The function of anti-estrogen drugs involves stopping the side effects associated with this hormone through estrogen drugs. It does so by not allowing it to become evident while you are using steroids. However, they are also commonly used at the end of a cycle in order to reinstate the production of endogenous testosterone.
For many years, many medications have productively been put to use in order to fight against estrogen. Though, it is just recently that these have become accessible in market. It has been made possible because of development in the breast cancer researches. These drugs are mostly employed for the treatment of breast cancer.
In a similar way, for athlete as well, there are a number of drugs to choice from. Because of this, there is great possibility that one may get confused while buying a medicine for a particular purpose. I feel that it is essential to take a look at the old and latest agents keeping in view that a number of factors like cost, availability, side effects and usefulness influence the buyer’s decision.
The term that is technically used for this purpose is Aromatization. Aromatization is an innate course which enables androgen like testosterone to convert into estrogen in your body. Very small number of Estrogens is made by the male body when it is in normal state. However, they yet have a vital function with regard to metabolism. They have an important role in processes like organ fat disposition, bone maturity and blood lipid regulation.
For athletes, estrogen may seem an intricate issue with the usage of anabolic/androgenic steroids. There can be problems pertaining to the build up of estrogen when the natural process of aromatization is in tact, androgen level is too high. It may also trigger side effects linked with estrogen like obvious fat and water retention, and the increase of female gynecomastia (breast tissue). For male athletes using steroids, Gynecomastia is a very problematic issue because the unpleasant increase of tissue mass is generally everlasting.
Regular mass building medicines like testosterone and Dianabol are readily aromatized even though many synthetic anabolic agents are defiant or not prone to aromatization by any means. Because of this reason, athletes look to take advantage of estrogen maintenance medications while using such steroids, which is a category of drugs that are taken as normal remedies for athletes.
Nolvadex and Clomid (estrogen receptor antagonists)
Commonly named as anti-estrogens, estrogen receptor antagonists are medicines which stop estrogens from triggering activity in your body. They are able to perform this function by particular element to connect to a part of the estrogen receptor, which is inactive. As a result, other estrogens are prevented from joining and activating the similar receptor spot. Clinically, an estrogen antagonist, most notably the medicine tamoxifen citrate called Nolvadex, is particularly used in advanced breast cancer treatment as the first line of resistance.
The use of this drug can well remove estrogen responsive cancer cells of essential hormone, which increases the rate of response in patients suffering from this type of cancer. After this drug option, usually the second choice is aromatase inhibitors which are strong agents. They can act as a substitute in case the usual antiestrogen treatment does not give the desired outcome.
Tamoxifen is given priority over other medications owing to many reasons. It is considered as the first choice in treatment because it is highly effective, but at the same time, it does not slow up the creation of estrogen in your body. It also makes Nolvadex treatment considerably less painful for the sufferer. Even though many females using estrogen maintenance drugs experience menopausal-like side effects, estrogen antagonists are a lot more bearable than medications that obstruct the production of estrogen. As a matter of fact, the work of tamoxifen is itself changeable. In some specific tissues, it can actually work as an activator of the estrogen receptor. Because of this, the activity of estrogen is not fully diminished; it does become less though.
In the present scenario, people understand that estrogens have a helpful function in the cardiovascular system. Researches prove that an increase in the estrogen level is directly associated with a reduction in LDL (bad) cholesterol, and an increase in HDL (good) cholesterol. The function of tamoxifen as an estrogen agonist in the liver gives the same outcome that is; it shows an estrogenic rather than antiestrogenic effect on blood lipid values.
According to the research carried out by the Department of Clinical Oncology in the Netherlands Cancer Institute during 1998, as a result of extended therapy with tamoxifen, a decreased LDL cholesterol level and considerably raised HDL cholesterol and HDL-C/total-cholesterol proportion can be seen. Consequently, it reduces the risk for heart disease and makes the treatment easier. For athlete who use steroids and are already encountering off-putting adjustment in lipid profiles, this sort of outcome could is surely an essential concern.
Clomid is very much like Nolvadex as both these medicines are triphenylethylene compounds and are also used for similar treatment that is, for breast cancer and female infertility therapy. Moreover, Nolvadex, like Clomid, is a fractional agonist/antagonist of the estrogen receptor; however, this depends on the tissue which is targeted. Athletes normally consider Clomid as only a testosterone-stimulating drug, which is to be taken at the end of steroid cycles as the activity of this drug is similar to Nolvadex. It must not be taken as a medicine alone which has its own functions, in fact, it should be considered as another useful cure for gynecomastia just as Nolvadex.
It had all the ability to substitute Nolvadex as a defensive agent for gynecomastia when you are on your cycles with aromatizable steroids, without clearly shifting the level of outcome, similar to the way Nolvadex can be put to use to boost the combination of testosterone at the end of steroid treatment.
Aromatase inhibitors are another mode of treating estrogen, which is considered more direct and effective. This medication acts on the enzyme responsible for the biosynthesis of estrogen instead of stopping it at its receptor. Circulation of estrogen can be significantly reduced by restraining this enzyme. This category of medications is a focal point for most people related to medical field community because a reliable inhibitor of aromatase can be more useful for patients who are suffering form related types of cancer compared to antiestrogenic agents.
Similarly, athletes feel that aromatase inhibitors, which are recently developed, are the most powerful treatment for the prevention of side effects related to them. Before we proceed to further discuss the different sorts of various inhibitors of aromatase, it is imperative to talk about the hitches of this kind of treatment. One of the most visible shortcomings is its unconstructive impact on cholesterol level. Using steroids surely have a negative effect on cholesterol levels, but when aromatization is inhibited, this risky inclination is all the more increased.
In 1990, a study was published which demonstrated this likelihood in a very obvious manner. During the course of this research which spanned to about 12 weeks, the working of testosterone enanthate was compared to the function of the similar quantity combined with an aromatase inhibitor. Significant decrease in HDL cholesterol values was observed in the group which was using testosterone only, while the other group which was taking the combination of testolactone had great reduction, almost 25%, during the fourth week of this treatment.
People with heart diseases are obviously not too sure if they should use an aromatase inhibitor while taking steroids. As an alternate, going for an antiestrogen like Nolvadex does not give full assurance that lipid values will not become all the more worse if no other estrogen maintenance drug is being used at all. During researches combining tamoxifen with estrogen replacement therapy, it was seen that this composite could get in the way with of the positive effects of estrogen-based medications on lipid values; however, it will not fully reduce these.
In view of the fact that the outcome of Nolvadex during steroid therapy like testosterone are not entirely studied, we still do not know if it is useful with regard to lipid values when taken along with an aromatizable steroid. However, we can yet take it as a safer substitute compared to other aromatase inhibitors.
Testolactone is another steroidal aromatase inhibitor, which is comparable to testosterone in its structure. It was initially brought in market during 1960’s when androgenic steroids were used in traditional breast cancer treatments. Testolactone was developed while trying to create a useful medication for breast cancer which was free of virilizing activity, and for that matter, testolactone fits fine as it is entirely free of androgenic activity. It was not found to work by inhibiting aromatase until the year 1975. By that period, testolactone had loss the interest of the medical community because of its low rate or response, and its use of stronger elements like aminoglutethimide.
Even though testolactone is accessible, it is not a very good option for athlete as it has numerous drawbacks. It is not cheap and you have to take at least 4 tablets daily for an adequate level of estrogen. Moreover, Teslac can also be an antagonist of the androgen receptor to a considerable extent, which is an unnecessary outcome for the one using steroid. As it is a derivative of testosterone, it is a controlled drug in the USA.
Although it does function as a feeble aromatase inhibitor, the pain to get it and other side effects make it not very easy to find nowadays.
Cytadren is another aromatase inhibitors, which was developed earlier on. It was the foremost medication which was acceptance for this purpose by most people. Just as testolactone, it was accessible in market a long time before its functions were fully investigated. As a matter of fact, the history of this medicine is very interesting. It is a derivative of the hypnotic glutethimide and its sale as an anticonvulsant medication began in United States during 1960. After about 6 years, there were repots of adrenal insufficiency by patients taking this medicine and as a result, it was banned in market.
Afterwards this drug was investigated and finally it was brought back into consumption. With the passage of time, Aminoglutethimide came to be one recommended and researched aromatase inhibitors in the market. It is also a useful treatment for Cushing’s syndrome, when your body produces excessive cortisol; it has significant effect on cortisol secretion.
The decision pertaining to the dosage of this drug has also been an issue. When it was initially given to patients, it turned out to be effective only momentarily at lowering inhibiting adrenal steroid secretion which lasted for merely for 3 to 7 days. It was evident that the body would experience the lowered output of cortisol, and generate more of ACTH in response when dubbed the adrenal escape trend.
This reinstates the normal discharge of adrenal steroids and reverses the outcome of this drug. A small dosage of this medication is used clinically to avert this effect. This was also an accepted practice for treatment of breast cancer for a while.
Later on, after thorough investigations, it was found out that the primary system in which this medication is useful for the patients of breast cancer is not the same as which it impedes with adrenal hormones. It was also observed that the quantity was essential in initiating each particular reaction. It is found out that aromatase inhibition is obtained at a considerably minor dosage than is required to stop the production of steroid by the adrenal gland. At the same time, as a 1000 mg daily is required to inhibit the demolase enzyme, (it is the enzyme which converts cholesterol to pregnenolone, and is also the target when lesser adrenal production is required), highest inhibition of aromatase and estrogen levels is obtained by 250 to 500 mg.
With regard to response rate in patients as well, there does not seem to be any advantage by adding cortisol. As a result, there is need to increase cortisol while using this medicine for inhibiting aromatase and for athletes as well, to apply a rotating dosage program. Besides, another use for athletes is that of an anti-catabolic, however, this subject requires a separate discussion.
As far as effectiveness is concerned, this drug is extremely effective as it makes aromatase activity decrease as low as 92% only after a dose of 250 mg. the study of patient’s response too proves that this medicine is as good as tamoxifen treatment in healing estrogen dependent cancer cells, in some specific conditions though.
Because of many functions of this drug including the potential inhibition of cortisol and estrogens as well as aldosterone and androgens, it does not prove to be very comfortable for patients. This does not imply that the complaints are very common since this drug is well known to be safe. Similarly, athletes can take it as very useful treatment for estrogenic side effects only if it is accessible at least at the same price as Nolvadex.
This drug is not technically categorized as an anti-aromatase, but an oral androgenic steroid. Proviron, particularly, contains a derivative of dihydrotestosterone, and is only different by the addition of one methylation. Its usage as antiaromatase has came as a result of studies which have proved a nonaromatizing androgen like ihydrotestosterone can hinder this enzyme response. This drug is believed to impede with aromatase by opposing an aromatizable steroid like testosterone for joining with the enzyme site. With Proviron interacting with this enzyme, without causing any reaction, the enzyme is stopped from altering other hormones momentarily, and as a result, an anti-estrogenic effect is attained.
Nevertheless, Proviron is not as good as any of these antiestrogens or aromatase inhibitors although it can give certain benefits when is used with medications like tamoxifen. This drug does not seem to be as potent an aromatase inhibitor for longer use during strong cycles. Just as in case of testolactone, Proviron is also a controlled substance and it is mostly harder to get compared to many of the other medications.
Anastrozole is a non-steroidal aromatase inhibitor which has been recently designed. This drug is a very effective treatment for breast cancer since it can proficiently stop aromatase activity and does not even cause any effect enzymes which are engaged in the biosynthesis of other adrenal steroids. For this reason, the activity of this drug is significantly more specific compared to aminoglutethimide. This attribute also makes it more bearable for the user. According to many researches as well, this medication is superior inhibitor compared to earlier therapies. These also include numerous such treatments in which patient responded positively to anastrozole after not responding to tamoxifen. As a matter of fact, Arimidex is most effective and reliable compared to all the other inhibitors mentioned in this article.
The advised dose for this medication is a 1 mg once daily which is the lowest dosage that has proved to generate highest suppression of estrogen levels. To spite expectations of better outcome, dosage of up to 10 mg per day did not show significant boost to the long-standing response rate.
Normally, 1 mg will produce estrogen suppression near 100% because of which there is no real requirement for the athletes to take more of it. Moreover, as this drug is very expensive, most people will not be able to do it anyways. Tamoxifen will normally cost around $1 per tablet, whereas anastrozole may coast up to $10. Owing to this price factor, many people adhere to take lower dosages like 1-2 tablets per day or they modify the timetable to save money.
Formestane (4-OH androstenedione)
Formestane is a new category of steroidal-based aromatase inhibitors which are available in Europe and will soon reach U.S market as well. Structurally it is a derivative of androstenedione; 4-OH androstenedione, which is an aromatized steroid. For this reason, it likewise allows interface with the aromatase enzyme. Its function in your body is like of a suicide inhibitor, implying that the composite will become bound to the aromatase enzyme as soon as it will come in contact with it. Because of this, its effect is relatively more lasting compared to reversible, competitive inhibitors. Keeping this in view, it is obvious that formestane has proved to be 60 times more powerful compared to aminoglutethimide. Just as Arimidex, this medication can help you to attain almost complete suppression of aromatase.
Because of meager oral bioavailability, this drug is manufactured in the form of injections. The recommended dose is 250 mg after every two weeks. Despite the fact that estrogen suppression can be marked with these dosing models, certain researches, propose that by the subsequent week estrogen levels may start to get better.
Even though it is better to take it more frequently, the cost of this drug makes this hard to manage. Presently, I am seeking for mail-order list in which a single 250 mg ampule of formestane is available for $249, as this would make the total sum for a month $500 approximately, which is double the cost of anastrozole dosage. Moreover, it is also not guaranteed that with the high potency of this medication an athlete may have to encounter issues with regard to the advised schedule.
The BEST estrogen maintenance drug?
When you have to make the choice of an estrogen maintenance drug, there are many things that you have to consider other than effectiveness alone. The differences in cholesterol alterations among anti-estrogens and aromatase inhibitors as we discussed in this chapter surely deserve attention. In light of this, an antiestrogen like tamoxifen or clomiphene is the best choice. The cost of the medication can also be an issue for some people since the latest aromatase inhibitors can cost you approximately $250 and $500 monthly.
This price is almost opposite to what aminoglutethimide, Nolvadex or Clomid may cost you; $100 or even less on monthly. With regard to the most effective drug for estrogenic side effects, technically, Arimidex and formestane are the right options. Formestane which is more costly, proved to be slightly somewhat less reliable compared to Arimidex. Therefore, its cost should not make us believe that it is better that the other. Finally, there is no assurance that any of these new selective aromatase inhibitors will prove to give more effective results compared to well tried and accepted estrogen maintenance medications including Nolvadex, Clomid and aminoglutethimide. This is for reason that these agents deal with the buildup of estrogen in a significantly effective manner. Moreover, besides this medical setting, the lofty prices off these latest medications will not allow many people to use them conveniently.