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Selective androgen receptor modulators (SARMs)

SELECTIVE ANDROGEN RECEPTOR MODULATORS (SARMS)

SARMs have been around in the bodybuilding scene for quite some time now. Although there is an abundance of information on these, like with any topic within the bodybuilding industry, there can be some misinformation or conflicting ideas. As a result, it still seems that people know little about what they do in the body and how they can aid one’s physique development. Therefore, the aim of this article with be to explain exactly what SARMs are and discuss their role within female bodybuilding as well as their side effects.

What are SARMs?

If you are relatively new to this game, you may have heard a lot of educators, including myself, talk about androgen receptors (AR) when discussing PEDs. If you’re busy wondering what the hell that means, that’s perfectly normal: I still remember that feeling from years back before I learnt about this stuff! So, let’s address that first.

AR belong to a family of steroid hormone receptors, where molecules such as testosterone or dihydrotestosterone (DHT) can bind. When this binding occurs, these hormones have a direct effect on that given cell’s DNA; in this case with steroid hormones (or PEDs), would lead to subsequent muscle growth. These receptors can be found in nearly all bodily tissues, and as such, the use of anabolic steroids will promote binding (and thus influence the DNA) in all those tissues/cells, not just muscle! Think of steroids binding to the AR as a lock and key mechanism. The AR is the lock and testosterone/DHT is the key you need: when they bind, the key “opens” the lock, and get things moving (influences DNA, i.e., promoting supraphysiological growth).

This is a very simplistic way of looking at it, but one that helped me understand the science of PEDs in the early days, as understanding the physiology of how steroids interact with AR is fairly complex.

Now that you understand how steroids elicit their effect on a cell, it’s important to note that SARMs interact with the AR in the same fashion, except this time, the SARM is the key (instead of steroids). The main difference between steroids and SARMs is that whilst steroids bind to androgen receptors in all bodily tissues, SARMs will only bind to some tissues but not others – hence why they’re “selective”. The precise molecular mechanisms of tissue selectivity for SARMs are not fully understood. However, they were designed in such a manner to target the AR in muscle cells, but to spare other tissues. That does not mean that binding to the AR in other tissues is completely spared, but it does mean that their effects in those tissues are lower than those which would be observed when compared to steroids.

You could therefore say that SARMs are designed to have similar anabolic properties to steroids (such as muscle growth) but to have reduced androgenic side effects: that is, all other side effects except for muscle growth are reduced, such as the development of male characteristics, oily skin, and skewed liver enzymes and/or lipid profile.

SARMs were initially designed to be used in the medical field to help treat clinical diseases such as Osteoporosis, Alzheimer’s, Muscular dystrophy and even breast and prostate cancer. The properties of SARMs mean that they can have an agonist effect on the AR: on the one hand, it can bind and promote activation of a certain part of the DNA by “opening” the door via the lock and key mechanism; and on the other hand, it can bind and inactivate the AR, like “locking” the door. In other words, for different medical diseases, SARMs can promote the growth of certain tissues (e.g., muscle or bone cells), or they can halt or slow down the growth of these tissues (e.g., for different cancer tumours). Of course, as bodybuilders, we are interested in the muscle growth effect of SARMs.

So now that we’ve discussed what SARMs do, you might be thinking: “A compound that has similar effects as steroids, but has minimal androgenic side effects, surely it must be a winner?!”. We all think this!!! But is that really the case? Are there any side effects you should be aware of? Would you get more out of taking this when compared to steroids?

Side effects

No PED is without its side effects, and as such, although SARMs such as Ostarine and Ligandrol are marketed to be a similar but safer alternative to steroids, we must be aware that it can still skew the same health markers that are affected by the use of anabolic steroids. Importantly, many of the clinical studies done on SARMs are typically done at lower dosages than those which are taken in the bodybuilding community, and for shorter periods of time too. For example, the recommended use of Ostarine in the bodybuilding community will typically be 10 times that of clinical doses. But then again, how much steroids bodybuilders take is often above dosages used in clinical trials, particularly when compounds are stacked together.

Liver
It’s well documented that an oral steroid, such as Anavar can increase our liver enzymes and can cause hepatotoxicity (chemical driven liver damage). Although SARMs do not share the same chemical make-up as the different oral steroids, they have been shown to still impact liver enzymes and liver function, albeit to a lesser extent. Thus, it would make sense to support your liver throughout usage if you were to take them, as you would do if you were using steroids.

HPG axis
Just like the use of anabolic steroids, SARMs can negatively impact the hypothalamic pituitary gonadal axis, the system that ties your brain to the gonads telling them make testosterone/oestrogen. There can also be a slight reduction in bone mineral density, like what you’d see through steroid use.

Cholesterol
It’s common knowledge that steroid use can negatively impact your cholesterol profile, causing a reduction in high-density lipoprotein (HDLs or “good cholesterol”), and an increase in low density lipoprotein (LDLs or “bad cholesterol”). SARMs have been shown to reduce levels of HDLs, although levels quickly return to baseline levels after usage has stopped. This illustrates how SARMs can still affect our health in a similar way to steroids, but just to a lesser extent.

Blood sugar and insulin
There are some SARMs that are also known as growth hormone secretagogues such as MK677, promising similar effects to that of growth hormone. However, what you will tend to see is a large negative impact on blood glucose levels and insulin insensitivity. This can lead to a sharp increase in body fat but also a lot of water retention.

Uses in females

In the assisted bodybuilding scene, SARMs such as Ostarine and Ligandrol have become more and more popular for female competitors. This is simply down to the fact that many will see little to zero virilisation (the development of male characteristics) resulting from their usage, when compared to anabolic steroids.

If a female were to use certain steroids at higher dosages, she may develop a deeper voice, body hair/facial hair growth, acne, and a reduction in breast size, which are typically undesirable for these competitors. These side effects are observed due to the raised levels of testosterone production caused by AAS, which are of course above the normal range for most females. Thus, the appeal of SARMs is that it does not increase one’s testosterone levels, but can have similar effects on muscle growth when binding to the AR. In Layman’s terms, it just means that a female taking SARMs instead of AAS would see more muscle growth without any virilisation, and therein lies their appeal.

Of course, this isn’t a blanket statement, and there will be women who have taken SARMs and still experienced some of those adverse side-effects. From researching the topic, I struggled to find any data that suggested virilisation at clinical dosages but remember that the doses of compounds that bodybuilders will take will typically be above clinical dosages. From my experience when working with females, I’ve seen no development of any male characteristics, but the question does remain open as to what would occur, and whether there is a dose-response threshold.

As a curious side note, SARMs have been shown to increase libido in females, which can be the complete opposite from steroid use – so perhaps all the side effects aren’t negative, and at least would point towards their preferred use over AAS in females.

In summary, SARMs interact with the AR in a similar fashion to that of steroids. They have been designed in a manner that generates the same hypertrophy benefits you’d see from taking AAS, but with lower side effects that impact on health and virilisation. However, the usage of SARMs can still skew some health markers such as liver enzymes, cholesterol and even insulin sensitivity albeit to a lesser extent. As a result, their use has gotten more and more popular within females and might be preferred over the usage of anabolic steroids in competitive female bodybuilders.

Vaughan Wilson Bsc Hons

References:

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6326857/

https://www.sciencedirect.com/topics/medicine-and-dentistry/selective-androgen-receptor-modulator

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4111291/

https://www.uspharmacist.com/article/recreational-use-of-selective-androgen-receptor-modulators

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2913771/