Anastrozole (Arimidex) 1 mg 30 tabs Generic
Information about the drug
Arimidex belongs to a category and class of drugs known as aromatase inhibitors (AIs). Aromatase inhibitors belong to an even broader class of drugs known as anti-estrogens. The other subcategory of drugs under the anti-estrogen category is known as selective estrogen receptor modulators (SERMs), such as Nolvadex and Clomid. 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. 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 Estrogen 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 by binding to and disabling the aromatase enzyme, which is the enzyme responsible for the conversion (or aromatization) of androgens into Estrogen.
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. The reason why both aromatase inhibitors and SERMs act to block Estrogen’s effects in different manners is that 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.
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 have 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's 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 their 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.