INtroduction to aas: orals

If you’ve thought about going down the assisted route in bodybuilding, you’ve probably told yourself “I don’t want to inject, but I’m happy to take orals”. I say this because I remember telling myself and saying it out loud to peers. Of course, at the time I knew nothing about oral steroids and thought they were just the same as injectables.

Without doing much research, I just cracked on with my first “cycle” – for reference, this was also around the time I didn’t track calories nor my training, and you’ll never guess what happened: … not a whole lot. Does this sound familiar? Do you know someone who has experienced the same thing?

Because it’s such a common experience, the purpose of this article is simply to provide information about orals steroids, their side effects, and why they might be used by bodybuilders. I will also go into why we might see bodybuilders take these in the later stages of a contest prep. As a disclaimer, the following article is written for informational purposes only and should not be deemed or taken as advice in any way.

C-17 alpha alkylated orals

Before we get into it, for the following article to make sense, I would strongly advise you read the Introduction to AAS-Testosterone and Introduction to ASS-DHT Derivatives and Nandrolone. Once you have understood the underlying principles of how anabolic androgenic steroids (AAS) work, it will make learning about other compounds much easier.

One of the main reasons for oral steroids being developed is that without some sort of chemical alteration, the natural steroid hormones (i.e., testosterone, nandrolone and dihydrotestosterone (DHT)) would be broken down by the liver before reaching circulation when consumed orally. They also have a naturally short half-life, which led scientists to develop a way to avoid compound breakdown, as well as extend the steroid activity in the body until it’s excreted.

Once more this is the “sciency bit” that might go over your head, but it is important to know the difference. Chemists realised that by replacing the hydrogen at the steroid’s 17th alpha position (a process known as alkylation), it’s structure would be notably resistant to breakdown by the liver. If you’re unsure of the chemical structure of testosterone and the exact carbon atom which is alkylated (yellow arrow) please refer to Figure 1.

The carbon atom is typically added in the form of a methyl group (three hydrogen atoms bonded to a carbon atom), and steroids with this alteration are often referred to as “C-17 alpha alkylated orals”. I know this might go over your head but stick with me!

These types of orals tend to have a lower affinity to bind to the androgen receptor (AR) than their injectable counterparts. However, because the steroid’s half-life is greatly prolonged, (due to alkylation), we see increased anabolic/androgenic tendencies. In layman’s terms, although they might be weaker, their extended half-life means that we still see some muscle growth/androgenic sides effects. Most oral steroids elicit their effects by androgen receptor mediated pathways, meaning that they don’t act as competition to an injectable steroid (which will bind to the AR). This is why an injectable is often stacked with an oral in a bodybuilder’s cycle.

Unfavourable side effects

Although scientists had found a way to prolong oral steroid’s half-lives, and thus their potency, they found one drawback and that was the negative impact these compounds had on the liver. Although they had designed molecules which could purposefully not be metabolised by the liver (breakdown), it is this very factor which makes them very toxic to the liver. In short, it means that the continuous use of these compounds can lead to chemically driven liver damage. These compounds can also negatively impact our HDLs (good cholesterol) and increased LDLs (bad cholesterol).

In addition, some orals carry a greater chance for estrogenic side effects such as gynecomastia. This is because although they have a lower tendency to bind with the aromatase enzyme (i.e., the enzyme responsible for the conversion of androgens to oestrogens), when they do and produce oestrogen, they produce a far more potent biologically active form of oestrogen. An example of this would be Methyltestosterone.

In some cases, the alpha alkylation process can actually enhance the steroid’s ability to bind and activate the oestrogen or progesterone receptor.  Examples of this are seen in Methandrostenolne (oral form or Equipoise) otherwise known as Superdrol. In its injectable form, Equipoise is known for producing little estrogenic side effects; however, its oral counterparts seem to do the opposite. With that in mind, you can understand why a bodybuilder who was using this in their stack design would also use an aromatase inhibitor alongside it.

Non-alkylated orals

Bearing in mind that steroids were originally developed to help treat a range of medical conditions such as muscle wasting, cancer and HIV (to name a few), the fact that orals caused some sort of damage in the body (liver toxicity) was less than ideal.

Therefore, oral steroids were modified by making different chemical alterations to those which we saw above in the C-17 alpha alkylated orals. Steroids such as Proviron or oral Primobolan, are instead alkylated at the one position where a methyl group is added (remember a methyl group is three hydrogen atoms bonded to a carbon atom).

What this means is that they are absorbed in the intestinal lining through lymphatic ducts, bypassing the first pass through the liver. In layman’s terms, it means that they are not toxic to the liver when compared to their C-17 alpha alkylated counterparts.

Why are they used in bodybuilding?

If you’re still with me you’re probably wondering why on earth these might still be used in bodybuilding. To answer your question, I will briefly cover the three most commonly used oral steroids in bodybuilding: Anavar, Winstrol and Proviron.

Anavar is typically used in a dieting phase, particularly towards the back end of contest prep. The main reason for its use would be help enhance performance. When we reach low levels of body fat, combined with calories being low, our strength can decrease or begin to stall. This is mainly due to how strong one has gotten in an off season with higher calories, and ultimately their added bodyweight can help moving weight in the gym (aka mass moves mass). How some bodybuilders get around this roadblock is by using Anavar, perhaps an hour pre-workout, as it has been shown to help increase strength and aid performance when training.

It’s a well-tolerated drug by the body apart from the hepatoxicity and its impact on HDLs (good cholesterol), meaning that it can only be used for roughly 4 weeks at a time. Being a DHT, it cannot aromatise or be reduced and has strong anabolic properties relative to its androgenic properties. It is also the most used steroid by female bodybuilders in low doses.

Winstrol is like Anavar in that is has strong anabolic properties compared to androgenic properties, and it cannot aromatise and/or be reduced. It is mostly used by bodybuilders for its cosmetic effects. By that, I mean that if an individual has low levels of body fat, when they use Winstrol, they will tend to look drier and harder. This is of course advantageous for those stepping on stage to help present a better look that might ultimately help their placing.

Proviron, as described earlier, is a non-alkylated oral, meaning it has little impact on our liver. It does not have strong anabolic properties, it cannot be reduced, and will not aromatise. This might leave you wondering why it’s even used at all? Well, it’s use is mostly driven by its high affinity to bind with Sex Hormone Binding Globulin (SHBG), a plasma binding protein. Steroids can bind to SHBG which renders them inactive; thus, by using Proviron alongside an injectable, it allows more of the injectable steroid to work its way around the body in a “free” or active state. In its active state, the injectable steroid can elicit its effect on the AR.

In summary, C-17 oral steroids can have negative impacts on our health, most notably on our liver. Scientist overcame this unfavourable side by developing oral steroids with different molecular structures such as Proviron. The majority of orals will only be used for a short period of time in a bodybuilder’s cycle and will be used mostly in a contest prep for strength or cosmetic purposes.

Vaughan Wilson Bsc Hons

References

Llewellyn, W. (2017). ANABOLICS 11th Edition (11th ed.). Molecular Nutrition.

https://www.ncbi.nlm.nih.gov/books/NBK548931/

https://www.medicalnewstoday.com/articles/246373#medical-uses