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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Zymoplex

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Zymoplex (Tamoxifen Citrate, Nolvadex)

Nolvadex (Tamoxifen) belongs to a category and class of drugs known as selective Estrogen receptor modulators (SERMs). Selective Estrogen receptor modulators belong to an even broader class of drugs known as anti-estrogens. The other subcategory of drug under the anti-estrogens category is known as aromatase inhibitors (AIs), such as Aromasin (Exemestane) and Arimidex (Anastrozole). AIs and SERMs make up anti-estrogens. Aromatase inhibitors differ greatly from SERMs in their action and how they deal with the issues of estrogen control.

This drug is a potent nonsteroidal anti-estrogen. It is indicated for use in estrogen dependent tumors, i.e. breast cancer. Steroid users take Nolvadex to prevent the effects of estrogen in the body. This estrogen is most often the result of aromatizing steroids.

Nolvadex can aid in preventing edema, gynecomastia, and female pattern fat distribution, all of which might occur when a man’s estrogen levels are too high. Also, these effects can occur when androgen levels are too low, making estrogen the predominant hormone. This can occur when endogenous androgens have been suppressed by the prolonged use of exogenous steroids.

Nolvadex works by competitively binding to target estrogen sites like those at the breast. This drug is not toxic nor have any side effects been seen in athletes who used the drug’ as an anti-estrogen. This drug is the most popular anti- estrogen amongst steroid users. Although it does not turn out to be 100% effective for everyone, it does seem to exhibit some level of effectiveness for the majority.

It works so well for some bodybuilders they can take drugs like Anadrol right up to a contest as long as they stack it with Nolvadex. It would seem wise to take this drug in conjunction with any steroid cycle. Most reported a dosage of 10 mg to 20 mg daily got the job done.

Dose of Zymoplex (Tamoxifen Citrate, Nolvadex)

Dosage of Zymoplex (Tamoxifen Citrate, Nolvadex) is prescribed by health providers particularly. The main condition that influences on dose is the disease of the patient. If patients have breast cancer or kidney cancer, they must take 20-40 mg of Zymoplex (Tamoxifen Citrate, Nolvadex) 1-2 times daily (in the morning and in the evening). Persons that suffer of endometrial cancer usually take 20-30 mg of this drug 1-2 times per day. Tablets of this drug must be swallowed with a glass of water. They must not be chewed. Daily quantity is taken at once in the morning or it’s divided in 2 and it’s applied in the morning and in the evening. Duration of therapy with Zymoplex (Tamoxifen Citrate, Nolvadex) lasts usually long period of time. Benefits can be reached, if this drug is administrated needed time continually. Sometimes treatment with this medicine is combined with beam or cytostatic therapy.

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Nolvadex

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Nolvadex (Tamoxifen Citrate)

Nolvadex and Gynocomastia

This drug is used as a first line defense against breast cancer. In the late 80’s, Dan Duchaine speculated that it could also be used by bodybuilders to halt the development of another type of tumor in the mammary gland, Gynocomastia. He introduced this find to the Steroid-using-community in his “Contest Prep” issue of the UnderGround Steroid Handbook Update Newsletters (the contest prep-issue was actually 3 issues in one, for those who had a subscription to the newsletter).

Nolvadex is commonly referred to in quite a few ways: as a SERM (Selective Estrogen Receptor Modulator), as an anti-estrogen (that is actually incorrect, as we will later see), and finally as a triphenylethylene. I happen to stick with calling Nolvadex a SERM, because out of my three options, it happens to be correct (as we know that calling it an anti-estrogen is incorrect), and pronouncable (as we know that I have no idea how to say “triphenylethylene”). Selective estrogen receptor modulators (SERMs) act as either estrogen receptor agonists or antagonists in a tissue-selective manner, lets see what that means to us&

Nolvadex actually has quite a few applications for the steroid using athlete. First and foremost, it’s most common use is for the prevention of gynecomastia. Nolvadex does this by actually competing for the receptor site in breast tissue, and binding to it. Thus, we can safely say that the effect of tamoxifen is through estrogen receptor blockade of breast tissue, especially since total body estradiol increases with use of tamoxifen. Clearly, if you are on a cycle which includes steroids which convert to estrogen, you may want to consider nolvadex as a good choice to run along side them.

Nolvadex Cycle

Nolvadex, however, is not the most potent ancillary compound we can use on a cycle, but it is probably the safest considering it doesn’t actually reduce estrogen in your body keeping some estrogen floating around could have many benefits on muscle growth, as well. Estrogen is also important for a properly functioning immune system, and not only that, but your lipid profile (both HDL and LDL) should also show marked improvement with administration of tamoxifen. Many bodybuilders actually use this stuff during their cycle for the health benefits provided by it. If, however, you are preparing for a bodybuilding contest, you need to use something which will suck most (if not all) of the estrogen out of your body. I am speculating that you may be able to use Nolvadex for the majority of a contest prep cycle, to keep yourself relatively healthy, and then switch over to Letrozole for the last 8 weeks.

Nolvadex also has some important features for the steroid using athlete. In hypogonadic and infertile men given nolvadex, increases in the serum levels of LH, FSH, and most importantly, testosterone were all observed. The best (rough) estimate I can give you from my research is that 20mgs of Nolvadex will raise your testosterone levels about 150%. And this would of course greatly aid post-cycle-recovery. What this means to us is that if you take Nolvadex after a cycle, when you are trying to raise your levels of testosterone, LH, and FSH back to normal, it will greatly aid recovery. In fact, if I were limited to just one compound to aid me in post-cycle-recovery, Nolvadex would be my choice. If you want a comparison, it would require 150mgs of Clomid to accomplish that type of elevation in testosterone, but nolvadex also significantly increased the LH response to LH, after 6 weeks.

Some of the more harsh ancillary compounds available today will give you a more “dry” look that nolvadex can’t, but nolvadex is simply safer to use in long (over 16 week) cycles.

Side Effects

Unfortunately, Nolvadex isn’t perfect. Anecdotally, it has been linked to reduced gains in some bodybuilders. This isn’t due, as previously thought, to its reducing estrogen levels (which it doesn’t), but rather to it’s ability to possibly reduce IGF levels, which are important for muscle growth.

Characteristics

While practically similar compounds in structure, few people ever really consider Clomid and Nolva to be similar. Its not just a common myth in steroid circles, but even in the medical community. This misconception originates from their completely different uses. Nolvadex is most commonly used for the treatment of breast cancer in women, while clomid is generally considered a fertility aid. In bodybuilding circles, from day one, clomid has generally been used as post-cycle therapy and Nolvadex as an anti-estrogen.

But as I intend to demonstrate this is in essence the same. I believe the myth to have originated because Nolva is clearly a more powerful anti-estrogen, and the people selling Clomid needed another angle to sell the stuff, so it was mostly used as a post-cycle aid. But few users really understand how Clomid (and also Nolvadex, logically) works to bring back natural testosterone in the body after the conclusion of a cycle of androgenic anabolic steroids. After a cycle is over, the level of androgens in the body drop drastically. The body compensates with an overproduction of estrogen to keep steroid levels up. Estrogen as well inhibits the production of natural testosterone, and in the period between the return of natural testosterone and the end of a cycle, a lot of mass is lost. So its in everybody’s best interest to bring back natural test as soon as humanly possible. Clomid and Nolvadex will reduce the post-cycle estrogen, so that a steroid deficiency is constated and the hypothalamus is stimulated to regenerate natural testosterone production in the body. That’s basically how the mechanism works, nothing more, nothing less.

Both compounds are structurally alike, classified as triphenylethylenes. Nolvadex is clearly the stronger component of the two as it can achieve better results in decreasing overall estrogen with 20-40 mg a day, than Clomid can in doses of 100-150 mg a day. A noteworthy difference. Triphenylethylenes are very mild estrogens that do not exert a lot, if any activity at the estrogen receptor, but are still highly attracted to it. As such they will occupy the receptor and keep it from binding estrogens. This means they do not actively work to reduce estrogen in the body like Proviron, Viratase or arimidex would (by competing for the aromatase enzyme), but that it blocks the receptor so that any estrogen in the body is basically inert, because it has no receptor to bind to.

This has advantages and disadvantages. The disadvantage is that when use is discontinued, the estrogen level is still the same and new problems will develop much sooner. The advantage is that it works much faster and has results sooner than with an aromatase blocker like Proviron or arimidex. Therefor, when problems such as gynocomastia occur during a cycle of steroids one will usually start 20 mg/day of Nolva or 100 mg/day of Clomid straight away, in conjunction with some Proviron or arimidex. The proviron or arimidex will actively reduce estrogen while the Clomid or Nolvadex will solve your ongoing problem straight away. This way, when use is discontinued there is no immediate rebound.

So which one should you use? Well personally, I’d have to say Nolvadex. Both as an on-cycle anti-estrogen and a post-cycle therapy. As an anti-estrogen its simply much stronger, demonstrated by the fact that better results are obtained with 20-40 mg than with 100-150 mg of Clomid. For post-cycle, this plays a key role as well. It deactivates rebound estrogen much faster and more effective. But most importantly, Nolvadex has a direct influence on bringing back natural testosterone, where as Clomid may actually have a slight negative influence. The reason being that Tamoxifen (as in Nolvadex) seems to increase the responsiveness of LH to GnRH (gonadtropin releasing hormone), whereas Clomid seems to decrease the responsiveness a bit.

Another noteworthy fact about Nolvadex is that it acts more potently as an estrogen in the liver. As you remember, I mentioned that clomiphene and tamoxifen are basically weak estrogens. Well, tamoxifen is apparently still quite potent in the liver. This offers us the positive benefits of this hormone in the liver, while avoiding its negative effects elsewhere in the body. As such Nolvadex can have a very positive impact on negative cholesterol levels2 in the body, and therefore too should be considered a better choice than Clomid. It will not solve the problem of bad cholesterol levels during Steroid use, but will help to contain the problem to a larger degree.

Another reason why I promote the use of Nolvadex over Clomid post-cycle (as if being 3-4 times stronger and having more of a direct effect on restoring natural test wasn’t enough) is because it’s a lot safer. Not just because it improves lipid profiles, but also because it simply doesn’t have the intrinsic side-effects that Clomid has. Clomid causes more acne for sure, but that’s mainly because you need to use a 3-4 times higher dose. But Clomid seems to also affect the eyesight. Long-term Clomid therapy causes irreversible changes in eyesight3 in users. Irreversible. For me that alone is reason enough to prefer Nolvadex.

Lastly, one should be aware that use of these compounds can reduce the gains made on steroids. Nolvadex more so than Clomid, simply because it is stronger. Estrogen is responsible for a number of anabolic factors such as increasing growth hormone output, upgrading the androgen receptor and improving glucose utilization. This is why aromatizing steroids like testosterone are still best suited for maximum muscle gain. When reducing the estrogen levels, we therefore reduce the potential gains being made. For this reason one may opt to try Clomid during a cycle instead of Nolvadex. Although I would imagine that the problem that needed solved would be of more concern, in which case Nolva remains the weapon of choice. It’s a plain fact that there is a high correlation between gains and side-effects. Either you go for maximum gains and tolerate the side-effects, or you reduce the side-effects, and with it the gains. That’s life, nothing is free.

Stacking and Use

If problems of Gynocomastia or other estrogen related symptoms tend to pop up during a cycle the use of 20-30 mg of Nolvadex or 100 mg of Clomid daily should easily contain the problem, and be used until a few days after the problem subsides. For best results and the least amount of problems upon cessation it is best stacked with Proviron (Masterlone) (50 mg) or arimidex (0.5 mg) for this duration as well. Its not advised that these products be ran concomitantly with the steroid for the entire duration of the stack, as this will reduce your gains. Instead cease the usage of anti-estrogens once the problem is contained, and should the problem resurface, simply recommence the use of the products in the same manner as described above.

Once a cycle of steroids is concluded one should always initiate a post-cycle therapy to help bring back natural testosterone as soon as possible. This will help you to retain the mass you gained. How this is done depends highly on the type of steroid used. If only orals were used, therapy should start immediately, even the last day of the stack. If short-acting esters or water-based injectables were used, therapy should commence within 4-7 days after last injection, and if long-acting esters were used then it should commence 1.5 to 2 weeks after the last injection was given. The length of the therapy will vary as well, from 3-5 weeks. The longer acting the product was, the longer therapy should be continued to make sure all suppressive factors are cleared before use of Clomid/Nolvadex is discontinued.

For best results, it is best stacked with HCG, which functions as an LH analog and can help bring testicle size back up. HCG use starts the last week of a cycle, and on from there every 5-6 days (usually 1500-3000 IU) and discontinued 1.5 to weeks prior to the cessation of Nolvadex/Clomid. The reason being that HCG itself is also suppressive of natural testosterone and should be out of the body before therapy is over, or it will inhibit natural testicle function. But I can not stress enough that HCG possibly plays a more important role in post-cycle therapy than Clomid/Nolvadex. For Clomid and Nolvadex, doses are usually tapered down.

  • Its best to start with 40-50 mg of Nolvadex or 150 mg of Clomid for the first week or the first two weeks,
  • and then finish the program with 20-25 mg of Nolvadex or 100 mg of Clomid for an additional two weeks.

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Femara (Letrozole)

About Femara

Femara® (generic name is letrozole) is a new drug developed for the treatment of advanced breast cancer in women. Femara is the second in a new class of third-generation selective oral aromatize inhibitors. It acts by blocking the enzyme aromatize, subsequently blocking the production of estrogen. Since many forms of breast cancer cells are stimulated by estrogen, it is hoped that by reducing amounts of estrogen in the body the progression of such a disease can be halted. This is the basic premise behind Nolvadex. Except this drug blocks the action and not production of estrogen.

Dosing

The effects of Femara can be quite dramatic to say the least. A daily dose of one tablet (2.5 mg) can produce estrogen suppression greater than 80 % in treated patients. With the powerful effect this drug has on hormone levels, it is only to be used (clinically) by post-menopausal women whose disease has progressed following treatment with Nolvadex. Consequently side effects like hot flushes and hair thinning can be present, and would no doubt be much more severe in pre-menopausal patients.

Male athlets

For the steroid using male athlete, Femara shows great potential. So up to this point, drugs like Nolvadex and Proviron have been our weapons against excess estrogen. These drugs, especially in combination, do prove quite effective. But Femara appears able to do the job much more efficiently, and with less hassle. Its use is only now catching on, but early reports have been excellent. A single tablet daily, the same dose use clinically, seems to be all one needs for an exceptional effect (some even report excellent results with only 1/4 tablet daily). When used with strong, readily aromatizing androgens such as Dianabol or testosterone, gynecomastia and water retention can be effectively blocked.

In combination with Propecia (Finasteride), we have a great advance. With the one drug halting estrogen conversion and the other blocking 5-alpha reduction (testosterone, methyltestosterone and Halotestin only), related side effects can be effectively minimized. Here the strong androgen testosterone could theoretically provide incredible muscular growth, while at the same time being as tolerable as nandrolone. Additionally the quality of the muscle should be greater, the athlete appearing harder and much more defined without holding excess water.

Conjunction

Furthemore there are some concerns with using an aromatize inhibitor such as this during prolonged steroid treatment however. While it will effectively reduce estrogenic side effects, it will also block the beneficial properties of estrogen from becoming apparent (namely its effect on cholesterol values). Studies have clearly shown that when an aromatize inhibitor is used in conjunction with a steroid such as testosterone, suppression of HDL (good) cholesterol becomes much more pronounced. Apparently estrogen plays a role in minimizing the negative impact of steroid use. Since the estrogen receptor antagonist Nolvadex does not display an anti-estrogenic effect on cholesterol values, it is the preferred from of estrogen maintenance for those concerned with cardiovascular health.

About a price

Femara has another principle drawback, namely the great price of this drug. Tablets can be quite costly with regular use, but it can ward off the side effects of strong androgens much better than Nolvadex and/or Proviron, making heavy cycles much more comfortable. As the number of countries manufacturing this drug increases, we may be able to look forward to a reduction in price. Privately compounded versions of “liquid Femara have also been formulated “for research purposes” and are currently circulating the black market.

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