A Disclaimer – Please Read
SARMs (Selective Androgen Receptor Modulators) should only be used by individuals over the age of 21. It is not advisable to use SARMs if you are a child, teenager, pregnant, nursing or trying to get pregnant.
Some professional organisations have banned the use of SARMs, so ensure you conduct your due diligence when competing so find out what substances are banned. If you are considering to use SARMs then contact your doctor to advise them, particularly if you have a family history of prostate enlargement, prostate cancer, heart disease, if you are using another dietary supplement, prescribed drug or OTC drug.
If you exceed the suggested dosage of SARMs please be aware that you are doing so at your own risk. This article is meant to advise you, not to treat, diagnose, cure or prevent a disease.
Table of Contents
Introduction To SARMs
SARMs, or Selective Androgen Receptor Modulators, are very well known to have the same effects as prohormones, and anabolic steroids, but with less of the nasty and well-documented side-effects. In short, SARMs increases muscle growth or key receptors in the body that increase muscle growth and decrease the unwanted side effects that are linked with prohormone usage.
In clinical trials, SARMs have been shown to increase muscle mass, bone mass and reduced fat percentages without large increases in estrogen, or the closure of the HPG axis (Hypothalamic-pituitary-gonadal axis.
On this page we shall look at the history, mechanics, benefits and side effects of SARMs as well as popular SARM products and where to buy them, if you choose to use them, thus allowing you to make an informed decision on whether or not SARMs might be right for you and your bodybuilding targets.
Comparison To Testosterone
The most common forms of steroid use or HRT (Hormone Replacement Therapy) is usually injected or through the skin a delivery method of testosterone release into the blood stream. When Injectable methods of testosterone induction are used (for instance, testosterone propionate, enanthate or cypionate), these tend to produce undesirable amounts of testosterone in the blood stream, especially straight after an injection and then low afterwards. Some skin patches are able to deliver a constant percentage of testosterone into the blood stream, but they are irritable and with the application, most people find that this is rather annoying.
SARMs allows these molecules to be delivered to muscle cells orally and selectively target the androgen receptors in those muscle cell tissues differently. Through research, there has been recorded evidence of anabolic results in muscle or bone tissue without producing the androgenic effects normally associated with anabolic steroids. In some cases with a ratio of 3:1 and using RAD-140, as much as 90:1. This is far higher than the ratio of 1:1 that is often felt with testosterone injections.
From a medical perspective, this will mean that SARMs shows a useful effect when used women that are suffering from osteoporosis, or men seeking virilizing effects when used at high doses – for instance, Bodybuilders.
One of the most noticeable advantages that has been noticed with clinical trials from the first generation of SARMs use, is that the drugs can be taken orally and haven’t been recorded to cause long-term liver damage, which can then become life threatening for a user.
NonMuscle Building Benefits For Both Men And Women
There are benefits for using SARMs on specifically targeted issues or medical conditions for both men and women. For instance, a SARM that specifically targeted older men with osteopenia or osteoporosis, thereby increasing bone mass and muscle tissue would be highly beneficial if there were no negative effects linked to detrimental issues with the prostate or testes.
In women, SARMs would be useful in stimulating bone retention, libido or other sexual function that androgens can influence, without the known negative side-effects that are normally associated with testosterone use and the development of typical male characteristics (virilization), increased LDL/HDL ratios and liver dysfunction.
Key Terms For This Article
There are a number of Key Terms that we use on this page, and to fully understand the meaning of those terms we need a list of acronyms and links to useful resources for those terms:
- 5-alpha reductase – an important enzyme during the steroid metabolism process.
- AICAR – 5-Aminoimidazole-4-carboxamide ribonucleotide. Analog of adenosine monophosphate (AMP) that can stimulate AMPK.
- ALT – Alanine aminotransferase. An enzyme found in the blood that when high, may indicate liver injury.
- AMPK – 5′ AMP-activated protein kinase. An enzyme playing a key role in energy homeostasis at the cellular level. AMPK activation can oxidize fatty acids, stimulate muscle glucose uptake, as well as inhibit cholesterol, fat cell, and triglyceride synthesis.
- Aromatization – the process of converting a compound into an active androgen or estrogen
- AST – Aspartate aminotransferase. An enzyme found in the blood that when high, may indicate liver damage.
- BMD – Bone mineral density. The amount of mineral matter per square centimetre of bone; used as an indirect indicator of osteoporosis and bone fracture risk.
- DHT – Dihydrotestosterone. Sex steroid and androgen hormone synthesized from testosterone in the prostate, testes, hair follicles, and adrenal glands.
- EB – Estradiol benzoate. A substance necessarily to maintain sexual behaviour in rats during experiments.
- ED50 – The median effective dose. This is the dose that produces the desired effect(s) in 50% of the population.
- Estradiol – Form of estrogen. Small amounts are released by the testes in males to prevent sperm from dying too early and in women has played a large role in the growth and development of the womb, Fallopian tubes, vagina, and breasts.
- FSH – Follicle stimulating hormone. A hormone associated with reproduction and the development of eggs in women and sperm in men.
- HDL – high-density lipoprotein. Also known as “good cholesterol”.
- HPG axis – Hypothalamic-pituitary-gonadal axis. A term used to describe three glands in the endocrine system (hypothalamus, pituitary gland, and gonads) as one entity.
- LH – Luteinizing hormone. A hormone released by the pituitary gland. Too much or too little LH may result in infertility and other issues with sexual reproductive organs.
- LPL – Lipoprotein lipase. An enzyme responsible for storing calories as fat.
- Ovariectomized – Ovaries removed. Sometimes used as a more technical term for castrated females.
- Orchidectomized – Testes removed. Sometimes used as a more technical term for castrated males.
- PPARδ – Peroxisome proliferator-activated receptor delta. They play a critical role as lipid sensors and regulators of lipid metabolism (i.e. fat storing and burning).
- PSA – Prostate-Specific Antigen Test. A blood test measuring the amount of a specific protein produced by cells in the prostate gland; values below 4.0 ng/ml are considered healthy, whereas values above 4.0 are recommended to get an in-depth prostate examination.
- PCT – Post cycle therapy. Compounds used to restart natural testosterone production.
- SHBG – Sex hormone-binding globulin. Binds tightly to testosterone, DHT, and estradiol; measured to determine if males have low testosterone and if females produce too much testosterone.
- TP – Testosterone propionate. Testosterone derivative that is typically injected into the muscles.
- VLDL – very-low-density lipoprotein. A subset of LDL, also known as “bad cholesterol”.
This History And Development Of SARMs
In the 1940s researchers modified the chemical structure of the testosterone molecule and discovered SARMs. They were initially considered steroidal because of their derivation from the testosterone molecule. Science organisations and other pharmaceutical companies enhanced the structure of early SARMs to develop nonsteroidal SARMs. Ligand Pharmaceuticals were the first company to develop the first series of compounds to be classed as nonsteroidal SARMs.
Research over the past ten years has made leaps and bounds in improving the way in which SARMs is ingested and broken down in the small and large intestine, decreasing the toxicity of the compound. Androgen receptors are found in several key tissues and cells throughout the body.
Over the past two decades, there has been a rise in the number of men diagnosed with Hypogonadism, a particular condition when the body does not produce sufficient amounts of testosterone. Men who are born with this condition develop symptoms later in life, such s fat gain, muscle mass reduction, depression and a lower libido.
Over the past two decades, there has been a rise in the number of men diagnosed with Hypogonadism, a particular condition when the body does not produce sufficient amounts of testosterone. Men who are born with this condition develop symptoms later in life, such s fat gain, muscle mass reduction, depression and a lower libido.
With the administration of exogenous androgens to a male patient suffering from Hypogonadism has been shown to increase their quality of life, by reversing or reducing the main issues that come with that disease, such as muscle reduction and age-related deterioration which affect the prostate gland.
With the administration of exogenous androgens to a male patient suffering from Hypogonadism has been shown to increase their quality of life, by reversing or reducing the main issues that come with that disease, such as muscle reduction and age-related deterioration which affect the prostate gland.
Therefore SARMs should have little effect on the prostate and produce a strong positive anabolic effect on the bone and muscles of an individual user.
Therefore a SARM should have little effect on the prostate and produce a strong positive anabolic effect on the bone and muscles of an individual user.
Not Yet Fully Tested and Banned In Competitive Sports
Given the potential of SARMs for modern athletes, it does make you wonder why this hasn’t yet been introduced to medical patients by doctors treating Hypogonadism and other conditions. The reason is, there a number of clinical trials currently running, but none has reached stage IV, where long-term use of the drugs on the general public has yet to be examined.
Testing so far has been conducted on rats, of which some have been castrated. Castrated rats have higher levels of LH and FSH compared to non-castrated rats. Scientists are then able to measure their muscle growth via the levator ani muscle, weigh their prostate gland and bone formation rates.
There has yet to be regulatory approval of SARMs, as SARMs are not aromatized or 5-alpha reduced. Which means they do not convert into active estrogen or androgen compounds, neither are they separated during the steroid metabolism process.
Not surprisingly, large pharmaceutical companies are in the process of developing drugs that can be sold to the medical professional wide world, once SARMs have been passed by regulatory bodies worldwide. SARMs have been used in a fitness world for a few years now, however, many of the large pharmaceutical companies have a bigger audience in mind – the general public particularly aging adults and post menopausal women. These two sections of the general public are the first to suffer from fat gain, decreased mobility, loss of strength, muscle mass reduction, and heightened risk of bone fractures.
From January 2008, the IOC (International Olympic Committee) placed SARMs to its long list of prohibitive anabolic substances. It has also been banned by the following sporting organizations:
• NCAA (National Collegiate Athletic Association)
• WADA (World Anti-Doping Agency)
Why Use SARMs?
So far in studies and research, scientists have seen three main benefits for SARMs – increases in muscle mass, reduction in body fat and increased bone mass.
Although for this website and the products that we recommend for SARMs the main purpose is for solely muscle gains. However, there is a large population of people that would benefit from using SARMs if they have any of the following conditions: sports injuries, muscle wasting disorders (e.g. Amyotrophic lateral sclerosis, cystic fibrosis, and Sarcopenia), a body wasting illness such as HIV or cancer, and aging frailty conditions that happen at the latter stages of people’s lives.
You can clearly see the benefit that SARMs potentially has to not only individuals looking for a better physique, but also for those that may be chronically ill.
So far the main assessment of SARMs on rats has shown marked increases in muscle mass without any significant prostate weight gain, be it up nor down. Both variations in weight displacement for the prostate gland will imply serious health complications.
There have been a few phase 1 trials on humans with muscle wasting conditions, the results showed increases in muscle mass to be 1.0 to 1.5kgs over a 4-6 week period. None of the research so far has been conducted on healthy individuals who are training for an athletic competition.
In Comparison To Testosterone Enanthate
A typical weight training athlete will aim to use between 300-600mg a day of testosterone Enanthate over a 4-6 week period and look to gain anywhere between 5-7kg of fat-free muscle. However, that comes at a cost, the harsh side effects of testosterone.
It has been demonstrated that SARMs has the ability to prevent muscle trophy when muscles are not used in casts. This implies that SARMs can greatly enhance muscle mass, power, strength and the recovery process of any training session.
There is further evidence that SARMs might be a safer long-term muscle building supplement when compared to testosterone derived steroidal compounds. Only when used in high dosages (3-4 times the recommended) has there been a recorded suppression of LH and FSH levels, which is the case when using testosterone derived compounds.
Increases In Bone Strength And Formation
Bone formation is increased with androgens, while bone formation is decreased or depressed when there is the introduction of estrogen. This implies that SARMs helps to build stronger bones, protect the organs, store calcium and provide levers for movement.
There is also evidence that SARMs decrease endocortical and trabecular bone turnover. If there is a particularly high one turnover rate then, this leads to cancellous bone loss, leaving them spongy, more flexible.
This implies that SARMs would be an excellent and suitable treatment for any individual diagnosed with the condition osteoporosis. Women of postmenopausal age are most at risk of developing osteoporosis and this would suggest that SARMs would be an ideal treatment for such a condition to help minimise fractures and to strengthen bones.
SARMs Within The Fitness Industry
Because of the benefits of SARMs when compared to testosterone cycles, you can see why SARMs has increased in popularity over the past five years. Its ability to increase muscle mass, decrease fat, rehabilitate those with injuries through improved bone and muscle strength would certainly be deemed a positive aspect of any such supplement for weight trainers and bodybuilders alike.
There have been cases where some fitness enthusiasts have stacked SARMs in between prohormone and testosterone cycles for post cycle therapy. Those doing this will have seen large increases in body muscle mass over a short period of time and increases in strength. However, this comes at a cost to the user, as the result in extremely harsh side-effects. Side effects often include the following:
- Baldness
- Acne
- Excessive body hair growth
- Male breast development (Gynecomastia)
- High blood pressure
- Cholesterol
- Heart Growth
- The elimination of natural testosterone production
- Prostate cancer development
With these side effects, it becomes clear that these substances should not be taken lightly or incorrectly at all. But the fitness industry is extremely competitive and many will want to perform their best to win a competition, but at what cost to their health?
References:
https://content.tigerfitness.com/ultimate-guide-sarms-selective-androgen-receptor-modulators/
http://www.usada.org/selective-androgen-receptor-modulators-sarms-prohibited-class-anabolic-agencts/
https://en.wikipedia.org/wiki/Selective_androgen_receptor_modulator
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