Dr. Testosterone
By George Touliatos, MD

17-ALKYLATED AAS

17-alkylated androgenic-anabolic steroids (AAS) is a class of synthetic derivatives of testosterone, which have undergone a specific modification (methylation) in the 17 position. This enables oral steroids to sustain the first entrance to the liver. However, this fact stresses hepatic parenchyma, thus elevating liver enzymes known as transaminases (alanine transaminase ALT/SGOT and aspartate transaminase AST/SGPT).

17-alkylated AAS include:

1. stanozolol (both oral and injectable form)

2. oxymetholone

3. methandienone (there was an injectable form by Ciba)

4. oxandrolone

5. fluoxymesterone

6. methyltrienolone (M3)

They are not aromatized, except methandienone-methandrostenolone, perhaps the most widely abused AAS pill.They are powerful anabolic agents, while during a dieting period they have a strong anti-catabolic effect. They also provide necessary aggressiveness during training, especially in periods of harsh dieting.

Methandrostenolone – methandienone (Dianabol) is a derivative of methyl-testosterone. Methandienone aromatizes and the administration of an anti-estrogenic agent is necessary (anastrozole-letrozole-exemestane or tamoxifen-mesterolone) in order to avoid gynecomastia, or the retention of water and lipogenesis-fat storage. The edema followed by aromatization process is beneficial for muscle glycogen formation. This is something very important for anabolism, since strength and stamina are enhanced. Muscle are able to contract much better and look fuller and “pumped.” This water retention, due to estrogenic activity, lubricates synovial cavities – hence it protects the joints.

Methandienone is medically used during postoperative syndromes, when the patient is malnourished and needs immediate assimilation of nutrients and tissue regeneration. It is also very useful against muscle wasting and cachexia.

Dianabol’s half-life is estimated around six hours; therefore it should be administrated four times a day during the course of 24 hours.

Dianabol’s use is often linked to acne and skin inflammation. This could be the result of aromatization and its moderate androgenic index.

Oxymetholone (Anadrol 50) is medically prescribed for aplastic anemia and it increases EPO production from the kidneys. Iron absorption improves in the small intestine and erythrocytosis process improves. As a result, hemoglobin protein elevates, and so does hematocrit. From a chemical point of view, oxymetholone is a DHT derivative. Therefore, aromatization is something out of the question.

However, oxymetholone’s metabolites have showed a great affinity for the estrogen receptors. This is something observed under an estrogenic environment. When oxymetholone is administrated alone, while beta-estradiol levels are relatively low, there is no particular aromatization. However, under the presence of other AAS with estrogenic activity, aromatization occurs. This explains why within a gaining cycle with testosterone, nandrolone, boldenone and methandienone, oxymetholone seems to aromatize and be able for extreme water retention. Increased blood pressure, due to sodium retention, is a common side effect of it, while often the feeling of nausea and the tendency to vomit appears. Its androgenic property leads to acne and aggressive behavior. Its half-life is around nine hours, which means it should be administrated twice a day.

Oxandrolone (Anavar) is a powerful anabolic steroid pill (per os), with a more powerful anabolic index than oxymetholone comparing mg/mg. Its low androgenic index makes it preferable among females, in order to avoid the non-reversible side effects of androgens (hirsutism, voice deepening, clitoris enlargement).

Oxandrolone is a derivative of dihydrotestosterone (DHT). Since there is no aromatization and considerable low androgenic activity, the suppression of HPTA is less. Adversely, it is hepatotoxic, causing elevation of the liver enzymes, known as transaminases (SGOT-AST, SGPT-ALT). It also distorts atheromatic index and lipoprotein ratio (HDL/LDL). Oxandrolone can increase ATP/CP production, thus making it a useful tool among explosive sports in track athletics (sprinting, jumps).

The fact it does not lead to any aromatization, water retention and edema, makes oxandrolone a favorable AAS among athletes with the weight class. Among bodybuilders, oxandrolone is highly abused during pre-contest preparations, while dieting. In doses >50mg daily, it increases serum free thyroxine (FT4) and contributes to catabolism of adipose tissue and lipolysis (beta-oxidation). Its half-life is approximately eight hours, so it should be taken three times during the day.

The hepatotoxic fluoxymesterone (Halotestin) is a testosterone derivative, highly androgenic (eight times more than testosterone) and anabolic as well. It is ideal for sports, dealing with weight class (boxing, wrestling, bodybuilding, and weightlifting). Halotestin provides an enormous increase in strength, which in combination with a low-carb diet, offers muscle density and thickness. Fluoxymesterone’s supreme androgenicity favors prostate enlargement-hypertrophy, acne, androgenic alopecia, hirsutism, erythocytosis plus beta-oxidation of adipose tissue and aggressiveness.

As a 17-alkylated AAS, causes distortion of the atheromatic index and the lipoproteins ratio (HDL/LDL cholesterol) and pharmaceutical hepatitis. Furthermore, it increases systemic blood pressure and along with the adverse side effect on lipoproteins, increases the risk of cardiovascular disease and myocardial infarction.

Fluoxymesterone is speculated to cause neurotoxicity, affecting the central nervous system. Episodes of insomnia, aggression (physical and verbal), irritability, anxiety, neurosis, mood swings-emotional instability, hypomania and depression have been associated with this substance abuse. However, these effects are correlated with the severity of abuse in terms of dosage and time period, the psychiatric background of the individual, and the simultaneous use of different neurotoxic chemicals (ethanol or narcotics).

As a testosterone derivative and as a highly androgenic agent, fluoxymesterone is highly suppressive to the HPTA. Fluoxymesterone shouldn’t be abused for longer than four weeks, along with proper supplementation (milk thistle, NAC, glutathione).

Since it does not aromatize and convert to estrogen, Halotestin is a preferable drug during pre-contest preparation and prolonged dieting. Although it is considered to be highly anabolic, the fact it does not lead to any form of edema makes this steroid a poor bulking agent. However, it is more likely to be used during off-season timing, for gaining strength purposes, or among powerlifters and Olympic weightlifters.

Methyltrienolone (M3) is a trenbolone’s derivative, perhaps the most hepatotoxic oral among the 17-alkylated AAS. It was initially medically used against advanced breast cancer, as an alternative treatment to the rise of estrogens. It has a similarity to trenbolone, with an enormous androgenic/anabolic ratio. Its effectiveness is so high, that it requires minimum doses of 0.5-1mg. M3 does not convert to estrogens, therefore there is no aromatization process. As a result, methyltrienolone is an ideal steroid during pre-contest preparation and sports dealing with weight categories (wrestling, weightlifting, boxing, and bodybuilding).

The extreme liver toxicity involves pharmaceutical hepatitis, where liver transaminases are elevated (>100) and cholestasis, where serum elevations of cholestatic markers such as ALP, gamma-GT, bilirubin-direct/indirect, are present. Methyltrienolone also distorts the atheromatic index (HDL/LDL) and liver lipoproteins ratio, increasing the risk of cardiovascular disease and myocardial infarction.

The injectable (parenteral) form of stanozolol (Winstrol depot) is less toxic to the liver, since it avoids the first hepatic entrance and enters directly into circulation. It is a suspension and usually painful, when administrated intramuscularly. Its half-life is around 24 hours, which practically means that has to be daily administrated, preferably an hour before workout. Injectable stanozolol could lead to local inflammation accompanied with fever, while in extreme cases; it may lead to an intramuscular abscess.

Generally, suspension steroids are more likely to develop microbes compared to oily injections. Contamination is something easier to occur in suspensions (stanozolol, testosterone, trenbolone base). Unlike other oily injectable steroids, stanozolol tends to remove water from the joints. This is something based on the aldosterone inhibition (mineral corticosteroid). Therefore, stanozolol is an anabolic steroid that does not lead to any water retention. Consequently, joints aren’t lubricated and synovial cavities dry and literally get "toasted.” Stanozolol should not be combined with Accutane (retinoic acid), a drug against cystic acne. Accutane dries mucous membranes, causing dry skin and reduction of sebum production. This effect, combined with the drain of water from synovial space, leads to tendons and ligaments rupture.

Stanozolol suspension has a milky-whitish appearance, with a relatively low concentration (50mg/ml). As with all anabolic steroids, stanozolol is capable for tissue growth and repair. It also has the ability for collagen fibers connective tissue synthesis. Its authenticity is checked, after we let an ampoule vertically for about an hour. Afterwards, we should observe the water and the sediment ratios (1/1). If the water’s percentage is superior to the white powder, then it is highly possible to be underdosed. By that, we refer to the suspension’s concentration. This case scenario seems better, related to a faked steroid, where the supposed substance does not exist. However, that could be also related to the size of particles within the suspension. Usually, expensive compounds are faked with cheaper ones. For instance, methenolone (Primobolan) and oxandrolone (Anavar) are faked by nandrolone (Deca-Durabolin) and methandienone (Dianabol).

Winstrol depot should be preferably administrated one hour prior to the gym, since the absorbability is immediate (100%), as with all suspensions.

George Touliatos, MD is an author, lecturer, champion competitive bodybuilder and expert in medical prevention regarding PED use in sports. Dr. Touliatos specializes in medical biopathology and is the medical associate of Orthobiotiki.gr and Medihall.gr, Age Management and Preventive Clinics in Athens, Greece. Heis the author of four Greek books on bodybuilding, has extensively developed articles for www.anabolic.org and is the medical associate for the book Anabolics, 11th Edition (2017). Dr. Touliatos has been a columnist for the Greek editions of MuscleMag and Muscular Development magazines, and has participated in several seminars across Greece and Cyprus, making numerous TV and radio appearances, doing interviews in print and online. His personal website is https://gtoul.com/

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