Estrogen blockers are chemical compounds that block the effects of estrogen. Antiestrogen drugs are used in the treatment of various diseases. They are widely used to treat breast cancer processes in order to slow tumor growth or prevent relapse. As with other drugs that interact with hormones in the body, these drugs should be used under medical supervision.
The benefits and harms 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 levels of this natural hormone. Excessive volume, however, can cause a syndrome known as hyperestrogenia. This disease can lead to oncological processes in the chest and endometrial cancer. Antiestrogen drugs and estrogen blockers or aromatase inhibitors can all fix this. Such drugs, however, have a positive and negative effect on women and men.
Types of estrogen blockers, their use
There are a number of different types of estrogen blockers. Aromatase inhibitors actually block estrogen production. Selective estrogen receptor modulators, such as Tamoxifen, Clomiphene, are designed to block estrogen receptors, and behave differently for different types of tissue. Antiestrogens also block estrogen receptors.
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 target specific estrogen receptors. Blockers, including Clomiphene, are also sometimes used to treat infertility and can help some women who have difficulty getting pregnant. These medications are also used by some clinicians to treat children who have slowed puberty until they are 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 to estrogens, aromatase inhibitors can be used to stop the formation of muscle mass by excess estrogen, while maintaining a low level in the body. This practice has attracted many, especially when antiestrogen drugs are used mainly for cosmetic purposes. In this case, people use pills and nutritional supplements without medical supervision.
Side effects
There are side effects of antiestrogen drugs. They can cause dizziness, headaches, sweating, flushing and confusion. Only an endocrinologist can determine the appropriate dosage for the patient, depending on the situation, and an acceptable threshold for side effects. An endocrinologist can also prescribe regular blood samples for hormone levels when assessing the patient’s general health status to confirm that the use of antiestrogens is safe and functional for the patient.
Treatment for men
With age, a man 's testosterone level decreases. However, if testosterone is rapidly or significantly reduced, then this can lead to the development of hypogonadism. This condition, characterized by the body’s inability to produce this important hormone, can cause many symptoms, including:
- loss of libido;
- decreased production and sperm quality;
- erectile dysfunction;
- fatigue.
If we are talking about estrogen, then first of all they 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 estrogen in men. It plays a vital role in maintaining the function of male joints and brain tissue. Antiestrogen drugs also allow sperm to develop properly.
Hormonal imbalance - an increase in estrogen levels and a decrease in 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;
- prostate problems.
A number of steps can be taken to restore balance to estrogen levels. For example, if your excess estrogen is associated with low testosterone levels, then testosterone replacement therapy as an estrogen blocker may come in handy.
Pharmaceutical estrogen blockers
Some pharmaceutical products may produce an estrogen-blocking effect in men. As a rule, most often they are intended for use by women, but are gaining popularity among men, especially those who want to have children. Testosterone supplements can lead to infertility. But estrogen-blockers, such as Clomid, can restore hormonal balance without compromising fertility.
Some drugs, known as selective estrogen receptor modulators, are commonly sold as drugs for the treatment of breast cancer. But they can also be used to block estrogen in men. These drugs are used for various conditions associated with low testosterone levels, including:
- infertility;
- low sperm count;
- gynecomastia;
- osteoporosis.
These medicines should be used selectively, depending on the condition of the patient. Such anti-estrogenic drugs are used. In the pharmacy you can purchase:
- Tamoxifen.
- Arimidex.
- "Letrozole".
- "Raloxifene."
Bone action
According to clinicians, prolonged exposure to estrogenic drugs 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 drug, however, is also able to inhibit the positive effects of estrogen on bone density. A new drug, Lazofoxifen, can fix this problem. It inhibits bone loss in postmenopausal women and reduces bone fragility. Using this medication is generally safe, but may increase blood clotting.
Drug interaction
Tamoxifen estrogen blocker can help prevent cancer. Cancer patients often experience depression, and drugs in this group can negatively interact with antidepressant medications. Paroxetine should be used because women taking Tamoxifen and Paroxetine are less at risk of death than women taking Tamoxifen and any other antidepressant. This is because Paroxetine acts selectively.
Antiestrogen drugs and preparations
Descriptions of all these agents indicate that each drug is used individually in a particular case.
Clomid, or Clomiphene Citrate, was one of the original drugs used in the treatment of gynecomastia, because it raises the level of production of testosterone in the body. There are some side effects from prolonged use, such as vision problems. There are 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, a medicine is usually prescribed to women as an aid in infertility, as it has a pronounced ability to stimulate ovulation, which is achieved by blocking / minimizing the effects of estrogen in the body. To be more specific, Clomid is a chemical synthetic estrogen with agonist / antagonist properties. In some target tissues, it may 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 enhance the release of LH and FSH. All this leads to ovulation.
For sports purposes, "Clomiphene Citrate" in women has no 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 especially beneficial for an athlete at the end of the steroid cycle when endogenous testosterone levels are depressed. Without testosterone (or other androgens), Cortisol predominates and affects muscle protein synthesis. But he quickly “eats” most of the newly acquired muscles after cancellation. Clomid can play a significant role in preventing this accident to achieve athletic performance. For women, the benefits of clomid are the possible management of endogenous estrogen levels. This will increase fat and muscle loss, especially in areas such as the hips and buttocks. Clomiphene citrate, however, often produces side effects in women, but is nevertheless in demand among this group of athletes.
Tamoxifen blocks estrogen receptors in breast cancer cells. This stops estrogen from interacting with them and inhibits cell growth and division. While Tamoxifen acts as an antiestrogen in breast cells, it acts as estrogen in other tissues: the uterus and bones.
In women with dependent invasive breast cancer , Tamoxifen can be used for 5–10 years after surgery to reduce the likelihood of metastasis. It also reduces the risk of developing cancer in the other breast. For the early stage, this drug is mainly used for patients who have not had menopause. Aromatase inhibitors are the preferred treatment for menopausal women.
Tamoxifen may also stop growth and even shrink tumors in patients with metastatic cancer. It can also be used to reduce the risk of developing breast cancer.
This drug is taken orally, most often in the form of tablets.
Side effects of antiestrogen drugs include fatigue, hot flashes, vaginal dryness, or heavy discharge and mood swings.
In some women with bone metastases, pain and swelling in the muscles and bones may occur. This usually does not last long, but in some rare cases, women may also develop high levels of calcium in the blood, which you cannot control. If this happens, then treatment may be suspended for a while.
Rare, but more serious side effects are also possible. These drugs can increase the risk of developing myometrial cancer in women with menopause. Increased blood coagulation is another possible serious side effect. Deep vein thrombosis occurs, but sometimes a piece of a blood clot can come off, and eventually block an artery in the lungs (pulmonary embolism).
Rarely, Tamoxifen was the cause of strokes and heart attacks in postmenopausal women.
Depending on the woman’s menopausal status, Tamoxifen may have different effects on the bones. In premenopause, Tamoxifen can cause thinning of bones, but in postmenopausal women, calcium levels increase, which is necessary for bone strength.
The benefits of this medicine outweigh the risks for almost all women with hormone-dependent invasive breast cancer.
A similar drug is Toremifen, 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 eliminates the ability of receptors to bind. It acts as an antiestrogen 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 tiredness. Theoretically, it can weaken bones (osteoporosis) if taken for a long time.
This drug has gained recognition for use in postmenopausal women who are not responsive to Tamoxifen or Toremifen. It is sometimes used for its intended purpose in premenopause, 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 keep bones strong, reducing the chance of fractures.
Raloxifene may also prevent the occurrence of invasive forms of breast cancer after menopause. It is not an estrogen hormone, but acts like 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. It does not relieve various menopausal syndromes. Raloxifene belongs to a class of drugs known as selective estrogen receptor modulators-SERMs (estrogenic and anti-estrogenic drugs).
Antiestrogen drugs and sports
Some drugs are widely used by bodybuilders to build muscle.
Cyclophenyl is a non-anabolic / androgenic steroid. It works as an antiestrogen and as a stimulant for testosterone production. Cyclophenyl is a very weak and mild estrogen, but it binds estrogen receptors and prevents the binding of natural estrogens to receptors. In fact, it works so well that some athletes take the drug during steroid treatment to maintain low estrogen levels. 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 could potentially be taken in preparation for the competition. Bodybuilders, however, use it less often, as they prefer the more affordable Nolvadex and Proviron.
Like Clomid, Cyclofenil is ineffective in women, as it only has a positive effect on hormone production in men. The increase in testosterone caused by this drug is not enough to talk about dramatic improvements, but it will provide an increase in 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. The results of use become noticeable only after a week.
In some cases, athletes observe rashes such as acne, increased sexual desire and hot flashes. These symptoms are especially indicative of evidence that the compound is actually effective. After discontinuation, some report depressed mood and a slight decrease in physical strength. Those who take the drug as an antiestrogen during the steroid course of treatment can observe the opposite effect when the effect of the drug stops.
Proviron is one of the oldest anabolic androgenic steroids on the market. Officially known as Mesterolone, it remains one of the most unclaimed anabolic steroids among users.
On a functional basis, Proviron 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, since it increases the volume of circulating free testosterone, which is more important for anabolic processes in bodybuilders. A simple way to look at this: if you are taking anabolic steroids, then muscle mass is getting bigger.
Proviron also has the ability to interact with the aromatase enzyme, which is responsible for converting testosterone to estrogen. By binding to aromatase, Proviron can actually inhibit its activity, thereby providing protection against estrogenic side effects.
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