Sustanon® 100 (testosterone blend)
Description:
Sustanon® 100 is an oil-based injectable testosterone blend that contains three different testosterone esters: testosterone propionate (20 mg); testosterone phenylpropionate (40 mg); and testosterone isocaproate (40 mg). This product is manufactured by Organon, and is essentially a lower dosed version of their Sustanon® 250. Like Sustanon® 250, Sustanon® 100 makes use of multiple esters of testosterone to produce a desired slow-acting effect. The different esters have different levels of oil solubility, and likewise rates of release from the site of injection. The design is such that the rapid distribution of testosterone is followed by a sustained release of hormone. Sustanon® 100 is shorter acting than Sustanon® 250, as it lacks the longer decanoate ester, and is usually administered on a biweekly basis. This drug is ultimately very similar to testosterone cypionate or enanthate, but with a slightly shorter window of therapeutic effect.
History:
Sustanon® 100 is a modern adaptation of the well-known injectable testosterone blend Sustanon® 250, both of which were developed by the international pharmaceutical giant Organon (now Merck/MSD). Sustanon® 100 is essentially a lower dosed equivalent of Sustanon® 250, supplying the same hormone in a similar (though not exact) time-released fashion. Sustanon® 100 is recommended for the same medical uses as Sustanon® 250, namely treating male androgen insufficiency, which can manifest itself with such symptoms as reduced sex drive, impotence, infertility, and bone loss. Increased adiposity (fat mass) and reduced lean mass are also common with patients suffering from low androgen levels. In addition to these uses, Sustanon® 100 is also recommended to induce masculinization in female-tomale transsexuals. Sustanon® 100 is produced only in a handful of countries at this time, and is not widely available.
How Supplied:
Sustanon® 100 is available in select human drug markets. All products are supplied in 1 mL glass ampules.
Structural Characteristics:
Sustanon® 100 contains a mixture of three testosterone compounds, which weere modified with the addition of carboxylic acid esters (propionic, propionic phenyl ester, and isocaproic acids) at the 17beta hydroxyl group. Esterified forms of testosterone are less polar than free testosterone, and are absorbed more slowly from the area of injection. Once in the bloodstream, the ester is removed to yield free (active) testosterone. Esterified forms of testosterone are designed to prolong the window of therapeutic effect following administration, allowing for a less frequent injection schedule compared to injections of free (unesterified) steroid. Sustanon 100 is designed to provide a rapid peak in testosterone levels (24-48 hours after injection), and maintain physiological concentrations for approximately 14 days.
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. An anti-estrogen such as clomiphene citrate or tamoxifen citrate may be necessary 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 antiestrogens, however, and may also have negative effects on blood lipids.
Estrogenic side effects will occur in a dose-dependant manner, with higher doses (above normal therapeutic levels) of testosterone more likely to require the concurrent use of an antiestrogen or aromatase inhibitor. Since water retention and loss of muscle definition are common with higher doses of testosterone, this drug is usually considered a poor choice for dieting or cutting phases of training. Its moderate estrogenicity makes it more ideal for bulking phases, where the added water retention will support raw strength and muscle size, and help foster a stronger anabolic environment.
Side Effects (Androgenic):
Testosterone is the primary male androgen, responsible for maintaining secondary male sexual characteristics. Elevated levels of testosterone are 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. Those concerned about hair loss may find a more comfortable option in nandrolone decanoate, which is a comparably less androgenic steroid. 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 5alpha 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.1
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 nonaromatizable), 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.
Testosterone tends to have a much less dramatic impact on cardiovascular risk factors than synthetic steroids. This is due in part to its openness to metabolism by the liver, which allows it to have less effect on the hepatic management of cholesterol. The aromatization of testosterone to estradiol also helps to mitigate the negative effects of androgens on serum lipids. In one study, 280 mg per week of testosterone ester (enanthate) had a slight but not statistically significant effect on HDL cholesterol after 12 weeks, but when taken with an aromatase inhibitor a strong (25%) decrease was seen.2 Studies using 300 mg of testosterone ester (enanthate) per week for 20 weeks without an aromatase inhibitor demonstrated only a 13% decrease in HDL cholesterol, while at 600 mg the reduction reached 21%.3 The negative impact of aromatase inhibition should be taken into consideration before such drug is added to testosterone therapy.
Due to the positive influence of estrogen on serum lipids, tamoxifen citrate or clomiphene citrate are preferred to aromatase inhibitors for those concerned with cardiovascular health, as they offer a partial estrogenic effect in the liver. This allows them to potentially improve lipid profiles and offset some of the negative effects of androgens. With doses of 600 mg or less of testosterone per week, the impact on lipid profile tends to be noticeable but not dramatic, making an antiestrogen (for cardioprotective purposes) perhaps unnecessary. Doses of 600 mg or less per week have also failed to produce statistically significant changes in LDL/LDL cholesterol, triglycerides, apolipoprotein B/C-III, C-reactive protein, and insulin sensitivity, all indicating a relatively weak impact on cardiovascular risk factors.4 When used in moderate doses, injectable testosterone esters are usually considered to be the safest of all anabolic/androgenic steroids.
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 testosteronestimulating 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.
Administration (General):
Testosterone propionate is often regarded as a painful injection. This is due to the very short carbon chain of the propionic acid ester, which can be irritating to tissues at the site of injection. Many sensitive individuals choose to stay away from this steroid completely, their bodies reacting with a pronounced soreness and low-grade fever that may last for a few days after each injection.
Administration (Men):
To treat androgen insufficiency, the prescribing guidelines for Sustanon® 100 call for a dosage of 100 mg (1 ampule) every 2 weeks. Although active in the body for a longer time, Sustanon® 100 is usually injected every 7 to 10 days for muscle-building purposes. This schedule will allow for the higher doses most commonly applied by athletes, and more stable elevations in hormone level. The usual dosage among male athletes is in the range of 200-600 mg per week, taken in cycles 6 to 12 weeks in length. This level is sufficient for most users to notice exceptional gains in muscle size and strength. Testosterone is ultimately very versatile, and can be combined with many other anabolic/androgenic steroids depending on the desired effect.
Administration (Women):
Sustanon® 100 is rarely used with women in clinical medicine. When applied, it is most often used to induce masculinization in female to male transsexuals. Sustanon® 100 is not recommended for women for physique- or performance-enhancing purposes due to its strong androgenic nature, tendency to produce virilizing side effects, and slow-acting characteristics (making blood levels difficult to control).
Availability:
Sustanon® 100 is less widely distributed on the black market than Sustanon® 250, due to the fact that source countries producing this drug are limited. The moderate total amount of drug contained in each ampule (100 mg) also makes this product far less desirable to consumers than Sustanon® 250. Sustanon® 100 is mainly located in the Netherlands, Egypt, and the United Kingdom.
1 Enzyme induction by oral testosterone. Johnsen SG, Kampmann JP, Bennet EP, Jorgensen F. 1976 Clin Pharmacol Ther 20:233-237.
2 High-density lipoprotein cholesterol is not decreased if an aromatizable androgen is administered. Karl Friedl, Charles Hannan et al. Metabolism 39(1) 1990:69-74.
3 Testosterone dose-response relationships in healthy young men. Bhasin S, Woodhouse L et al. Am J Physiol Endocrinol Metab 281: E117281, 2001.
4 The effects of varying doses of T on insulin sensitivity, plasma lipids, apolipoproteins, and C-reactive protein in healthy young men. Singh A, Hsia S, et al. J Clin Endocrinol Metab 87:136-43, 2002.