Tamoxifen(Nolvadex) Overview & Features

Nolvadex Overview and History

Nolvadex (Tamoxifen) belongs to the category and class of drugs known as Selective Estrogen Receptor Modulators (SERMs).

Selective Estrogen Receptor Modulators belong to a much broader class of drugs known as Anti-estrogens.

Other sub-categories of drugs belonging to the Anti-estrogen category are known as Aromatase Inhibitors (AIs), such as Aromasin (Exemestane) and Arimidex (Anastrozole).

AIs and SERMs constitute Anti-estrogens.

Aromatase Inhibitors differ significantly from SERMs in their mode of action and how they address estrogen-related issues.

A misconception that SERMs like Nolvadex and Clomid serve to lower estrogen levels is one that must be addressed before delving deeper.

This is a rumor that has persisted, although it has recently begun to fade within the anabolic steroid using community.

SERMs function by blocking the action of estrogen at the receptor site by occupying the receptor site *instead* of estrogen, thereby preventing estrogen itself from exerting its effects in breast tissue via receptor site binding.

Conversely, SERMs also act as estrogen at the receptor sites in other cells in other parts of the body (for example, the liver in the case of Nolvadex).

SERMs do not lower circulating levels of estrogen in the blood plasma.

Aromatase Inhibitors perform this action by eliminating estrogen production through binding to and disabling the aromatase enzyme, the enzyme responsible for converting (or aromatizing) androgens into estrogen.

Nolvadex is specifically a non-steroidal SERM belonging to the triphenylethylene compound family, exhibiting both estrogen agonist and estrogen antagonist effects in the body.

That is, Nolvadex can block the effects of estrogen at the cellular level in certain tissues, but it can also enhance estrogenic effects in other parts of the body.

This can be either a positive or a negative effect.

For example, Nolva exhibits an estrogenic effect in the liver, which is a positive effect for all intents and purposes because it results in positive changes to cholesterol profile (something many people desire).

The area of concern for Nolvadex is specifically breast tissue, where it acts as an anti-estrogen and is a very powerful estrogen blocker.

It is utilized in medicine as a primary treatment for female breast cancer patients who are estrogen-responsive.

It is also utilized as a preventative measure for women known to be at high risk due to genetic factors, etc., even if they have not developed breast cancer.

It is easy to see how these compounds are used medically, as one of the biggest concerns for anabolic steroid users in the bodybuilding and athletic communities are the estrogenic effects resulting from the use of anabolic steroids (Testosterone, Dianabol, Equipoise, etc.), especially gynecomastia (breast tissue development).

If left unchecked, gynecomastia can develop and enlarge to a point where it becomes irreversible and can only be removed via surgery.

Nolvadex (Tamox) also possesses other very desirable effects, such as its ability to increase circulating levels of the endogenous gonadotropins Luteinizing Hormone (LH) and Follicle-Stimulating Hormone (FSH), and through this, increase endogenous Testosterone production.

This is a perfect example of Nolvadex’s mixed estrogenic antagonistic and agonistic properties, where it blocks estrogen’s ability to bind to receptors in the hypothalamus.

As a result, the negative feedback loop of the HPTA (Hypothalamic-Pituitary-Testicular Axis) is manipulated, resulting in increased production of gonadotropins (the hormones that signal the testes to begin or increase Testosterone production).

For this reason, Nolvadex is considered an absolutely essential component in Post Cycle Therapy (PCT) programs for several weeks following anabolic steroid use in order to restore endogenous Testosterone production function.

The effects of Nolvadex in this aspect will be covered in more detail later in this profile.

ICI first designed and developed Nolvadex (Tamoxifen) in 1962, and it was released on the US prescription drug market not long after.

Interestingly, the first medical use for Nolvadex was for the treatment of female infertility.

However, after various clinical tests, it was discovered in 1971 that Nolvadex was very effective in treating breast cancer patients.

In 1977, Nolvadex finally received FDA approval for the purpose of breast cancer treatment.

1988 was the year the FDA additionally approved the use of Nolvadex as a preventative treatment and measure for individuals at high risk of developing breast cancer who had not yet developed it.

Since then, Nolvadex and its uses have spread worldwide, with thousands of different brand and generic Nolvadex versions being manufactured and utilized.

However, in 2006, AstraZeneca ceased its production in the United States, and while this major brand name is no longer available in the US, Nolvadex continues to be utilized effectively as a breast cancer treatment under various generic brand names.

Nolvadex Chemical Characteristics

Nolvadex (Tamoxifen) is a non-steroidal Selective Estrogen Receptor Modulator (SERM) that possesses both mixed agonist and antagonist actions in relation to estrogen in various parts of the body.

Nolvadex belongs to a family of compounds known as triphenylethylene compounds, and Clomid (Clomiphene Citrate) is a very closely related compound to Nolvadex.

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Nolvadex Properties

It is already established that Nolvadex, being a SERM, does not lower circulating estrogen levels in the body, but instead works by occupying the receptor sites in breast tissue, preventing estrogen itself from binding to these receptors.

Simply put, Nolvadex acts as a ‘fake’ estrogen that acts as a placeholder at the receptor sites in breast tissue.

As a result, estrogen cannot activate gene transcription in those cells to form gynecomastia, and any existing estrogen already bound to the receptor sites is ‘forced’ off the receptor site by Nolvadex, which then occupies the receptor site instead.

This is very promising news for anabolic steroid users who wish to eliminate and reverse gynecomastia in its early stages, and for those who are very sensitive to gynecomastia side effects from elevated estrogen levels and wish to utilize Nolvadex as a preventative measure.

This is Nolvadex’s primary purpose and function, and the main reason bodybuilders and athletes use it in conjunction with anabolic steroids.

However, because Nolvadex only serves to block estrogen activity in the breast tissue area (where the primary estrogen side effect is a concern), it does not serve to block or reduce other estrogenic side effects.

Nolvadex does not serve to reduce abdominal bloating, water retention, increased blood pressure (from water retention), or acne formation, which are side effects resulting from increased blood plasma estrogen levels (the same applies to other SERMs).

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Nolvadex Side Effects

Nolvadex is a compound that is well-tolerated by the vast majority of its users, but there are some potential side effects that should be noted.

Due to the differences in androgen and estrogen receptor proliferation in male and female body cells, Nolvadex tends to produce quite different effects and experiences in males versus females.

This is why there are more negative experiences associated with Nolvadex side effects in females than in males, but that is a different story from bodybuilders and athletes using Nolvadex as an ancillary in relation to anabolic steroid use.

The official prescribing documentation for Nolvadex, when used as a breast cancer treatment for women, lists side effects including hot flashes, vaginal itching, upset stomach, headache, dizziness, bone/joint pain, and edema.

Rarer and less common side effects can include cholesterol changes, changes in white blood cell count, changes in platelet count, skin rash, endometrial changes, deep vein thrombosis, and pulmonary embolism.

These are the side effects of Nolvadex associated with female use, as documented officially in clinical studies and included in the pamphlet of the prescription product itself.

The Nolvadex side effects listed above are known to almost never occur in male users, so they are side effects that male users hardly need to worry about.

However, there is a persistent and long-standing myth that when Nolvadex is used in conjunction with compounds such as Trenbolone or Nandrolone (Deca Durabolin), it upregulates progesterone receptors and increases sensitivity to these compounds.

Therefore, it is presumed that using Trenbolone, Deca, or related 19-nor compounds (by virtue of the fact that they are progestins themselves) will result in increased progestogenic-related side effects.

This myth is not true.

The origin of the myth regarding Nolvadex side effects is rooted in various past studies that demonstrated Nolvadex upregulates progesterone receptors in females.

It is also based on the fact that it has been demonstrated in several past studies that Nolvadex acts as an estrogen antagonist in breast tissue, and in the process, also downregulates progesterone receptors (this is because progesterone receptor activity is closely tied to estrogen receptor activity).

These studies, of course conducted on breast cancer patients, showed that in these patients, progesterone receptors are upregulated.

Unfortunately, many individuals in the bodybuilding community read these specific study results out of context and assumed that all normal healthy individuals would respond in the same manner.

This is not true.

Nolvadex Administration and Dosage

Medically, Nolvadex (Tamoxifen) is a drug used to treat six different types of breast cancer in women.

In such cases, the prescribed dosage and administration of Nolvadex is 10-20mg taken twice daily, once in the morning and once in the evening.

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Nolvadex for Gynecomastia

In the realm of bodybuilding and performance enhancement, Nolvadex is utilized primarily as an ancillary supplement to combat, reduce, and/or prevent gynecomastia.

This is generally the case, especially when using moderately or highly aromatizable anabolic steroids in a cycle.

In this case, the dosage of Nolvadex is approximately 10-30mg per day.

The typical dosage tends to be 20mg of Nolvadex per day.

It is very important to understand that, contrary to common misconception, higher doses of Nolvadex above 20-40mg per day do not demonstrate a greater or faster effect on gynecomastia reduction or prevention.

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Nolvadex for Post Cycle Therapy (PCT)

Another primary use for Nolvadex among bodybuilders and athletes is its ability, as demonstrated in many studies, to stimulate and increase endogenous Testosterone production in males.

Nolvadex does this by acting on the pituitary gland and hypothalamus in the brain to signal increased production of FSH (Follicle-Stimulating Hormone) and LH (Luteinizing Hormone), which then signal the testes to produce Testosterone.

In this case, Nolvadex is typically administered during PCT, immediately after an anabolic steroid cycle is completed and all anabolic steroids have cleared the individual’s system.

In this administration, Nolvadex is used at a dosage of 20-40mg per day for approximately 4-6 weeks.

Studies have shown that taking more than 20-40mg per day does not result in a significant further increase in Testosterone production.

Furthermore, Nolvadex is usually included in PCT along with at least one or two other Testosterone-stimulating compounds (e.g., Aromatase Inhibitors, typically Aromasin and/or HCG) to heighten the effect of promoting proper HPTA function post-cycle.

Using Nolvadex during a cycle does not offset the Testosterone-suppressing effects of anabolic steroid use, and endogenous Testosterone production is not maintained while using the suppressive compounds.

Therefore, it is not recommended as it can be a product and cost waste.

Nolvadex possesses a very long half-life (approximately 5-7 days) for an oral compound, with some studies indicating it can last up to 14 days.

Therefore, there is no need to split the dosage throughout the day, and it can be safely consumed with or without food.

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Nolvadex Legality

Nolvadex is an uncontrolled substance in the vast majority of countries worldwide.

Specifically in Canada and the United States, it is a prescription-only product but not a controlled substance, meaning it is legal to own, purchase, and possess, but it cannot be purchased domestically without a prescription.

The legality of Nolvadex in the UK is the same.

In many countries in Eastern Europe, Asia, and the Middle East, Nolvadex is often available for purchase without a prescription.

Tamoxifen Citrate (aka Nolvadex)