Aromasin (Exemestane)

exemever-exemestane-aromasin
exemever-exemestane-aromasin

Exemever [Aromasin] (Exemestane) SC VERMODJE SRL (Moldova)
ANTI-ESTROGEN
POST CYCLE THERAPY

Introduction

Exemestane (Aromasin) is a third generation aromatase inhibitor. In medical practiceExemestane is used as a treatment for breast cancer in postmenopausal women. In sports it is popular among athletes for its ability to suppress estrogenic side effects of AAS.

Its mechanism of action is similar to other aromatase inhibitors, such as Letrozole and Arimidex (Anastrozole). However, unlike them, athletes often use Exemestane after steroid cycle.

Since many AAS are prone to aromatization (i.e. conversion into female hormones) it leads to estrogen related side effects. They include water retention and gynecomastia. The latter is probably the worst of them. As to the water retention, it may significantly increase blood pressure.

One should remember that non-aromatizable steroids may also cause estrogenic side-effects if they have progestogenic activity. For instance, Nandrolone Decanoate has 5 times less aromatization in comparison with Testosterone. However, it may cause gynecomastia through progestogenic activity.

Exemestane is able to eliminate the risks of estrogenic side effects. According to the recent study, it reduces the levels of estradiol by 85 percent. Besides, when taking Aromasin (Exemestane) after steroid cycle one can speed up the secretion of endogenous testosterone.

Therefore some bodybuilders include Exemestane into PCT plan. Letrozole and Arimidex (Anastrozole) have similar effects. They send a signal to pituitary about the necessity for gonadotropic hormones (luteinizing and follicle-stimulating).

However, Exemestane has some advantages over these drugs

  • Has low androgenic activity.
  • Accelerates secretion of insulin-like growth factor

Effects

By using Exemestane after steroidcycle one can faster restore the endogenous testosterone production. Besides, it increases the levels of insulin-like growth factor, thus enhancing anabolism.
The effects of Exemestane

  • Prevents gynecomastia.
  • Suppresses the level of female hormones.
  • Increases anabolism
  • Improves muscular relief.
  • Prevents hypertension.
  • Reduces the negative effect of estrogens on HPTA.

It is important to know that only aromatizable and progestogenic steroids can cause estrogenic side-effects. The primary aromatizable steroid is Testosterone. However, its derivatives can enhance the work of estrogens, for instance methandienone.

Meanwhile the rate of aromatization of Boldenone Undecylenate is 50 percent in comparison with Testosterone. This is not enouph for a rapid increase of estrogen levels. Although Trenbolone and Nandrolone Decanoate have very low level of aromatization, their progestogenic activity may increase the concentration of female hormones to critical level.

The susceptibility to estrogenic (progestogenic) side-effects greatly depends on genetic predisposition of an athlete. However if you use these drugs in combination with easily aromatizing steroid, the risk of estrogenic side effects increases.

No matter what steroid you use, Exemestane will protect you from side effects. In sports pharmacology there are steroids based on dihydrotestosterone derivatives. Basically they are not aromatizable. An exception to this rule is oxymetholone, which has estrogenic activity.But it does not interact with aromatase, therefore Aromasin (Exemestane) will have no effect during Anapolone cycle.

Dosage and Usage

Now let’s regard the usage of Exemestaneafter steroid cycle. We know that AAS can suppress the endogenous testosterone production. The degree of this negative effect depends on the doses of steroid you use.

One should remember that even the lightest steroid at high doses can negatively affect HPTA. After steroid cycle the body begins to produce testosterone again, but only when exogenous hormone is over.
It takes a lot of time for the body to recover and it depends on the individual characteristics of an athlete’s organism. In worst case it takes about a year. The testosterone deficiency is abnormal for the body, and it may lead to definite health issues. For example is increases the levels of cortisol, which destroys muscles, and decreases sex drive.

Therefore, you should follow PCT (Post Cycle Therapy) in order to speed up testosterone production. Some bodybuilders take Aromasin during PCT in order to accelerate testosterone synthesis and increase the level of insulin-like growth factor. However, we do not recommend it, since the balance of female and male hormones is also important for the body.

Scientists found out that estradiol regulates the balance of lipoproteins, affects the libido etc. Thus by suppressing its production you can adversely affect other functions of your body. That’s why we recommend using Exemestane only during steroid cycle.

The recommended doses of Aromasin (Exemestane) vary from 12.5 to 25 mg every other day. However, in most cases it is enough for an athletes to use 12.5 mg no more than three times a week. If you take maximal doses, then the duration of Aromasin (Exemestane) cycle should not be long.

Use 25 milligrams only in the case of cholesteroldis balance. In other cases take minimal doses. Competitive bodybuilders also take Exemestaneone or two weeks before the contest in order to improve muscular relief.

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Aromasin [Exemestane Tablets] / Arimidex (Anastrozole) / Femara (Letrozole)

General

by Anthony Roberts — Aromasin (Exemestane) is one of those weird compounds that nobody really knows what to do with. What we generally hear about it makes it very uninteresting It’s a third generation Aromatase Inhibitor (AI) just like Arimidex (Anastrozole) and Femara (Letrozole). Both of those two drugs are very efficient at stopping the conversion of androgens into estrogen, and since we have them, why bother with Aromasin? It’s a little harder to get than the other two commonly used aromatase inhibitors, because it’s not in high demand, and there’s never been a readily apparent advantage to using it. And I mean lets face it: It’s awkward-sounding. Aromasin doesn’t have much of a ring to it, and exemestane is even worse. Arimidex has a bunch of cool abbreviations (“A-dex” or just ‘dex) and even Letrozole is just “Letro” to most people. Where’s the cool nickname for Aromasin/exemestane? A-Sin? E-Stane? It just doesn’t work. It’s the black sheep of AI‘s. And why do we even need it when we have Letrozole, which is by far the most efficient AI for stopping aromatization (the process by which your body converts testosterone into estrogen)?

Letro can reduce estrogen levels by 98% or greater; clinically a dose as low as 100 mcgs has been shown to provide maximum aromatase inhibition! So why would we need any other AI‘s? Well, first of all, estrogen is necessary for healthy joints as well as a healthy immune system. So getting rid of 98% of the estrogen in your body for an extended period of time may not be the best of ideas. This may be useful on an extreme cutting cycle, leading up to a bodybuilding contest, or if you are particularly prone to gyno, but certainly can’t be used safely for extended periods of time without compromising your joints and immune system.

So that leaves us with Arimidex, which isn’t as potent as Letrozole, but at .5mgs/day will still get rid of around half (50%) of the estrogen in your body. Problem solved, right? Use Arimidex on your typical cycles, and if you are very prone to gyno or are getting ready for a contest, use Letro.

But what about Post Cycle Therapy (PCT)?

I think at this point most people are sold on the use of Nolvadex (Tamoxifen Citrate) instead of Clomid for PCT, since both compete estrogen at the receptor site, both increase serum test levels, and both drugs may also alter blood lipid profiles favorably (6). But since 20mgs of Tamoxifen is equal to 150mgs of clomid for purposes of testosterone elevation, FSH and LH, but Tamoxifen doesn’t decrease the LH response to :LHRH:. I think most people agree to Nolvadex’s superiority for PCT.

I’ve always been in favor of using Nolvadex during PCT, along with an AI (Aromatase Inhibitor), because reducing estrogen levels has been positively correlated with an increase in testosterone so in my mind, it’s be beneficial to increase testosterone by as many mechanisms as possible while trying to recover your endogenous testosterone levels after a cycle. SO which AI do we use? Letro or A-dex? Well, why don’t we just keep using whichever one we used during the cycle, and add in some Nolvadex? Unfortunately, Nolvadex will significantly reduce the blood plasma levels of both Letrozole as well as Arimidex. So if we choose to use one of them with our Nolvadex on PCT, we’re throwing away a bit of money as the Nolvadex will be reducing their effectiveness.
This, of course, is where Aromasin comes in, at 20-25mgs/day.

Aromasin, at that dose, will raise your testosterone levels by about 60%, and also help out your free to bound testosterone ratio by lowering levels of Sex Hormone Binding Globulin (SHBG), by about 20% SHBG is that nasty enzyme that binds to testosterone and renders it useless for building muscle. But what about using it along with Nolvadex for PCT?

To understand why Aromasin may be useful in conjunction with Nolvadex while both Letro and A-dex suffer reduced effectiveness, we’ll need to first understand the differences between a Type-I and Type-II Aromatase Inhibitor. Type I inhibitors (like Aromasin) are actually steroidal compounds, while type II inhibitors (like Letro and A-dex) are non-steroidal drugs. Hence, androgenic side effects are very possible with Type-I AIs, and they should probably be avoided by women.
Of course, there are some similarities between the two types of AIs both type I & type II AI‘s mimic normal substrates (essentially androgens), allowing them to compete with the substrate for access to the binding site on the aromatase enzyme. After this binding, the next step is where things differ greatly for the two different types of AI’s. In the case of a type-I AI, the noncompetitive inhibitor will bind, and the enzyme initiates a sequence of hydroxylation; this hydroxylation produces an unbreakable covalent bond between the inhibitor and the enzyme protein. Now, enzyme activity is permanently blocked; even if all unattached inhibitor is removed. Aromatase enzyme activity can only be restored by new enzyme synthesis. Now, on the other hand, competitive inhibitors, called type II AI’s, reversibly bind to the active enzyme site, and one of two things can happen:

1.) either no enzyme activity is triggered or

2.) the enzyme is somehow triggered without effect.

The type II inhibitor can now actually disassociate from the binding site, eventually allowing renewed competition between the inhibitor and the substrate for binding to the site. This means that the effectiveness of competitive aromatase inhibitors depends on the relative concentrations and affinities of both the inhibitor and the substrate, while this is not so for noncompetitive inhibitors. Aromasin is a type-I inhibitor, meaning that once it has done its job, and deactivated the aromatase enzyme, we don’t need it anymore. Letrozole and Arimidex actually need to remain present to continue their effects. This is possibly why Nolvadex does not alter the pharmacokinetics of Aromasin.

Before we close the book on Aromasin, it’s worth noting that you can (and should) still use one of the non-steroidal AI‘s during your cycle to reduce estrogen, if necessary. When you are ready for PCT, you can then switch over to Aromasin and still experience the full effects of an AI, since there is no cross-over tolerance experienced between steroidal and non-steroidal AI‘s. Since Aromasin is about 65% efficient at suppressing estrogen, it’s certainly a very powerful agent, especially considering you won’t experience reduced effectiveness because of your concurrent use of Nolvadex or from any sort of tolerance developed by using other AI‘s on your cycle. There is also a decent amount of preclinical data suggesting that Aromasin has a beneficial effect on bone mineral metabolism that is not seen with non-steroidal agents, and it may also have beneficial effects on lipid metabolism that are not found in the non-steroidal Letro and A-dex.

Finally, as we’re going to be using Nolvadex for PCT anyway, and we ought to be using an AI with it for maximum recovery I think Aromasin- considering it’s compatibility with Nolvadex and beneficial effects on bone mineral content and lipid profile, has finally stopped being the black sheep of AIs and found a home in our Cycles.

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