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Exemestane (Aromasin) is a steroidal anti-estrogen aromatase inhibitor used by bodybuilders to combat estrogen related side effects like gynecomastia - male breast development. Such side effects are a common problem with anabolic steroid use and need to be prevented for obvious reasons. Exemestane is an anti-estrogen aromatase inhibitor very similar in structure and action to drugs like Formestane, although it is significantly more potent in comparison.

As a class of drugs, anti-estrogen aromatase inhibitors offer their anti estrogenic effect by blocking the enzyme responsible for synthesizing or converting male hormones like Testosterone into female hormones like Estrogens.

Exemestane (Aromasin) is an approved drug for the treatment of breast cancer in women, specifically in post menopausal patients whose cancer has progressed following therapy with Tamoxifen (nolvadex). Male Bodybuilders and chemically enhanced athletes often use the drug for non approved purposes, namely to counter the estrogenic side-effects associated with the use of certain anabolic steroids. These side-effects caused by higher estrogen levels in men may include gynecomastia (breast growth), fat buildup, and water retention. Exemestane (Aromasin) is one of the most potent aromatase inhibitors presently available. The most commonly cited study reports a lowering of estrogen around 85% on average in clinical studies with women.

Exemestane was developed by Pharmacia & Upjohn, which gained approval for sale of the drug in late 1999. It was introduced under the "Aromasin" brand name in early 2000. Although the drug proved to be effective in doses as low as 2.5mg per day in some patients, the company developed it in a standard and near universally effective dosage of 25mg per tablet. The company has since introduced the drug to many other nations under the same trade name of "Aromasin".

While not quite as strong as Letrozole, Exemestane is considerably stronger than Anastrozole. Typically, one will begin the use of aromasin the same day they begin a steroid cycle.

Of added interest to the bodybuilder when selecting an anti-estrogen aromatase inhibitor, is Aromasin's ability to increase free Testosterone and IGF (Insulin Growth Factor) levels in the body. Because of this, this drug is also very useful during PCT (Post Cycle Therapy) regimes when one is trying to restore natural Testosterone production levels in order to avoid a post cycle "crash". As it is such a powerful anti-estrogen aromatase inhibitor, it is important to keep doses of Aromasin reasonable. You see, too little estrogen can cause its own set of problems and result in hindered muscle gains and the loss of sex drive. One 25mg tablet per day should be sufficient for effectively keeping estrogen related side-effects out of the picture, or for effectively raising natural testosterone levels during Post Cycle Therapy.

Exemestane reaches peak plasma concentrations within 2 hours after taking a 25 mg pill. The active life of the drug is between 24 and 30 hours. This is significant since it is much shorter than the non-steroidal anti-estrogen aromatase inhibitor. A single oral dose of 25 milligrams of Exemestane causes a relatively long-lasting reduction in plasma and urinary Estrogen levels, with maximal suppression occurring approximately 2 to 3 days after dosing and persisting for about 4 to 5 days.

Interestingly, it has been shown that 25 milligrams of Exemestane is basically just as effective as 50 milligrams at suppressing Estrogen so it is therefore unnecessary to go higher in dose than 25 milligrams per day. Exemestane use even when not taking synthetic steroids has been known to cause an increase in natural Testosterone levels, and levels of IGF (Insulin Growth Factor). Due to the active life of the compound Exemestane is usually administered roughly once every 24 hours. Users often start the drug on the first or second week of a steroid cycle and continue to take it throughout the cycle and for a few weeks afterwards in order to prevent any type of estrogen rebound once the steroids are discontinued.

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Here's some links to other EliteFitness.com articles on anti-estrogen aromatase inhibitors:

And here's some threads on the EliteFitness.com Forums for discussions about Exemestane - Aromasin:

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