SARMs – Selective Androgen Receptor Modulators

SARMs belong to a group of molecules that selectively bind to sex hormone receptors. By their action they are similar to SERMs -Selective Estrogen Receptor Modulators (e.g. :clomiphene: and :tamoxifen:) with the only difference that they bind to androgen receptors.

As SARMs are not steroids, they do not undergo conversion by steroid enzymes, therefore there are no undesirable side-effects. The initial aim of SARMs was to reduce the adverse effects of testosterone on prostate. But later scientists found out that they can increase muscle mass. Since that time bodybuilders started to test these compounds on themselves even before clinical trials.

In the following article it was shown that GTx-024 (ostarine, enobosarm) is well tolerated and produces a dosage dependent gain of muscle mass in elderly men and postmenopausal women.

For instance, according to the trials  3mg of Ostarine (orally) during 12 weeks increases lean muscle mass by 1.4kg and reduces body fat by 300 grams without any physical load. It is also effective to prevent muscle loss (due to excessive catabolism) in cancer patients.

Nowadays there are several types of SARMs which have already passed human trials and very soon will appear on the market. However none of them is actually selective. In general they have high anabolic properties. The ratio of anabolic to androgenic properties vary from 3:1 to 10:1 (comparing to testosterone, which is 1:1)

Almost all selective androgen receptor modulators are freely available in the form of tablets. One should also mention that they don’t have liver toxicity. SARMs  became an optimal option for females, due to minimal influence on libido, blood cholesterol, liver and so on.

The major representatives of SARMs

Ostarine (MK-2866, GTx-024, Enobosarm) – affects bones and muscles

BMS-564,929 – muscle tissue

:ligandrol: (Anablicum, LGD-4033) – similar to Ostarine

LGD-2226 – bones and muscles, the trials are stopped due to high toxicity

S-40503 (Andarin) – mostly bone tissue, treatment of osteoarthritis (the research is suspended)

S-23 – male contraceptive

YK-11 (Myostine, Myostan) inhibitor of myostatin (under development)

RAD140 (Radarine, Radium) anabolic effect, increases endurance and has a neuroprotective effect

Reversol (Reverol, edrophonium, Endorol, Stenabol or SR9009) increases endurance (due to the formation of new mitochondria), treatment of obesity, muscular hypertrophy. It binds to Rev-ErbA, which in its turn performs different regulatory functions in human organism.

:ibutamoren: – Nutrobal (MK-677) – stimulates growth hormone production.

AICAR – increases endurance

Masteron (also Drostanolone, Drolban, Metormon, Permastril, Mastager, etc.) is an anabolic steroid which originates from dihydrotestosterone. It has high androgenic and moderate anabolic properties. Masteron is not an aromatizable steroid (i.e. there is no conversion into estrogen), moreover it acts as aromatase inhibitor.

Therefore there is no risk of estrogen related side-effects, such as gynecomastia and water retention. In clinical practice it was used as a cure for breast cancer in women, however, due to the high risks of virilization, it is practically out of use today.

Due to its anti-estrogenic properties and slight diuretic effect Masteron became popular among bodybuilders. They take it to keep muscle mass and strength during cuting cycles.

Drostanolone is of special interest among those athletes who want to improve muscular endurance before competition without gaining of excessive bodyweight. Moreover it increases strength and has apparent fat burning effect. For example Drostanolone cycle can reduce the amount of body fat by 5-7%.

All above mentioned features of Masteron make it attractive for athletes of all types of sports. This substance is also useful during weight losing diet. Its application maintains the muscle mass and reduces catabolism.

Side Effects of Masteron

As we said above Drostanolone is not aromatizable, therefore gynecomastia, water retention and high blood pressure do not occur. Nevertheless androgenic side-effects are possible: aggression, acne, alopecia, prostate hypertrophy and virilization in women. One should also mention that Masteron has low liver toxicity.

Dosage and Usage

The optimal dosage of Masteron is about 400-500mg/week. Higher doses do not produce further improvement of results, however the risk of side-effects may increase. As Drostanolone propionate has a short chain, you should take it three times a week (or EOD).

Combinations

Owing to high affinity to androgen receptors, it makes good combinations with such steroids as :winstrol: or :anavar:. They have less interaction with androgen receptors, therefore this stacking may produce synergistic effect during cutting cycle.

For a bulking cycle you can combine it with :testosterone-p:. However this combination suppresses natural testosterone production, so :gonadotropin: usage is required. Also bodybuilders combine Masteron with :trenbolone: or :boldenone:.

Primobolan (Methenolone) is an anabolic steroid, which originates from dihydrotestosterone. It has weak androgenic and moderate anabolic properties. This hormone is available in the form of tablets (Oral Primobolan), and injectable form (:primobolan:).

Injectable version of this substance (Primobolan Depot) is an Enanthate ester of Methenolone, which has prolonged action (about two weeks). It is regarded as one of the safest steroid. In medical practice it was successfully applied in treatment of underweight children, osteoporosis and sarcopenia. The major inconvenience is that its injection is rather painful.

A tablet version of Primobolan (Methenolone acetate) has shorter period of action (approximately five hours). Unlike other tablet steroids, Oral Primobolan has low liver toxicity. Nevertheless most bodybuilders prefer injectable version of Methenolone due to lower price and higher bioavailability of the hormone.

Characteristics

Anabolic properties – 88% of testosterone

Androgenic properties – 44% of testosterone

Transformation into estrogens – no

Liver toxicity – low

Available forms – tabs, injections

Half-life – 5-20 hours (tablets); 4-7 days (for injections)

Doping test – detectable during 100 days (tablets), or 6 months (injections)

Effects

Comparing to :decadurabolin: the anabolic effect of Methenolone is rather mild. Therefore most bodybuilders use it during cutting cycles, when the main goal is not to gain muscle mass but to preserve it.

Side effects

As Primobolan is not an aromatizable steroid, there is no risk of estrogen-related side-effects (gynecomastia and water retention).

Methenolone may decrease the level of natural testosterone synthesis to a little degree. However this effect is much weaker than in Testosterone and Nandrolone. For instance, the cycle of Oral Primobolan at the dose of 40mg/day can suppress the levels of endogenous testosterone by 50%.

In case of long cycles or high doses, the usage of gonadotropin is necessary (in order to avoid testicular atrophy). Methenolone does not affect the level of bad cholesterol (LDL) and does not increase blood pressure.

Due to the low androgenic activity the cases of baldness are very rare. Despite high safety rating the following side-effects may occur: aggression, excitability, insomnia, increase of liver enzymes etc.

Dosage and Usage

Usually athletes take Primobolan for cutting cycles or to preserve muscles. Owing to mild action the length of a cycle should last up to eight weeks. However longer period may increase the risks of adverse effects.

The common doses of Oral Primolaban are 50-100mg/day. In 2-3 days after the end of a cycle you should start PCT. The usual dosage of injectable Primobolan (Depot) is 400mg/once a week. Post Cycle Therapy should begin in 3 weeks since last injection.

Consult your doctor before taking Primobolan, make sure you don’t have contraindications.

Primobolan Combinations

Because of mild anabolic effect, bodybuilders often stack it with other steroids. For muscle gains it is usually combined with :nandrolone: (probably the safest cycle), :testosterone-c:, :anadrol: or :methandrostenolone:. For cutting cycles it is combined with :winstrol:.

Do not introduce more than one steroid into your combination. Take both steroids at half-doses. This method will decrease the risks of side-effects and enhance efficiency of your cycle.

 

Anavar (oxandrolone)

Oxandrolone (also Oxanoger,  Anavar, Oxandrin etc.) is one of the safest oral steroids. It has high anabolic index, meanwhile its androgenic properties are extremely low. This steroid greatly stimulates immunity and increases insulin sensitivity.

Therefore it was initially introduced into the medical practice as medication for immunocompromised HIV patients and overweight associated diabetes. It is also effective as a treatment of osteoporosis, osteochondrosis, Turner’s syndrome, anemia etc. Later, when its anabolic properties were discovered, it became popular among bodybuilders.

Steroid characteristics

• Anabolic properties – 400% of testosterone
• Androgenic properties – 25% of testosterone
• Transformation into estrogens – no
• Hepatotoxicity – moderate
• Administration – oral (tabs)
• Half-life – 8-12 hours
• Detection time – up to 60 days

The Effects of  Oxandrolone

• Improves relief and hardness of muscles
• Fat Burning
• Increases growth hormone levels
• Increases strength

Different experiments showed that Anavar is more efficient in fat burning than in gaining muscle mass. Therefore it is for those who have sufficient muscle mass and want to increase muscle hardness and reduce body fat.

Side Effects of Oxandrolone

Despite the fact that Oxandrolone has methyl group at 17th position, its liver-toxicity is negligible. Clinical studies revealed that Anavar, at the dosage of 20 mg/day (during 12 weeks) does not affect the level of hepatic transaminases – enzymes that indicate the liver damage.

As Anavar is a derivative of dihydrotestosterone, there is no conversion into estrogen. Therefore it doesn’t cause estrogen-related side-effects, such as gynecomastia and water retention.

Comparing to other steroids, moderate doses of Oxandrolone doesn’t greatly affect natural testosterone production and HPG axis.  However at high doses, the body reduces the levels of gonadotropin. Therefore the lack of stimulation can lead to testicular atrophy.

For instance, after 12 weeks of Anavar administration (at the dosage of 80 mg/day) the level of testosterone drops by 67%. This eventually leads to decreased libido. In order to avoid this side-effect you should combine Oxandrolone with gonadotropin or introduce androgenic steroids into your cycle.

Anavar may also cause decreased appetite, abdominal pain, nausea, headaches, high blood pressure etc. However, at moderate doses the side-effects of Anavar are rare, therefore it is known as one of the safest steroids.

Oxandrolone cycles

In “solo” cycles Anavar improves your muscle relief. The total duration of a cycle is 6-8 weeks. Start your cycle with small doses (20 mg/day). Divide the daily dosage into two portions and take it in the morning and after lunch. In one week increase the dosage up to 40mg/day. Maximal dosage is 80 mg/day, which should be divided into 3 portions.

In 2 days after the end of  Anavar cycle, start taking Tamoxifen at a dose of 10 mg/day to restore the natural testosterone production (for 1-2 weeks). Make sure that you don’t have contraindications before taking Oxandrolone (prostate hypertrophy, liver problems etc.).

Oxandrolone combinations

In order to prevent some side effects of oxandrolone (decreased libido, erectile dysfunction, liver toxicity) and to get muscle gains, it is recommended to combine Anavar with androgenic compounds: Testosterone, Sustanon, Primobolan etc.

When combined with other steroids, the daily dosage of Oxandrolone should be about 40 mg/day. Include proper sports nutrition and mass gaining diet into your cycle to achieve optimal results.

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Methandrostenolone (Danabol, Naposim, Methanoger)

Methandrostenolone is an anabolic steroid which was initially used as cure for burns and as medicine that improves the general tonus in women. Later, when it turned out that this substance can provide muscle gains, it became very popular among bodybuilders. Though nowadays this drug is banned by FDA, you can freely buy it in different countries of Asia and Eastern Europe.

This substance goes under different trade names such as: Dianabol, Danabol, Nerobol, Naposim, DBOL, Methandienone, Methanoger, Anabolin, Bionabol, Dehydromethyltestosterone, Metasthenol, Novabol, Perabol, Perbolin, Pronabol, Stanolon, Anaboral, Vanabol, Dianoget and so on.

Today there’s a lot of misinformation on Dianabol. Usually its toxic features are overstated, whereas anabolic propertied are underestimated. Nevertheless, a 6-week cycle of Danabol at the dosage 30mg/day can increase muscle mass by 8-10kg. It is usually followed by a loss of 2-5 kg, which can be reduced if you do the cycle properly.

Injectable Methane

Injectable form of methandrostenolone is known as Averbol, Reforvit B, Methastenon, Methanoliq, Metabol-25, Methanoger, Pharmabol 100, Methanabone, Methandienone, Dianoged etc. It comes in the form of suspension or oil solution.

This substance is also alkylated at position 17, but some researchers say that liquid form is more bioavailable and has less hepatotoxicity, though it is not proven. Injectable form can be also used orally, but it has an awful taste.

Steroid characteristics

Anabolic properties (comparative to test.) – 200%
Androgenic properties (comparative to test.) – 50%
Transformation into estrogens – low
Liver toxicity – moderate
Available forms – tablets, injections
Duration of action – 6-8 hours
Doping test – detectable during 3 months from the last usage.

The Effects of Dianabol

• Provides a quick gain of muscle mass.
• Increases strength
• Increases appetite
• Moderate fat burning effect
• Strengthens bones

Side effects

Gynecomastia
Though Danabol has a low rate of transformation into estrogen, it may cause gynecomastia. In order to avoid this side-effect one should take aromatase inhibitors.

Liver Toxicity

As Danabol is methylated at 17α position it causes moderate liver toxicity. However, methylation in this position protects it from fast destruction by liver enzymes, and makes the tablet form possible. Methylation also reduces attachment of Danabol to SHB globulins.

When taken for a long time, Dianabol thickens the membranes of liver cells, and worsens the conductivity of bile ducts, which is peculiar to all oral steroids. This eventually causes stagnation of bile and makes painful sensations in the area of liver. In order to prevent this side-effect, cholagogues are used.

However, one should mention that cholagogues can be divided into two groups: choleretics, which increase production of bile (e.g. Allohol, Holenzim), and cholekinetics, which help the gall bladder to release the bile into intestine (e.g. Cholosas).

In order to reduce the liver damage choleckinetics are used along with the intake of Dianabol, whereas choleretics are used after the cycle. Don’t make mistake, as simultaneous usage of choleretics with Danabol may worsen the situation. So, it’s better to use such hepatoprotector as ademetionine after Dianabol cycle.

Water retention

It belongs to estrogen related side-effects. As it occurs mainly in muscles, it gives them a puffy look. Therefore after discontinuation of the drug usage, the volume of gained muscles is reduced by 10-50%. You can avoid this phenomenon by taking aromatase inhibitors during your cycle.

Other side effects

Acne, hair loss, heartburn, high blood pressure (you can avoid it by taking aromatase inhibitors during your cycle), increased libido during cycle and temporary decline after it, testicular atrophy (in case of high doses and long-term usage), virilization (in women), myocardial hypertrophy (in case of overdose or genetic predisposition) etc.

Usage and Dosage

First of all do not use Dianabol if you are under the age of 21, or if you have contraindications – high blood pressure, hypertrophy of prostate, heart or liver problems etc. Don’t forget to consult your doctor to make sure that you don’t have contraindications.

Secondly, do not exceed the daily dosage, which is 30mg/day. The dosage is usually divided into 2 -3 parts. Due to the liver toxicity it’s better to take methandienone after food intake.

One should begin the Danabol cycle with 10mg, and in a couple of days gradually increase the dosage up to 20-30mg/day. Usually the cycle lasts 6 weeks. After the first week of the cycle it’s necessary to take aromatase inhibitors (e.g. Anastrozole 0.5mg/every 3 days). They will reduce water retention and risks of gynecomastia.

You should begin PCT in 2-3 days after the end of your cycle – Tamoxifen 20mg for 2-4 weeks. At the last week gradually reduce the dosage of Tamoxifen up to a complete discontinuation.
Check your blood pressure regularly. In case of high pressure reduce the dose, or take antihypertensives (Enalapril, 5mg)

Use testosterone booster for 3-4 weeks after the end of your cycle to restore the natural testosterone.
Also use sports nutrition and proper diet in order to get the maximum results.

Danabol Combinations

Combinations of Danabol with other steroids can improve efficiency of your cycle and reduce possible side-effects. In order to increase muscle mass Danabol is usually combined with: Testosterone; Sustanon or Omnadren; Primobolan; Trenbolone + testosterone; Nandrolone + testosterone. During combined cycles Dianabol is usually taken for the first 4 weeks.

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Testosterone propionate is considered one of the most popular steroids among bodybuilders. It can

be used for gaining muscle mass and strength, but due to its specific properties it is also used for cutting cycles.

Testosterone serves as a core molecule for creation of numerous hormonal (androgenic) compounds. By adding or removing atoms in testosterone molecule one can change its properties. For instance, testosterone propionate is created by attaching of propionic acid ester to testosterone molecule. Thus propionic residue determines pharmacological properties of this substance.

Steroid characteristics

• Anabolic activity – 100% of testosterone
• Androgenic activity – 100% of testosterone (high)
• Aromatization (transformation into estrogen) – high (anti-estrogens are required)
• Suppression of hypothalamic-pituitary-testes axis – yes
• Hepatotoxicity: Liver friendly
• Method of usage: injection
• Duration of action – 2-3 days
• Doping tests – detectable during 40-60 days

Mechanism of action

• Testosterone propionate initiates transcription of genes involved in metabolism of nitrogen. Thus it causes accumulation of nitrogen.
• It also increases the level of insulin-like growth factor in muscles and liver.
• It stimulates proliferation of satellites cells in muscles, which in turn cause muscle enlargement and enhanced muscle recovery.

One should mention that all testosterone esters have the same mechanism of action. The only difference is in their durability and preferential direction of action.

The Effects of Testosterone propionate

• Muscle mass enlargement
• Fat Burning
• Improvement of muscular relief
• Increase of strength
• Increased libido
• Lowers blood cholesterol levels
• Reduces the risk of cardiac ischemia and heart disease.

Due to a short propionic residue it has a short half-time, therefore injections should be done every other day. Probably this is the major disadvantage of propionate, in comparison with its long-living relatives, e.g. testosterone enanthate. A higher price can be also regarded as disadvantage, but its multifunctionality make it outstanding as it can be used both for gaining and cutting cycles.

Its short duration of action can also be regarded as advantageous – it provides ability to quickly adjust the dose and avoid allergic reaction in case you have intolerance to one of the drug constituents (e.g. oil).

At proper dosages it doesn’t make water retention in the organism, and doesn’t cause the rapid increase of body weight. Therefore the gained muscle mass is more qualitative than with other testosterone esters (for example enanthate).

After injection it is quickly absorbed into the bloodstream, so you can quickly feel the result. For these reasons testosterone propionate is suitable both for beginners and for experienced bodybuilders.

 

Dosage and Usage

You can use testosterone propionate standalone, but optimal results can be achieved by stacking it with other steroids. The usual dosage for beginners is 50 mg/ every other day. Professional bodybuilders can do 100mg daily or more.

In order to avoid gynecomastia and other estrogen related side-effects you should take anti-estrogen (for example  Proviron) or aromatase inhibitors starting from the second week of your cycle. When your cycle is completed a Post Cycle Therapy is required (tamoxifen or analogues). Usage of cortisol blockers will be also helpful in order to avoid the loss of gained muscle mass. Follow the diet for gaining weight and use sports nutrition.

Testosterone Propionate Combinations

For cutting cycles testosterone propionate is stacked with Stanozolol, Trenbolone acetate, Masteron, Primobolan and some other steroids. Besides, Propionate is an obligatory component of testosterone ester mixtures, such as Sustanone or Omnadren – it provides immediate effect of these compounds.

Here is an example of propionate cycle for beginners:

• Propionate 50mg/ EOD
• Winstrol 30mg/day (starting with 10 mg, and adjusting the dose to the optimum within 1 week).
• After 6 weeks you should discontinue using anabolics and start PCT after 3-4 days.

In this cycle you will see synergistic effect of these drugs. This means that the effect of their simultaneous usage is greater than the effects of their separate usage. Moreover, the risk of side effects in this cycle is reduced. Some bodybuilders inject propionate into the target muscle (e.g. biceps, deltoids etc.), but the effectivity of this method is not yet proven.

Side effects of propionate

The usual complain about propionate usage is pain, irritation and redness at the spot of injection. The side effects of testosterone propionate are similar to other testosterone esters when taken at high dosages:

• Gynecomastia
• Acne
• Hair loss (scalp)
• Increased growth of body hair
• Prostate enlargement (especially in the elderly)
• Virilization (in women)

Testosterone propionate suppresses natural testosterone production, which usually returns to the normal level in 2-3 months after the end of the cycle. If you do a prolonged cycle, then you should take gonadotropin at the dosage 500 IU/ week, starting from the second week of your cycle. At proper dosages it doesn’t make any adverse effect to such organs as liver or kidneys. Women should avoid it due to high risks of androgenic side-effects.

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