Aromasin (Exemestane)

 

Overview and History of Aromasin

When it comes to the class of drugs called aromatase inhibitors (AIs), Aromasin belongs to this category. Aromatase inhibitors are themselves part of the anti estrogen class of drugs. There is a second subcategory of anti estrogen, which are known as selective estrogen receptor modulators or SERMs for short. While Aromasin, which is the brand name for Exemestane, is an anti estrogen, the difference between the two subcategories and how they control estrogen varies dramatically.

Throughout the anabolic steroid using athletic and bodybuilding communities, there has been the misconception that selective estrogen receptor modulators (SERMs), such as Clomid and Nolvadex work by lowering estrogen levels. This has resulted in individuals misunderstanding the difference between estrogen elimination and estrogen blocking. In reality, selective estrogen receptor modulators only serve to block estrogens activity in specific bodily tissues by blocking estrogens action in breast tissue receptor sites. They do this by occupying the sites so that estrogen is unable to exert effects via receptor site binding.

Selective estrogen receptor modulators also mimic estrogen throughout other cells in the body. These include cells found in the liver and is where the selective part of SERMs becomes apparent. However, they do not possess the ability to be able to reduce the levels of estrogen found circulating in blood plasma. On the flip side of the coin, aromatase inhibitors are able to eliminate estrogen production by binding to the aromatase enzyme and disabling it. Aromatase enzymes are responsible for aromatization of androgens, which are converted into estrogen.

Aromasin is a potent suicidal steroidal aromatase inhibitor. Prescription packaging of Aromasin states that it is able to decrease the levels of estrogen by up to 85% as shown in studies on patients suffering from breast cancer. Being a suicidal aromatase inhibitor, it permanently disables aromatase enzymes when binding to them. However, the body will manufacture more enzymes, but as the currently bound enzymes are disabled permanently, there is no risk of estrogen rebound from occurring.

This is where Aromasin differs from too other Aromatase Inhibitors, Letrozole (Femera) and Arimidex. Letrozole and Arimidex are both not suicidal AIs that only temporarily disabled aromatase enzymes. Should Letrozole or Arimidex be ceased abruptly, any aromatase enzymes that are inhibited but have yet to be metabolized will once again become free. This can result in the aromatization of androgens into estrogen at an increased rate.

Initially designed for treating female breast cancer, 1999 saw Exemestane gain FDA approval for the prescription drug market. Since 2000, it has been marketed and sold as Aromasin. It is currently used in nearly every country worldwide, and Aromasin comes in a standard dose of 25 mg. However, research has shown it to be effective with doses as low as 2.5 mg a day.

Aromasin 25mg Capsules – Pfizer

Unsurprisingly, Aromasin caught the attention of anabolic steroid using bodybuilders and athletes as a means of controlling estrogen levels. It gained popularity due to its effects of controlling side effects related to estrogen, such as water retention, gynecomastia, high blood pressure and bloating. It has been shown to improve the levels of natural testosterone production in males. Although Aromasin is often considered to be superior and its effectiveness to Arimidex. Arimidex is still the most popular choice among anabolic steroid users due to its availability.

Aromasin offers several advantages not found with other aromatase Inhibitors, these include the stimulation and increase of igf-1, suicide inhibition and a reduced negative impact on the levels of cholesterol in the body. This separates it from many other aromatase inhibitors available on the market, including Arimidex.

Properties and Actions of Aromasin

Being a steroidal suicidal AI, Aromasin possesses a carbon structure consisting of 4 ring cycloalkane. This is common for all molecules of a steroidal structure. As a steroidal aromatase inhibitor, it binds permanently to aromatase enzymes. Aromatase enzymes are attracted to Androgen structures, where it is aromatized into estrogen. Aromasin effectively tricks aromatase enzymes to bind with it, where they become permanently disabled. The strength of the binding is so great, the bond deactivates it, preventing any risks of estrogen rebound from occurring should the compound be immediately halted.

Aromasin has been proven to possess potent effects at a dose of 25 mg a day. These effects reduce the levels of serum circulating estrogen in the body by as much as 85%. It is commonly used as a second line treatment for breast cancer and is so effective at reducing estrogen levels and inhibiting aromatase enzymes, that, like Arimidex, it is only ever prescribed to females who are postmenopausal or when other first line breast cancer treatments have failed. This is down to the fact that females who are postmenopausal possess different endocrine functions and hormone levels when compared to women who are premenopausal.

Individuals, bodybuilders and athletes who use anabolic steroids will appreciate AIs, such as Aromasin doe to their strong effect in avoiding, medicating and reducing side effects of an estrogenic nature. Side effects occur because of aromatization of androgens into estrogen. This often leads to elevated levels of estrogen in the body. Aromasin prevent this from occurring by dealing with estrogen at its root cause. By disabling aromatase enzymes, the levels of supraphysiological androgens of an aromatase Isabel nature are unable to be converted into estrogen. Therefore, any side effects associated with estrogen are eliminated.

Side Effects of Aromasin

The majority of individuals will not experience any side effects when using Aromasin. However, that is not to say that side effects are not a possibility and there are certain side effects that raise concerns. Typically, these are a direct result of estrogen levels being reduced to quickly or two levels that are too low. They can also occur if the suppression of estrogen goes on for an extended period of time. It should also be noted that Aromasin presents with more side effects for females than it does for males.

One of the more common side effects that is often encountered is bone or joint pain. This is down to the fact that estrogen helps maintain bone density and mineralization in bone tissue. While this is common with all aromatase inhibitors, Aromasin has actually demonstrated and ability to strengthen bone tissue.

Another frequently experienced side effect is fatigue and lethargy. This is a commonly reported side effect of all types of aromatase inhibitors. As estrogen plays a vital role in maintaining the CNS, when levels begin to go below normal levels, chronic fatigue can be experienced. Typically, allowing estrogen levels to return to normal should help eradicate this side effect.

Cholesterol changes with a negative impact are a risk that can be experienced with any aromatase inhibitor. Aromasin is not the exception to the rule period as estrogen plays a pivotal role in maintaining and managing cholesterol health, reduced cholesterol levels can have negative impacts on the HDL and LDL values. However, studies have shown Aromasin to possess less of a negative impact on cholesterol levels than other AIs. Risks are still a possibility, therefore it is important to have regular blood work and check ups.

Aromasin possesses a unique side effect. This is the possibility of experiencing side effects of an androgenic nature. It is believed that this is down to Aromasin possessing a structure similar to androgenic steroids. This can lead to side effects such as male pattern baldness, increases of body and facial hir growth, and oily skin. Mood changes, such as aggression can also be experienced from using Aromasin.

Administration and Dosing of Aromasin

Aromasin is used for treating breast cancer in postmenopausal patients and is used as a second line treatment when first line treatment fail. For the years as a cancer treatment, it is given as a 25 milligram dose each day. It is also recommended to take aromasin after consuming food.

Aromasin ‘on cycle’ Estrogen and Gynecomastia

To control estrogen levels during an anabolic steroid cycle and treat gynecomastia, the typical dose of Aromasin range is between 12.5 to 25 mg each day. Certain anabolic steroid users choose to use 12.5 mg every other day, but this depends on the type of anabolic steroid being used, along with the dosage levels of it.

The majority of people keep Aromasin to hand but choose not to use it until they start experiencing estrogen related side effects. In situations such as these, 25 mg is typically taken until side effects disappear. This is followed on by reducing the dosage to 12.5 mg each day, and then 12.5 mg every other day.

Using Aromasin for PCT

As Aromasin has been shown to increase the levels of natural testosterone in men, 25 mg a day for approximately a fortnight can see testosterone levels boosted by up to 60%. With a half-life of 27 hours, it can be taken throughout the day. However, it is recommended to take Aromasin with food for improved absorption.

It should also be noted that it takes 7 days for blood plasma levels to reach their peak. When using Aromasin, it should be remembered that it is used to reduce estrogen levels, not completely eliminate them. If estrogen levels cannot be properly controlled, the use of aromasin should be ceased. Dramatic reductions of estrogen can lead to the onset of adverse side effects while having a negative impact on muscle gains over the long term.

Availability and Legality of Aromasin

In Canada, the United States and the United Kingdom, it is legal to purchase, possess and own Aromasin. However, it is not available over the counter in these countries and can only be obtained with a valid and genuine doctor’s prescription. In countries throughout Eastern Europe, the Middle East and Asia, Aromasin is available over the counter and does not require a prescription to purchase it.

It tends to be widely available. However, it is currently deemed to be less popular than other AIs, such as Letrozole. This is most likely due to the fact that Aromasin didn’t gain the attention of the anabolic steroid users and bodybuilding communities until a much later date.

Buying Aromasin Online & Costs

When it comes to the three main aromatase inhibitors, Letrozole, Arimidex and Aromasin, Aromasin tends to be the least popular. However, it is still extremely popular for use as and anti estrogen for those looking to experience fewer side effects when performing a cycle. The majority of anabolic steroid websites, sources and dealers have Aromasin in their product lineup. There are lots of different brands and grades available. These can be found as pharmaceutical grade Aromasin to underground laboratory grade compound. The actual price will largely depend on the brand, quality and availability of Aromasin and this can vary dramatically between different retailers and online sources.

As is typical with all medications and compounds, pharmaceutical grade Aromasin attracts a much higher price tag than underground laboratory grade Aromasin. It can also be obtained as research chemical grade compound. This is typically available as a liquid form compound. When purchased via the black market, the price of Aromasin can vary. 1 x 25 mg Aromasin tablet from an underground laboratory typically costs between $1.45 to $5. 1 x 25 mg aAomasin tablet of a pharmaceutical grade will cost between $5 to $10 period when looking at research grade compounds, a 30 ml bottle is priced between $30 to $70 and contains 25 mg per milliliter.

It is always recommended to purchase Aromasin and other aromatase inhibitors from a reputable retailer or online source. Avoid purchasing any compounds that appear to be priced within a range that is too good to be true. It is an unfortunate fact that the internet is filled with unscrupulous sellers only out for your hard-earned money. Spend a little bit of time researching the retailer and check-out any customer reviews. Finally, you should be aware of any import laws for your country. While the compound may be perfectly legal, importing chemical compounds and substances may require a license or prescription to do so.

References & Medical Data:

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[3] Update on the use of aromatase inhibitors in breast cancer. Brueggemeier RW. Expert Opin Pharmacother. 2006 Oct;7(14):1919-30.

[4] Pharmacokinetics and dose finding of a potent aromatase inhibitor, aromasin (exemestane), in young males. Mauras N, Lima J, Patel D, Rini A, di Salle E, Kwok A, Lippe B. J Clin Endocrinol Metab. 2003 Dec;88(12):5951-6.

[5] No adverse impact on serum lipids of the irreversible aromatase inactivator Aromasin [Exemestane (E)] in first-line treatment of metastatic breast cancer (MBC): companion study to a European Organization of Research and Treatment of Cancer (Breast Group) Trial with Pharmacia Upjohn. Lohrisch C., Paridaens R., Dirix L. Y., Beex M., Nooij M., Cameron D. Proc. Am. Soc. Clin. Oncol., 20: 43a 2001.

[6] Plasma changes in breast cancer patients during endocrine therapy: lipid measurements and nuclear magnetic resonance (NMR) spectroscopy. Engan T., Krane J., Johannessen D. C., Kvinnsland S. Breast Cancer Res. Treat., 36: 287-297, 1995.

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[8] Inhibitory effect of combined treatment with the aromatase inhibitor exemestane and tamoxifen on DMBA-induced mammary tumors in rats. Zaccheo T, Giudici D, Di Salle E. J Steroid Biochem Mol Biol. 1993 Mar;44(4-6):677-80.

[9] Tamoxifen reduces serum insulin-like growth factor I (IGF-I). Michael N. Pollak MD, Hung The Huynh PhD, Susan Pratt Lefebvre BSc. Breast Cancer Research and Treatment 1992, Volume 22, Issue 1, pp 91-100.

[10] Pharmacology and pharmacokinetics of the newer generation aromatase inhibitors. Buzdar AU. Clin Cancer Res. 2003 Jan;9(1 Pt 2):468S-72S.

[11] Effects of the Steroidal Aromatase Inhibitor Exemestane and the Nonsteroidal Aromatase Inhibitor Letrozole on Bone and Lipid Metabolism in Ovariectomized Rats. Paul E. Goss1, Shangle Qi, Angela M. Cheung, Haiqing Hu, Maria Mendes, and Kenneth P. H. Pritzker. Clin Cancer Res September 1, 2004 10; 5717.

[12] Testosterone dose-response relationships in healthy young men. Bhasin S, Woodhouse L. et al. Am J Physiol Endocrinol Metab 281:E1172-81, 2001

[13] The minimal effective exemestane dose for endocrine activity in advanced breast cancer. Bajetta E., Zilembo N., Noberasco C., Martinetti A., Mariani L., Ferrari L., Buzzoni R., Greco M., Bartoli C., Spagnoli I., Danesini G. M., Artale S., Paolini J. Eur. J. Cancer, 33: 587-591, 1997.

[14] Risks and benefits of aromatase inhibitors in postmenopausal breast cancer. Michaud L. B., Buzdar A. U. Drug Saf., 21: 297-309, 1999.

[15] Exemestane’s 17-hydroxylated metabolite exerts biological effects as an androgen. Eric A. Ariazi, Andrei Leitão, Tudor I. Oprea, Bin Chen, Teresa Louis, Anne Marie Bertucci, Catherine G.N. Sharma, Shaun D. Gill, Helen R. Kim, Heather A. Shupp, Jennifer R. Pyle, Alexis Madrack, Anne L. Donato, Dong Cheng, James R. Paige and V. Craig Jordan. Mol Cancer Ther November 2007 6; 2817