Tamoxifen citrate (aka Nolvadex)

Overview and history of Nolvadex

Nolvadex (tamoxifen) belongs to a category and family of medications known as selective estrogen receptor modulators (SERMs).

Selective estrogen receptor modulators belong to a much broader class of medications known as anti-estrogens.

Another subcategory of drugs in the anti-estrogen category is known as aromatase inhibitors (AIs), such as aromasin (exemestane) and arimidex (anastrozole).

AIs and SERMs make up the class of anti-estrogens.

Aromatase inhibitors differ significantly from SERMs in how they work and how they address estrogen regulation.

The misconception that SERMs like Nolvadex and Clomid are responsible for lowering estrogen levels should be addressed before delving further.

This is a myth that has only recently begun to die down in the anabolic steroid-using community, but it still persists.

SERMs act to block the action of estrogen by taking up receptor sites instead of estrogen, preventing estrogen itself from exerting its effects in breast tissue through receptor site binding.

Conversely, SERMs also act as estrogen at the receptor site on other cells in other parts of the body (e.g., the liver in the case of Nolvadex).

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

Aromatase inhibitors do this by eliminating estrogen production by binding to and neutralizing the aromatase enzyme, the enzyme that converts (or aromatizes) androgens into estrogen.

Nolvadex is a non-steroidal SERM that belongs specifically to the triphenylethylene compound family, which means it has both estrogen agonist and estrogen antagonist effects on the body.

This means that Nolvadex can block the effects of estrogen at the cellular level in certain tissues, but it can enhance the effects of estrogen in other parts of the body.

This can be both a positive and negative effect.

For example, Nolva has an estrogenic effect in the liver, which is for all intents and purposes a positive effect because it leads to positive changes in cholesterol profile (which is what many people want).

A particular area of concern with Nolvadex is breast tissue, where it acts as an anti-estrogen, and a very potent estrogen at that.

It is utilized in medicine as a first-line treatment for female breast cancer patients who respond to estrogen.

It is also utilized as a preventative measure in women who have not developed breast cancer but are known to be at high risk due to genetic factors.

It's easy to see how these compounds have medical uses, as one of the biggest concerns of anabolic steroid users in the bodybuilding and athletic community is the estrogenic effects of anabolic steroid use (testosterone, Dianabol, boldenone, etc.), specifically gynecomastia (breast tissue development).

If left untreated, gynecomastia can develop and grow irreversibly to the point where surgical removal is the only option.

Nolvadex (Tamox) has other highly desirable effects as well, such as the ability to increase circulating levels of the endogenous gonadotropins luteinizing hormone (LH) and follicle stimulating hormone (FSH), which in turn increases endogenous production of testosterone.

This is a perfect example of Nolvadex's mixed estrogen antagonistic and agonistic properties, as it blocks the ability of estrogen 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 (hormones that signal the testes to start or increase production of testosterone).

For this reason, Nolvadex is considered an absolutely essential component of a Post Cycle Therapy (PCT) program during the weeks following anabolic steroid use in order to restore the ability to produce endogenous testosterone.

The effectiveness of Nolvadex in this regard will be discussed in more detail in this profile.

ICI first designed and developed Nolvadex (tamoxifen) in 1962, and it was introduced to the US prescription drug market shortly thereafter.

Interestingly, Nolvadex's first use in medicine was to treat female infertility.

However, after various clinical tests, in 1971, Nolvadex was found to be highly effective in treating breast cancer patients.

In 1977, Nolvadex was finally approved by the FDA for the treatment of breast cancer.

In 1988, the FDA further approved the use of Nolvadex as a preventive treatment and measure for people at high risk of developing breast cancer who have not yet developed breast cancer.

Since then, Nolvadex and its uses have proliferated worldwide, with thousands of different brands and generic Nolvadex being manufactured and utilized.

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

Nolvadex Chemical Properties

Nolvadex (tamoxifen) is a non-steroidal selective estrogen receptor modulator (SERM) that has both mixed and antagonistic actions with respect to estrogen at various sites in the body.

Nolvadex belongs to a class of compounds known as triphenylethylene compounds, and Clomid (clomiphene citrate) is a compound that is very closely related to Nolvadex.

Properties of Nolvadex

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

In other words, Nolvadex acts as a “fake” estrogen that acts as a placeholder at receptor sites in breast tissue.

As a result, estrogen is unable to activate gene transcription in those cells to form gynecomastia, and existing estrogen that has already bound to the receptor site is 'forced' out of the receptor site by Nolvadex, which takes over the receptor site instead.

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

This is the primary purpose and function of Nolvadex, and the primary reason why bodybuilders and athletes use anabolic steroids.

However, Nolvadex only acts to block estrogenic activity in the breast tissue area (where major estrogenic side effects are of concern), so it does not act to block or reduce other estrogenic side effects.

Nolvadex does not act to reduce abdominal bloating, water retention, increased blood pressure (due to water retention), or acne formation, which are side effects of increased plasma estrogen levels (as do other SERMs).

Nolvadex Side Effects

While Nolvadex is a compound that is well tolerated by the overwhelming majority of users, there are a few potential side effects to be aware of.

Due to differences in androgen and estrogen receptor proliferation in the body cells of men and women, Nolvadex tends to produce significantly different effects and experiences in men and women.

That's why there are more negative experiences related to Nolvadex side effects in women than in men, but it's a different story when bodybuilders and athletes use Nolvadex as an adjunct to anabolic steroid use.

Official prescribing documents for side effects of Nolvadex used as a treatment for breast cancer in women include hot flashes, vaginal itching, upset stomach, headache, dizziness, bone and joint pain, and swelling.

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

These are the Nolvadex side effects associated with female use, which are officially documented in clinical studies and included in the prescription product's own pamphlet.

The Nolvadex side effects listed above are of little concern to male users, as they are reportedly rarely experienced by male users.

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

Therefore, it is assumed that the use of trenbolone, deca, or related 19-nor compounds (due to the fact that they themselves are progestins) will increase progestin-related side effects.

This myth is not true.

The origins of the myth about Nolvadex side effects are rooted in various past studies that have demonstrated that Nolvadex upregulates progesterone receptors in women.

The origin of this myth is also rooted in the fact that various studies in the past have demonstrated that Nolvadex acts as an estrogen antagonist in breast tissue, and in the process also downregulates progesterone receptors (since progesterone receptor activity is closely related to estrogen receptor activity).

These studies have shown that progesterone receptors are upregulated in breast cancer patients, although of course this also occurs in normal healthy people.

Unfortunately, many in the bodybuilding community have read the results of these specific studies out of context and assumed that all normal healthy people react the same way.

This is simply not true.

Dosing and Management of Nolvadex

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

The prescribed dose and administration of Nolvadex in these cases is 10 to 20 mg twice daily, in the morning and evening.

Nolvadex for gynecomastia

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

This is typically the case especially when moderate or aromatizing anabolic steroids are used in a cycle.

In this case, the dosage of Nolvadex ranges from about 10 to 30 mg per day.

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

It is very important to understand that contrary to a common misconception, higher doses of Nolvadex, 20 to 40 mg per day or more, do not produce greater or faster effects in the reduction or prevention of gynecomastia.

Nolvadex for Post Cycle Therapy (PCT)

Another primary use of Nolvadex among bodybuilders and athletes is its ability to stimulate and increase endogenous testosterone production in men, as demonstrated in many studies.

Nolvadex does so 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 in turn signals the testes to produce testosterone.

In this case, Nolvadex is typically administered during PCT, which is shortly after the anabolic steroid cycle is complete and all anabolic steroids have been removed from the individual's system.

In this dosing regimen, 20 to 40 mg of Nolvadex per day is administered for approximately 4 to 6 weeks.

Studies have shown that doses higher than 20 to 40 mg per day do not result in a significant increase in testosterone production.

Nolvadex is also typically included in the administration of at least one or two other testosterone stimulating compounds (e.g., an aromatase inhibitor, typically aromasin and/or HCG) during PCT to increase its effectiveness in promoting proper HPTA function after the cycle ends.

The use of Nolvadex during the cycle will not offset the testosterone suppressing effects of anabolic steroid use, nor will endogenous testosterone production be sustained while using suppressive compounds.

Therefore, it is not recommended as it would be a waste of product and money.

Nolvadex has a very long half-life for an oral compound (approximately 5-7 days), with some studies showing it to last as long as 14 days.

As such, there is no need to split doses throughout the day and it is safe to take with food or on an empty stomach.

Nolvadex legality

Nolvadex is an uncontrolled substance in most countries around the world.

In Canada and the United States in particular, it is a prescription-only product, but as it is not a controlled substance, you can legally own, purchase, and possess it, but it is not available over-the-counter domestically.

In the United Kingdom, the legality of Nolvadex is the same. In many countries in Eastern Europe, Asia, and the Middle East, Nolvadex is often available without a prescription.