Powder Anastrozole (arimidex)

Description

Arimidex is an aromatase inhibitor developed by Zeneca Pharmaceuticals (now AstraZeneca) that was originally synthesized and designed for the treatment of female patients suffering from advanced breast cancer. It was approved for use by the FDA and released onto the American prescription drug market in 1995. Arimidex is regarded as one of the newer aromatase inhibitors, known as a third generation aromatase inhibitor[1]. The reason as to why both aromatase inhibitors and SERMs act to block Estrogen's effects in different manners is because it has been found that the vast majority of breast cancers are stimulated and accelerated by Estrogen.

Arimidex is used among breast cancer treatments as what is known as an adjunct treatment. This usually refers to an additional treatment when other standard treatments have failed to meet proper expectations. Prior to the development and release of Arimidex as a breast cancer treatment medication, the primary medication utilized for treatment for decades prior was Nolvadex (Tamoxifen). Nolvadex is considered to be utilized as the first and standard treatment for breast cancer patients. When Nolvadex treatment,for one reason or another, fails to meet expectations during breast cancer treatment, second-line adjunct drugs such as Arimidex are utilized.

One such study on Arimidex on over 9,000 post-surgery female breast cancer patients observed its efficiency in comparison to Nolvadex (both alone as well as both utilized simultaneously), resulting in far more favorable outcomes for Arimidex over Nolvadex. The study, which was performed in 2002, concluded that Arimidex was far more effective at cancer regression, as well as increasing the survival rate of the breast cancer patients following treatment. It was then this study (as well as others) that then of course prompted individuals among the anabolic steroid using community to take notice of it and begin investigating the benefits of its effects on strong Estrogen levels suppression. A study conducted later on demonstrated that the risk of recurrence of breast cancer was eliminated by 40% with Arimidex use, but the patients experienced an increase in bone fractures. This is because Estrogen plays a central role in the proper maintenance of bone and its mineral retention, and this will become significantly reduced following the vast reduction of Estrogen levels resultant of Arimidex administration.

Because Arimidex was the very first aromatase inhibitor for many bodybuilders to have taken notice of, it is the most popular aromatase inhibitor used among anabolic steroid users for the purpose of Estrogen control. The use among anabolic steroid using athletes is for the control of almost all Estrogen-related side effects: the manifestation of gynecomastia, water retention and bloating, rising blood pressure (as a result of water retention increases from Estrogen). This is in contrast with SERMs such as Nolvadex, which only serve to block gynecomastia. Studies have in fact demonstrated that Arimidex use in males has been effective enough to reduce circulating blood plasma levels of Estrogen by 50% at only a dose of 0.5 – 1mg daily. This is a very considerable decrease in men, but can be seen as quite different from the 80% reduction in female breast cancer patients, but it must be remembered that Estrogen and how it relates to the female physiology is different from males.

Aside from the use in bodybuilders, Arimidex has also been medically used in males as well. Some males exhibit abnormally high Estrogen levels of many different reasons and Arimidex has been utilized in order to combat these ailments. In particular, Arimidex has been used to treat male adolescents that exhibit excessive Estrogen levels during purberty, resulting in unwanted pubertal gynecomastia. In addition, excessive Estrogen levels in adolescent males during puberty can often result in stunted growth due to the fact that Estrogen plays a key role in fusing the growth plates of the bones shut, preventing any further linear growth, and Arimidex has also been used to treat these conditions as well.

Properties of Arimidex

Arimidex's effects on serum Estrogen level control can be quite drastic even at a dose of 1mg daily. The amount of Estrogen suppression resulting from this dose has been demonstrated to be over 80% in patients. Arimidex can be so effective at inhibiting the aromatase enzyme and thereby reducing Estrogen levels that this compound is typically only administered to post-menopausal females, and/or utilized when other first-line treatments for breast cancer has failed.

Arimidex and Letrozole are both classified as non-steroidal and non-suicidal aromatase inhibitors that compete with the substrate for binding to the enzyme active site. This is very different from Aromasin (Exemestane), which is a steroidal and suicidal aromatase inhibitor that acts as a mechanism-based steroidal inhibitor that mimics the substrate, is converted by the enzyme to a reactive intermediate, and results in the inactivation of the aromatase enzyme . For ease of understanding, what this means to the layman is that Aromasin's chemical structure resembles the traditional 'targets' that aromatase binds to (Testosterone, for example) and that it essentially 'fools' the aromatase enzyme into binding with it, only to become inhibited/deactivated. Because the binding strength is so great, this inhibition becomes permanent for the aromatase enzyme that Aromasin has become bound to. Arimidex and Letrozole, being non-suicidal aromatase inhibitors, both compete with the enzyme's traditional 'targets' rather than being assured a permanent spot (which is the advantage that Aromasin has over the other two).

Bodybuilders and athletes utilizing anabolic steroids will usually favor aromatase inhibitors such as Arimidex for its ability to eliminate rising Estrogen levels at its root cause: aromatase. By disabling the aromatase enzyme, supraphysiological levels of aromatizable androgens (such as Testosterone, Dianabol, Boldenone, etc.) cannot convert into Estrogen, thereby eliminating any possible risk of Estrogen-related side effects.

Effects of Arimidex

As an anti-estrogen, Arimidex is valuable to the breast cancer patient as many forms of breast cancer feed off of the estrogen hormone. While perhaps an oversimplification, by administering Arimidex the effect starves the cancer. For decades Nolvadex was used for this purpose. Nolvadex has the ability to bind to the estrogen receptors, which in turn prevents estrogen from binding. However, AI's like Arimidex actively inhibit the production of estrogen and reduce the actual amount of circulating hormone. In short, there is no estrogen available to cause damage to the breast cancer patient. In recent years, Arimidex has become the leading anti-estrogen in the treatment of hormone receptor-positive breast cancer, especially among post-menopausal women. Once the cancer has subsided, it is not uncommon for Nolvadex to be introduced in order to keep the cancer at bay.

For the anabolic steroid user, the effects of Arimidex are greatly appreciated in its ability to protect against estrogenic related side effects. Many anabolic steroids have the ability to promote estrogenic side effects due to the testosterone hormone's interaction with the aromatase enzyme. As aromatization occurs, estrogen levels rise and this can lead to gynecomastia and excess water retention. When excess water retention becomes severe, this can also promote high blood pressure. Not all anabolic steroids aromatize, and as such, not all can lead to estrogenic related effects. However, many common steroids do carry the ability to promote estrogenic activity including Dianabol, all forms of Nandrolone and Boldenone to a degree and of course, all forms of testosterone heavily.

By including Arimidex in an anabolic steroid cycle that contains aromatizing steroids, the individual can protect against gynecomastia and water retention. This will also protect against high blood pressure. Some steroids can still cause high blood pressure without water retention, but heavy excess water retention is the number one culprit of high blood pressure among anabolic steroid users. Without question, AI's like Arimidex are the most effective anti-estrogens for combating estrogenic related side effects. SERM's like Nolvadex can also be useful and while not as effective should be the first choice when possible. Arimidex has the ability to negatively affect cholesterol as we will see in the side effects section. However, we will also find cholesterol issues can be avoided.

As a testosterone stimulating compound, Arimidex can be appealing for low testosterone treatment plans and for Post Cycle Therapy (PCT) for anabolic steroid users. In the case of low testosterone treatment, it's often not enough. However, it can still be beneficial in conjunction with exogenous testosterone therapy in protecting against estrogenic side effects. As for PCT use, some will attempt it and it can have a positive effect, but it is generally not recommended. The main purpose of a PCT plan is to stimulate natural testosterone production in order to protect lean muscle tissue, keep body fat under control and promote a better state of health. However, the overall purpose is normalization, which cannot be reached when using Arimidex post cycle due to the tremendous estrogen reduction. Although high levels of estrogen can be problematic, some is necessary to proper bodily function, especially regarding the immune system and cardiovascular health. For the anabolic steroid user, AI's should be saved for on cycle use with SERM's being used for PCT.

Arimidex Side Effects

Being that Arimidex (Anastrozole) is an ancillary compound for the purpose of Estrogen control within the body, it is a compound that is generally well tolerated by male users. There are, however, some Arimidex side effects to be concerned about. This primarily exists in the form of excess reduction of blood plasma levels of Estrogen in the body, as well as long-term Estrogen suppression. Arimidex does affect females in a far greater and significant manner than it does in male users as well.

When it comes to Estrogen reduction and suppression, it must be understood that unlike SERMs (Selective Estrogen Receptor Modulators) such as Nolvadex or Clomid (Clomiphene Citrate), Arimidex belongs to the family of aromatase inhibitors. This means that it serves to disable the aromatase enzyme, which is responsible for the aromatization – or, conversion – of Testosterone into Estrogen. In other words, Arimidex reduces total circulating Estrogen levels at the root source as opposed to SERMs, which serve to merely block the activity of Estrogen at select receptor sites.

Studies have demonstrated that Arimidex use results in the increased incidence and probability of experiencing bone fractures. Although this is a more female-specific side effect of Arimidex use, Estrogen does play an important role in the promotion and retention of bone mineral content in males as well. There have been studies conducted that discovered that Arimidex does negatively impact calcium turnover levels in bone tissue with even short term use.

Lethargy and fatigue is commonly associated with Arimidex use. As with nearly all Estrogen reduction compounds, a reduction in circulating Estrogen levels means that the important role that Estrogen plays in the CNS (Central Nervous System) is reduced, thus resulting in possible instances of chronic fatigue. This is usually the result of Estrogen levels being reduced to levels that are considered far too low to be healthy.

One particularly prominent side effect of Arimidex use is the negative impact on blood cholesterol profiles. As with nearly all Estrogen reducing compounds, Arimidex will also decrease HDL (good) cholesterol and increase LDL (bad cholesterol). This is because Estrogen is responsible for the promotion of healthy cholesterol levels in the body, and a disruption of normal blood plasma levels of Estrogen will indeed throw that off. Of course, it also goes without saying that the more severe reduction of Estrogen, the more severe the cardiovascular impacts will be in this area.

One Arimidex side effect of importance is the possibility of Estrogen rebound. This exists in particular with two of the three most popular aromatase inhibitors (Arimidex and Letrozole). The third aromatase inhibitor, Aromasin (Exemestane) does not share this same attribute of the possibility of Estrogen rebound. This is because unlike Aromasin, Arimidex is a non-suicidal aromatase inhibitor. This means that Arimidex will bind with and disable the aromatase enzyme, but it does not do it permanently. At some point, Arimidex will dissociate with the enzyme and the enzyme will then be free to do its job again in the body. What this means for the end user is the risk of a rebound of Estrogen levels (and thus, Estrogen related side effects) if Arimidex use is halted too soon or abruptly after beginning use.

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