The use of antiestrogens

What do they represent? antiestrogens and why do we need them so much?! It is unlikely that anything more effective than anabolic and androgenic steroids . No matter how sad it may sound, there is no alternative to steroid drugs. Alas, without exception, all drugs of this type have many different side effects. These include excess fluid accumulation in the nipple area in men, the so-called female breasts. The scientific name of this defect isgynecomastia . Gynecomastia without proper treatment can result in serious problems and ultimately can only be cured with the help of surgery.
One thing pleases me, in the arsenal bodybuilder, there are a huge variety of means to combat this disease. And they are called antiestrogens, but before talking about them, I suggest learning a little about the culprit of this problem, namely estrogen.

What is estrogen?! ​

The male body, unlike the female body, is not capable of independently producing the female sex hormone (by the way, women are unique in their own way, because only their body is capable of independently producing both male and female sex hormones - estrogen, testosterone).
IN male body female sex hormones are obtained only by converting them from testosterone; to be precise, only one hormone is obtained in this way estradiol, the most powerful of the list of antiestrogens for men. This transformation becomes possible only with the participation of special substances - enzymes called aromatosis. The conversion process itself is called aromatization.
Estradiol is present in the blood of all men without exception. A lack of estrodiol, just like its excess, leads to a decrease in synthesis natural testosterone. Estradiol also has a positive effect on a man’s mood, his tone and the actual success of training. But all this becomes possible only with a normal level of this hormone in the blood. When the balance between estradiol and testosterone is disturbed, the aromatization process I described above occurs. Anti-estrogen for men has a lot of weight.

A little about steroids, aromatizing and more. ​

Long-term use of steroid drugs can lead to an increase in the level of estrodiol in the blood and, as a result, to aromatization. I should immediately note that only so-called aromatizing steroids have this property. The most prone to this process Testosterone is considered, of course. In second place is a steroid such as methandrostenolone. Boldenone and fluximetreon have less weak aromatizing properties.
There are steroids that can be converted to estradiol without the aromatization process, these include nandrolone, norethandrolone and ethylestrenol. However, this does not make it particularly easier, whatever one may say, and the level of estrogen from these drugs increases in any case.
It should also be noted that among non-aromatizing drugs there are, so to speak, outcasts, I mean drugs that can cause the accumulation of water in the nipple area without the participation of estrogens. First of all, it is oxymethalone.
But let's go back a little and talk about this. Is it possible that the level of estrodiol in a man’s blood will increase even with short-term use of steroid drugs. I will answer without delay, no, it is not possible. Like any side effect, this defect requires long-term use or overdose.
And the last thing I would like to discuss is that each person can react to estrogens in the blood in their own way, because we are all different, no matter how trivial it may sound, some are generally immune to the aromatization process, while others, on the contrary, may be particularly predisposed to this problem.

Restoring natural balance. ​

I propose to finish with the theory and return to where we actually started and what I wanted to tell you about, i.e. To antiestrogens . It is a mistake to assume that an anti-estrogen is a drug created specifically for men; it was supposedly created to suppress the development of the feminine principle in the male body. It’s quite the opposite; initially, antiestrogens were created specifically for women who had problems with excess estrogen in their bodies. For example, particularly large amounts of estrogenic hormones can lead to the development of infertility in women. However, such cases are very rare, and no more than a hundred such cases are registered per year.
Now let's talk about the antiestrogens themselves. All of them are divided into two groups according to their characteristics and properties. The first is aromatase inhibitors. The second is estrogen receptor blockers. In the first case, aromatase inhibitors join aromatase enzymes, sorry for the tautology, just like testosterone and, as a result, reduce the amount of these enzymes to a minimum and reduce the risk of aromatization.
Blockers, on the other hand, act completely differently, they attach to estrogen receptors, do not activate them, but quite the opposite, they begin to act, creating interference and preventing estrodiol from performing its functions.
Those. we find that in the first case, antiestrogens simply stop converting testosterone into estradiol, and in the second case, estradiol simply stops working or is blocked, as you prefer.

What to choose from?! ​

I will say right away that the list of anti-estrogenic drugs is not so long, but there is still plenty to choose from. There are six antiestrogens in total, but two of them have never reached our market. For this reason, I will next talk about four drugs that are not difficult to find here. For greater convenience, I have arranged all antiestrogens drugs in alphabetical order.

Arimidex (anastrozole) ​

Arimidex, perhaps the most effective and most expensive anti-estrogen on the cycle. This drug is produced by only one pharmacological company from Norway - AstraZeneca. Arimidex is an aromatase inhibitor and, as I already said, it is very powerful, even half a milligram of the drug is a sufficient dosage that can combat aromatization in most cases.
An exception would be when taking particularly high doses of aromatizing steroids, in which case you will need dosages greater than 1 mg. The only thing that can discourage an athlete from purchasing this drug is its price; even in the US market, it is considered almost the most expensive pharmacological substance.

Clomid (clomiphene citrate) ​

In the CIS, this drug is also known as clostilbegit. Main Feature clomid lies in its versatility, it not only does an excellent job of blocking aromatase, but is also able to restore the level of luteinizing hormone in the male body.
Clomid, unlike most antiestrogens, can, and in some cases even needs to be taken throughout the entire steroid course. The average daily dose of the drug is 50 mg, i.e. one tablet, in critical situations, the dosage can be doubled. Antiestrogens on the course are increasingly becoming part of our daily lives.

Nolvadex (tamoxifen) ​

According to its structure and properties Nolvadex or tamoxifen similar to another pharmacological drug, namely with clomiphene. It is exactly similar, because... There are also differences, for example, Nolvadex is a more powerful drug, but unlike clomiphene, it does not affect the level of the LH hormone.
Another feature of the drug is its strong anti-estrogenic effect on the liver and, as a result, a decrease in the level of synthesis of the insulin-like factor IGF-1, as you understand, this feature is negative. The usual daily dose of the drug is in the range from 20 to 40 mg, I would recommend taking the minimum indicated dose, because... Nolvadex is a fairly powerful drug.

Proviron (mesterolone) ​

Proviron a drug undeservedly forgotten by bodybuilders. At its core, Proviron is not a classic anti-estrogen, which makes it stand out from general list. Further, more, Proviron is an active anabolic steroid that promotes the development of muscle tissue.
In its structure, Proviron resembles methenolone, but only resembles it because there is also a significant difference. In terms of its antiestrogenic characteristics, Proviron is more reminiscent of an aromatase inhibitor. Ask why exactly it resembles more?! It's very simple, for the most part, Proviron is an inhibitor, and to a lesser extent, Proviron is a blocker. So, in one steroid drug the properties of two anti-estrogenic groups were mixed. Another attractive aspect of Proviron is its price and reliability.

Orimethene (aminoglutethimide) ​

This drug is not publicly available, but if you really want to, you can still get it, which is why I included it on my list. Helpful information for those who are interested, called Orimethen, this drug is produced only in Europe; abroad it goes by the name Cytadren. Orimethene, like Armidex, is an aromatase inhibitor, but much weaker. The negative aspects of the drug also include its ability to block the activity of the desmolase enzyme. The good news is that this side effect occurs only when using particularly large doses of orimethene. The standard daily dose of 250 mg cannot in any way affect the activity of the above enzyme.

Cyclophenyl ​

The last drug on my list. It will be great luck to find cyclophenyl in free retail in the CIS. Cyclofenil in its structure is a weak estrogen, but the antiestrogenic properties of the drug lie in the occupation of estrogen receptors, i.e. This drug is classified as an aromatase blocker. Cyclofenil has some similarities with Clomid, since it is also able to increase the level of synthesis of its own testosterone.
The action of cyclophenyl can be called very slow, because the drug begins to act only a week after taking it. The standard daily dose of the drug is 400-600 mg, i.e. 2-3 tablets per day, which is much more than any other anti-estrogen.
In conclusion, I want to tell you something else. Flavoring is not always evil. Indeed, largely thanks to estradiol, testosterone and methandrostenolone have their properties for building muscle mass. Estradiol also helps increase the secretion of growth hormone, which for some athletes is the key to success in training. Estradiol itself is not harmful, only its imbalance is dangerous. But how can you find out your estrodiol level, or is it impossible and you will have to take antiestrogens for the rest of your career? There are several ways. The first, perhaps the most expensive in a financial sense and in terms of time, is to do a blood test. This method is also the most accurate of all. The second way, it can be called the old-fashioned way, is to start taking antiestrogens immediately after the first pain appears in the nipple area. Don’t ignore your body’s signals; even the smallest tingling sensation can signal the onset of gynecomastia. I would advise the third method only to experienced chemists, start use of antiestrogens when the first symptoms appear and stop when they disappear. Dangerous? Of course, yes, but if you don’t see any other way, and you don’t have free time, this method will be a way out of this situation.
Therefore, there is no reason to panic and there is no need to resort to constant use of antiestrogens. Again, it’s up to you to decide what to do. You have the time and desire to get tested, but if you are not able to allocate half a day for this procedure, resort to time-tested methods.
Based on materials: AthleticPharma.com

Aromatase inhibitors (AIs) belong to a group of medications used in the treatment of cancer caused by tumor sensitivity to estradiol (most often breast cancer); The essence of the work of drugs in this group is to block the work of the aromatase enzyme, which is involved in the change of androgenic hormones into estrogens. AIs are popular in sports due to their ability to reduce the level of female sex hormones due to high consumption of steroids, subject to conversion by the enzyme aromatase (under its influence, testosterone is converted to estradiol and androstenedione, and then androstenedione is transformed into estrone, but estrone is 5 times more biologically active times less active than estradiol, and therefore it is not considered as an active participant in the side effects of estrogen during aromatization); AIs are also used to combat the consequences of high estrogen levels, such as the fight against gynecomastia (female-type breast growth) or its prevention; in rare cases, the consumption of inhibitors is aimed at increasing the levels of LH and FSH, which leads to an increase in the level of endogenous testosterone ( that is, for post-cycle therapy). In BB, aromatase inhibitors are consumed during the anabolic steroid cycle to:

1. Prevention of gynecomastia (excessive levels of estradiol and estrone due to aromatization of steroids under the influence of aromatase can potentially lead to female-type growth of the mammary glands in an athlete, thus, taking AI will block aromatase, as a key enzyme involved in the direct increase in estradiol levels).

2. Getting rid of excess water (as is known, with increased levels of estrogen, the accumulation of water increases, this happens because estradiol is able to regulate the balance of sodium in the cells and an increase in sodium levels leads to the accumulation of excess water, this is what is noticeable in some athletes whose face resembles an inflated balloon , and the eyes are quite consistent with those of a resident of China).

3. Suppression of excess blood pressure, is a consequence of the second point. An increase in fluid content due to a high level of estradiol leads to an increase in blood pressure, while the consumption of AI can reduce the level of estradiol, and therefore reduce the manifestations of hypertension.

4. Reducing the impact of high levels of estradiol on the HPA axis, which means preventing problems with the restoration of endogenous (native testosterone) after a cycle of steroid use.

5. Increasing the level of endogenous testosterone in the body. This effect of aromatase inhibitors is based on the feedback principle - the suppression of estrogen below the normal level in the body signals the hypothalamus and pituitary gland to increase this level to normal values ​​(the body always strives for balance), but the male body does not produce estrogen, it does not have ovaries, therefore the brain begins to produce GnRH and then LH and FSH to increase the level of endogenous testosterone, which will later be converted into estrogen under the influence of the aromatase enzyme. But AIs block aromatase, which means the transformation of testosterone to estradiol and estrone does not occur, so we can observe a vicious circle - an increase in the level of testosterone with the aim of converting it into female sex hormones, but since the necessary enzyme is not there, an increase in the level of estrogen does not occur , and the brain has no choice but to further stimulate the production of new portions of androgens.

When planning a cycle of taking AS, you need to understand that not all steroids are susceptible to aromatization, so taking AI may not always be justified. For example, steroids exposed to the aromatase enzyme include: all testosterone esters, boldenone (several times less than testosterone, but still), methyltestosterone, and to some extent fluoxymesterone.

The approach to consuming aromatase inhibitors during a steroid cycle can be different; in general, three approaches can be distinguished:

A. Wait for signs of high estrogen levels to appear (signs of gynecomastia, water retention, hypertension) and then use AIs to suppress side effects.

b. Selecting an average dosage of AI and consuming it every other day to prevent an increase in the level of female sex hormones.

V. Taking tests to identify the level of estradiol during the course of AS (about 2 weeks when consuming short-lived drugs or 4-5 weeks after using long-lived drugs), prescribing a dose of aromatase inhibitors and repeating a blood test for estradiol to clarify the dosage of AI.

Rarely used drugs of the AI ​​class include Aminglutemide (the first AI, suppresses not only aromatase, but also endogenous glucocorticoids and thyroid hormones) and Vorozole (similar in action to Letrozole, which will be discussed later). In everyday life, Mesterolone (aka Proviron) is often equated to inhibitors, but it does not belong to the class of aromatase inhibitors; it is an androgen with some antiestrogenic activity, whereby it both “binds” aromatase and blocks estrogen receptors, it should be noted that this the drug has significantly weaker anti-estrogenic activity than real AIs, and athletes who are too sensitive to female sex hormones may experience the side effects of increased estrogen levels even when taking Mesterolone on an AC course.

Like all medications, drugs of the aromatase inhibitor class have a number of side effects: nausea, vomiting, pain in the stomach area, vomiting, fatigue, insomnia, constipation, excessive sweating, increased levels of “bad cholesterol” - LDL.
Let's look at the most commonly used AIs in bodybuilding practice:

Letrozole. Created, like all drugs of its class, for the treatment of oncological diseases associated with the sensitivity of tumor tissue to estrogen levels (mainly breast cancer in women). The essence of its work is the targeted binding of aromatase, which leads to the inability of the enzyme to communicate with androgens, disrupting the mechanism for increasing estrogen levels. The efficiency of drug binding to aromatase (at 2.5 mg per day) is 95%, which shows quite effective work drug. A very important feature of Letrozole in the treatment of cancer in women is the absence of an increase in the levels of luteinizing and follicle-stimulating hormones, which eliminates the possibility of signs of virilization. However, in men the situation is opposite and an increase in the level of endogenous testosterone is observed. It should be noted that there is no correlation between taking Letrozole and changes in the activity of the thyroid gland, as well as its absence in the occurrence of strokes and heart attacks, which indicates the potential for using the drug in patients with disorders of the cardiovascular system.

After administration, the absorption of the drug occurs quite quickly (faster on an empty stomach, taking with food doubles the absorption time - up to two hours), while the bioavailability is almost 100%. Treatment of cancer requires taking 2.5 mg of the drug daily for several years. In sports, taking such high doses is not advisable and the average dosage is 1.25 mg every other day (a preliminary “load” of 2.5 mg per day for 7-8 days is possible). Of course, the ideal option for selecting the dose of Letrozole is a blood test for estradiol, which will allow you to more accurately select the right amount of the drug.

Exemestane. It is a third generation drug, the only commonly used aromatase inhibitor with steroidal “roots”. It has weak androgenic activity and does not affect the activity of glucocorticoids and mineralocorticoids. It is similar in action to Letrozole (as well as Anastrozole) in relation to the growth of endogenous testosterone (even small dosages of Exemestane lead to this). To urgently combat the manifestations of gynecomastia, it is advisable to use the drug at a dosage of 25 mg per day (however, the prophylactic dose ranges from 25 to 12.5 mg every other day). When taking 25 mg per day, aromatase binding occurs by 98%.

The characteristic features of Exemestane are:

1. Improved absorption when taken with food by 40%.
2. Irreversible binding of aromatase

The highest concentration of Exemstan after oral administration is observed 120 minutes after ingestion.

Anastrozole. One of the most commonly used aromatase inhibitors in sports when taking steroids. Just like Letrozole and Exemestane are third generation AIs, the molecular structure of Anastrozole is similar to that of Letrozole. Shows outstanding activity when blocking the work of aromatase when taking steroids. Nevertheless, estrogens have a protective function against LDL, which explains the lower number cardiovascular diseases in women (pre-menopause) than in men, thus a strong suppression of estrogen levels leads to an increase in the level of “bad cholesterol”, which requires additional intake Omega3 or synthetic inhibitors of HMG-CoA reductase (the HMG-CoA enzyme is involved in the synthesis of cholesterol). Another disadvantage of increasing LDL due to taking AI is the compaction of cell membranes, which impairs the penetration of AS molecules into the cell, which means the intensity of protein synthesis will not be so high.

The dosage of Anastrozole varies depending on the dosage of the steroids used and the goal of the athlete (for example, when blocking gynecomastia, 1 mg per day can be taken), prevention is possible at a dose of 0.5-1 mg. The drug is taken on an empty stomach, in which case the maximum content of the drug in the blood is achieved within 60-120 minutes.

Thus, the use of aromtatase inhibitors when taking AS is due to the goal of combating side effects associated with an excessive increase in estrogen levels due to steroid use, as well as (in rare cases, since estrogen receptor blockers are mainly used for this) for The goal is to increase the level of endogenous testosterone, however, a decrease in estrogen levels can provoke an increase in “bad cholesterol”, which requires adjustment of the blood lipid profile by taking appropriate medications.

Article by Pathophysiologist!
How to deal with excess Aromatization (questions and answers)

Here is the promised article, since nothing has been said about Aromatase Inhibitors on this forum, let’s start with the simplest and most accessible, but not at all useless.
Since our body (a man’s body), due to its characteristics, cannot produce female sex hormones, with the help of certain enzymes the process of converting male sex hormones into Estrandiol (one of the most powerful Estrogens) is activated, which is called the process of AROMATIZATION. We must immediately make a reservation that Aromatization is NOT a NEGATIVE process, since an insufficient amount of endogenous estradiol, as well as its excess, leads to suppression of the body’s production of endogenous testosterone, and the aromatization process is a prerequisite for building muscle mass (increases the utilization of glucose by cells as well as the secretion growth hormone, improves the sensitivity of androgen receptors, etc.). Concluding from everything written above, the main condition for the successful use of male sex hormones to build muscle mass is the balance between testosterone and estradiol; in general, this is not as difficult as it seems.
Well, let's start first, probably the most famous drug Tamoxifen, this drug is considered as one of the main modern antiestrogens. The mechanism of the antiestrogenic action of tamoxifen is explained by its ability to competitively bind to estrogen receptors in target organs and thus prevent the formation of the estrogen receptor complex with the endogenous ligand 17-b-estradiol. Due to this property, Tamoxifen is mostly used to block the process of excessive aromatization during the cycle, however, in the case of this drug, I consider this not practical, and I will explain why. It’s not customary to mention this, but still, Tamoxifen is an excellent drug for restoring the body’s natural hormonal levels(I am an ardent opponent of the use of Gonadotropin as a drug after a course of therapy, since sometimes the consequences of its use are more dire than the suppression of the production of endogenous testosterone, and I undertake to prove that courses of Arc restoration can be carried out without it with the achievement of faster results), since Tamoxifen is one from Triphenylethylenes, it increases the sensitivity of the pituitary gland to GnRH, which in turn leads to greater production of luteinizing hormone, which is actually required during the recovery period. Also, taking Tamoxifen in a temporary period of more than 7 days during the recovery period leads to an increase in the level of Endogenous Testosterone by more than 25%, also taking this drug has a positive effect on the level of high-density cholesterol, which cannot but rejoice since athletes of power sports are the first in terms of the number of cardiovascular diseases. The only negative is the suppression of the body's production of insulin-like growth factor, and it is for this reason that I consider Tamoxifen a drug for the period of restoration of natural hormonal levels and not a course drug for combating excess aromatization. Now about the dosage: during the course, dosages are usually used from 20 to 40 mg per day; during the recovery course, dosages range from 10 to 30 mg per day.
Next, let's talk about a drug like Clomid. In general, I am very skeptical about this drug, since I consider it to be a duplicate of Tamoxifen, only with the amendment that using Clomid after a course of therapy requires higher dosages (from 50 to 150 mg per day) since its effect on the Endocrine system is weaker; I think it’s insulting to talk about the antiestrogenic properties of Clomid since this effect of this drug is negligible. More than taking Clomiphene Citrate helps to increase the level of sex hormone binding globulin, which is not a positive effect at all. And yet, it must be said that the presence of Tamoxifen and Clomid on the market gives a choice in preferences, since both drugs more or less successfully restore the Endocrine system, so the choice is yours, friends.
Well, now let’s move on to the drug Mesterolone, which is excellent in all respects and is referred to in the world as Proviron. If anyone is not familiar with me, then you need to know that I consider it the best of the drugs available to absolutely any steroid user. Let me explain the reason for my “pink drool” regarding this drug. Mesterolone is a derivative of dihydrotestosterone, that is, Androgen. Despite this, Mesterolone has a blocking effect on the process of excessive aromatization, that is, it suppresses the “production” of estrogens, while stopping the use of Mesterolone does not cause a relapse in the process of excessive conversion of Testosterone into Estrandiol, and Mesterolone also has a binding effect on sex hormone binding globulin. So, I consider Mesterolone to be a many-sided drug; let’s say it provides excellent assistance during the course in the fight against excessive aromatization from 25 mg to 75 mg per day. Also, due to its original function, Mesterolone is perfect for restoring the Endocrine system after a course, increasing Testosterone levels and the main positive factor increasing Libido and Potency, the quantity and quality of sperm, these problems are undoubtedly the main ones during the restoration of the natural endocrine system and simply after an intensive course. To restore the endocrine system, 25 to 50 mg per day is usually sufficient. It is also worth noting the positive effect Mesterolone has during “drying”, that is, increasing muscle rigidity and the ability to give muscles amazing definition. In general, I consider Mesterolone a drug capable of becoming some kind of alternative to the more expensive Anastrozole, Letrozole and Aromasin, which will be discussed below.
Anastrozole, Letrozole and Aromasin. The first 2 drugs are third-generation aromatase inhibitors, and the latter is an irreversible steroidal aromatase inhibitor and has been the subject of scientific debate and experience among Endocrinologists for a very long time. Their use in medicine is oncological diseases, characterized by an increased amount of estrogen and progesterone in the patient’s body. So why are these drugs used in BB? When using high-androgenic drugs, the effect of converting a certain amount of androgens into estrogens occurs under the action of the aromatase enzyme. Which is not bad at all, but in excess this effect leads to some negative consequences, which we are trying to fight by all means, is Gynecomastia, etc. Since the drugs of this pharmacological group are designed to block excess estrogen production by inhibiting aromatase, and we also use them to combat the undesirable consequences of excessive aromatization.
Well, let's take turns, the first will be Aromasin (exemestane), because it is a steroidal aromatase inhibitor, what does this mean, and the fact that it is similar in structure to the natural steroid androstenedione, which was written about in the topic Prohormones. The peculiarity of the mechanism of action of this drug is its irreversible binding to the active fragment of the Aromatase enzyme, which causes inactivation of this enzyme, thereby achieving the effect of reducing the concentration of estrogen. Aromasin has minor androgenic activity (when used in high doses) and minor progestogenic and estrogenic activity. Aromasin also had no effect on the biosynthesis of cortisol and aldosterone in the adrenal glands; this feature is used in third-line hormonal therapy, excluding Aminoglutemide, which is already not harmless for the endocrine system, from the list of uses, and therefore there is no need for replacement therapy with glucocorticoids and mineralocorticoids. Also, a feature of the drugs of this pharmacological group is an increase in the levels of LH and FSH, that is, the restoration of the secretion of endogenous testosterone due to the feedback principle at the level of the pituitary gland: a decrease in the concentration of estrogen stimulates the secretion of gonadotropins in the pituitary gland. It is recommended to take it after a meal (food improves absorption: the level of exemestane achieved in the blood plasma is 40% higher than after taking the drug on an empty stomach). BB Aromasin recommends taking half a tablet 1 time/day daily. The main thing worth noting is the appearance of signs of lethargy, asthenia (general weakness) and dizziness, as well as loss of concentration and a decrease in the speed of psychomotor reactions, indicating excessive blocking of the effect of Aromatization.
Next we will talk about the active substance Anastrozole and Letrozole, these are highly selective non-steroidal aromatase inhibitors, their main area of ​​application is the fight against excessive activity of the aromatase enzyme, so Estrogens are formed only from androgens, the production of which in men occurs mainly in the testicles and a small amount in the adrenal glands . And the transformation into estrogens occurs with the participation of the aromatase enzyme, which is not bad, since without aromatization the normal effect of androgens on the body is not possible, which means muscle growth is not possible, but as a result of the excessive aromatization process, androgens are converted into estrone sulfate and estradiol, contributing to the manifestation of negative effects, so-called Gynecomastia, accumulation of fat deposits according to the female type, etc. Anastrozole and Letrozole provide stable suppression of estradiol in the blood serum throughout the entire duration of its action, that is, it reduces the concentration of estrogens in the body. He, Letrozole and Arimidex literally save the lives of women who are not susceptible to Tamoxifen. The main reason why Anastrozole and Letrozole are used in BB is that they do not have an adverse effect on steroidogenesis, that is, when using Anastrozole and Letrozole, replacement (complementary) steroid therapy is not required when using aminoglutethimide, this information also applies to BB. Anstrozole and Letrozole resistance explained high level prolactin, therefore, during the period of restoration of the Endocrine system when using Anastrozole and Letrozal, it is necessary to take antiprolactin drugs, although both drugs have some positive effect on the inhibition of prolactin, however, you should not refuse to use UPS since they are more specific to this effect. Also interesting is the combination of Anastrozole and Letrozole with exemestane (a steroidal aromatase inhibitor, which I wrote about above), which is not inferior to Aminogluthemide in terms of its effect on restoring the endocrine system. It must also be said that Letrozole is more potent active drug than Anastrozole (proven by clinical experiments), but this difference is understandable only in the treatment of oncological pathologies, that is, it will not be noticeable to us.
By the way, it should be said that drugs such as Testosterone (Hertilate, Cypionate, Enanthate, etc.) and combinations of its esters (Omnadren, Sustanon, Testenone, etc.) have the greatest tendency to excessive aromatization. Methandienone (its analogues Anabol, Naposim, Methanox, etc.), Methyltestosterone is prone to aromatization.
And of course, it is not correct not to notice that there are drugs (these are Nandrolone, Norethandrolone, Oxymetholone, Trenbolone, etc.) that can be converted into estradiol without the participation of aromatase, copying the action of the second of the female sex hormones - progesterone, we will talk about this later since this question has been raised more than once.
Well, in conclusion, a list of practically non-aromatizing drugs oxandrolone, methenolone, drostanolone, stanazolol, etc.
In conclusion of all that has been written, it must be said that the scope of use of Aromatase Inhibitors in BB is very extensive, since inhibitors are used on a course to suppress the side effects of Aromatization, and outside the course, since the class of these drugs helps restore the endocrine system after steroid courses. And it must be said that this class of drugs is capable of suppressing estrogens in general as such, which entails a large number of side effects.

When adding AAS, or, in other words, synthetic male sex hormones or their derivatives, to your diet, it is worth remembering that our body strives to maintain homeostasis, that is, it is in balance. The balance of sex hormones is no exception. Our hormonal system works on a feedback principle. An increase in one of the hormones is followed by an increase or, conversely, a decrease in the other, depending on their nature and function. Let me make a reservation right away that we will talk mainly about aromatizing drugs, more specifically about testosterone. In general, this article will be useful to everyone, including those who are already using AAS or are still planning to, for a general acquaintance with the main hormones and their functions.

Sex hormones can be divided into two large groups: androgens (male) and estrogens (female).

From the group of androgens, we will highlight the two most important hormones for us - testosterone and dihydrotestosterone. From the group of estrogens - estradiol. Progesterone
and prolactin belong to other groups of female sex hormones, but there is no need to focus on which ones in this article.
Nevertheless, the above hormones should be remembered for yourself when using AAS, since it is mainly with them that we will deal, invading our endocrine system. I believe that due attention should be paid to their content in the blood plasma. Why is it important? Knowledge of the current state of affairs in the field hormonal balance the body will help to avoid a number of side effects associated with increased levels of estradiol, prolactin and progesterone, understand and evaluate the response of your system. And in general, as in many other cases, awareness does not hurt. We will try to briefly review the main male and female hormones, identify some patterns and understand the principle of their action. Let's begin.

Testosterone function

Testosterone is the main male sex hormone, androgen. Responsible for the complex formation of a man. Testosterone is involved in the development of secondary sexual characteristics (male voice, body hair, male body constitution, etc.), regulates spermatogenesis, sexual behavior, and also affects nitrogen and phosphorus metabolism, accelerates the growth of muscle mass.

Testosterone fractions

Free testosterone is a hormone not bound to the proteins albumin and globulin. About 60% of testosterone in the blood is associated with SHBG (sex hormone binding globulin), while the other part is associated with albumin. Approximately 4% is the free portion of testosterone in the body.

It is believed that the biologically active form is only testosterone that is free and bound to albumin proteins. It is known that testosterone bound to SHBG is protected in the circulation from proteolytic degradation, that is, from the destruction of hormone molecules. Data regarding the activity of testosterone associated with globulin are very contradictory. In the context of this topic, it is important for us to have a general understanding of testosterone, to understand the difference between free and general.

So, let’s briefly summarize: total testosterone is all testosterone in the body, including free testosterone, free testosterone is exclusively that which is not bound to the proteins albumin and globulin.

Testosterone levels for men

Let me immediately explain that biologically active testosterone is free testosterone + testosterone bound to albumin proteins. I also note that in men who regularly exercise with weights, especially at a young age, the indicator may be overestimated, which is not a pathological deviation.

Symptoms of testosterone deficiency:

• Decreased mental abilities and memory;
• Depression, irritability;
• Hair loss, lack of hair;
• Increased deposition of adipose tissue;
• Erectile disfunction;
• Decreased libido.

Conversion of testosterone to dehydrotestosterone

Testosterone and DHT molecule

To one degree or another, depending on the individual characteristics of each person, testosterone in the body is converted into dihydrotestosterone (abbreviated DHT). This process occurs under the influence of the enzyme 5-alpha reductase. If we delve a little deeper into the details, under the influence of the above enzyme, two hydrogen atoms are added to the structure of the testosterone molecule (hence the name “dihydrotestosterone”), and the 4-5 double bond of testosterone is also removed.

Dihydrotestosterone occupies a significant position in the organization and functioning of the central nervous system.

Here we come to the meaning of the indicated transformations. The steroid created under the influence of these reactions is able to bind more successfully
with androgen receptors than testosterone itself, which makes the activity of DHT 3-4 times stronger than the activity of its predecessor, testosterone. I’ll add that the hormone progesterone, which we’ll look at a little later, is a DHT antagonist. The body can respond to an increase in DHT with a logical action - an increase in progesterone
in order to avoid too strong conversion.

DHT action and side effects

DHT manifests itself most aggressively in issues related to the prostate, skin, scalp, liver and various regions of the central nervous system. This is due to the fact that 5-alpha reductase is localized primarily in these tissues. Hence, unfortunately, the well-known side effects: baldness, prostate hypertrophy, sebaceous glands, as a result, an increase in skin oiliness and the appearance of acne, etc. However, it is worth understanding that there are also significant advantages to the strong androgenic activity of DHT. For example, dihydrotestosterone occupies a significant position in the organization and functioning of the central nervous system.

A large number of nerve cells have active androgen receptors. Based on this fact, the importance of DHT in ensuring the full functioning of the central nervous system is explained. It is worth understanding that the normal functioning of the central nervous system is not just an improvement in mental activity, reaction, recovery, etc. The interaction between the nervous system and skeletal muscles is significantly improved. This interaction is called the neuromuscular connection.
the importance of which is spoken about very, very often.

I can only repeat myself and say that it is necessary to feel the work of the target muscle group during training. Briefly, it can be simplified and expressed in the following formula: we feel the muscle better, we work better, we grow better.

Is conversion blocking necessary?

Blocking the conversion of testosterone to DHT can lead to worse results on the testosterone cycle, that is, inhibition of the growth of muscle mass and strength. Blocking is done by adding a 5-alpha reductase inhibitor, for example a drug such as finasteride. However, I will say that DHT should not be viewed as an exclusively negative and unnecessary hormone; it is extremely important in building muscle mass and increasing strength.

I would like to add that a person with elevated levels of DHT will not necessarily have any side effects associated with the latter.
In many ways, the unpleasant effects are caused not only by excess conversion, but also by the individual number of androgen receptors in certain tissues.

So, we found out that DHT is an extremely strong anabolic and androgenic agent. With a large number of androgen receptors in certain tissues or with an increased background of DHT, the hormone can lead to a number of side effects. However, without it, the progress of muscle fiber hypertrophy and strength growth will be significantly lower or completely absent.

Testosterone, aromatization. Estradiol

Flavoring

Under the influence of the aromatase enzyme, testosterone is able to convert into estradiol, hence the process called aromatization. Interestingly, the molecules of testosterone and estradiol differ only slightly, namely in the absence of one methyl group and several hydrogen atoms. In the male body, estradiol is a derivative of testosterone. This means that, as a rule, increased estradiol is a consequence of increased testosterone, excluding individual special cases, which are not the rule.

In excess amounts, estradiol harms a man, turning him into a woman.

Let's figure out what estradiol is and why we need it. Estradiol, as we defined at the beginning, belongs to the group of female sex hormones, estrogens. This hormonal substance in a man’s body performs a number of important functions, for example: active participation in the process of ejaculate secretion, improving oxygen metabolism, regulating the functioning of the nervous system, increasing blood clotting, stimulating metabolism, etc. It is believed that in excess quantities the hormone can lead to to such side effects, such as female-type fat deposition, nervousness, decreased libido and erectile dysfunction, gynecomastia, etc. In other words, to simplify, we can say that in excess estradiol harms a man, turning him into a woman.

Testosterone norm for men Estradiol (E2) 3–70 pg/ml

So, we found out that excess and deficiency of estradiol are harmful, a golden mean is necessary.

Aroma suppression

I would like to dwell in more detail on the excess value of estradiol. Indeed, the norm indicated in many medical sources is in the range from 3 to 70 pg/ml. But, as already mentioned, estradiol is a derivative of testosterone, therefore the value of the female hormone will be higher than normal if AAS, that is, testosterone, is used. And does this mean that in this case estradiol will be harmful and it’s time to frantically look for a way to lower it? No. Why?

The point is not in the amount of estradiol, but in its ratio to testosterone. Different sources describe it differently, however, the most common numbers are 1:3–4, where 1 is testosterone, 3–4 is estradiol.

Here, based on personal experience, the experience of others, I want to say that there is not always a clear need to reduce estradiol levels. Many also believe that the appearance of gynecomastia is impossible from an increased background of estradiol. Unfortunately, it is impossible to accurately calculate the value and ratio for a specific person, especially for the average man.

I also want to say that, especially at first, the body may react to the introduction of exogenous testosterone with too much aromatization, this must be taken into account. Alas, what
I can’t give you an exact formula, and perhaps many will disagree with me. Nevertheless, I believe that you should experiment with the dosages of aromatase inhibitors or with other antiestrogenic drugs, thereby finding a middle ground for yourself, focusing on your well-being and tests. Remember, what works for others will not necessarily work for you, and vice versa.

Ways to suppress aromatization

We will not pay much attention to this section, but we will briefly go through the most popular drugs and methods.

Clomid acts on estrogen receptors in the pituitary gland and ovaries. Binds estrogen receptors in the pituitary gland. Clomid breaks the negative feedback mechanism, that is, if usually estrogens, acting on the pituitary gland, reduce the production of FSH and LH by the latter, then this does not happen when taking Clomid. Clomid does not affect the level of estrogen in the blood itself, and in the same way it does not affect the level of estrogen in the blood, since its mechanism of action is reduced to a blockade different types estrogen receptors, including those in the pituitary gland. Quite a toxic drug. Tamoxifen also increases the number of progesterone receptors.

(letrozole, anastrozole, exemestane) – this is a class medicines, intended primarily to reduce the concentration of estrogen in the blood. Unlike tamoxifen and Clomid, it does not block estrogen receptors and acts directly on aromatization, suppressing it. It is also used to increase the level of your own testosterone and gonadotropic hormones.

Reducing the amount of adipose tissue. Do not neglect the condition of having a large or moderate large quantity subcutaneous fat. After all
The more obese the person, the stronger the aromatization. Reducing the percentage of subcutaneous fat will significantly reduce aromatization. Also, as a rule, on low-carbohydrate/no-carbohydrate diets, there is a decrease in the conversion of testosterone to estradiol.

Prolactin and progesterone

Progesterone– female sex hormone, progestin. Otherwise known as the “pregnancy hormone” because female body, mainly, it is he who is responsible for maintaining pregnancy and regulating menstrual cycle. Men also need progesterone; it performs a number of important functions. Progesterone is a precursor to testosterone and cortisol and regulates the functioning of the central nervous system. Progesterone also acts as a counterweight to dihydrotestosterone, reducing the latter’s excessive activity.

Norm of progesterone in men Progesterone 0.5–6.0 nmol/l

Fluctuations in progesterone are acceptable, which can exceed up to 100% of reference values.
With an elevated level of progesterone, testicular atrophy, infertility, and suppressed libido are at great risk.

Interestingly, there was previously a practice of using drugs based on this hormone to suppress male sexual desire. They were administered to male criminals in order to reduce the activity of their sexual instincts.

Here, as in other cases, a rational approach to progesterone control is required. In general, when using testosterone, progesterone should not rise due to the lack of progestogenic activity of testosterone.

There is an opinion that progesterone occupies the No. 1 place for the development of gynecomastia. Why? If progesterone is elevated, then, firstly, the number of estradiol receptors in the gland tissues increases, and secondly, progesterone itself increases prolactin. Therefore, even with low estradiol, the development of gynecomastia can be observed.

What can cause an increase in progesterone levels?

1. Conversion to dihydrotestosterone;
2. Taking aromatase inhibitors, “building up” estradiol;
3. Low prolactin.

Prolactin

Prolactin is a peptide hormone consisting of 199 amino acids, which in its structure resembles growth hormone, while performing other functions,
although there are some functional similarities.

The functions of prolactin in the male body are reduced to the regulation of secretion
sex hormones and sperm, also regulation of sexual function, immunostimulation and control of sperm motility.

Prolactin is also responsible for lactation. That is, it is responsible for the development of gland lobules in the breast and the milk duct from the gland to the nipple. If prolactin is high, then the nipple begins to grow in size.

Men also need progesterone; it performs a number of important functions. Progesterone is a precursor to testosterone and cortisol and regulates the functioning of the central nervous system.

Prolactin itself does not cause gynecomastia in men, but sometimes it can contribute to its development, as it enhances the effect of estrogens, which are always present in the blood of the male body.

Only elevated prolactin is harmful. Many people like to eat half a tablet of Dostinex or Bergolac (the active ingredient is cabergoline) weekly without being tested, which I think is wrong. As a result, prolactin drops to zero, and progesterone rises.

Norm prolactin Prolactin 53–360 mU\l

Conclusion

The logic of the reasoning comes down to only one thing: there is no need to blindly try to fix something, without even knowing what. The elements of the body system are interconnected. Especially the hormonal system: if you lower something, it does not remain without a trace. Therefore, before you “knock down” the level of any of the hormones, look at your tests. Always remember that each organism and case is individual.

What may not have consequences for some may have consequences for others. In my opinion, the path of a person who engages in bodybuilding is always the path of an experimenter, from the choice of products to the choice of pharmacology. No one can give you better advice than your body, so listen to it.

Aromatization is the process of transforming testosterone into estradiol. In the male body, estrogens are synthesized only in this way, and in the female body they are synthesized in the ovaries.

Testosterone aromatization occurs in target cells, or estrogen receptors. Testosterone, binding to them, becomes estradiol.

It is noteworthy that the more testosterone in a man’s body, the stronger it aromatizes and the more estradiol there will be, unless, of course, you use aromatase inhibitors or antiestrogens (more on them below), however, the level of aromatization is different for all men.

Aromatization in the required quantities is vitally important, because estradiol in a man’s body is responsible for water balance, restoration of the nervous system, water-salt balance and much more, but excessive aromatization of testosterone will give us the following negative side effects:

In fairness, it is worth noting that not critically increased estradiol greatly helps in gaining mass, due to the fact that joints and ligaments become stronger, which allows you to work with heavy working weights. Also, due to the same fluid retention, according to some theories, more water enters the cells nutrients, which accelerates muscle growth. By the way, a slightly increased estradiol (by 10-15%) in some cases can lead to an increase in libido and time of sexual intercourse.

To summarize the above: Testosterone aromatization is needed, but in the required quantities. You should not allow estradiol levels to exceed the upper reference test values; in this case, you will get all the advantages of estradiol and avoid the disadvantages.

How to suppress testosterone aromatization

First of all, it is worth understanding that taking antiestrogens during the cycle is not the best choice. Antiestrogens will greatly limit your body's ability to aromatize, to the point that they can block it altogether if the dosage is incorrectly selected. Taking antiestrogens on a course is justified only if you have gynecomastia, and aromatase inhibitors cannot cope with it; in all other cases, taking antiestrogens is strictly not recommended.

So what should you take in this case? Aromatase inhibitors. They do not suppress the aromatization of testosterone in estrogen receptors, they directly bind existing estradiol in the blood, therefore, even if you reduce it to critical values, then after a few days new estradiol will begin to be synthesized in the required amount, but in the case of aromatase inhibitors, the process restoration of testosterone aromatization may take much longer.

How to determine a critically low level of estradiol in the blood?

As already mentioned, critically low estradiol is just as bad as critically high one, and it is not difficult to determine both cases. If estradiol is critically low, you will experience a condition similar to the flu: your joints will ache, your temperature will rise, you may feel feverish, you will be very extreme thirst. In this case, you must immediately stop taking any aromatization blockers and, if possible, take 100-200 mg of testosterone propionate in addition to your main course. It is best to use testosterone phenylpropionate, but it is difficult to find; the dosage will be 200-300 mg.