because of their ability to minimize risk of gynecomastia (abnormal growth of breast tissue in males) and enhance recovery of natural testosterone production after a cycle, use of antiestrogens such as aminoglutethimide (Cytadren) and clomiphene (Clomid) has become popular in bodybuilding. Antiestrogens also can minimize bloating associated with anabolic/androgenic steroid use, and may avoid health risks associated with elevated estrogen levels. Medically, the drugs are used not only for treatment of breast cancer but also for improvement of fertility in both men and women, and occasionally for boosting testosterone levels in men such as endurance athletes with low testosterone. There are two categories of antiestrogens: aromatase inhibitors and receptor blockers. Both shall be considered here.
Estrogens
As with androgens, where any hormone that has the activity of testosterone is an androgen and as a result all anabolic steroids are androgens, any hormone that has the activity of estradiol, the principal female sex hormone, is an estrogen. the most active natural estrogens in humans are estradiol and estrone.
These hormones are related to each other rather similarly to how the andro prohormones are related to each other. just as androdiol has a hydroxy (or –ol) group at both the 3- and 17- positions, estradiol similarly has a hydroxy group at those positions. Estrone, like androstenedione, has keto (or –one, pronounced “oan”) groups at those positions.
Estradiol is the most potent (effective per milligram) of the natural estrogens. It is produced either from testosterone by means of the aromatase enzyme, or from estrone by means of the estrogenic 17b-HSD enzyme.
Estrone is less potent, but all this indicates is that one needs a lot more of it to accomplish the same job. It is produced either from androstenedione by means of aromatase, or from estradiol by means of the same 17b-HSD enzyme working in reverse.
From the standpoint of the bodybuilder using anabolic/androgenic steroids (AAS), if nothing is done about the situation, high estrogen levels can cause gynecomastia, will inhibit natural testosterone production, and will cause bloating. High estrogen levels also make it a lot more tough to lose fat, and tend to cause female pattern fat distribution even in males.
Estradiol also has carcinogenic metabolites, and a liver problem often associated with AAS use, hepatic cholestasis, is caused not by androgen but by an estrogen metabolite.
It is also not unusual for bodybuilders to feel poorly on beginning a cycle of high dose testosterone without antiestrogens, and for this reason lots of have advocated starting with a low dose and building up. However, I strongly suspect that the real problem is estrogenic effect on mood, and the problem can be avoided with use of an aromatase inhibitor.
Aromatizable steroids
Though a lot of bodybuilders feel they know which steroids aromatize and which do not, often the beliefs are in error. This is because progestogenic activity (activity like that of progesterone, another female hormone) is easily mistaken for estrogenic activity. Both hormones can cause bloating, and both can cause gyno. So AAS which are capable of activating not only the androgen receptor but also the progesterone receptor are typically wrongly assumed to aromatize. (Note: these androgens do not “convert to progesterone” but rather are themselves, without any change needed, able to act on that receptor.)
Nandrolone is proven to be a progestin. This fact is of clear value in bodybuilding, because while moderate Deca-only use actually lowers estrogen levels as a consequence of minimizing natural testosterone levels and thus allowing the aromatase enzyme less substrate to work with, Deca nonetheless can cause gyno in some individuals. Furthermore, just as progesterone will to a point increase sex drive in women, and then typically decrease it as levels get too high, high levels of progestogenic steroids can kill sex drive in male bodybuilders, though there is a terrific deal of individual variability as to what is too much.
Incidentally, this progestogenic activity also inhibits LH production, and in contrast to common belief, even small amounts of Deca are quite inhibitory, around as much so as the same amount of testosterone.
What relevance does this have to an post on antiestrogens? Well, antiestrogens can do nothing about these side effects of Deca.
The same appears to be true of oxymetholone (Anadrol®) and of norethandrolone (Nilevar).
Methenolone (Primobolan), stanozolol (Winstrol), dromostanolone (Masteron), oxandrolone (Anavar), mesterolone (Proviron), stenbolone (Anatrofin), trenbolone, and DHT do not aromatize, and thus, antiestrogens are not relevant to these AAS either.
The steroids where aromatization is of particular worry are testosterone, methandrostenolone (Dianabol), boldenone (Equipoise), and to some extent fluoxymesterone (Halotestin). however the latter is normally used in doses low enough that aromatization is not an issue.
Among the prohormones, androstenedione is the principal offender with regard to aromatization, being readily converted to estrone. With androdiol, only that small portion which converts to testosterone can Camiseta PSV Eindhoven be converted additionally to estradiol, and that will occur only in the same percentage that other testosterone converts to estradiol.
Norandrodiol cannot convert directly to estrogen, and even after conversion to nandrolone is not readily converted to estrogen.
Norandrostenedione can be converted to estrone by aromatase, but is a very poor substrate for that enzyme. It can actually act as a competitive inhibitor, blocking better substrates such as androstenedione or testosterone. It is possible then, though unproven, that norandrostenedione might have some value as an aromatase inhibitor in bodybuilding. I do think, however, that the pharmaceuticals created for the purpose must be assumed to be better choices.
Aromatase inhibitors
The a lot of frequently used aromatase inhibitor in bodybuilding is aminoglutethimide (Cytadren). This drug also inhibits an enzyme (desmolase) needed for synthesis of cortisol, but fortunately, aromatase can be inhibited with levels of drug that cause only limited inhibition of desmolase.
Contrary to popular belief, it is normally not desirable to inhibit cortisol production. Doing so will likely cause joint problems, and moreover once the inhibition ends, the price of above-normal cortisol production need to normally be paid.
For an average male, a dose of 250 mg/day (one tablet) appears optimal. The half-life is 8 hours, so the drug is better taken in divided doses. the best plan seems to be to take half a tablet on arising, and quarter tabs six and twelve hours later. This keeps levels normally fairly constant, but allows a small drop in the hours shortly before arising, which is then compensated for by the higher dose on arising. With this scheme, inhibition of cortisol production is normally too low to be noticed, and normally there is no rebound effect on discontinuance. however it is not a bad idea nonetheless to taper off, first omitting the midday quarter tab dose for a few days, then omitting Camiseta Selección de fútbol de Serbia both quarter tab doses, then minimizing the initial dose to one quarter tab, and then ending completely. A week is sufficient for the taper.
Some people suffer a degree of lethargy or sedation from aminoglutethimide, even at this low dose, but a lot of do not.
Anastrozole (Arimidex) is a remarkable aromatase inhibitor which does not have the above side effects. It is, however, very expensive. With moderate doses of testosterone it seems that 1 mg/day is sufficient, and some have claimed half a tab to be sufficient. I do not have blood test data to verify that, however.
Receptor blockers
Clomiphene (Clomid) and tamoxifen (Nolvadex) are the most popular drugs of this class. They are a lot more precisely referred to as “selective estrogen receptor modulators.” This is because their mode of action is not so basic as merely blocking the estrogen receptor. Estrogen receptors require not only hormone but also activation of regions of the receptor called AF-1 and AF-2. AF-1, to be activated, requires phosphorylation, while AF-2 can be activated by any of a number of cofactors, such as IGF-1.
As it happens, clomiphene and tamoxifen are estrogen receptor antagonists (blockers) in cells that depend on activation of the AF-2 region, while in cells which activate AF-1, these compounds are estrogens.
In some cells these drugs activate one of the types of estrogen receptor (ERa ) but are antagonists of the other type (ERb ).
The result is that these compounds are antiestrogenic in breast tissue, fat tissue, and in the hypothalamus, which is what we want in bodybuilding, but are estrogenic in bone tissue and with respect to positive effect on blood lipid profile, both of which are, again, desirable. They also appear to have some estrogenic effect on mood, though this may be in only parts of the brain (the matter is not studied.)
Cyclofenil is a similar drug to the above two. Clomiphene will do everything that the other two will do, but for some unknown reason, has been found a lot more effective than tamoxifen both medically and in bodybuilding for boosting LH production.
Raloxifene (Evista) is a new selective estrogen receptor modulator that, for women, has the advantage of being an antiestrogen in the uterus, whereas clomiphene and tamoxifen are estrogens in that tissue. For this reason, the latter two drugs can promote uterine cancer, while raloxifene actually must help stop it, and is as a result a remarkable drug for women. It is not known how effective it may be in boosting LH production.
While on high dose androgens it is impossible to maintain LH production in any case, and clomiphene can do no good in that regard. As androgen levels return to normal, however, a dose of 50 mg/day of clomiphene if estrogen levels are reasonable, or 100 mg/day if estrogen levels are high, is normally effective in restoring natural testosterone production.
Because the drug has a long half-life, when one takes 50 mg/day the amount in the system is not only the 50 mg just taken, but also around another 250 mg from previous days. Thus, to right away arrive at the therapeutic level, one would take 300 mg (50 mg six times) on the first day, and then continue with 50 mg/day.
A small percentage of individuals suffer vision problems from use of clomiphene, which is normally reversible upon discontinuance. These persons, of course, must not use the drug after discovering the problem.
It also need to be pointed out that these are prescription drugs, and must be obtained and used only by precription with medical advice, though the selective estrogen receptor modulators have exceptional safety records.
After a cycle, it is affordable to continue clomiphene Camiseta Eintracht Frankfurt use until at least four weeks after the last injection of long acting ester, or at least two weeks after the last use of an oral, or until natural testosterone production is clearly back to normal, whichever comes last.
Conclusion
Other than acne and accelerated hair loss, the two a lot of common problems of AAS use are gynecomastia and difficulty in recovering natural testosterone production. Antiestrogenic drugs can successfully address both problems and are safe for a lot of individuals. Ideally, if aromatizable drugs are used, the problem is corrected at the source by limiting production of estrogen by using an aromatase inhibitor. However, it is also effective to use a selective estrogen receptor modulator such as Clomid. The latter drug is also of particular use in helping to restore natural testosterone production after a cycle.
Article courtesy of Mesomorphosis.com
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—————————————————————————About the Author:
Bill Roberts holds a bachelor’s degree in Microbiology and Cell Science, and was doctoral candidate(Ph.D.) in Medicinal Chemistry. He is working on the completion and defense of his doctoral thesis:“Synthesis, characterization, and determination of transdermal flux of 3-alkylcarbonyloxymethyl derivativesof 5-fluorouracil, and development of models for prediction of transdermal flux from physical parameters. “His education was indispensable so far as being able to design/improve nutritional supplement compounds,since it was in the field of creating drug molecules and secondarily some work in transdermal delivery.It was not specifically “geared” toward androgens other than proficiency with pharmacological principles havingbroad applications. This has allow bill to supply special insight into the field of anabolic pharmacologywith knowledge of points which he would not have known otherwise. He is a former writer for Dan Duchaine’sDirty Dieting newsletter, and is an avid lifter.