Antiestrogen Therapy Drugs

Understanding Aromatization in Bodybuilding

This kind of stuff is used too often in the world of bodybuilding in search of the innumerable benefits that different steroids offer. These derivatives of the male hormone testosterone increase muscular development and strength considerably. It is also worth mentioning that there are possible side effects. One of the negatives is a process called aromatization.

What is Aromatization?

This aromatization is a biochemical process in which an androgenic activity substance turns to estrogenic. That may sound confusing, so let’s make this clear: basically, the androgenic activity from anabolic steroids changes into the female sex hormone, estrogen. This leads to excess female hormones in the male body, resulting in undesirable side effects.

Effects of Aromatization

Among the common effects that result from aromatization is gynecomastia, where one gets fatty deposits under the skin of the nipples, resembling female breasts. Although this can be surgically corrected, the process is nowhere near fun. An additional effect is that water and fats may accumulate excessively in the body, which may actually turn out to be disastrous for bodybuilders whose aim is to have a lean, muscular physique.

The question then arises – how does one prevent or manage aromatization? The answer lies in antiestrogen therapy.

Exploring Anti-estrogen Therapy

Anti-estrogen therapy, however, has compounds known as antiestrogens; they inhibit the process of aromatization and, hence, help bodybuilders avoid unwarranted effects in their bodies.

Mechanism of Antiestrogens

Now, let’s dig a bit in-depth on the subject of how antiestrogens work. Steroids will aromatize when a molecule of such steroid interacts with an enzyme and converts it into estrogen. Thus, this newly formed molecule of estrogen goes and binds to the receptor of estrogen present in the body, thus eliciting location-based response effects. Side effects from this process can be eliminated through either one of the following two methods:

Prevent the steroid from interacting with aromatase.

Stop the formed estrogen molecule from binding with the estrogen receptor. All that uses the first approach fall under the categorization of anti-aromatase drugs, while all that uses the second fall under what is referred to as estrogen antagonists.

Anti-aromatase Drugs: An Overview

The function of the anti-aromatase drugs would be to act in the same way: to antagonize the aromatase but not to convert into estrogen. So, in this way, they keep the aromatase busy, not giving the steroid molecule an opportunity to bind with it. Proviron, Cytadren, and Arimidex are some of the anti-aromatase drugs.

Proviron

What makes Proviron so special is the fact that it has anti-aromatase activity. It is used medically to treat male sexual disorders. But most interesting is the fact that it comes into interaction with aromatase and androgen receptors once it penetrates the body. This then contributes to the appearance of “harder” looking muscles, which brings about improved vascularity and definition. The exact cause of this effect has, however, not yet been fully elucidated.

So the dosage of Proviron should be up to individual needs, keeping in mind what steroids are used at the same time.

Cytadren

Cytadren is a popular synthetic anti-aromatase drug among bodybuilders. This can, however, be attached not only to the fact that it helps in fighting estrogen but rather to the ability to stop the production of cortisol. Cortisol being a hormone that inhibits protein synthesis, therefore, stopping its production might have one contributing to muscle growth. Cytadren use should be closely follow in some cases, as it might lead to side effects such as drowsiness, depressive states, especially in genotypically susceptible individuals.

Arimidex

Arimidex acts as a potent synthetic anti-aromatase drug. Comparatively, it is more costly than others in its class and also has been established to bring about the desired reduction in estrogenic effects among bodybuilders. The average half-life of Arimidex is usually taken to be within 60 hours. This would mean much less frequent every-day administration, then – in this way, relatively easier for the user.

Estrogen Antagonists: An In-depth Look

Though they do not directly shut the activity of aromatase down, estrogen antagonists play a very key role in antiestrogen therapy. The way estrogen antagonists work is by occupying and activating the estrogen receptor without actual activation, hindering the binding of the typical estrogen to the receptor and activating it. Two of the most well-known and often used estrogen antagonists in bodybuilding are Nolvadex and Clomid.

Nolvadex

The drug Nolvadex, in the form of tamoxifen citrate, falls in the very few compounds category, which shows this ability to work in a very unique way. It can work as an estrogen or an estrogen antagonist, dependent on the interacting tissue. It can be used to promote a harder and much more defined appearance of muscle. Some athletes have, however, expressed that it reduces the level of the effectiveness of the steroid cycle slightly, because of the antiestrogenic influence of the drug on the liver, which in turn brings about the reduction of insulin-like growth factor (IGF-1).

Clomid

Clomid or clomiphene citrate is an artificially created estrogen that has a great amount in common with tamoxifen. With all, Clomid is capable of restoring both spermatogenesis and the endogenic synthesis of testosterone in the body.

This is done through a direct impact on the hypothalamus-pituitary-testes axis; thus, Clomid becomes an ideal candidate for the end of the steroid cycle. This should be appreciated by the fact that Clomid has proved to be a very useful adjunct in antiestrogen therapy, though far less potent than Tamoxifen in this respect.

A Note on Dosage and Side Effects

The same as in all drugs, doses of antiestrogens should be administered with a certain amount of care. Exceeding the blockade of estrogen may produce undesirable effects, including reduced libido, depression, and mood swings. Therefore, the objective is always to strike a balance between the minimal aromatization side effect and over-blocking the crucial body functioning of estrogen.

Conclusion

It is often laced with complications in the side effects of steroids, one of the critical parts of bodybuilding. Aromatization is one of those side effects where a male’s body produces more female hormones than necessary. However, these can be well controlled by an appropriate anti-estrogen therapy use, among which are mentioned antiaromatase drugs and estrogen antagonists. The concept is to be in a position to strike some sort of balance between gaining the full benefits from steroid use but keeping away from their downsides. This balance ensures the bodybuilder can achieve their fitness goals without compromising health.