Estrogen blockers are chemical compounds that block the actions of estrogen. Antiestrogen drugs are used in the treatment of various diseases. They are widely used for the treatment of breast cancer in order to slow down tumor growth or prevent recurrence. 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 a steroid hormone, is synthesized primarily 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 hyperestrogenism. This disease can lead to oncological processes in the breast and endometrial cancer. Antiestrogen drugs and estrogen blockers or aromatase inhibitors can fix this. Such drugs, however, have positive and negative effects on women and men.
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, Clomiphene, are designed to block estrogen receptors, and behave differently for different types of tissue. Antiestrogens also block estrogen receptors.
Antiestrogen prevents the conversion of testosterone to estradiol, and estrogenic hormones stop working or are blocked.
In the treatment of cancer, these drugs are used to slow tumor growth. In this case, selective estrogen receptor modulators can target specific estrogen receptors. Blockers, including clomiphene, are also sometimes used in the treatment of infertility and may help some women who have difficulty getting pregnant. These drugs are also used by some clinicians in the treatment of children who have delayed puberty until they are old enough.
It is common among bodybuilders to use estrogen blockers due to the estrogenic effect of high testosterone levels in the body. Testosterone is a precursor to estrogen, aromatase inhibitors can be used to stop excess estrogen from building muscle mass, keeping levels low in the body. This practice has attracted many, especially when antiestrogen drugs are used primarily for cosmetic purposes. In thatcase, people use pills and nutritional supplements without medical supervision.
Side effects
There are side effects of antiestrogenic drugs. They can cause dizziness, headaches, sweating, hot flashes, and confusion. Only the endocrinologist can determine the appropriate dosage for the patient, depending on the situation, and the acceptable threshold for side effects. The endocrinologist may also order regular blood tests for hormone levels when evaluating the patient's general he alth to confirm that antiestrogen use is safe and functional for the patient.
Treatment for men
As men age, testosterone levels drop. However, if testosterone decreases rapidly or significantly, this can lead to the development of hypogonadism. This condition, characterized by the body's inability to produce this important hormone, can cause a variety of symptoms, including:
- loss of libido;
- decrease in sperm production and quality;
- erectile dysfunction;
- tired.
When talking about estrogen, they first of all 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 you to properlydevelop spermatozoa.
Hormonal imbalance - rising estrogen levels and falling testosterone - creates problems. Too much estrogen in the male body can lead to:
- gynecomastia (overdevelopment of breast tissue);
- cardiovascular problems;
- increased risk of stroke;
- weight gain;
- prostate problems.
There are a number of steps you can take to rebalance your estrogen levels. For example, if your excess estrogen is associated with low testosterone levels, then testosterone replacement therapy as an estrogen blocker may be useful.
Pharmaceutical estrogen blockers
Some pharmaceutical products can produce an estrogen-blocking effect in men. They are generally most often intended for use by women, but are gaining popularity among men, especially those who wish to have children. Testosterone supplements can lead to infertility. But estrogen blockers like Clomid can restore hormonal balance without compromising fertility.
Some drugs, known as selective estrogen receptor modulators, are commonly marketed as treatments for breast cancer. But they can also be used to block estrogen in men. These drugs are used for a variety of conditions associated with low testosterone, including:
- infertility;
- low quantityspermatozoa;
- gynecomastia;
- osteoporosis.
These drugs should be used selectively, depending on the condition of the patient. Such antiestrogen drugs are used. Available at the pharmacy:
- "Tamoxifen".
- "Arimidex".
- "Letrozole".
- "Raloxifene".
Action on bone tissue
According to clinicians, long-term exposure to estrogenic drugs can cause endometrial cancer in women. "Raloxifene" - a selective estrogen receptor modulator - can prevent the development of cancer, selectively blocks the absorption of estrogen. This drug, however, is also able to inhibit the beneficial effects of estrogens on bone density. A new drug, Lazofoxifene, could fix this problem. It prevents bone loss in postmenopausal women and reduces bone fragility. The use of this drug is generally safe, but may increase blood clotting.
Drug Interactions
Estrogen blocker Tamoxifen may help prevent cancer. Cancer patients often experience depression, and drugs in this group can interact negatively with antidepressant medications. Paroxetine should be used because women taking Tamoxifen and Paroxetine have a lower risk of mortality than women taking Tamoxifen andany other antidepressant. This is because Paroxetine is selective.
Antiestrogen drugs and drugs
Descriptions of all these remedies 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, as it raises the body's own testosterone levels. There are some side effects from long-term use, such as vision problems. There are better compounds on the market that do the same, but Clomid is still an effective and inexpensive blend for any athlete.
This is not an anabolic steroid, the drug is usually prescribed to women as an aid to 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 can block the ability of estrogen to bind to the corresponding receptor. Its clinical benefit is to counter the negative feedback of estrogens in the hypothalamic-pituitary-ovarian system, which increase 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 the athlete at the end of a steroid cycle when endogenous testosterone levels are depressed. Without testosterone (or other androgens), "Cortisol" dominates and influences muscle protein synthesis. But he quickly "eats" most of the newly acquired muscle after withdrawal. Clomid can play a significant role in preventing this accident in order to achieve athletic performance. For women, the benefit of Clomid is the possible management of endogenous estrogen levels. This will increase the loss of fat and musculature, especially in areas such as the thighs 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 such as the uterus and bones.
Women with dependent invasive breast cancer Tamoxifen may be used for 5-10 years after surgery to reduce the chance of spread of metastases. It also reduces the risk of developing cancer in the other breast. For the early stage, this drug is mainly used for patients who do not havemenopause has come. Aromatase inhibitors are the preferred treatment for menopausal women.
Tamoxifen can also stop the growth and even shrink tumors in patients with metastatic cancer. It may also be used to reduce the risk of developing breast cancer.
This drug is taken by mouth, most commonly in tablet form.
Side effects of antiestrogenic drugs include fatigue, hot flashes, vaginal dryness or heavy discharge, and mood swings.
Some women with bone metastases may experience pain and swelling in the muscles and bones. This usually does not last long, but in some rare cases, women may also develop high blood calcium levels that cannot be controlled. If this happens, treatment may be suspended for a while.
Rare but more serious side effects are also possible. These drugs may increase the risk of developing myometrial cancer in menopausal women. Increased blood clotting is another possible serious side effect. Deep vein thrombosis occurs, but sometimes a piece of the clot can break off and eventually block an artery in the lungs (pulmonary embolism).
Tamoxifen has rarely been the cause of strokes and heart attacks in postmenopausal women.
Depending on the woman's menopausal status, Tamoxifen may have different effects.effect on bones. In premenopausal women, Tamoxifen can cause bone thinning, but in postmenopausal women, calcium levels increase, which is necessary for bone strength.
The benefits of this medication 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 the estrogen receptor and then also eliminates the receptor's ability to bind. It acts as an antiestrogen throughout the body.
Fulvestrant is used to treat advanced metastatic breast cancer and is most commonly used after other hormonal drugs (Tamoxifen and aromatase inhibitors) have stopped working.
Common side effects may include hot flashes, night sweats, mild nausea and fatigue. Theoretically, it can weaken bones (osteoporosis) if taken for a long time.
This drug has gained acceptance for use in postmenopausal women not responding to tamoxifen or toremifene. It is sometimes used off-label in premenopausal women, often combined with a luteinizing hormone-releasing agonist to shut down the ovaries.
"Raloxifene" is used by women for prevention and treatmentbone 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 certain parts of the body, such as the bones. In other parts of the body (uterus and breasts), 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 testosterone stimulant. "Cyclophenyl" is a very weak and mild estrogen, but it binds to estrogen receptors and prevents natural estrogen receptors from binding. In fact, it works so well that some athletes take the drug during steroid treatment to keep their estrogen levels low. 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 drugs that could potentially be taken in preparation for a competition. Bodybuilders, however, use it less often as they prefer it moreavailable "Nolvadex" and "Proviron".
Like Clomid, Cyclofenil is ineffective in women, as it has a positive effect only on the production of hormones in men. The increase in testosterone levels caused by this drug is not enough to speak of dramatic improvements, however, it will provide an increase in strength, even a small increase in body weight, a marked increase in energy and an increase in regeneration are possible. These results are especially noticeable in advanced athletes who have little or no experience with steroids. The results of use become noticeable only after a week.
In some cases, athletes experience acne-like rashes, increased sex drive and hot flashes. These symptoms are particularly indicative of proof that a compound is in fact effective. After discontinuation, some report depressed mood and a slight decrease in physical strength. Those who take the drug as an antiestrogen during a steroid regimen may experience a rebound effect when the drug wears off.
"Proviron" is one of the oldest anabolic androgenic steroids on the market. Officially known as "Mesterolone", it remains one of the most underused anabolic steroids among users.
On a functional basis, Proviron performs four main functions that largely determine its mode of action. First of all, he appearsone of the most powerful anabolic steroids, as it increases the volume of circulating free testosterone, which is more important for anabolic processes in bodybuilders. An easy way to look at it: if you take anabolic steroids, then your muscle mass gets bigger.
"Proviron" also has the ability to interact with the aromatase enzyme, which is responsible for the conversion of testosterone to estrogen. By binding to aromatase, Proviron can indeed inhibit its activity, thereby providing protection against estrogenic side effects.
The "Mesterolone" also has a strong affinity for the androgen receptor. This anabolic steroid does not suppress gonadotropins in a similar way to other anabolic steroids. This allows you to increase sperm production, since androgens are necessary to stimulate spermatogenesis. This not only increases the amount of sperm, but also improves its quality.
Side effects of Proviron do not include gyno or excess fluid. It will also significantly reduce the risk of high blood pressure associated with anabolic steroid use. In fact, Proviron has an antiestrogenic effect by stopping the conversion of testosterone to estrogen, or at least slowing down this process.
The above drugs do not reduce estrogen levels, but affect metabolism in general.
The group of antiestrogen drugs also includes agonists of releasing factors of gonadotropic hormones ("Buserelin" and itsanalogues), megestrol acetate ("Megeis"), "Parlodel" and "Dostinex" are used as drugs that stop the secretion of prolactin. It is irrational to use them in treatment on your own.
Cancer treatment
In addition to Tamoxifen, the following estrogen receptor blockers are used.
Three drugs that stop estrogen production in postmenopausal women have been approved to treat both early and advanced breast cancer: Letrozole (Femara), Anastrozole (Arimidex) and Exemestane ("Aromasin").
The mechanism of action of antiestrogenic drugs of this group is the blocking of an enzyme (aromatase) in adipose tissue, which is responsible for small amounts of estrogen in postmenopausal women. They do not affect the ovaries, so they are only effective for women whose ovaries are not working, either due to menopause or exposure to a luteinizing hormone analogue. These drugs are taken daily in tablet form. They work equally well in the treatment of oncological processes in the breast and prostate.
Sometimes the treatment of breast cancer requires medication to turn off the ovaries. This can be done with luteinizing hormone-releasing hormone (LHRH) analogs, such as Goserelin (Zoladex) or Leuprolide (Lupron). These drugs block the signal that the body sends to the ovaries to produceestrogen. They can be used alone or with tamoxifen, aromatase inhibitors, fulvestrant for premenopausal hormone therapy.
