Antiestrogenic drugs: description, application

Estrogen-blockers are chemical compounds that block the action of estrogen. Antiestrogenic drugs are used in the treatment of various diseases. They are widely used for the therapy of breast cancer processes in order to slow down tumor growth or prevent relapses. As with other drugs that interact with hormones in the body, these drugs should be used under the supervision of a doctor.

The use and harm of estrogen

Estrogen, or steroid hormone, is synthesized mainly by the ovaries. It affects a number of body processes. Women of childbearing age have the highest level of this natural hormone. Excessive volume, however, can cause a syndrome known as hyperestrogenism. This disease can lead to oncological processes in the breast and endometrial cancer. Antiestrogenic drugs and estrogen blockers or aromatase inhibitors can fix this all. Such drugs, however, have a positive and negative impact on women and men. antiestrogenic drugs

Types of estrogen-blockers, their use

There are a number of different types of estrogen-blockers. Aromatase inhibitors actually block the production of estrogen. Selective estrogen receptor modulators, such as "Tamoxifen", "Clomifene," are designed to block estrogen receptors, and behave differently for different types of tissue. Antiestrogens also block estrogen receptors.

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Antiestrogens prevent the conversion of testosterone to estradiol, and estrogen hormones cease to function or are blocked.

In the treatment of cancer, these drugs are used to slow the development of the tumor. In this case, selective estrogen receptor modulators can be targeted to specific estrogen receptors. Blockers, including Clomiphene, are also sometimes used in the treatment of infertility, they can help some women who are difficult to get pregnant. These drugs are also used by some clinicians to treat children who are slowed by puberty until they become old enough.

Among bodybuilders, it is customary to use estrogen-blockers because of the estrogenic effect of high levels of testosterone in the body. Testosterone is a precursor of estrogens, aromatase inhibitors can be used to stop the formation of muscle mass with an excess of estrogen while maintaining a low level in the body. This practice has attracted many, especially when anti-estrogen preparations are used mainly for cosmetic purposes. In this case, people use tablets and food supplements without medical supervision.

antiestrogenic drugs in the pharmacy

Side effects of

There are side effects of antiestrogenic drugs. They can cause dizziness, headaches, sweating, hot flashes and confusion. Only an endocrinologist can determine the appropriate dosage for the patient, depending on the situation, and an acceptable threshold of side effects. An endocrinologist can also assign regular blood samples to the hormone content when assessing the patient's overall health to confirm that the use of antiestrogens is safe and functional for the patient.

Treatment of men

With age, the male testosterone level falls. However, if testosterone decreases rapidly or significantly, it can lead to the development of hypogonadism. This condition, characterized by the inability of the body to produce this important hormone, can cause a variety of symptoms, including:

  • loss of libido;
  • decreased production and quality of sperm;
  • erectile dysfunction;
  • fatigue.

If we talk about estrogen, we first think that it is a female hormone, but its presence ensures that the male body functions properly. There are three types of estrogens: estriol, estrone and estradiol. Estradiol is the main type of active estrogens in men. It plays a vital role in maintaining the function of male joints and brain tissue. Antiestrogenic preparations also allow the sperm to develop correctly. antiestrogenic drugs and estrogen blockers

Hormonal imbalance - increased estrogen levels and decreased testosterone - creates problems. Too much estrogen in the male body can lead to:

  • gynecomastia( excessive development of breast tissue);
  • cardiovascular problems;
  • increased risk of stroke;
  • weight gain;
  • problems with the prostate.

You can take a number of steps to restore balance in the level of estrogen. For example, if your estrogen excess is associated with a low testosterone level, testosterone replacement therapy as an estrogen blocker may be useful.

Pharmaceutical estrogen-blockers

Some pharmaceutical products can produce an estrogen-blocking effect in men. Typically, most often they are intended for use by women, but are gaining popularity among men, especially those who want to have children. Supplements with testosterone can lead to infertility. But estrogen-blockers, such as Clomid, can restore the hormonal balance without compromising fertility.

Some drugs known as selective estrogen receptor modulators are usually marketed as drugs for the therapy of breast cancer. But they can also be used to block estrogen in men. These drugs are used for various conditions associated with low levels of testosterone, including:

  • infertility;
  • low number of spermatozoa;
  • gynecomastia;
  • Osteoporosis.

These medications should be used selectively, depending on the condition of the patient. Such antiestrogenic drugs are used. In the pharmacy you can buy:

  • "Tamoxifen".
  • "Arimidex".
  • Letrozole.
  • "Raloxifene".

Effect on bone tissue

According to clinicians, prolonged exposure to estrogen preparations can cause endometrial cancer in women."Raloxifene" - a selective modulator of estrogen receptors - can prevent the development of cancer, selectively blocks the absorption of estrogen. This preparation, however, is also able to inhibit the positive effects of estrogens on bone density. A new drug - "Lazofoksifen" - can fix this problem. It prevents the loss of bone density in postmenopausal women and reduces the fragility of bone tissue. The use of this drug is generally safe, but can increase blood thickening. side effects of antiestrogenic drugs

Drug Interaction

Estrogen-blocker "Tamoxifen" can help prevent cancer. Oncological patients often experience depression, and drugs of this group may interact negatively with antidepressant medications. Paroxetine should be used because women taking Tamoxifen and Paroxetine are less likely to die than women taking Tamoxifen and any other antidepressant. This is because "Paroxetine" acts selectively.

Antiestrogenic drugs and preparations

The descriptions of all these drugs indicate that each drug is used individually in a particular case.

"Clomid", or "Clomiphene citrate" was one of the original drugs used in the therapy of gynecomastia, as it raises the body's level of producing its own testosterone. There are some side effects from prolonged use, such as vision problems. There are also more effective substances on the market that work the same way, but "Clomid" is still an effective and inexpensive mixture for any athlete.

This is not an anabolic steroid, the drug is usually prescribed to women as an aid in infertility, since it has a pronounced ability to stimulate ovulation, which is achieved by blocking / minimizing the effect of estrogen in the body. To be more specific, "Clomid" is a chemical synthetic estrogen with the properties of an agonist / antagonist. In some target tissues, it can block the ability of estrogen to bind to the corresponding receptor. Its clinical benefit is to withstand the negative feedback of estrogens in the hypothalamic-pituitary-ovarian system, which increase the release of LH and FSH.All this leads to ovulation.

mechanism of action of antiestrogenic drugs

For sports purposes, "Clomiphene citrate" in women does not give an effect. In men, however, there is an increase in the production of follicle-stimulating and( primarily) luteinizing hormone, which stimulates the natural production of testosterone. This effect is particularly useful for the athlete at the end of the steroid cycle, when the level of endogenous testosterone is in depression. Without testosterone( or other androgens), "Cortisol" predominates and affects the synthesis of protein in the muscles. But he quickly "eats" most of the newly acquired muscles after cancellation. Clomid can play a significant role in preventing this accident in order to achieve athletic performance. For women, the benefit of clomid action is the possible management of the endogenous level of estrogen. This will increase fat and muscle loss, especially in areas such as thighs and buttocks."Clomiphene citrate", however, often produces side effects in women, but, nevertheless, is in demand among this group of athletes.

"Tamoxifen" blocks estrogen receptors in breast cancer cells. This stops estrogen from interacting with them and hinders the growth and division of cells. While Tamoxifen acts as an anti-estrogen in breast cells, it acts as an estrogen in other tissues: the uterus and bones.

Women with invasive invasive breast cancer "Tamoxifen" can be consumed within 5-10 years after surgery to reduce the likelihood of spread of metastases. It also reduces the risk of developing cancer in another breast. For an early stage, this drug is used mainly for patients who have not had menopause. Aromatase inhibitors are the preferred method of treatment for women with menopause.

"Tamoxifen" can also stop growth and even reduce tumors in patients with metastatic cancer. It can also be used to reduce the risk of development of oncologic processes in the mammary gland.

This drug is taken orally, most often in the form of tablets. estrogenic and antiestrogenic drugs

Side effects of anti-estrogen drugs include fatigue, hot flashes, dryness in the vagina or copious discharge and mood swings.

Some women with metastases in bone tissue may have pain and swelling in the muscles and bones. It usually does not last long, but in some rare cases, women can also develop high levels of calcium in the blood that you can not control. If this happens, then the treatment can be suspended for a while.

Rare, but more serious side effects are also possible. These drugs can increase the risk of developing myometrium cancer in women with menopause. Increased coagulation is another possible serious side effect. There is a deep vein thrombosis, but sometimes a piece of blood clot can come off, and eventually block the artery in the lungs( pulmonary embolism).

Rarely, "Tamoxifen" was the cause of strokes and heart attacks in postmenopausal women.

Depending on the menopausal status of a woman, "Tamoxifen" may have a different effect on the bones. In pre-menopause, "Tamoxifen" can cause thinning of the bones, but in post-menopause, the calcium level in women is increased, which is necessary for the strength of bones.

The benefits of this drug outweigh the risks for almost all women with hormone-dependent invasive breast cancer.

A similar drug is "Toremifene", which is approved for the treatment of metastatic breast cancer. But this medicine will not work if "Tamoxifen" was used, but without effect.

Fulvestrant is a drug that first blocks estrogen receptors, and then also removes the ability of receptors to bind. It acts as an anti-estrogen throughout the body.

"Fulvestrant" is used to treat advanced metastatic breast cancer, and is most often used after other hormonal drugs( "Tamoxifen" and aromatase inhibitors) that have stopped working.

Common side effects may include hot flashes, night sweats, mild nausea and fatigue. Theoretically, it can weaken the bones( osteoporosis) if taken for a long time.

This drug has won recognition for use in postmenopausal women who do not respond to "Tamoxifen" or "Toremifene."It is sometimes used for its intended purpose in premenopausal, often in combination with a luteinizing hormone-releasing agonist to turn off the ovaries.

"Raloxifene" is used by women to prevent and treat bone loss or osteoporosis after menopause. It helps to keep the bones strong, reducing the likelihood of fractures.

"Raloxifene" can also prevent the occurrence of invasive breast cancer after menopause. It is not an estrogen hormone, but acts as an estrogen in some parts of the body, such as bones. In other parts of the body( uterus and chest), "Raloxifene" acts as an estrogen blocker. He does not take off various climacteric syndromes. Raloxifene belongs to the class of drugs known as selective estrogen receptor modulators-SERMs( estrogenic and antiestrogenic drugs).

Antiestrogenic drugs and sports

Some drugs are widely used in bodybuilders to build muscle mass.

"Cyclophenyl" is a non-anabolic / androgenic steroid. It works as an anti-estrogen and as a stimulant for producing testosterone."Cyclophenyl" is a very weak and mild estrogen, but it binds estrogen receptors and prevents the binding of natural estrogens by receptors. Strictly speaking, it works so well that some athletes take the drug during steroid treatment in order to maintain a low level of estrogen. The result is a decrease in the amount of fluid in the body that is created by steroids and a decrease in gynecomastia. The athlete has a tougher appearance, using such drugs that can potentially be taken in preparation for the competition. Bodybuilders, however, use it less often, because they prefer the more affordable "Nolvadex" and "Proviron".use of antiestrogens

Like "Clomid", "Cyclophenyl" is ineffective in women, since it has a positive effect only on the production of hormones in men. The increase in testosterone level caused by this drug is not enough to talk about cardinal improvements, however it will provide a gain of strength, even a slight increase in body weight, a noticeable increase in energy and an increase in regeneration are possible. These results are noticeable especially for advanced athletes, who have little or no experience with taking steroids. Results of use become visible only after a week.

In some cases, athletes observe rashes such as acne, increased sexual desire and hot flashes. These symptoms are particularly indicative of the evidence that the compound is actually effective. After stopping the reception, some report a depressed mood and a slight decrease in physical strength. Those who take the drug as an anti-estrogen during a steroid course of treatment can observe the opposite effect when the effect of the drug is discontinued.

Proviron is one of the oldest anabolic androgenic steroids on the market. Officially known as Mesterolon, it remains one of the most unclaimed anabolic steroids among users.

On a functional basis, prociron performs four basic functions, which largely determine its mode of action. First of all, it turns out to be one of the most powerful anabolic steroids, as it increases the volume of circulating free testosterone, which is more important for bodybuilding anabolic processes. A simple way to look at this: if you take anabolic steroids, then muscle mass becomes more and more.

Proviron is also able to interact with the aromatase enzyme, which is responsible for converting testosterone to estrogen. By binding to aromatase, Proviron can indeed inhibit its activity, thereby providing protection against estrogenic side effects.

The "Mestereron" also has a strong affinity for the androgen receptor. This anabolic steroid, which does not inhibit gonadotropins, is similar for other anabolic steroids. This makes it possible to increase sperm production, since androgens are necessary for stimulation of spermatogenesis. This not only increases the amount of sperm, but also increases its quality.

Side effects of "Proviron" do not include gynecomastia or excess fluid. This will also significantly reduce the risk of high blood pressure associated with taking anabolic steroids. In fact, "Proviron" has an antiestrogenic effect by stopping the conversion of testosterone into estrogen or at least slowing down this process.

The above levels of estrogen do not decrease, but affect metabolism in general.

The group of antiestrogenic drugs also includes agonists of releasing factors of gonadotropic hormones( Buserelin and its analogues), megestrol acetate( Megeys), Parlodel and Dostinex are used as drugs that stop the secretion of prolactin. Independently use them in treatment is irrational.

Treatment of oncological diseases

In addition to "Tamoxifen", the following estrogen receptor blockers are used.

Three drugs that stop the production of estrogen in postmenopausal women have been approved for the treatment of both early and advanced breast cancer: letrozole( Femara), Anastrozole( Arimidex) and Exemestane( Aromazine)).

The mechanism of action of this group of anti-estrogen preparations is the blocking of the enzyme( aromatase) in adipose tissue, which is responsible for small amounts of estrogens in postmenopausal women. They do not affect the ovaries, so they are effective only for those women whose ovaries do not work, either because of menopause or because of the influence of the luteinizing hormone analogue. These drugs are taken daily in the form of tablets. They work equally well in the treatment of oncological processes in the mammary gland and prostate.

Sometimes treatment of breast cancer requires medical ovarian outage. This can be done with the help of analogues of luteinizing releasing hormone( LHRH), for example, "Goserelin"( "Zoladex") or "Leiprolide"( "Lupron").These drugs block the signal that the body sends to the ovaries, so that they produce estrogen. They can be used alone or with "Tamoxifen", aromatase inhibitors, "Fulvestrant" for hormone therapy in premenopause.