Anabolics

1. Testosterone: The Foundation of Anabolism

Testosterone is the reason males carry more muscle mass than women, as the two sexes have vastly contrasting amounts of this hormone.

The primary male hormone. Testosterone, produced mainly in the testes, is the key androgen responsible for male characteristics, including a deepened voice, facial hair, and libido. It also plays a crucial role in muscle growth, making it the foundation upon which all anabolic steroids are built. The hormone exerts its effects by binding to androgen receptors within cells, triggering a cascade of events that ultimately lead to increased protein synthesis and muscle accumulation.

Anabolic vs. Androgenic. Testosterone's effects are both anabolic (muscle-building) and androgenic (masculinizing). While anabolic steroids aim to enhance the anabolic effects, complete separation from androgenic properties remains elusive. The ratio of these effects varies among different steroids, influencing their suitability for different users and goals.

Hormone levels. Men typically produce 2.5 to 11 mg of testosterone per day, while women produce only about 1/4 mg. This difference explains the significant disparity in muscle mass between the sexes. Understanding testosterone's basic functions is crucial for grasping how anabolic steroids work and their potential effects on the body.

2. Unlocking Muscle Growth: Direct and Indirect Mechanisms

As follows, if we are able to increase our androgen level from an external source by supplementing testosterone or a similar anabolic steroid, we can greatly enhance the rate in which protein is retained by the muscles.

Direct androgen receptor activation. The primary mode of action for anabolic steroids is the direct activation of the cellular androgen receptor, leading to increased protein synthesis. This means that by increasing androgen levels through supplementation, the rate at which muscles retain protein is significantly enhanced, directly contributing to muscle growth.

Indirect mechanisms. Beyond direct receptor activation, anabolic steroids may also affect muscle growth through indirect mechanisms. These include:

• Anti-glucocorticoid effect: Reducing the catabolic effects of cortisol, which breaks down muscle tissue.
• Creatine synthesis: Enhancing creatine synthesis in muscle tissues, improving energy storage and muscle endurance.
• IGF-1 modulation: Influencing the release and responsiveness to Insulin-Like Growth Factor 1 (IGF-1), another anabolic hormone.

No dichotomous groups. It's important to recognize that all commercial steroids promote both muscle growth and androgenic effects, with no complete separation of these traits. While some steroids may have a stronger affinity for the androgen receptor or influence indirect mechanisms differently, the primary mode of action remains androgen receptor activation.

3. Free Testosterone: The Active Hormone

The level of free testosterone available in the blood is likewise an important factor mediating its activity, as only a small percentage is really active at any given time.

Bound vs. Free. Only a small fraction of testosterone exists in a free, unbound state, ready to interact with cellular receptors. The majority is bound to proteins like SHBG (sex hormone-binding globulin) and albumin, temporarily preventing its activity. The distribution in men is typically 45% bound to SHBG, 53% to albumin, and only 2% free.

Altering Binding Affinity. As testosterone is modified to create new anabolic steroids, the affinity with which it binds to plasma proteins also changes. A higher percentage of free hormone translates to a more potent compound on a milligram-per-milligram basis. For example, Proviron binds more avidly to SHBG than testosterone, while mibolerone shows virtually no affinity.

SHBG Levels. The level of SHBG in the body is variable and influenced by factors like estrogen and thyroid hormone concentrations. A heightened androgen level from steroid administration can also lower SHBG levels, increasing free testosterone. Manipulating the tendency of a hormone to exist in an unbound state is an effective way to alter drug potency.

4. Estrogen's Role: More Than Just a Female Hormone

It appears that reasons go beyond the simple size, weight, and strength increases that one would attribute to estrogen-related water retention, with this hormone actually having a direct effect on the process of anabolism.

Estrogen synthesis. Testosterone is the primary substrate for estrogen (estradiol) synthesis in men, facilitated by the aromatase enzyme. This process occurs in various tissues, including adipose, liver, and skeletal muscle. While often viewed negatively, estrogen plays a crucial role in several anabolic processes.

Benefits of Estrogen:

• Glucose Utilization: Estrogen affects glucose utilization in muscle tissue, promoting an anabolic state.
• GH/IGF-1 Production: Estrogen plays a role in the production of growth hormone and IGF-1, both anabolic hormones.
• Androgen Receptor Proliferation: Estrogen can increase the concentration of androgen receptors in certain tissues, enhancing androgen sensitivity.
• Mental Alertness: Estrogen promotes wakefulness and a mentally alert state.

Cautious approach. While anti-estrogens are necessary to combat estrogenic side effects, a cautious approach is warranted if mass gain is the primary objective. The added estrogen from testosterone or Dianabol, for example, might aid in muscle buildup or keep you energetic.

5. DHT Conversion: A Double-Edged Sword

Dihydrotestosterone is no different than any other steroid except that it is a more potent activator of this receptor than most, and can be formed locally in certain androgen-sensitive tissues.

Testosterone's Potent Metabolite. Testosterone's potency is increased in androgen-responsive tissues through conversion to dihydrotestosterone (DHT) via the 5-alpha reductase enzyme. DHT is approximately three to four times stronger than testosterone and is the most potent steroid found naturally in the human body.

Androgenic Side Effects. This local potentiation can lead to undesirable side effects such as acne and male pattern hair loss. However, it's a misconception that DHT is solely responsible for these effects. All anabolic steroids exert their activities through the same androgen receptor, and DHT is simply a more potent activator.

Benefits of DHT. DHT plays an important role in the central nervous system, with studies showing it has a greater impact on neural cells compared to testosterone. The strong interaction between the central nervous system and skeletal muscles is key for athletes, and inhibiting DHT formation may interfere with strength and muscle mass gains.

6. AAS History: From Medical Marvel to Controlled Substance

During the infancy of such experimentation, many believed they had crossed paths with a true “fountain of youth.”

Early Experiments. The understanding of testosterone began to form in the 1800s, with the first experimental androgen injections produced by filtering urine or extracting testosterone from animal testicles. Chemists finally synthesized testosterone in the mid-1930s, sparking interest in its therapeutic uses.

The Quest for a Pure Anabolic. Researchers aimed to manufacture a steroid with strong anabolic activity but little or no androgenic/estrogenic properties. By the mid-1950s, over one thousand testosterone, nandrolone, and dihydrotestosterone analogues had been produced, but none proved to be purely anabolic.

One Receptor Theory. The failure to reach this goal was primarily due to an initial flawed understanding of testosterone's action. Scientists had noticed high levels of DHT in certain tissues, and believed this indicated an unusual receptor affinity for this hormone. More recently, scientists have come to understand that only one type of androgen receptor exists in the human body.

7. Synthetic AAS: Tailoring Steroids for Specific Effects

Chemists realized that by replacing the hydrogen atom at the steroid's 17th alpha position with a carbon atom (a process referred to as alkylation), its structure would be notably resistant to breakdown by the liver.

Oral Dosing Challenges. Natural steroid hormones like testosterone are ineffective when taken orally due to rapid liver breakdown. Chemists solved this by alkylating the steroid's 17th alpha position, making it resistant to liver metabolism. This led to the development of effective oral steroids like methyltestosterone and Dianabol.

Esters and Injectable Compounds. Injectable steroids often list long chemical names like testosterone cypionate, which indicates the presence of an ester. Esters are attached to the 17-beta hydroxyl group of the steroid molecule, increasing its active lifespan. Once injected, the esterified compound forms a depot in the muscle tissue, slowly releasing the hormone into circulation.

Anabolic/Androgenic Dissociation. Scientists had some success in separating the androgenic and anabolic properties of testosterone, developing synthetic anabolic steroids with varying degrees of each. This was often assessed using rats as a model, measuring the growth of seminal vesicles, ventral prostate, and levator ani muscle.

8. Clinical Applications: AAS Beyond Bodybuilding

The most widely used medical application for anabolic/androgenic steroids in the world is that of androgen replacement therapy.

Androgen Replacement Therapy (HRT/TRT). The most common medical use of anabolic steroids is to supplement testosterone in men with low hormone levels (hypogonadism). This therapy alleviates symptoms like reduced libido, erectile dysfunction, loss of energy, and decreased strength.

Other Clinical Uses:

• Hereditary angioedema: Oral steroids can stabilize complement system protein levels, reducing the frequency and severity of attacks.
• Anemia: Steroids stimulate erythropoietin synthesis, increasing red blood cell production.
• Breast Cancer: Androgens can inhibit the growth of hormone-responsive tumors.
• Growth Failure: Anabolic steroids may be prescribed to treat growth failure in children, both with and without growth hormone deficiency.

HRT Benefits. Unlike steroid abuse, hormone replacement therapy may have benefits with regard to cardiovascular disease risk. For example, studies tend to show hormone replacement as having a positive effect on serum lipids.

9. Steroid Side Effects: Understanding the Risks

According to one study, the exact frequency of tangible side effects in a group of steroid abusers was 96.4%.

Cardiovascular System. Steroid use can have adverse effects on the cardiovascular system, including unfavorable alterations in serum cholesterol, thickening of ventricular walls, increased blood pressure, and changes in vascular reactivity. Long-term abuse increases the risk of early death due to heart attack or stroke.

Cholesterol/Lipids. Steroids can adversely affect HDL (good) and LDL (bad) cholesterol values, often lowering HDL and increasing LDL levels. Oral steroids, especially c-17 alpha alkylated compounds, are particularly potent at stimulating hepatic lipase and suppressing HDL levels.

Other Side Effects:

• Acne
• Hair Loss (Androgenetic Alopecia)
• Stunted Growth
• Tendon Injury
• Water and Salt Retention
• Virilization (in women)
• Psychological (aggression, depression, dependency)

10. Acute Steroid Safety: Studies with Real-World Dosages

The risk of an otherwise healthy person suffering a heart attack from an isolated steroid cycle is extremely remote.

Limited Data. There's a lack of pertinent medical studies on the effects of steroid abuse due to ethical concerns. However, some studies provide valuable insights into the acute safety of steroids at supratherapeutic dosages.

Key Studies:

• Testosterone dose-response study: Examined the effects of various testosterone enanthate doses (25-600 mg/week) on body composition, strength, and health markers.
• Nandrolone study: Charted the lean-mass-building effects of nandrolone decanoate (600 mg/week) in HIV+ men.
• Oxymetholone study: Looked at the effects of oxymetholone (50-100 mg/day) on elderly men.

Results. These studies, involving 121 men, revealed that the main negative impact of steroid use was a reduction in HDL cholesterol values. Other health markers remained relatively stable.

11. The Endocrinology of Muscle Growth: A Symphony of Hormones

Muscle growth is always a circular process, with a step back (damage) being necessary to take any steps forward.

Muscle Hypertrophy. Muscle growth involves the fusion of new cells (satellite cells) with existing muscle fibers, increasing the cell size and protein content. This process is triggered by muscle damage during intense training.

The Anabolic Chain:

• Trigger: Localized cellular damage from weight training.
• Phase I: Initial Response: Release of arachidonic acid and formation of prostaglandins, cytokines, and other active messengers.
• Phase II: Localized Tissue Priming: Increase in growth factor expression (IGF-1, MGF) and tissue sensitivity to anabolic hormones.
• Phase III: Repair: Repair and hypertrophy mediated by androgens, insulin, IGF-1, MGF, and other growth factors.

Importance of Training. Weight training is fundamental to growing muscle tissue. Without the localized cellular damage produced by intense training, growth is difficult to stimulate.

12. Practical Application: Cycling, Stacking, and Sourcing

The user must simply endure more side effects when acquiring his or her new muscle with this type of drug.

Steroid Selection. While all anabolic steroids can promote muscle gains, different agents have varying properties. Estrogenic steroids are best for mass building, while non-estrogenic steroids are favored for lean mass and definition.

Dosage and Cycling. Anabolic steroids are most effective at moderately supratherapeutic dosages. Cycles typically last 6-8 weeks, followed by an equal or longer period of abstinence.

Stacking and Sourcing. Stacking involves combining multiple steroids for synergistic effects. Sourcing steroids requires careful consideration to avoid counterfeit products and ensure safety.

Last updated: March 6, 2025