Arimidex (Anastrozole)

History and Overview of Arimidex

Arimidex belongs to the class of drugs known as AI’s (aromatase inhibitors). Aromatase inhibitors are part of the anti estrogen class of drugs. Selective estrogen receptor modulators, such as Clomid and nolvadex are they other subcategory of anti estrogen drugs. However, it is important to note that anti estrogens greatly differ from selective estrogen receptor modulators.

There is a common misconception that Clomid and Nolvadex are able to effectively control estrogen. Selective estrogen receptor modulators work by blocking estrogens actions in the breast tissues receptor sites. This prevents estrogen from being able to exert its effect via site binding. They also act as estrogen in various cells and receptor sites in the liver and other parts of the body.

Selective estrogen receptor modulators do not reduce the levels of estrogen circulating in blood plasma. When looking at aromatase inhibitors, they work by eliminating estrogen production by binding with and disabling aromatase enzymes. These enzymes are responsible for aromatization of androgens into estrogen.

ARIMIDEX – AstraZeneca

Developed by AstraZeneca, which was formerly known as zeneca Pharmaceuticals Arimidex was originally designed and synthesized for treating advanced breast cancer in female patients. It was released into the prescription drug Market in America after gaining approval by the FDA in 1995. It is a 3rd gen aromatase inhibitor. The estrogen reducing effects of SERMs and AIs have different mechanisms. It is known that estrogen stimulates and accelerates the majority of breast cancers in females.

Typically, Arimidex is used as an adjunct treatment, which is an additional treatment used when standardized treatments fail to work. Before Arimidex was developed, tamoxifen what’s the primary treatment for patients suffering from breast cancer. Nolvadex is typically the standard first line treatment for breast cancer. Should the treatment fail, adjunct treatments such as Arimidex are used.

In 2002, a study of 9000 post surgery breast cancer patients compared its efficiency to nolvadex. The outcome was more favorable for Arimidex. It came to the conclusion that Arimidex was superior to nolvadex when it comes to cancer regression. It also proved to be more effective at increasing the overall rate of survival of post-treatment breast cancer patients. A further study found that Arimidex use reduced the risk of breast cancer reoccuring by 40%.

The results of this study brought Arimidex to the attention of athletes and bodybuilders. It is now considered to be among the most popular AIs used for estrogen control in the steroid using community. The majority of anabolic steroid users who use Arimidex do so to control estrogen related side effects. These include high blood pressure, bloating, water retention and gynecomastia.

Studies have shown that use of the 0.5mg to 1mg of Arimidex in men can reduce the circulating levels of estrogen in blood plasma by up to 50%. While this decrease is considerable, to say the least, in women the decreased is as much as 80%. However, estrogen works differently on male physiology than it does female.

Moving away from the use of Arimidex by steroid using athletes and bodybuilders, it also has medical uses among males suffering with various conditions. One example is when men have extremely high levels of estrogen. This can be caused by one of many reasons. However, regardless of the reason, Arimidex has been successfully used to regulate estrogen levels.

It has also been used for treating adolescent males experiencing abnormally high levels of estrogen during puberty. When estrogen levels are high during puberty, they can lead to the growth of male breast tissue, also known as gynecomastia. Abnormally high levels of estrogen during puberty can also lead to stunted growth. This is down to estrogens action of fusing the growth plates found on the bones. When the growth plates are shut, linear growth is prevented.

Arimidex Chemical Characteristics

When looking at the chemical characteristics of Arimidex, it is classified as an NSAI (non steroidal aromatase inhibitor). In simple terms, this means that Arimidex does not have a 4 ring cyclo alkane carbon structure as is commonly found in all anabolic steroids.

Arimidex Properties & Functions

As little as 1 mg of Arimidex daily can have drastic effects on the control of serum estrogen levels. 1 mg has been shown to suppress estrogen in more than 80% of individuals given it. It inhibits aromatase enzymes so effectively that it is often only prescribed to post menopausal women.

Arimidex is classified as a non suicidal and non steroidal aromatase inhibitor. It binds to the enzyme’s active site by competing with the substrate. This makes it different from aromasin, which is classified as a suicidal and steroidal aromatase inhibitor. Aromasin works by tricking the aromatase enzyme. It then binds to the enzyme and then becomes deactivated due to the strength of the bond. This is a permanent deactivation off the enzyme that aromasin has bound to.

Athletes and bodybuilders who use anabolic steroids will commonly use aromatase inhibitors to eradicate increases of estrogen at the root cause. This makes Arimidex and extremely popular choice. Once the aromatics enzyme has been disabled, androgens that typically aromatize, such as boldenone, Dianabol and testosterone can no longer be converted into estrogen. This eradicates the risk of experiencing side effects that are estrogen related.

Arimidex Side Effects

The majority of men will be able to tolerate Arimidex with little to no side effects. This is due to the fact that Anastrozole is a compound used for control and estrogen levels within the body. With that said, there are certain side effects that may raise concerns. For the most part, this surrounds the reduction of estrogen blood plasma levels in the body. Chronic estrogen suppression is also a concern. Women are affected in a much more significant way than men are.

When dealing with estrogen suppression and reduction, Arimidex works bye disabling aromatase enzymes. Aromatase enzymes are what converts testosterone into estrogen, also known as aromatization. This results in decreased levels of estrogen circulating by targeting it at the root source.

Arimidex has been shown to increase the risk of experiencing a bone fracture in studies. While this is a side effect more likely to be experienced by women, estrogen plays a vital role in the retention and promotion of bone mineral content in men too. Studies have shown that erivery midex has no negative impact on the levels of calcium turnover in bone tissue.

Two of the most commonly experienced side effects when using Arimidex are fatigue and lethargy. As estrogen plays a vital role with regulating the central nervous system, the reduced levels result in periods of chronic fatigue. In the majority of cases, this is a direct result of the levels of estrogen being below what is considered healthy.

As is common with almost all estrogen reducing compounds, Arimidex can have a negative effect on blood cholesterol profiles. It can increase bad cholesterol, also known as LDL while decreasing good cholesterol, also known as HDL. Estrogen promotes optimal levels of healthy cholesterol in the body. When the estrogen blood plasma levels are disrupted, so are the cholesterol levels. This can have a detrimental impact on the cardiovascular system.

Lastly, estrogen rebound is a possibility when using Arimidex. As it is an aromatase inhibitor that is not suicidal, it binds to and disables aromatase enzymes. However, this is not a permanent action. After a certain amount of time, Arimidex detaches from the enzyme allowing it to once again get to work in the body. This can lead to estrogen levels to rebound and is one of the reasons why it is not a good idea to abruptly cease use of the compound.

Typically, those using the recommended dose of Arimidex will not experience side effects. However, they are always a possibility and if an individual experiences them, it is important not to abruptly discontinue use. The amount of Arimidex used should be gradually reduced over a period of 7 to 10 days to prevent estrogen rebound from occurring.

Administration and Dosing of Arimidex

Arimidex is one of several different medical treatments used for breast cancer in postmenopausal women who have developed cancer due to estrogen. Arimidex is prescribed to be taken once each day until the cancer has shown signs of stopping its progression.

When looking at the dosage level of Arimidex for the treatment of postmenopausal breast cancer, a tablet of 1 mg is administered orally one time each day.

A dose of 0.5 mg to 1 mg each day is typically sufficient for athletes and bodybuilders who are using steroids. While it is possible to increase the dose for those who can tolerate it, it is not recommended to do so. The higher the dose is, the more likely the individual is to experience unwanted side effects.

On-Cycle Estrogen and Gynecomastia Control

On cycle estrogen and gynecomastia control can be achieved with between 0.5 to 1 mg of Arimidex each day. The total dosing amount can be adjusted as per the individuals reaction and tolerance to the compound.

No two people are the same and responses may vary. For some people, 0.5 mg of Arimidex each day may prove to be insufficient. On the flip side of the coin, others may find this to be too much. It is important to remember that Arimidex for estrogen control should do just that. It is not intended for complete elimination of estrogen during a cycle.

Arimidex for PCT

Studies have shown that Arimidex is able to assist with generating natural testosterone in men. For the majority of people, a dosage range of between 0.5 mg to 1 mg each day is typically more than sufficient throughout the duration of all Post Cycle Therapy (PCT) lengths.

The half-life of Arimidex is approximately 48 hours. It will take 7 days of consistent use before peak levels of blood plasma are achieved. When using Arimidex for PCT, it can be taken day or night and with or without a meal.

Arimidex Availability and Legality

In the United States, United Kingdom and Canada, Arimidex is available with a genuine doctor’s prescription only. While a prescription is required in these countries, it is currently not classified as a controlled substance. This makes it perfectly legal to possess, purchase or own Arimidex in any of these countries.

Other countries around the world, including the Middle East, Asia and Eastern Europe, Arimidex can typically be purchased over the counter and without the need for a prescription. In most countries, it is classified as an uncontrolled substance thus making it perfectly legal to purchase, possess and use.

How to Buy Arimidex Online

Out of Aromasin, Letrozole and Arimidex, Arimidex is by far the most popular of the three aromatase inhibitors and anti estrogen. This makes it an extremely popular compound commonly used among athletes and bodybuilders using various anabolic steroids. It is because of its popularity that it is typically easy to find available for purchase.

The majority of online anabolic retailers should have Arimidex as part of their inventory. It is also important to note that Arimidex is not cheap by any means. In fact, it is among the most expensive compound in its class to purchase. Arimidex is available as research chemical grade, underground laboratory grade, and pharmaceutical grade. Depending on the grade that you purchase, the price, quality and consistency can vary drastically.

As a general guideline, research grade Arimidex typically comes in liquid form and a 30 milliliter container can be priced anywhere between $40 and $70. Underground laboratory grade Arimidex is more often manufactured as a 1 mg tablet. You can expect to pay anywhere between $1.40 to $8 per tablet. Lastly, pharmaceutical grade tablets 1mg typically cost between $6 to $12 per tablet.

When purchasing Arimidex online, it is important to know whether it is legal to purchase and import the compound into your country of residence. You should also only purchase Arimidex from a reputable online retailer and avoid sites that advertises prices that are too good to be true.

References & Medical Data

[1] Preclinical pharmacology of “Arimidex” (anastrozole; ZD1 033)–a potent, selective aromatase inhibitor. J Steroid Biochem Mol Bioi 1996 Jul;58(4):439-45.

[2] Anastrozole alone or in combimation with tamoxifen versus tamoxifen alone for adjunctive treatment of postmenopausal women with early breast cancer. Frist results of the ATAC randomized trial. Lancet 2002; 359:2131-39.

[3] History and Advancement of Anastrozole in the Treatment of Breast Cancer. Edited by Aman Buzdar &Michael Baum. RSM Press, February 2003.

[4] “Switching of postmenopausal women with endocrine-responsive early breast cancer to anastrozole after 2 years’ adjuvant tamoxifen: combined results of ABCSG trial 8 and ARNO 95 trial”. Jakesz R, Jonat W, Gnant M, Mittlboeck M, Greil R, Tausch C, Hilfrich J, Kwasny W, Menzel C, Samonigg H, Seifert M, Gademann G, Kaufmann M, Wolfgang J (2005). Lancet 366 (9484): 455–62. doi:10.1016/S0140-6736(05)67059-6. PMID 16084253.

[5]  “Effects of aromatase inhibition in elderly men with low or borderline-low serum testosterone levels”. Leder BZ, Rohrer JL, Rubin SD, Gallo J, Longcope C (March 2004). J. Clin. Endocrinol. Metab. 89 (3): 1174–80. doi:10.1210/jc.2003-031467. PMID 15001605.

[6] “Estrogen suppression in males: metabolic effects”. Mauras N, O’Brien KO, Klein KO, Hayes V (July 2000). J. Clin. Endocrinol. Metab. 85.

(7): 2370–7. doi:10.1210/jc.85.7.2370. PMID 10902781.; Dougherty RH, Rohrer JL, Hayden D, Rubin SD, Leder BZ (February 2005). “Effect of aromatase inhibition on lipids and inflammatory markers of cardiovascular disease in elderly men with low testosterone levels”. Clin. Endocrinol. (Oxf) 62 (2): 228–35. doi:10.1111/j.1365-2265.2005.02205.x. PMID 15670201.

[8 “Delayed closure of epiphyseal cartilages induced by the aromatase inhibitor anastrozole. Would it help short children grow up?”. Faglia G, Arosio M, Porretti S (December 2000). J. Endocrinol. Invest. 23 (11): 721–3. PMID 11194703.

[9] “Pharmacokinetics and pharmacodynamics of anastrozole in pubertal boys with recent-onset gynecomastia”. Mauras N, Bishop K, Merinbaum D, Emeribe U, Agbo F, Lowe E (August 2009). J. Clin. Endocrinol. Metab. 94 (8): 2975–8. doi:10.1210/jc.2008-2527. PMID 19470631.

[10] “Delayed closure of epiphyseal cartilages induced by the aromatase inhibitor anastrozole. Would it help short children grow up?”. Faglia G, Arosio M, Porretti S (December 2000). J. Endocrinol. Invest. 23 (11): 721–3. PMID 11194703.

[11] “Anastrozole increases predicted adult height of short adolescent males treated with growth hormone: a randomized, placebo-controlled, multicenter trial for one to three years”. Mauras N, Gonzalez de Pijem L, Hsiang HY, Desrosiers P, Rapaport R, Schwartz ID, Klein KO, Singh RJ, Miyamoto A, Bishop K (March 2008). J. Clin. Endocrinol. Metab. 93 (3): 823–31. doi:10.1210/jc.2007-1559. PMC 2266949. PMID 18165285.