Tamoxifen Citrate is a Selective Estrogen Receptor Modulator (SERM) that was created in 1961 by ICI now known as AstraZenaca. There are numerous brands including generic forms of Tamoxifen Citrate on the market, but Nolvadex is the most well known. Often referred to as an anti-estrogen, Tamoxifen Citrate is actually both an antagonist and agonist. This means it will act as an anti-estrogen in certain areas of the body while acting as an estrogen in other areas.
Tamoxifen Citrate has been used medically for decades and has been highly successful in breast cancer treatment, specifically hormone-responsive breast cancer. It is also a medication that is used by many anabolic steroid users, but it is not a steroid. This is a drug steroid users will sometimes use during steroid use to help with estrogenic related side effects brought on by specific steroids. However, it is most commonly used during Post Cycle Therapy (PCT). PCT is the 3-6 week period following steroid use that is implemented in order to help with natural testosterone production that is suppressed during anabolic steroid use.
Tamoxifen Citrate Functions & Traits
Tamoxifen Citrate is a SERM that acts as both antagonist and agonist in relation to the estrogen hormone. It is an anti-estrogen in that it binds to estrogen receptors in certain parts of the body, particularly in the mammary tissue. This action prevents estrogen from acting on its originally intended point of binding. This makes Tamoxifen Citrate valuable to breast cancer patients as breast cancer feeds off of estrogen. And it’s valuable to steroid users as increased estrogen levels can bind to the mammary tissue and lead to gynecomastia.
The relationship Tamoxifen Citrate has in being an anti-estrogen is fairly straightforward and well understood by many, but it’s its relationship to being an estrogen in other areas that’s surprising to some. Tamoxifen Citrate acts as an estrogen on the liver. Liver related estrogenic activity has been shown to improve cardiovascular health, particularly as it relates to cholesterol. This can be very advantageous for the bodybuilding steroid user as most steroids have a negative impact on cholesterol levels.
Beyond its estrogen related activity Tamoxifen Citrate possesses strong testosterone stimulating properties. The use of Tamoxifen Citrate will stimulate the pituitary to increase its production of Luteinizing Hormone (LH) and Follicle Stimulating Hormone (FSH) with a strong emphasis on LH. LH and FSH are the gonadotropins that signal to the testicles to produce testosterone. Without LH and FSH there is no testosterone production.
Effects of Tamoxifen Citrate
For the anabolic steroid user the positive effects of Tamoxifen Citrate can be seen both during and post anabolic steroid use with post use being primary. Anabolic steroids like Testosterone and Nandrolone among others will increase the body’s serum estrogen levels. This occurs by the testosterone hormone converting to testosterone, which happens due to it being metabolized by the aromatase enzyme. Once aromatized you have more estrogen, and this can lead to gynecomastia and water retention. It can also lead to high blood pressure if water retention becomes severe. Tamoxifen Citrate does not lower serum estrogen levels, but it will bind to the receptors in the chest preventing the estrogen from binding. It will not do a lot for water retention if that is an issue. It is also not enough gynecomastia protection for all men, but that depends on how high estrogen levels go as well as genetics. If more or stronger protection is needed Aromatase Inhibitors (AI’s) are recommended. AI’s are anti-estrogens that inhibit aromatase activity and lower serum estrogen levels.
We then have the testosterone stimulating effects of Tamoxifen Citrate. This is by far the most important effect for the anabolic steroid user. When we use anabolic steroids we suppress our natural testosterone production, and this will occur regardless of the steroids used. Steroid use creates a negative feedback and tells your pituitary to stop making LH and FSH. This is why almost all steroid cycles include exogenous testosterone so that the negative feedback doesn’t cause a low testosterone level. Once steroid use is complete something is then needed to jump start testosterone production. It will occur on its own, but it will be slow and Tamoxifen can both speed it up and make it more efficient. Tamoxifen Citrate is introduced, LH and FSH levels go up and as a result testosterone is produced.
Important Note: PCT use that includes Tamoxifen Citrate or any SERM, for it to be successful this assumes no prior low testosterone condition existed. It also assumes no damage was done to the Hypothalamic-Pituitary-Testicular-Axis (HPTA) during use. If prior low levels existed Tamoxifen Citrate won’t magically fix this. If severe damage was done to the HPTA you will not recover and may be in need of low testosterone treatment.
Important Note: Many steroid users believe that a good PCT brings about full recovery, but this is a false belief. A PCT that includes Tamoxifen Citrate will stimulate recovery, but it will not end it. It will still take several months for full recovery to occur, but it stands a much better chance with PCT than without.
For the breast cancer patient the effects of Tamoxifen Citrate are perhaps even more straightforward than they are for the anabolic steroid user. Estrogen attaches and feeds the cancer, but Tamoxifen Citrate prevents it from attaching and starves the cancer. This is a simple yet effective means of treatment. This is not the only drug used in treatment; commonly treatment will begin with an AI and then will be switched to a SERM like Tamoxifen Citrate. It is also sometimes used as a preventative measure in those that have a strong family history of breast cancer.
Side Effects of Tamoxifen Citrate
Possible side effects of Tamoxifen Citrate do exist, but it is one of the more well-tolerated SERM’s on the market. Most men will not have an issue with this medication, although it is possible. Side effects of Tamoxifen Citrate do appear to be more common in women, but they are still not what we’d call “common.” The most common side effects of Tamoxifen Citrate include:
- Vaginal Itching, bleeding, discharge or discomfort
- Hot Flashes
- Upset Stomach
The above side effects of Tamoxifen Citrate are not extremely common but possible. Other possible side effects of the SERM’s use but less common than the above include:
- Decreased White Blood Cell Count
- Endometrial Changes
- Increased Triglyceride Levels
- Pulmonary Embolism
Important Note: Women who are pregnant or who may become pregnant should not use Tamoxifen Citrate or any SERM as use will potentially damage the developing child and with strong probability.
Tamoxifen 20mg is an antagonist of the estrogen receptor in breast tissue via its active metabolite, 4-hydroxytamoxifen. In other tissues such as the endometrium, it behaves as an agonist, and thus may be characterized as a Selective estrogen-receptor modulator. Tamoxifen is the usual endocrine (anti-estrogen) therapy for hormone receptor-positive breast cancer in pre-menopausal women, and is also a standard in post-menopausal women although aromatase inhibitors are also frequently used in that setting.
Some breast cancer cells require estrogen to grow. Estrogen binds to and activates the estrogen receptor in these cells. Tamoxifen is metabolized into compounds that also bind to the estrogen receptor but do not activate it. Because of this competitive antagonism, tamoxifen acts like a key broken off in the lock that prevents any other key from being inserted, preventing estrogen from binding to its receptor. Hence breast cancer cell growth is blocked.