12-06-2016, 09:06 PM #1
Nolvadex (tamoxifen) Facts/Profile
Overview and History of Nolvadex
Nolvadex (Tamoxifen) belongs to a category and class of drugs known as selective Estrogen receptor modulators (SERMs). Selective Estrogen receptor modulators belong to an even broader class of drugs known as anti-estrogens. The other subcategory of drug under the anti-estrogens category is known as aromatase inhibitors (AIs), such as Aromasin (Exemestane) and Arimidex (Anastrozole). AIs and SERMs make up anti-estrogens. Aromatase inhibitors differ greatly from SERMs in their action and how they deal with the issues of estrogen control. The misunderstanding that SERMs, such as Nolvadex and Clomid, serve to lower estrogen levels must first be addressed before jumping into any further details.
This is a persistent rumor among the anabolic steroid using community that has begun to erode as of late, but the rumor still persists. SERMs serve to block the action of Estrogen at the receptor sites in breast tissue by occupying the receptor sites in place of Estrogen so that Estrogen itself cannot exert its effects there through receptor site binding. Conversely, SERMs will also act as Estrogens at receptor sites at other cells in other areas of the body (the liver, for example in Nolvadex’s case). SERMs do not lower circulating levels of Estrogen in blood plasma. Aromatase inhibitors serve to do this by eliminating the production of Estrogen through binding to and disabling the aromatase enzyme, which is the enzyme responsible for the conversion (or aromatization) of androgens into Estrogen.
Nolvadex is specifically a non-steroidal SERM belonging to the triphenylethylene family of compounds that exhibits both Estrogen agonist and Estrogen antagonistic effects on the body. This means that although Nolvadex might block the effect of Estrogen at the cellular level in certain tissues, it can enhance Estrogenic effects in other areas of the body. These can be positive effects as well as negative effects. Nolva exhibits Estrogenic effects in the liver, for example, which for all intents and purposes is a positive effect, as its effects here result in a positive change in cholesterol profiles (something desired by many). The area of concern with Nolvadex is particularly in breast tissue, where it serves to act as an anti-Estrogen in this area (and a very strong one at that).
This is where it is utilized in medicine, as a first-line treatment in Estrogen-responsive female breast cancer patients. It is even utilized in females that do not possess breast cancer, but are known as being in a high risk category (due to hereditary genetics or otherwise) as a preventative measure. It is through its medical application that one can easily see how such a compound would easily attract the anabolic steroid using bodybuilding and athletic community, as one of the more prominent concerns among anabolic steroid users is that of the Estrogenic effects caused by the use of aromatizable androgens (such as Testosterone, Dianabol, Boldenone, etc.), mores specifically: gynecomastia (the development of breast tissue). If gynecomastia is left unchecked, it can develop and grow beyond a reversible point whereby the only option for removal is that of surgery.
Nolvadex (Tamox) possesses other very desirable effect, such as its ability to increase circulating levels of endogenous gonadotropins Luteinizing Hormone (LH) and Follicle Stimulating Hormone (FSH), and through this, increasing the endogenous production of Testosterone. This is a perfect example of the mixed Estrogen antagonistic and agonistic properties of Nolvadex, where it works to block the ability for Estrogen to bind to receptors at the hypothalamus. This results in the manipulation of the negative feedback loop of the HPTA (Hypothalamic Pituitary Testicular Axis), and results in the increased output of gonadotropins (the hormones that signal the testes to begin or increase the output of Testosterone production). It is for this reason that Nolvadex is considered an absolutely essential component of a PCT (Post Cycle Therapy) program during the weeks following anabolic steroid use in order to restore the function of endogenous Testosterone production. Nolvadex’s effect in these aspects will be further covered in detail in this profile.
Questions NolvadexICI first designed and created Nolvadex (Tamixofen) in 1962, and shortly afterwards was released onto the prescription drug market in the United States. What is interesting is the fact that Nolvadex’s first applications in medicine was for the treatment of female infertility. However, after various clinical testing, Nolvadex was found to be highly effective in the treatment of breast cancer patients in 1971. In 1977, Nolvadex was finally approved by the FDA for the purpose of breast cancer treatment. 1988 was the year in which the FDA further approved the use of Nolvadex as a preventative treatment and measure for individuals with a high potential for the development of breast cancer who have not yet developed it. The rest his history, and Nolvadex and its uses has spread internationally ever since its creation where thousands upon thousands of different brands and generics of Nolvadex have been manufactured and utilized. AstraZenica, however, in 2006 ceased production of the drug in the United States, and while this major brand name is no longer available in America, Nolvadex continues to be utilized as an effective breast cancer medication under different generic brand names.
Chemical Characteristics of Nolvadex
Nolvadex (Tamoxifen) is a non-steroidal selective Estrogen receptor modulator (SERM) that possesses both mixed agonistic as well as antagonistic properties in relation to Estrogen in different areas of the body. Nolvadex belongs to a family of compounds known as triphenylethylene compounds, of which Clomid (Clomiphene Citrate) is also a member of, and a very closely related compound to Nolvadex.
Properties of Nolvadex
It has already been established that Nolvadex, being a SERM, does not reduce circulating Estrogen levels in the body, but instead serves to occupy the receptor sites in breast tissue so that Estrogen itself cannot bind to these receptors due to Nolvadex’s stronger binding strength to it. In layman’s terms, Nolvadex essentially 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 the cells there in order to formulate gynecomastia, and any existing Estrogen that has already bound to receptor sites will essentially be ‘forced’ out of the receptor sites by Nolvadex which then occupies the receptor site instead.
This is very promising news for anabolic steroid using individuals that wish to eliminate and reverse formulating gynecomastia in its early stages, as well as for those individuals very sensitive to the gynecomastia side effect of rising Estrogen levels that might wish to utilize Nolvadex as a preventative measure. This is the primary purpose and function of Nolvadex, and is the primary desired effect that anabolic steroid using bodybuilders and athletes utilize it for. Nolvadex will not serve to block or reduce any other Estrogenic side effects, however, as it serves only to block Estrogenic activity at the breast tissue area (when major Estrogenic side effects are concerned). Nolvadex does not (nor do any SERMs) serve to reduce bloating, water retention, rising blood pressure (as a result of water retention), or acne formation – these are all side effects resultant from increasing blood plasma Estrogen levels.
Nolvadex Side Effects
Nolvadex is a compound that is tolerated quite well by the overwhelming majority of users, though there are some potential side effects to be aware of. Because of the difference in androgen and Estrogen receptor proliferation among cells in the male and female bodies, Nolvadex tends to generate quite different effects and experiences in men versus women. This is why there are greater amounts of negative experiences where Nolvadex side effects are concerned among women than men, but this is a different story in comparison to its use among bodybuilders and athletes using Nolvadex as an ancillary compound surrounding their anabolic steroid use.
The official prescription documentation for Nolvadex side effects in regards to its use as a female breast cancer treatment drug includes: hot flashes, vaginal itching, upset stomach, headaches, dizziness, bone and joint pains, and edema. Lesser and infrequent side effects may include: cholesterol changes, altered white blood cell count, altered platelet count, skin rashes, endometrial changes, deep vein thrombosis, and pulmonary embolism. These are Nolvadex side effects associated with use in females, and are officially documented as evidenced in clinical studies and contained on the pamphlet within the prescription product itself.
The Nolvadex side effects listed above are practically a non-concern for male users, as the overwhelming majority of said side effects are reportedly almost never experienced among men.
There is, however, a persistent and long standing myth that Nolvadex – if utilized with compounds such as Trenbolone or Nandrolone (Deca-Durabolin) – will up-regulate Progesterone receptors and increase their sensitivity to these compounds. Thus, what supposedly results is an increase in Progestin-related side effects from the use of Trenbolone, Deca, or any related 19-nor compounds (due to the fact that they are Progestins in and of themselves). This myth is simply not true.
The origin of this Nolvadex side effect myth is rooted in various studies in the past that have demonstrated that Nolvadex does up-regulate Progesterone receptors – in females. Another piece of the origin to this myth is the fact that several studies in the past have also demonstrated that Nolvadex acts as an Estrogen antagonist in breast tissue, and in doing so, down-regulates the Progesterone receptors as well (this is because Progesterone receptor activity is closely linked with Estrogen receptor activity). These studies demonstrated that this of course occurs in normal healthy humans, but in breast cancer patients it results in an up-regulation of the Progesterone receptor. Unfortunately, many in the bodybuilding community read into these particular studies out of context and made the assumption that all normal healthy humans react the same way. It is not true.
Dosing and Administration of Nolvadex
Medically, Nolvadex (Tamoxifen) is utilized as a medication in the treatment of 6 different types of female breast cancer. The prescription dosing and administration of Nolvadex in these cases call for 10 – 20mg taken twice per day, in the morning and evening respectively.
Nolvadex For Gynecomastia
Within the bodybuilding and performance enhancement world, Nolvadex is primarily and commonly utilized as an ancillary aid to combating, reducing, and/or preventing the development of Gynecomastia. This is normally especially the case when a particularly moderate or aromatizable anabolic steroid is utilized in a cycle. Dosing of Nolvadex in this case is approximately 10 – 30mg per day. The common dosing tends to be 20mg per day of Nolvadex. It is very important to understand that higher and higher dosages of Nolvadex, greater than 20 – 40mg per day, does not produce any greater or faster effect on reducing or preventing gynecomastia, despite common misconceptions.
Nolvadex For Post Cycle Therapy (PCT)
The other primarily utilized purpose for Nolvadex among bodybuilders and athletes is its ability to stimulate and increase the male production of endogenous Testosterone, as evidenced by many studies. It does so by acting on the pituitary and hypothalamus gland in the brain, and signaling an increase in production of FSH (Follicle Stimulating Hormone) and LH (Luteinizing Hormone), which then signal the testes to produce Testosterone. In this case, Nolvadex is usually administered during PCT, which is immediately after the anabolic steroid cycle is complete and all anabolic steroids are clear from the individual’s system.
In this application of administration, 20 – 40mg per day of Nolvadex per day for approximately 4 – 6 weeks. Studies have demonstrated that venturing higher than 20 – 40mg per day does not generate any significantly greater amount of Testosterone production. Nolvadex is also normally included with the administration of at least one or two other Testosterone stimulating compounds during PCT (such as an aromatase inhibitor, usually Aromasin, and/or HCG) in order to enhance its effects on promoting proper HPTA function following the conclusion of a cycle.
The use of Nolvadex during a cycle will not counter-act the Testosterone suppression of anabolic steroid use and will not keep endogenous Testosterone production going amidst the use of suppressive compounds. It is therefore not recommended to do so, as it would be a waste of product and money.
Nolvadex possesses an extremely long half-life for an oral compound, approximately 5 – 7 days, and some studies demonstrating as long as 14 days. There should therefore be no requirement to split dosages up throughout the day, and it is safe to consume with food or on an empty stomach.
Nolvadex Chemical Information:
Tamoxifen Citrate (AKA Nolvadex)
Chemical Name: (Z)-2-[4-(1,2-diphenylbut-1-enyl)phenoxy]-N,N-dimethylethanamine
Molecular Weight: 371.515 g/mol or 563.638 g/mol (citrate salt)
Original Manufacturer: ICI
Half Life: 5 – 7 days (some reports as long as 14 days)
Detection Time: 2 months
Anabolic Rating: N/A
Androgenic Rating: N/A
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