Prohormone: Definition, Uses, Safety, Side Effects, Alternatives, and Regulation

They are the most powerful muscle builders out there. They are very varied and very complex and there is a general lack of knowledge surrounding them.

An androgen prohormone, or proandrogen, is a prohormone (or prodrug) of an androgenic anabolic steroid (SAA). They can be testosterone prohormones or synthetic androgenic anabolic steroids such as nandrolone (19-nortestosterone).

Dehydroepiandrosterone (DHEA), dehydroepiandrosterone sulfate (DHEA-S), and androstenedione can be considered proandrogens of testosterone.

Technical definition

Prohormones are compounds that are converted through an enzymatic process into anabolic hormones in the body.

As such, they will cause similar effects in the body to anabolic steroids, inducing rapid muscle and strength gains, but of a lesser magnitude than anabolic steroids, due to the rate-limiting effect caused by enzyme conversion.

However, this technical definition is currently considered outdated due to the innovation shown in the supplement industry since the introduction of the first prohormone, androstenedione.

Testosterone prohormones and other anabolic androgenic steroids

In the past two decades, bodybuilders, athletes, and non-medical users of anabolic androgenic steroids and other hormones have also used prohormones to refer to substances that are expected to become active hormones in the body.

The intent is to provide the benefits of taking an androgenic anabolic steroid without the legal risks, and to achieve the expected benefits or advantages without the use of anabolic androgenic steroids.

Many of these compounds are legal to make, sell, possess, and ingest, eliminating the legal problems associated with the Schedule III androgenic anabolic steroid.

The typical definition of “prohormone” includes a steroid molecule that has the opposite molecular structure to testosterone at position 3a / b or at position 17b.

Testosterone has a ketone group at carbon 3 and a hydroxyl at carbon 17b. A steroid with modifications of testosterone in one or both areas is commonly known as a “prohormone.” These enzyme changes occur with bi-directional enzymes in the body.

On October 22, 2004, President Bush signed into law the Anabolic Steroid Control Act of 2004 (118 Stat. 1661). The bill was written to go into effect in 90 days, which was on January 20, 2005.

This legislation places androgenic anabolic steroids and some androgen prohormones on a list of controlled substances (a new type of “regulatory control”). Legal definition of anabolic androgenic steroid:

“The term ‘anabolic steroid’ means any drug or substance that is hormonally, chemically and pharmacologically related to testosterone (other than estrogens, progestins, corticosteroids and dehydroepiandrosterone).”

The Act also lists substances called prohormones, qualifying them as anabolic-androgenic steroids.

However, these substances were included mainly in the list due to the generalization of the definition of anabolic-androgenic steroid.

That makes it impossible at present to synthesize additional substances linked to testosterone for the needs of athlete supplementation.

Prohormone Safety

If you’ve ever been tempted to use anabolic steroids to build stronger muscles and burn more fat, but you didn’t like the idea of ​​using an illegal and potentially dangerous substance, then you might have considered turning to prohormones.

Prohormones offer an alternative to steroids that are legal in some cases and in some countries and appear to have fewer risks. But what exactly are they? Are they really much safer than steroids?

Steroids vs testosterone boosters vs prohormone

When it comes to prohormones, testosterone boosters, and steroids, there is a lot of confusion regarding what each is and how they differ. This can lead to some drastic mistakes, so let’s make sure we are clear first …

Steroids : Anabolic steroids are synthetic compounds designed to “look like” testosterone. Specifically, this means that they will bind to androgen receptors in the same way, leading to the same anabolic effects.

This then increases the body’s ability to build muscle and burn fat, as well as increase fertility and aggression.

Unfortunately, it can also lead to some dangerous side effects as the body begins to produce less testosterone to try to restore balance, and sometimes estrogen production also increases, leading to the development of secondary sexual characteristics.

Besides being illegal, steroids carry the risk of many side effects, such as acne, hair loss, mood disorders, impotence, and many more.

Steroids can lead to huge gains in strength and muscle gain, but the correct diet and training techniques still need to be used along with that.

Testosterone Boosters : Testosterone boosters are supplements that act simply to stimulate the body to increase its own testosterone production.

These include things like ‘tribulus terrestris’ and ‘tongkat ali’, which are herbs that have been found to somehow increase testosterone levels when taken orally.

Another example would be ZMA, which is a mixture of zinc and magnesium that leads to elevated levels of testosterone.

Because testosterone boosters stimulate the body to produce more hormones on its own, this means that they do not lead to tolerance or any other side effects.

However, with that said, they are also considerably less effective. For most people under the age of 40, you are unlikely to see any major effects, less than you would simply by changing your diet and lifestyle.

Prohormones : Prohormones on the other hand, are somewhere between steroids and boosters. These are compounds that act as chemical precursors to hormones and steroids.

In other words, they contain the “bits” that the body needs to create these steroids. In the case of bodybuilders, this generally means precursors to testosterone.

Prohormones are generally a bit milder in effect than steroids that you take directly and therefore give slightly less results with slightly less risks.

That said, they can still lead to increased muscle mass and strength, and still carry most of the same risks. In particular, it is very important to avoid taking them if you are under the age of 19, in which case you may risk permanently damaging your endocrine system.

It’s also worth noting that prohormones show up in drug tests and suggest the use of anabolic steroids.

Prohormones, an unsafe alternative to steroids

In conclusion, prohormones should not be considered a “safe alternative” to steroids. In fact, the use of prohormones is even worse than the use of steroids, as the methylated nature means that they are often harder on the liver.

The benefits are also less pronounced, so you really put your liver and natural testosterone production at risk for no good reason.

Unless you are a professional bodybuilder, there is very little chance that you would have reached the maximum of what you are capable of without these types of supplements.

So, instead of using potentially dangerous prohormones to try to increase muscle mass, simply try increasing your protein intake and the intensity and efficiency of your workouts.

Side effects and better alternatives

Prohormones can often seem like the easy route. But using prohormones has many hidden costs, including health.

Prohormones affect each individual differently. For some, the side effects are severe. And for some, mild. But even when the side effects are mild, they are still there.

Despite the relative paucity of information on its effects, prohormone supplementation has become a popular practice.

Unlike synthetic androgenic anabolic steroids, many of these over-the-counter androgens are endogenously produced by adrenal, gonadal, and peripheral steroidogens as part of the normal reproductive and sexual hormonal environment.

It has been claimed that peripheral enzymatic conversion of these prohormones to testosterone or nortestosterone (through ingestion of androstenedione / androstenediol or 19-norandrostenedione / androstenediol, respectively) could lead to anabolic and / or ergogenic effects.

Existing data suggest that acute oral ingestion of> or = 200 mg androstenedione or androstenediol modestly and transiently increases serum testosterone concentrations in men; however, this is accompanied by greater increases in circulating estrogens.

At doses <300 mg / d, oral supplementation for up to 12 weeks with androstenedione or androstenediol has no effect on body composition or physical performance and lowers high-density lipoprotein cholesterol.

Similarly, oral supplementation with norandrostenedione and norandrostenediol for up to eight weeks has no effect on body composition or physical performance.

In light of these data, new products have been developed using alternative modes of administration of prohormones (sublingual / transbuccal complexing and cyclodextrin).

Future studies should critically examine the effects of these approaches. However, within the framework of the reviewed research, over-the-counter oral prohormone supplementation is ineffective for increasing muscle mass or athletic performance.

As a result of the potential health concerns that have been raised, the risk-benefit ratio of using these substances orally appears unfavorable.

Prohormones Added to Schedule 3 (III) List of Anabolic Androgenic Steroids

The 108th Congress amended the Controlled Substances Act to include androgenic anabolic steroids and to add information on steroids and steroid precursors. This amendment is sometimes called the Anabolic Steroid Control Act of 2004.

The first thing this amendment did was insert a definition of anabolic androgenic steroid as follows:

“The term ‘anabolic steroid’ means any drug or hormonal substance chemically and pharmacologically related to testosterone (other than estrogens, progestins, corticosteroids and dehydroepiandrosterone).”

In addition to the definition, the document lists the currently known prohormones:

  • Androstanediol (3β, 17β-dihydroxy-5α-androstane y 3α, 17β-dihydroxy-5α-androstane).
  • Androstanedione (5α-androstan-3,17-dione).
  • 1-Androstenediol (3α, 17β-dihydroxy-5α-androst-1-eno).
  • 4-Androstenediol (3β, 17β-dihydroxy-androst-4-eno).
  • 5-Androstenediol (3β, 17β-dihydroxy-androst-5-eno).
  • 1-Androstenedione (5α-androst-1-en-3,17-dione).
  • 4-Androstenedione (androst-4-en-3,17-dione).
  • 5-Androstenedione (androst-5-en-3,17-dione).
  • Norandrostenediol (19-nor-4-androstenediol o 3β, 17β-dihidroxiestr-4-eno).
  • 19-Nor-4-androstenediol (3α, 17β-dihidroxiestr-4-eno).
  • 19-Nor-5-androstenediol (3β, 17β-dihydroxiester-5-eno y 3α, 17β-dihydroxiester-5-eno).
  • Norandrostenedione (19-nor-4-androstenedione or estr-4-en-3,17-dione).
  • 19-Nor-5-androstenedione (estr-5-en-3,17-dione).
  • Any salt, ester, or ether of a drug or substance listed above.

Please note that this list contains examples and is not a closed list: any other compound that affects testosterone, by definition is an androgenic anabolic steroid under US law.

“Designer Steroids” and Adulterated Supplements

In light of a 2004 outright ban, manufacturers are unable to release the next androgenic anabolic steroid, they are currently interested in substances that are related to hormones, but do not affect testosterone.

These include derivatives, e.g. methoxydienone (methoxygonadiene, ethyl methoxy gone), methasterone (called Superdrol or S-Drol), and many others, sometimes called “designer steroids.”

Such compounds, while harmful, do not violate the Anabolic Steroid Control Act because they have no impact on the testosterone level.

Due to the same reason, they did not help build muscle and are not applicable in support; It is typical that the descriptions of these compounds try to manipulate the chemical concepts, but they do not even mention the possibility of increasing testosterone, because they do not even have that potential.

That is why, in practice, agents labeled with these compounds of this type were falsified because they contained, not stated in the composition, typical anabolic-androgenic steroids.

After publicizing the fraud in the media, many manufacturers lost trust and the US health authorities began to remove suspicious products.

Research carried out by state laboratories confirmed that “designer steroids” are, in fact, pharmaceuticals such as methandienone, stanazolol, methylstenbolone, boldenone, chlorodidomethyltestosterone, dihydrotestosterone (DHT) and oxandrolone, added to supplements randomly.

Supplements with different names and ingredients described may have the same steroid (such as Chlorodehydromethylandrostenediol (Halodrol), desoxymethyltestosterone (Madol, Pheraplex), others) and sometimes supplements with similar names may have different ingredients (such as Finabolic).

Regulation in the United States and Europe

Following the introduction of the Anabolic Steroid Control Act, label products derived from plant extracts with the help of chemical symbols for organic substances found in these plants.

Creating names for these substances that refer to banned androgenic anabolic steroids became a popular marketing practice employed by American manufacturers.

No analogical act directed to the supplementation of athletes is in force in the European Union; however, each country has its own regulations on substances with medicinal properties.

Due to the above, one can come into contact with the sale of supplements with identical or similar names to those questioned by the recommended dietary allowance (ADR) in the United States (S-DROL, HALODROL, etc.).

Laboratory tests indicate that products claiming to include prohormones, banned in the US, do in fact contain the older generation ‘classic’ anabolic-androgenic steroid.

Many consumers in Europe were unaware that it was illegally produced prohormones in the US After 2004 and thought they were consuming various versions of the previously acclaimed supplement, while in fact consuming steroids of unknown origin.

In situations such as those described above, the buyer of this fake substance does not know the type or dosage of the hormone ingested, and therefore cannot plan a safe gastrointestinal protection regimen or complementary treatment.

The consumer is also unable to gain access to information on the possible long-term consequences of treatment with the unspecified hormone.

This has led to the popularity of special forums where consumers could share their experiences with the substances, however, fake products could have radically different components, despite similar descriptions and names.

Supplement manufacturers who have made a name for themselves and want to stay on the market are currently making anabolic androgenic steroids based on natural substances (usually derived from plants).

In Europe, these products are called prohormones. Producers who still want to offer supplements that support hormonal balance can still use the natural compounds.

Known in the field of prohormones Patrick Arnold (the one who introduced 1-AD and the first prohormones) currently works on ursolic acid, while in Eastern Europe manufacturers launch supplements based on buteins, natural compounds considered the most important aromatase inhibitors. powerful.