Aromatase inhibitor drugs. Products to increase the male hormone testosterone. Aromatase inhibitors and estradiol

Aromatase inhibitors are a variant of a hormonal therapeutic regimen that is used to stop the development of an oncological process in a woman’s mammary glands. This pathology, even at the initial stage of its development, as well as for preventive purposes in case of a history of predisposition to cancer, requires a specific approach in terms of the choice of therapeutic measures. Hormone therapy, which is based on the use of aromatase inhibitor drugs, is considered successful and is effectively used in medical practice.

Aromatase - description and properties

We are talking about a special enzyme that is found in the liver, ovaries, adipose tissue, mammary glands and skeletal muscles. This enzyme causes the transformation of androgens into the hormone estrogen. During menopause, estrogen is actively produced by the body through an enzyme called aromatase. Preparations based on this enzyme help reduce the level of estrogen in the blood, which helps prevent the active reproduction of cancer cells and tumor growth. Aromatase inhibitors are also called antiestrogens. Antitumor drugs have been used in medical practice for more than 30 years.

To completely eliminate a malignant tumor, various therapeutic methods are used. Sometimes surgery and chemotherapy do not fully guarantee recovery. In most cases, an integrated approach is used, including hormonal therapy. This is a kind of guarantee of cancer recurrence. Why are aromatase inhibitors so effective?

Hormonal drugs help block receptors or completely eliminate female steroids.

Directions for therapy with these drugs

There are several areas of treatment for breast cancer pathology. The choice of treatment method and regimen is made taking into account a combination of various factors, including the stage of the pathology, complications, medical history, etc. In order for hormonal therapy to give an effective result, one of the following regimens is most often used:


  1. Preoperative. It is prescribed in cases where the size of the tumor is more than two centimeters and the lymph nodes are involved in the process of its development.
  2. Therapeutic. It is used to reduce tumor foci, as well as in the case of an inoperable type of tumor.
  3. Preventive. Prescribed when other therapeutic regimens have been used. The goal of prevention is to eliminate the likelihood of relapse.

Use of these products during premenopause

During premenopause, doctors prefer to use a different treatment regimen. An integrated approach involves surgical intervention, which may involve resection of the ovaries, which actively produce estrogens. During the transition period between chemotherapy and rehabilitation, specialists prescribe hormonal drugs such as Nolvadex and Zoladex.

How are they useful for women?

Aromatase inhibitors are considered the most effective non-invasive treatment for breast cancer. Drugs that inhibit the enzyme affect estrogens, which are able to circulate throughout the body. Estrogen interacts with cellular receptors, provoking the activation of various processes. In the case when the cells are healthy, such a process is not dangerous for the woman. If pathogenic cells come into action, estrogen can provoke the development of cancer pathology.


There are a number of aromatase inhibitor drugs that are used to block estrogen production. They all have different mechanisms of action on the body. For preventive purposes, Letrozole, Anastrozole and Exemestane are prescribed to inhibit estrogen during menopause. Tamoxifen is used to block estrogen receptors, and Faslodex is used to completely eliminate it.

A synonym for aromatase inhibitor is “Aromasin”. The drug is prescribed at the stage of diagnosing cancer. It is especially effective in the early stages of breast cancer, but side effects from taking it are numerous and unpleasant. Taking the drug is accompanied by asthenia, nausea, dry mouth, rash and swelling.

"Anastrozole Kabi"

Anastrozole Kabi is produced in the form of tablets for oral administration. The drug is produced in Germany. Its synonyms are “Selana”, “Anastera”, “Arimidex” and “Egistrazol”. Unlike other drugs, Anastrozole Kabi has a relatively small list of side effects, and its half-life from the body is quite long. In addition, the drug has good results from various studies on its effectiveness as a preventive agent that helps prevent cancer recurrence.

Long-term use of drugs that are part of the group of natural aromatase inhibitors can lead to the development of osteoporosis. To prevent thinning of bone tissue, patients are recommended to take regular observation by a specialist while taking Anastrozole, as well as supplementing their diet with foods containing calcium and vitamin D.

The main adverse reactions to the drug are periodontitis, increased fatigue and muscle weakness.


"Letrozole"

Letrozole is considered a highly selective drug, synonymous with Femara. This anti-estrogen is a non-steroidal agent and is applicable for all types of hormonal treatment. An aromatase inhibitor demonstrates a high degree of effectiveness in breast cancer, especially when prescribed in the early stages of cancer development, and also as a prophylactic agent to prevent relapse. The duration of taking the drug can be up to five years. Adverse reactions are mild and are not a reason to stop taking Letrozole.

Cost and features of taking this medication

Aromatase inhibitors for breast cancer are prescribed to women to reduce or completely suppress estrogen production. Especially often, such an appointment is made during menopause. The effectiveness of drugs in the treatment of breast cancer is due to their administration during the premenopausal period. Adverse reactions do not occur in every patient and, as a rule, disappear after a few weeks of use.

Treatment for breast cancer does not always involve surgery. Sometimes passive observation is used, accompanied by the use of drugs that inhibit the production of sex hormones. The cost of pharmaceutical aromatase inhibitors is quite high. Considering the need to take them regularly over a long period of time, such therapy costs quite a lot of money. Pharmacies offer the following prices for antiestrogens:

  1. “Aromasin” will cost an average of 1,600 rubles for 30 tablets.
  2. Anastrozole Kabi costs approximately 1,200 rubles for 28 pieces.
  3. "Selana" is available in pharmacies at a price of approximately 700 rubles for 28 tablets.
  4. Letrozole costs about 2,000 rubles.
  5. Arimidex costs about 6,000 rubles per package.

Any of the listed drugs should be taken only as prescribed by a doctor. The dosage regimen is selected depending on the severity of the disease and the patient’s condition. The standard dosage option is 1 tablet per day. All drugs require long-term use of at least two years.


Aromatase inhibitors for men

In bodybuilding, antiestrogens are often used during a cycle of anabolic steroids. The goals of such therapy are:

  1. Increased levels of anabolic steroids in the blood.
  2. Preventing the development of gynecomastia.
  3. Prevention of hypertension.
  4. Increased body contours achieved by suppressing estrogen.
  5. Reducing the influence of estrogen on the pituitary-hypothalamic axis.

Not all anabolic steroids require the use of antiestrogens. Their use is considered justified in combination with substances such as testosterone, methyltestosterone and methandrostenolone.

In most cases, athletes resort to the help of aromatase inhibitors when symptoms of gynecomastia occur while taking anabolic steroids, for example, redness and itching in the nipple area, swelling. This approach on the part of bodybuilders cannot be called optimal. Experts propose a treatment regimen that involves starting to take antiestrogens 10 days after anabolics such as Testosterone Propionate and Methandrostenolone, which are characterized by a short half-life. If we are talking about oblong esters, then taking antiestrogens should start after 3-4 weeks.

The use of drugs in bodybuilding

Anastrozole is taken 0.5 mg every other day. After 10 days, a control check of the level of estradiol in the blood is done and the dosage is adjusted. Adverse reactions to antiestrogens can include depression, decreased libido, and impaired erectile function. The appearance of these symptoms indicates the need to reduce the dosage taken.


Letrozole was the first aromatase inhibitor to become publicly available. The drug effectively increases the hormone gonadotropin in men, thereby displacing estrogens. When taking this drug, estrogen concentrations may drop by half. The components of the drug are eliminated over the course of 2-4 days, so you can take it every other day.

Anastrozole is no less popular among bodybuilders. It has been shown to effectively reduce estradiol levels in men. The aromatase inhibitor Anastrazole Kabi is also common and attractively priced in pharmacies.

Side effects of these medications

Side effects may occur when taking these medications. The greatest danger is a drop in estrogen in a man’s body to critically low levels. In this case, bodybuilders experience the following undesirable reactions:

  1. Stopping muscle growth.
  2. Joint pain or arthralgia.
  3. Decrease in libido and deterioration in general well-being.
  4. State of depression.
  5. Increased blood cholesterol levels.
  6. Reduced strength of bone tissue.

conclusions

Thus, although the use of aromatase inhibitors is quite common among bodybuilders, it is not worth abusing such drugs. In fact, experts do not recommend starting treatment without consulting a specialist, since the dosage for men is minimal and can be easily exceeded.

As for the use of antiestrogens in the treatment and prevention of breast cancer, in this case the use of such drugs is justified even despite the side effects that arise. However, here too it is necessary to strictly observe the prescribed dosages and follow the instructions for use.

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, which are 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 in its biological activity is 5 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 the aromatization of steroids under the influence of aromatase can potentially lead to the growth of mammary glands in an athlete according to the female type, 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, 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 binding of the drug to aromatase (at 2.5 mg per day) is 95%, which shows that the drug works quite effectively. 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 of 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 taking Omega3 or synthetic HMG-CoA reductase inhibitors (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.

Aromatase inhibitors (blockers) (AI)– drugs that are used to reduce the amount estrogen in the blood, and also help to increase the concentration of its own testosterone. In sports, aromatase blockers are mainly used during the course AC, performing the following tasks:

  • promote accelerated restoration of the hormonal system when using AS;
  • prevention gynecomastia;
  • increase in quantity gonadotropin.

Aromatase blockers

Do not forget that estradiol is necessary for the normal functioning of the body, so athletes need to monitor its concentration in the blood, especially during AC courses. It is worth noting that a moderate amount of estrogen is useful for muscle growth; aromatase inhibitors help keep their level normal and balance the hormonal system.

Please note that while taking AI, it is necessary to systematically monitor the concentration of estrogen in the blood, because if the level of this hormone drops excessively, muscle and bone tissue can be destroyed, and the nervous and cardiovascular systems suffer. These processes can be accompanied by mood swings, insomnia, memory loss, depression, decreased libido, joint pain and other unpleasant side effects.

Attention! Aromatase inhibitors are not used on PCT, it is advisable to use them only during the course and immediately after the end of the AS course (before PCT). During post-cycle therapy, estrogen receptor blockers are used ( Tamoxifen, Clomid).

Aromatase inhibitor drugs

Some of the most popular IAs are Anastrozole, Letrozole And Exemestane,
they can be purchased at the pharmacy. Of particular note is Proviron, which is a weak aromatase blocker.

Anastrozole is the leader among the above drugs. It works effectively by lowering the level of estrogen in the blood, while being well tolerated by the body. It is worth noting that Anastrozole is available in tablet form with a dosage of 1 mg. In sports, for preventive purposes, athletes use this drug at a dosage of 0.5 mg every other day, and if symptoms of gynecomastia occur, 1 mg per day until they disappear, after which it is necessary to reduce the dosage to 0.5 mg every other day. It is advisable to take Anastrozole after meals with plenty of water.

Letrozole and Exemestane are also highly effective drugs, and their cost is an order of magnitude lower than Anastrozole. Their disadvantages are that they suppress estrogen levels quite strongly (as you remember, an excessive drop in estrogen levels is fraught with unpleasant consequences), so the effect of these drugs is difficult to control. In addition, it is necessary to take into account that letrozole is available in tablets with a dosage of 2.5 mg, its prophylactic dose is 0.5 mg. For prevention, it is necessary to divide the tablet into 5 equal parts, which is extremely inconvenient.

Taking aromatase inhibitors

As you already know, aromatase blockers are not used during PCT; they are used during a cycle of anabolic steroids. However, when exactly should you start taking aromatase inhibitors? In the world of sports, there are many tactics for using them, the most popular of which are:

  1. start taking it 2 weeks after the start of the course;
  2. start taking it from the moment the first signs of gynecomastia appear;
  3. after 2-4 weeks (2 for drugs with a short half-life, 4 for long ones), conduct tests to determine the amount of estrogen in the blood. If their level is unsatisfactory, start taking AIs in a prophylactic dosage. 2 weeks after starting to use AI, conduct a control test for the amount of estrogen, and based on their results, further dosage is adjusted.

The last (3rd) option is considered the most optimal. However, due to the fact that it is the most costly, both in terms of time and finances, many athletes neglect taking tests, which is the wrong approach and can ultimately negatively affect the athlete’s health.

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Aromatase in men is an enzyme that converts testosterone into. Research shows that aging and the accompanying weight gain lead to a greater conversion of men into estradiol, the “bad estrogen” that is responsible for such well-known problems in men as prostatitis, decreased libido, and hormonal problems. Aromatase is found in fat cells, the number of which increases due to overeating and a sedentary lifestyle.

It is also involved in the creation of estrone (another female hormone) by converting it from (androgen, a male hormone).

AROMATASE INHIBITORS FOR MEN

Aromatase is one of the most harmful enzymes in the male body, as its main job is to convert testosterone and other androgens into estrogens (female hormones). To avoid the unpleasant consequences of aromatase, many men begin to take blockers of this enzyme that suppress its production, for example, Arimidex (anastrozole) or Letrozole (Femara). Inhibition (suppression, reduction) of aromatase in the male body.

However, such serious medications have many side effects; they should only be prescribed by a doctor if serious symptoms are present. If testosterone in the body is slightly reduced, natural aromatase blockers for men can be used instead of heavy drugs. The 7 foods listed below will help prevent conversion to female hormones by inhibiting the aromatase enzyme.

AROMATASE INHIBITORS TO INCREASE TESTOSTERONE IN MEN

  • Cruciferous

Cruciferous vegetables block aromatase in men thanks to nutrients that detoxify bad estrogen molecules. The main reason for this effect is the compound 3,3′-Diindolylmethane (DIM), which blocks estrogen and is rich in cabbage. DIM effectively “cleanses” the liver of excess estrogen, blocks the aromatase enzyme and enhances liver cleansing, disrupting the process of cancer cell formation.

Overall, this means that cruciferous vegetables lower aromatase in two ways: by inhibiting the enzyme and by improving estrogen metabolism. DIM is also sold in standardized supplements, but you can get it by simply eating various types of cabbage, radishes, turnips, and horseradish.

  • Celery stalk

Celery is an example of an aromatase-inhibiting food and an effective way to boost testosterone. It has been proven that its specific aroma can activate the process of testosterone production in men. The celery stalk contains androgens, including androsterone, a powerful pheromone that promotes the production of testosterone in men.

Celery also has a small effect on inhibiting the aromatase enzyme. It will not work as well as the medication, but it may lower aromatase to some extent. For the most part it is used as a vegetable.

Celery stalk is indeed a good natural test booster, but it is important to consume an organic plant grown without the use of pesticides, which have a disruptive effect on the male endocrine system. The best option would be celery grown in your own garden.

  • Oysters

Another natural aromatase inhibitor. They contain a lot of bioactive substances. This mineral is extremely important for a man's health, as it is closely related to the production of sperm and testosterone. Zinc is considered one of the most powerful and most natural aromatase inhibitors.

Instead of oysters, you can eat other foods rich in natural zinc (meat, fish, vegetables, nuts), or take the mineral in tablet form, although the synthetic form will not be as bioavailable to the body as naturally occurring zinc.

Red wine is also an aromatase enzyme inhibitor for men. 1-2 glasses of this drink help increase the main male hormone. However, its excess will have the exact opposite effect.

Red wine works as a natural aromatase blocker, which has been proven in numerous tests. In one of the experiments to study cancer, they say. glands, scientists have found that grape seeds and red wine work as aromatase inhibitors and are able to reduce serum levels of elevated estrogen.

Other scientists have found that phytochemicals in red wine block the aromatase enzyme, and the more of these compounds, the less aromatase enzyme. However, it is not recommended to greatly increase the dose, since the alcohol in red wine will reduce testosterone and lead to the opposite effect.

The third experiment showed that the most effective and best inhibitor of the aromatase enzyme in men is the Pinot Noir variety. Apparently, this effect is due to the polyphenol resveratrol, which lowers estrogen while raising testosterone. The polyphenol resveratrol is also available in the form of dietary supplements.

  • Olive oil

Olive oil is one of the best natural aromatase inhibitors for men. It contains a compound called oleuropein, which gives the oil its characteristic aroma. One experiment showed that oleuropein has strong aromatase-inhibiting properties.

Olive oil also helps convert cholesterol into testosterone and is beneficial for preventing cardiovascular disease.

It is better to choose organic cold-pressed oil, in which the oleuropein remains intact.

  • Mushrooms

Champignons are also able to block the aromatase enzyme. Experiments on women confirmed the effectiveness of reducing aromatase in the treatment of pierced cancer. glands. In men, this effect is likely to be similar.

In another experiment, scientists also discovered that mushrooms reduce the aromatase enzyme (the higher the dosage, the less of it in the body). The observation of Chinese doctors also showed that champignons in combination with inhibit aromatase.

In another study, researchers tried to reduce estrogen levels by half using champignon mushrooms. They failed to achieve the planned reduction, but they noted a noticeable suppression of the enzyme.

Adding regular parsley to a man's diet also helps suppress aromatase. The main reason for this effect is that the plant is rich in the flavonoid apigenin. According to research, apigenin can qualitatively inhibit the aromatase enzyme and also promotes the production of testosterone in the testicles. Parsley also contains natural nitrates, which increase nitric oxide and erection quality.

These seven foods on the list help inhibit the aromatase enzyme in men, and block its conversion to the female hormone estradiol. Nothing induces the aromatase enzyme in the male body more than excess weight. If a man really wants to block this enzyme, it is important to exercise more and burn excess fat.

In the life of most serious athletes, sooner or later there comes a time when taking exogenous hormones becomes a necessity. The body’s own resources are no longer enough, so we have to resort to external support.

This question is very serious, requiring maximum competence of the athlete or his coach. Unfortunately, many people approach taking AAS irresponsibly, so in the end they end up with nothing but problems. Among them: problems with libido, potency, female-type fat accumulation and much more.

Of course, the most common cause of these failures is hormonal imbalance. In particular, a violation of the proportions of female sex hormones to male ones. Such as: , progesterone, . Of course, estradiol, the main female sex hormone, occupies a special place here. It is to combat elevated estradiol levels that aromatase inhibitors are used.

The mechanism of increasing estradiol levels

At school we all studied such a phenomenon as homeostasis - a state of balance. This is what everything in nature strives for. Our body comes first. He strives to return all our functions to a state of balance as soon as possible.

In the male body, a certain proportion of female hormones to male hormones is established. For women, of course, this proportion is the opposite.

When a man has too much of the male sex hormone testosterone in his body, he tries to increase the level of estradiol in order to return the previous proportion. It does this by aromatizing testosterone into estradiol.

As you already understand, aromatization is the conversion of excess testosterone into estradiol. Excess testosterone appears from taking steroids - synthetic analogues of testosterone. True, there are steroids that do not undergo aromatization, but this is a topic for a completely different conversation.

Of course, an increase in estradiol levels is not good. Its low level, by the way, is even worse (we are talking about the level of estradiol, which is below the reference values). An increase in estradiol leads to the above-mentioned side effects: gynecomastia, female-type fat accumulation, decreased libido, etc.). This will also certainly reflect negatively on the results of the course.

How much aromatization will occur depends on several factors. The two most important of them are the activity of the aromatase enzyme and the amount of subcutaneous fat.

There’s nothing to even say about the second one - if you have excess fat reserves “for a rainy day,” don’t even think about starting a course of AAS without getting rid of them. You can talk for a long time about why, just know that there is no need.

But the first factor in this case is more important. Aromatase is an enzyme responsible specifically for aromatization; in some it is more active, in others it is less active. How to reduce its activity? It’s very simple – taking aromatase inhibitors.

Aromatase inhibitors and estradiol

Aromatase inhibitors are drugs that reduce the activity of the aromatase enzyme. There are many such drugs today. These are: Arimidex, Aromasin. The active ingredient is usually the same.

Anastrozole Today it is the most popular aromatase inhibitor due to its availability. This is both an “underground” anastrozole from sports pharmacology manufacturers and a pharmacy one, which is of much higher quality, but also somewhat more expensive. The cheapest of them is Selana. There is also Anastrozole-kabi, but it is now extremely difficult to get it.

Here it should be said right away - don’t skimp on your health and buy quality.

Anastrozole should be taken based on your own estradiol level. Therefore, you first need to get tested for estradiol levels in order to adjust the dosage based on this. The average universal dosage is 0.5 mg every other day. After 10 days, get tested again. If estradiol levels return to normal, reduce the dosage completely to 0.5 mg 2 times a week. If it is still high, continue taking it. Continue this way until estradiol returns to normal.