exemestane mechanism of action
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Exemestane Mechanism of Action

Exemestane is a steroid Aromatase Inhibitor (IA), best known as Aromasin. In fact, the name “Aromasin” is the pharmaceutical name Exemestane, according to the patented name of the drug company “Upjohn”. But, even under the strict control of the pharmaceutical giant, the drug is available worldwide.

When using the drug for medical purposes, it deprives cancer cells necessary for their life “recharge” estrogen. The effectiveness of using Aromasin for these purposes, no doubt. However, it is recommended to use Tamoxifen first. If this drug does not give positive results, you should start using Exemestane.

However, even with high efficiency, this drug is used in medicine less often than Anastrozole. This is due to the fact that Arimidex behaves in many ways similar to the primary aromatase inhibitor. And it happens not only in the treatment of breast cancer after menopause, but also during the treatment of other cancer diseases.

Mechanism of Exemestane to Suppress Side Effects

However, we are more interested in the mechanism of action of Exemestane in relation to the suppression of the negative effects of anabolic steroids. Having got acquainted with the properties and effects of the drug, it is already possible to draw certain conclusions in this matter. It is important to remember that when using steroids, side effects of the estrogen type may not occur.

If we talk specifically about estrogenic side effects, then for their development, steroids used by an athlete must have the ability to aromatize or progestogenic activity. Primary aromatizers steroid is Testosterone. However, drugs based on derivatives of this hormone substances can enhance the work of estrogen. A striking example here can be Methandienone.

Also such steroids include Boldenone Undecylenate, whose ability to aromatize is 50 percent of the Testosterone. This is not enough for a rapid increase in the concentration of female hormones. Among the steroids that can cause estrogenic side effects are still Trenbolone and Nandrolone. They are slightly flavored, but have a strong progestogenic activity.

This may be enough to allow the level of female hormones to exceed normal limits. This largely depends on the genetic characteristics of the organism. Trenbolone is not able to interact with the enzyme aromatase, however, due to the high progestogenic activity, the development of gynecomastia is possible. This happens again, with the genetic predisposition of the athlete. If these drugs are used in conjunction with aromatizing steroids, the risks of estrogen-type side effects increase.

Regardless of the steroid used, Exemestane is able to protect you from side effects. In sports, steroids are actively used, which are based on substances derived from dihydrotestosterone. They are in principle not able to aromatisiertes. An exception to this rule is Oxymetholone, which is inherent in estrogen activity. However, it is not able to aromatize and in cycle of Oxymetholone, Aromasin will not be effective.

exemestane mechanism

Mechanism of Action when Using Exemestane in Bodybuilding

And now consider the mechanism of action of the aromatase inhibitor, which are manifested when using Exemestane in bodybuilding after a steroid cycle. You should know that on a steroid cycle the process of synthesis of endogenous male hormone is suppressed. The extent of this negative effect of steroids depends on the drugs used and their dosages. However, even the lightest drug can adversely affect the operation of the pituitary axis.

After completing the anabolic cycle, the body will begin to synthesize testosterone again, but only after all exogenous hormones are utilized. This will require a long time period. Much depends on the characteristics of the athlete and in the worst case may take about a year. It is obvious that such a situation is unacceptable. PCT is carried out in order to accelerate the secretion of endogenous male hormone.

In itself, the state of low testosterone is abnormal, but there are additional negative moments. In particular, increases the level of cortisol that destroys muscles, as well as falling libido. We have already noted that Exemestane is able to accelerate the synthesis of testosterone.

At the same time, the drug is characterized by low androgenic activity, and it accelerates the secretion of insulin-like growth factor. All this leads to the fact that some athletes begin to use Exemestane in bodybuilding after a steroid cycle. At the same time they forget about the main purpose of this drug — the inhibition of the enzyme aromatase.

There is no doubt that the high concentration of estrogen leads to undesirable consequences for men. But the balance between male and female hormones is also extremely important. Scientists have proved that estradiol regulates the balance of lipoprotein compounds, normalizes the body’s defense mechanisms and affects the libido. The main objective of Post Cycle Therapy after steroid cycles is to stimulate the secretion of testosterone. But it is important to remember about the normalization of all body systems. If you strongly suppress the estrogen levels, to achieve the impossible. That is why we do not recommend using Exemestane in bodybuilding after a steroid cycle. The drug can be most useful during the cycle, but not after its completion.

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