What determines the activity of the aromatase enzyme? Products to increase the male hormone testosterone

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 antiestrogen. Antitumor drugs have been used in medical practice for more than 30 years.

Various therapeutic methods are used to completely eliminate a malignant tumor. Sometimes surgery and chemotherapy do not give a full guarantee of 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 contribute to the blocking of receptors or the complete elimination of 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:

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.
Therapeutic. It is used to reduce tumor foci, as well as in the case of an inoperable type of tumor.
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, its half-life from the body is quite long. In addition, the drug has good results in various studies of 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:

“Aromasin” will cost an average of 1,600 rubles for 30 tablets.
Anastrozole Kabi costs approximately 1,200 rubles for 28 pieces.
"Selana" is available in pharmacies at a price of approximately 700 rubles for 28 tablets.
Letrozole costs about 2,000 rubles.
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 course of anabolic steroids. The goals of such therapy are:

Increased levels of anabolic steroids in the blood.
Preventing the development of gynecomastia.
Prevention of hypertension.
Increased body contours achieved by suppressing estrogen.
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 at 0.5 mg every other day. After 10 days, a control check of the level of estradiol in the blood is made and the dosage is adjusted. Adverse reactions to antiestrogens can be a state of depression, a drop in libido, and erectile dysfunction. The appearance of these symptoms indicates the need to reduce the dosage taken.

Letrozole was the first aromatase inhibitor to go public. The drug effectively increases the hormone gonadotropin in men, thus 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 drugs. The greatest danger is a drop in estrogen in a man’s body to critically low levels. In this case, bodybuilders have the following undesirable reactions:

Stopping muscle growth.
Joint pain or arthralgia.
Decreased libido and deterioration in general well-being.
State of depression.
Increased blood cholesterol levels.
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.

Breast cancer is a common disease that is primarily caused by hormones. Disruption and improper production contributes to the production of hormones that lead to the formation and development of cancer. The use of aromatase inhibitors should reduce the risk of such development and reduce the size of the cancer tumor.

During the postmenopausal period, the incidence of breast cancer is especially high. The production of estrogen by the ovaries decreases, which is why this hormone begins to be produced in other ways. The adrenal glands secrete the hormone androgen, which is considered a male hormone, and a fat and muscle enzyme (aromatase) converts this hormone into estrogen. Aromatase inhibitors reduce the production and activity of these enzymes.

As a result of all these processes, the development of breast cancer stops if there is less estrogen produced in this way in the woman's blood. Scientists attribute breast cancer to hormone-dependent factors in 40% of cases. Only in other cases are we talking about other causes of the disease. Accordingly, aromatase inhibitors should prevent the development of hormone-based cancers.

Breast Cancer Treatment Options

Doctors have a variety of treatment options for breast cancer. Hormone-dependent cancer can be treated in the following ways:

An operation where the doctor removes the affected tissue.
Radiation therapy or chemotherapy, which stops the growth of cancer cells, as well as secondary lesions.
Additional methods.

Often, three treatment options are used at once to eliminate hormone-dependent breast cancer. Chemotherapy and surgery occur at stages 2-3. The main goal of all treatment is to eliminate excess estrogen, which promotes the growth of cancer cells.

Progestins and antiestrogens are often used. However, if they are ineffective, more toxic drugs are used:

Mamomit.
Orimethen.

Both drugs contain aminoglutethimide, which blocks aromatase and is prescribed in doses of 700-1500 mg. If the cancer cells decrease as treatment progresses, then the dosage is reduced to 500 mg. It all depends on the course of the disease. These drugs cause side effects that readers of the site should be aware of:

Nausea.
Skin rash.
Vomit.
Dizziness.
Cramps.
Swelling.
Apathy.
Sweating.
Drowsiness.
Loss of consciousness.

These side effects may appear after the first dose and last up to 3 months. Medicines based on aminoglutethimide of a less toxic nature are:

Herceptin.
Femara.
Chaga.
Arimidex.
Taxanes.

Aromatase inhibitors are not used alone. They are additional methods of treatment after surgery to remove the ovaries, uterine cancer, breast cancer, etc. Several drugs are used at once, which is considered an additional method in oncology.

Mechanism of action of hormone therapy drugs

What is the mechanism of action of chemotherapy drugs that help fight cancer? Each tablet contains poisons and toxins that enter the woman’s body. The female body has 3 types of progesterone and 5 types of estrogen. The cells of the tablets enter the outer shell of the infected cells of the body, establishing a connection with the receptors. They act on the nucleus, causing it to grow and multiply.

As a result, infected cells quickly increase in size without being able to divide into 2 or more. However, this method of chemotherapy is not yet guaranteed. Therefore, antitumor drugs and other therapies are prescribed together with it.

68% of cancer cells die after exposure to chemotherapy. Aromatase inhibitors act similarly on progesterone and estrogen. This is good in a situation where the cancer cells can be either male or female.

Testing of this drug was carried out, the results of which were:

Erz-positive. 75% of dependent cells are amenable to hormone therapy.
Pr-positive. Progesterone receptors are treatable, but require additional intervention.
Hormonally negative. 25% of negative cells is an indicator that indicates that hormone cells are not susceptible to the effects of hormone-containing drugs.
Hormonal status is unknown. The tissue sample cannot be analyzed. It is possible that it was taken incorrectly.

The effectiveness of hormone therapy

Studies have shown the effectiveness of hormonal therapy:

Treatment rates reach 79% when aromatase inhibitors are used along with medications that target progesterone and estrogen.
The effectiveness of treatment reaches 36% when aromatase inhibitors act on at least one type of receptor.
The effectiveness of treatment is 5-7% when the tumor status is unknown. In this case, hormonal therapy is not performed.

Obviously, all drugs that fight breast cancer are selected by doctors. There are many medications that can be used to treat this disease. Some drugs interfere with cell growth, while others affect cell reproduction and division. Doctors must carefully select medications and monitor the health status of patients.

All hormone therapy drugs affect the tissues of the walls of the ovaries and uterus:

Herceptin is an anticancer drug that reduces the survival of cancer cells by 35%. Dosage: at stage 1 – 8 mg/kg, at stages 2-4 – 4 mg/kg every 3 weeks.
Taxanes are anticancer drugs that block genes. The dosage depends on the content of the drugs: from 100 mg/3 weeks to 1250 mg/day twice a day.
ASD - drugs that increase immunity in cancer. Increase hormone blocking by targeting one type of estrogen. Dosage: from 5 to 45 drops for two months.
Chaga is a birch mushroom. Slows down and prevents the appearance and proliferation of cancer cells. The dosage is indicated in the instructions.

Indications for use

The main indication for use is the absence of a menstrual cycle. Either this occurs during postmenopause or is a consequence of chemotherapy. In any case, aromatase inhibitors are prescribed only when menstruation is absent. This sometimes forces the doctor to wait up to 6 months before prescribing medication.

Much depends on the accompanying procedures that are used in the treatment of breast cancer. Drugs are selected that will enhance the effect. The most effective drug is Herceptin. However, it has two disadvantages: a high price, which not every patient can afford, and outdated properties.

To replace this drug, other analogues are produced that are more suitable for modern treatment. For example, taxanes that affect the development of genes by blocking them become effective. They are the most common in the treatment of cancer tumors.

In parallel with hormones, vitamins are prescribed, which are used strictly with prescriptions. Indications:

To prevent the development of cancerous tumors.
Preventing the development of cancer cells.
Preparation for surgery at stage 1 cancer.
To prevent relapse of cancer cells after surgery.
Preparation for chemical treatment.

If an allergic reaction or individual intolerance to drugs is observed, then a vaccine is made both before and after the operation. It reduces the risk of developing edema. The vaccine is selected depending on the patient's well-being and the degree of the disease. If the vaccine is contraindicated, then preventive treatment is carried out.

Types of hormone therapy

Hormonal therapy is divided into the following types:

Adjuvant. Before surgery, ASD treatment is prescribed.
Non-adjuvant. Prescription of drugs that can cope with tumors larger than 5 cm.
Medical therapy. ASD, ASD2 and ASD3 are used. If the tumor is inoperable, then treatment is ineffective. In this case, vitamin complexes are prescribed.

Depending on the direction of treatment, one or another method is chosen. The following factors are taken into account:

The status of the body's hormonal dependence.
Somatic diseases.
Menopause syndrome.
Drug tolerance.
Stage of development of breast cancer.
Risk of relapse.

In parallel with inhibitors, selective modulators, containing tamoxifen, containing faslodex, etc., can be prescribed. They are prescribed for lesions of the mammary gland after surgery or chemotherapy.

Potent drugs include Chaga, a folk remedy that affects the nuclei of cancer cells, penetrating to them through the blood. It should be prepared strictly according to the recipe. An alcohol base is often used, and soda is often added. We will talk further about the effectiveness of young herbs that have a strong effect.

Folk remedies

One of the folk remedies is soda, which has a pulling effect. It can be taken directly with water. However, with the use of young herbs it becomes more effective.

Celandine is a herb that promotes the production of proper hormones that are not contaminated with chemical poisons. Can be used together with berries and vitamins. Recipes using celandine:

Celandine and saline solution for wiping the chest.
Celandine and soda for oral administration.
Celandine and grass juice.
Celandine and chaga mushrooms.
Celandine and herbs for tincture with alcohol.
Celandine, which is taken in its pure form.

Recipes using baking soda:

Soda and salt.
Pure soda.
soda in solution.
soda and alcohol.

Forecast

When it comes to breast cancer, any remedy is a good remedy. It is not necessary to give an unambiguously positive prognosis, since much depends on the individual characteristics of the organism and the stage of development of the disease.

There are hormonal medications that address hormonal imbalances that often contribute to the development of breast cancer. If the reason is something else, then doctors prescribe other drugs.

Breast cancer affects life expectancy. However, the outcome can be favorable if you use all the treatment methods offered by doctors.

Bodybuilders use drugs mainly during a course of anabolic drugs for the following purposes:

Prevention of gynecomastia;
Increased anabolic background;
Giving muscles relief;
Elimination of hypertension;
Reducing the effects of estrogen on the hypothalamic-pituitary-testicular axis.

When composing a course of steroids, you should remember that not every anabolic steroid has the ability to be converted into estrogens. Aromatase inhibitors must be used when the course includes testosterone esters, methandrostenolone, methyltestosterone.

Use of aromatase inhibitors during the course

Most athletes begin using blockers only after symptoms of gynecomastia appear. But this approach to business is completely ineffective. It is much easier to get tested for the presence of estradiol in the body 10 days after the start of the cycle, when short-term steroids are used, or after 4 weeks, if the cycle includes long-term drugs.

After receiving the results, a dosage of anastrozole should be prescribed, averaging 0.5 grams once every two days. As an alternative, you can take a lower dose of the drug, focusing on your own feelings. In case of decreased libido, erectile dysfunction, or depression, the dosage should be reduced.

Blocker Research

After the Letrozole (Letroza) brand entered the market, it instantly became the leader in popularity among athletes. A large number of studies have been conducted that have proven the high effectiveness of the drug. The effective dose is already about 0.02 milligrams, which is almost 100 times less than therapeutic. After using the drug, the level of gonadotropin content increases significantly, while reducing the content of estrogen by a third.

The effects of anastrozole on the body have now been studied no less well. Due to this, it is very widely used by athletes. During clinical trials, it was found that even with an amount of 0.5 to 1 milligram, the level of female hormones is reduced by half. In online stores, this product can cost several times less than in a pharmacy. Also in large cities you can find a cheaper version of the drug - anastrozole kabi.

Side effects of aromatase inhibitors

It has been established that in small quantities, female hormones are always present in a man’s body and are even beneficial. They are able to increase the sensitivity of androgen receptors and thereby increase the effectiveness of the steroid cycle. All side effects that aromatase inhibitors can cause are associated with their overdose and, as a result, a strong reduction in estradiol in the body. Among the main side effects after an overdose of blockers are:

Slowing the growth of muscle tissue mass;
Pain in the joints;
Decreased bone strength;
Increased cholesterol levels;
Deterioration in general health and loss of libido;
The appearance of a state of depression.

Pharmacological data of blockers

For the first time, aromatase blockers appeared on the drug market in parallel with tamoxifen. In the mid-80s, the completion of clinical trials of a new generation of blockers was announced. It was in the late 80s that almost all modern aromatase inhibitors appeared.

At first, drugs were used in the treatment of malignant tumors of the breast. This was due to the results of studies showing that more than a third of breast cancer is associated with the hormonal system.

When using blockers, the genotoxic effect is reduced, as well as the intensity of cell division, which has a positive effect in the initial stages of the formation of malignant tumors.

Aromatase inhibitors currently available can be divided into two categories: non-steroidal and steroidal. The first non-steroidal drug, aminoglutethimide, was created back in the 70s. However, it was quite toxic to the adrenal glands, and its use in medicine is very limited.

Anastrozole

This is one of the most powerful third-generation non-steroidal inhibitors. When using the drug in an amount of 1 mgc during the day, it leads to a decrease in estrogen levels by 80%. When using anastrozole in a dosage not exceeding 10 milligrams throughout the day, it has a strong progestogenic and androgenic effect on the body. In addition, it does not inhibit the synthesis of cortisol and aldosterone, thus not requiring additional use of corticosteroids. By the strength of its effect, the drug is 250 times or more superior to aminoglutethimide and, due to a longer decay period, is able to prevent symptoms of feminization in small doses.

In bodybuilding, the drug is very widely used to prevent the development of gynecomastia, as well as excess accumulation of fluid in the body. In case of overdose, the same side effects are possible that are characteristic of all drugs in the aromatase blocker group.

Letrozole

The mechanism of operation of this drug is the binding of aromatase to the cytochrome gene. With its help, you can prevent the aromatization effect in adipose tissue, liver, skeletal muscles, without affecting the synthesis of cortisol. Compared to anastrozole, the drug is more effectively able to block aromatase cytochromes, which significantly reduces the level of female hormones.

The permissible dosage of the drug is 1 tablet daily during the day. The drug is well absorbed by the gastrointestinal tract regardless of food intake. The drug should not be taken if there are liver problems. All side effects were recorded only with uncontrolled use of letrozole.

Vorozol

The drug is a representative of the third generation of drugs from the aromatase inhibitor group. Its mechanism of action on the body of the drug is very similar to letrozole. The drug is quite new and research into its safety and effectiveness is currently ongoing. It is used extremely rarely by athletes.

Exemestane

This drug belongs to the third generation steroid blockers. It is quite widely used in the USA by traditional medicine. Just like vorozol, it is used extremely rarely in sports.

Newest aromatase inhibitors

Work on the creation of new, more effective drugs from the aromatase inhibitor group continues to this day. Steroid-type drugs Ergo-pharm 6-OXO and T-Bomb II are currently at the stage of clinical trials. Their effect on the human body has not yet been fully studied and it is too early to talk about their use in sports.

Also, not very long ago, the drug krizin appeared on the sports pharmacology market. Despite the fact that the drug is already on sale, the mechanism of its effect on the body is still being studied. The creators of the drug are silent about the side effects when using chrysin, but so far no information on this matter has been received from athletes. However, chrysin is rarely used by athletes. After all, there are products on the market whose effectiveness and safety have been proven over time.

More information about Anastrozole (aromatase inhibitor) can be found in this video: