Decoding Estrogen Blockers: Balancing Hormones and Empowering Health

Monali Sharma
Medically reviewed by
Dr. Kaushal

Review medical content on WOW Rx Pharmacy, so that accurate drug use information is easily accessible to everybody.
Dr. Akansha is a licensed Clinical Pharmacologist. She possesses remarkable knowledge in Pharmacovigilance, prescription analysis, drug information, and drug safety services. Additionally, she is a keen learner and an educator.

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estrogen blocker

Estrogen blockers, as the name suggests, block or inhibit Estrogen functionality in the body.

They are also known as Estrogen receptor antagonists or anti-estrogens.

These blockers are primarily used to address an imbalance in the Estrogen-Progesterone ratio or to treat health conditions that benefit from reduced Estrogen activity.

However, hormone metabolism is a complex process, and their suitability and potential side effects should be considered before using them.

This article will explore Estrogen blockers in detail, including their advantages, different types, and potential side effects.

Estrogen blocker and their utilization

Sometimes, individuals may experience elevated Estrogen activity or Estrogen dominance within their bodies.

This can be attributed to excessive production of Estrogen, changes in Estrogen metabolism, or a relatively higher proportion of Estrogen compared to Progesterone.

An Estrogen blocker is a substance or compound that exhibits a blocking effect on the hormone and prevents it from overpowering its usual levels.

The underlying mechanism of blocking activity is interference with the binding of Estrogen to its receptors, thereby reducing its activity.

Estrogen blockers have a wide range of applications in hormone-related treatments for both males and females.

Balancing Hormones

Estrogen blockers are commonly used to address the disproportionate Estrogen and Progesterone levels.

This can be beneficial for individuals experiencing symptoms of Estrogen dominance.

In women, these symptoms may appear as weight gain, irregular menstrual bleeding, mood swings, depression or anxiety, breast tenderness, low sex drive, and fatigue.

In men, these symptoms can include poor erections, decreased sex drive, Erectile Dysfunction, and dry skin.

Treating Estrogen-related ailments

Estrogen blockers for Breast cancer treatmentSource: Rido
Breast cancer treatment

Estrogen blockers are employed in the treatment of many health conditions that require decreased Estrogen activity.

Some of these include:

  • Breast cancers
  • Ovarian cancers
  • Fibrocystic disease(painful, lumpy breasts)
  • Myomas or uterine fibroids(noncancerous growths of the uterus)
  • Endometriosis(tissue similar to the uterus lining grows outside the uterus)
  • Ovulation induction in the treatment of infertility
  • Polycystic Ovary Syndrome (PCOS)
  • Treatment of Prostate cancer, subfertility, Gynecomastia(abnormal breast growth), and Breast cancer in men

Types of Estrogen blockers

There are two primary types of pharmaceutical Estrogen blockers Aromatase Inhibitors(AIs) and Selective Estrogen Receptor Modulators (SERMs). 

Let’s understand each of these individually.

Aromatase inhibitors

Aromatase inhibitors function by inhibiting an Estrogen production process called aromatization.

In aromatization, Androgens are converted to Estrogen by the Aromatase enzymes.

A few commonly prescribed Aromatase inhibitor medicines include:

  • Anastrozole (Arimidex)
  • Letrozole (Femara)
  • Exemestane (Aromasin)
  • Testolactone (Teslac)
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Selective Estrogen Receptor Modulators (SERMs)

Selective Estrogen Receptor Modulators (SERMs) affix to Estrogen receptors, preventing Estrogen from binding.

These medications can function as both an Estrogen agonist(stimulator) and an antagonist( inhibitor), depending on the specific tissue being targeted.

Commonly prescribed SERMs include:

  • Tamoxifen (Nolvadex)
  • Toremifene (Fareston)
  • Raloxifene 
  • Lasofoxifene
  • Bazedoxifene
  • Clomiphene

Other anti-estrogen drugs

There are alternative medications akin to SERMs that have the capability to inhibit Estrogen, but unlike SERMs, they do not replicate the effects of Estrogen.

Consequently, these medications are referred to as pure anti-estrogens.

One example of such a drug is Fulvestrant (Faslodex).

Information :
While Tamoxifen, a SERM, demonstrates anti-estrogenic properties in breast tissue, it can exert estrogen-like effects in other tissues like bone and uterus.

Alternate or natural Estrogen blockers

Some natural food items exhibit Estrogen blocking effects on the human body.

These can be considered to aid in controlling Estrogen levels.

These include:

  • Cruciferous vegetables like broccoli, cabbage, Maca plant, and cauliflower have Indole-3-carbinol, which is linked to anti-estrogen activity
  • Oyster mushrooms have the potential to block Aromatase and can be seen as a natural Aromatase inhibitor
  • Curcumin, a yellow polyphenolic pigment found in turmeric, possesses the capability to decrease Estrogen levels
  • Whole soy foods help to shift Estrogen metabolism favoring controlled levels
  • High-caloric-density meals can contribute to elevated Estrogen levels, so individuals looking to regulate their Estrogen levels should monitor their fat intake
  • A high-fiber diet promotes Estrogen excretion and reduces Estrogen absorption, hence can contribute to blocking Estrogen activity

Alternate methods to promote Estrogen reduction can include:

  • Quitting alcohol may help, as It is possible to observe a fall in Testosterone levels and a rise in Estrogen levels with prolonged alcohol use
  • Exercise and weight loss should be encouraged as they contribute to balanced Estrogen levels in the body
  • Stress also disrupts the Estrogen to Progesterone ratio; hence stress management measures, relaxation exercises, and mind-body practices can also help

Side effects of Estrogen blocker

Nausea might be the side effect of the medicationSource: Africa_images
Nausea

Similar to other medications, Estrogen blockers also carry the risk of certain adverse effects.

Aromatase inhibitors may be accompanied by the side effects such as: 

  • Hot flashes, night sweats, vaginal dryness
  • Fatigue
  • Bone loss
  • Nausea
  • Joint pain
  • Mood swings and depression
  • Risk of blood clots
  • Genital pain during sex
  • Sexual dysfunction
  • Bone health deterioration, joint pain

Furthermore, SERMs can potentially cause adverse effects such as:

  • Hot flashes
  • Nausea
  • Vaginal discharge
  • Leg cramps
Warning:
Severe risks of Estrogen blockers include an increased likelihood of risk of heart and brain strokes; therefore, it is prudent to consult with a doctor regarding their usage.

Summary

Estrogen blockers inhibit or block Estrogen production or activity in the body by interfering with Estrogen receptor binding and reducing its activity.

Aromatase inhibitors, including Anastrozole (Arimidex), Letrozole (Femara), and Exemestane (Aromasin), target the enzyme aromatase, which converts Androgens into Estrogens.

SERMs, such as Tamoxifen (Nolvadex) and Toremifene (Fareston), are another type of Estrogen blocker that interact with Estrogen receptors to prevent Estrogen binding.

Estrogen blockers find their usefulness in treating hormone-related conditions like breast and ovarian cancers, fibroids, Endometriosis, and PCOS in women.

They also treat certain male health conditions such as Prostate cancer, subfertility, Gynecomastia, and Breast cancer.

Certain foods like cruciferous vegetables (broccoli, cabbage), oyster mushrooms, turmeric, soy foods, and a high-fiber, low-calorie diet can have Estrogen-blocking effects.

Lifestyle interventions such as regular exercise, weight management, and stress reduction can also help control the Estrogen-Progesterone ratio.

Therefore, it is essential to undergo a prior diagnosis and health analysis by an expert before initiating Estrogen blocker therapy.

Frequently Asked Questions

What are the most common Estrogen blockers?

The most common Estrogen blockers include Selective Estrogen Receptor Modulators (SERMs) like Raloxifene and Tamoxifen, Aromatase inhibitors (AIs) like Anastrozole and Letrozole, and anti-estrogens like Fulvestrant. These medications work differently to either block Estrogen receptors or inhibit Estrogen production, aiding in regulating hormonal balance.

Are Estrogen blockers a good idea?

Estrogen blockers can be good in specific scenarios, often prescribed for hormone-sensitive conditions like Breast cancer or to address hormonal imbalances. Nevertheless, it is crucial to consult a medical expert before deciding to use Estrogen blockers, considering individual health requirements and potential risks.

Is blocking Estrogen bad?

Blocking Estrogen is bad when your hormone levels are fine or lower-than-normal Estrogen in your body, as it can lead to Estrogen imbalance. However, they are beneficial in addressing certain conditions such as Breast cancer, Endometriosis, or uterine fibroids. Self-administrations of Estrogen blockers is not advisable; speak to your doctor first.

What is the strongest natural Estrogen blocker?

While there is no definitive “strongest” natural Estrogen blocker, certain compounds found in foods like flaxseeds, soy, and cruciferous vegetables (such as broccoli and cabbage) have been found to exhibit mild Estrogen-blocking properties. However, it is recommended not to rely solely on these foods as the primary method for Estrogen blocking.

Is there a natural way to block Estrogen?

While certain natural compounds present in foods like flaxseeds, soy, and cruciferous vegetables (such as broccoli and cabbage) have been observed to have mild Estrogen-blocking properties, their effectiveness as a sole method for blocking Estrogen is not widely established and can differ based on individual factors.

Citations:
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