johnsen SG, Kampmann JP, Bennet EP, Jorgensen F 1976 Clin Pharmacol Ther 20:233-237.
422. Testosterone replacement, cardiovascular system and risk factors in the aging male. Vigna GB, Bergami E. J Endocrinol Invest. 2005;28(11 Suppl Proceedings):69-74.