Dear Friend and Fellow Athelete,

Meet poor Billy. Billy stands over 6 feet tall and weighs around 270 pounds. Billy was born a healthy, normal man - good looking, good genetics, naturally strong. But now, when he's not working the talk show circuit, Billy has an exciting career as an exotic dancer. Some guys just love watching poor Billy shake and shimmy his double D's. How did Billy grow breasts like the guy in Fight Club with the huge knockers? Our friend Billy used anabolic steroids without anti-estrogens.

My good friends at AG-GUYS.COM sent me this amazing article on anti-estrogens titled the Anti-Estrogens Report Card. As you know from my article "Why Billy Has Breasts", excess testosterone can convert to estrogen - something that bodybuilders definitely don't want. The Anti-Estrogen Report Card from AG-GUYS.COM looks at what our options are for preventing this. Enjoy! Anti-Estrogen Report Card By J @ AG-GUYS.COM Remember when you were in school, and you got a report card? If you were like me, you dreaded that time of the semester. I typically got passing grades and on occasion a failing grade that would mean I had to pull straight A’s for the next half of the year in order to avoid repeating a class. What does this have to do with anything? Well I was trying to figure out a way to rate the most commonly used anti-estrogens on the market, and the best way I can think of is to do a report card for them. Why a report card? Well... because it’s pretty easy to understand, first of all. You can be in first place in a race and that’s good, but “1st” on a scale of 1-10 is bad… so lets ditch the number system. I mean… hell… we all know what an “A+” is (or at least, in theory we do), and if you’re anything like me, you certainly know what an “F” is also. So I’m going to rate the most popular anti-estrogens that are available on the market today, with the all-too-familiar school grading system of A - F. Also, I’d like to state right off the bat that I’m going to mainly be addressing the most commonly discussed and used ancillary compounds on the market today, for use during a cycle. Basically, if you can easily obtain it, you’ll be reading about it in this piece. Sooo... that means if you’re “old school” and are looking for a detailed description of Cytadren or Teslac, you’re out of luck. So why do we need anti-estrogens? Well, certain anabolic steroids convert to estrogen - this is via the aromatase enzyme, and is called aromatization. This is probably the cause of most of the side effects we experience like bloating, gynocomastia, (possibly) acne, and a host of other side effects we’d rather avoid. Estrogen can also cause additional growth, however, as well as having immunostimulating effects and is beneficial for healthy joints- so it’s important to note that we don’t want to eliminate all estrogen from our bodies. Anyway, before I get into it, I’m going to have to explain a bit about different types of Anti-Estrogens, ok? First we’ll take a look at SERMs, which stands for “Selective Estrogen Receptor Inhibitor.” There are basically two drugs in this class that we’re going to look at, namely Clomid (Clomiphene Citrate) and Nolvadex (Tamoxifin Citrate). Basically both of these drugs have the ability to act as an estrogen agonist (or activator, in simpler- though less precise- terms) in some tissue and as an antagonist (inactivator), in others. I’ll get into the specific actions of both of them shortly. The other class of medications I’m going to explain is Aromatase Inhibitors. Aromatase Inhibitors basically prevent the aromatase enzyme from doing its job.AIs are classified into two types: type I, also known as suicidal or noncompetitive inhibitors; and type II, known as competitive inhibitors. Aromasin and ATD are in the first category, while LiquidDex and Letrozole are in the second. Both type I & II mimic substrates (essentially androgens), and can compete with it for access to the binding site on the actual enzyme (aromatase). After this initial binding, the next step is where things begin to differ for the two different types of AI’s. Once a noncompetitive inhibitor has bound, the enzyme initiates a sequence of what’s called hydroxylation, and hydroxylation produces an unbreakable covalent bond between the inhibitor and the enzyme protein. This is important because now, enzyme (aromatase) activity is permanently blocked; even if all of the unattached inhibitor is removed, and now, enzyme activity can only be restored by new enzyme synthesis. Type II AI’s or competitive inhibitors, on the other hand, reversibly bind to the active enzyme site, and one of two effects is had: no enzyme activity is triggered, or the enzyme is somehow triggered without effect. The type II inhibitor can then actually disassociate from the enzyme, eventually allowing renewed competition between the inhibitor and the substrate for binding to the site (estrogen synthesis). Now that SERMs have been explained as well as AI’s, we can see how each of them rates on my “on-cycle report card.” Clomid is a drug given to women as a fertility aid, which acts by binding to the estrogen receptor and thereby blocking estrogen from doing the same in some tissues. It can bind to breast tissue, and prevent estrogen from binding there to cause gynocomastia -although it is not nearly as effective as nolvadex. It can also stimulate the HPTA (Hypothalamic-Pituitary-Testicular-Axis), and stimulates LH (Luteinizing Hormone) and FSH (Follicle Stimulating Hormone). LH and FSH stimulate the release of testosterone. Unfortunately, Clomid does this only weakly, and there are much better ancillary products on the market. It works, but I think Nolvadex is much better. Final Grade:C- Buy research clomid Buy Pharmaceutical Clomid Nolvadex is a Selective Estrogen Receptor Modulator. This means that it acts on the Estrogen receptor (called the "ER" but having nothing to do with George Clooney or Anthony Edwards). Now, this also means that it acts as an estrogen in some tissues which acts as an anti-estrogen in some tissues. The estrogen receptor's ligand binding domain is just of a number of amino acid sequences "folded" into a series of helixes, which have the ability to change conformation. Different stimuli (such as Nolvadex) are well documented to have the ability to change the conformation of a very important helix (helix 12, for those keeping score at home). When estradiol binds the ER, this particular helix takes on a conformation that allows DNA transcription to mRNA, and estrogenic effects are then expressed in the body. When Nolvadex (Tamoxifen) binds to it, the antagonist changes the shape of this helix in such a way that it now folds (or bends) in such a way to prevent proper binding of estrogen, and subsequent transcription of DNA to mRNA. Sadly, if you take progesteronic (I made that word up) steroids and use nolvadex, you may be at an increased risk for progesteronic sides, as nolvadex may increase progesterone receptors (Gynecol Oncol. 1999 Mar;72(3):331-6). So besides competing with estrogen at the receptor, these drugs both increase serum test levels, and both drugs may also alter blood lipid profiles. With regards to Clomid and Nolvadex, I’ve found some research that indicates that 20mgs of tamoxifen is equal to 150mgs of clomid for purposes of testosterone elevation, FSH and LH, but tamoxifen did not decrease the LH response to LHRH (Fertil Steril. 1978 Mar;29(3):320-7). Interestingly, Nolvadex can even be used in small doses just as effectively as larger doses, when it comes to sperm indices and spermatogenesis. (“Effect of lower versus higher doses of tamoxifen on pituitary-gonadal function and sperm indices in oligozoospermic men”. Dony JM, Smals AG, Rolland R, Fauser BC, Thomas CM.)So in this case, we can actually use much lower doses than the egregiously recommended 40-60mgs/day. 5mgs a day seems to be as effective as 20, with regards to basal or LHRH stimulated gonadotropin and testosterone response or the E2/T ratio (Ibid). So that makes Nolvadex great for preventing gyno, and superb for Post Cycle Therapy even at lower dosages, but not my favorite Ancillary product during a cycle, unless I need to help my lipid profile or just prevent gyno. I give nolvadex a … Final Grade:B- Buy research Nolvadex Buy Pharmaceutical Nolvadex Aromasin basically is an aromatase inactivator...It actually makes estrogen receptors useless in a sense, because it inhibits the aromatase enzyme from creating more estrogen. This is like having a wall socket but no radio to plug into it… kind of useless, right? Instead of just inhibiting production (as a Type-II anti-aromatase would do) it irreversibly cuts off estrogen production from the enzyme it attaches to. Aromasin can also cause androgenic sides, so it’s not ideal for women, however. It’s not particularly harsh on cholesterol, and can be effectively used with Nolvadex. I’ve seen studies indicating that it reduces estrogen in your body by about 80%, possibly making it too strong, for maximum gains and staying healthy on a long (12 weeks or more) cycle. Aromasin, at 20mgs/day, will raise your testosterone levels by about 60%, and will even help out your free to bound testosterone ratio by lowering your body’s levels of Sex Hormone Binding Globulin (SHBG), by roughly 20% (The Journal of Clinical Endocrinology & Metabolism Vol. 88, No. 12 5951-5956)… It’s perfect for use in PCT, for many other reasons (it interacts more favorably with Nolvadex than other AIs). But it’s not 100% what we want during a cycle… for this reason, I give it a strong… Final Grade:B+ Buy research Aromasin LiquidDex From the research I've done, this seems to be the best ancillary compound around for use on a cycle. First off, 1mg per day of this stuff (J Clin Endocrinol Metab 2000 Jul;85(7):2370-7) was shown to decrease estrogen by about 50% and increase testosterone levels by 58%. That’s a level of estrogen suppression I’m very comfortable with on virtually any cycle. Interestingly, that same study showed that those results were had with .5mgs/day as well. So, since you can elevate testosterone, lower estrogen (but not excessively), and keep healthy joints and lipids, and do this at a half mg per day, I give this my highest rating for an ancillary product to use on a cycle… Final Grade:A Buy research LiquidDex Buy Pharmaceutical Arimidex Letrozole is another type II (competitive) AI. Letrozole is actually a lot more effective than LiquidDex in its ability to pass thru the cell membrane of lipid (fat) cells as well as inhibit the activity of aromatase. In some studies, circulating estrogen levels are totally undetectable in most patients taking Letrozole, and just like LiquidDex, it has even been used in specific cases to increase testosterone to normal levels (from sub-normal ones) and increase LH, and FSH (Epilepsy Behav. 2004 Apr;5(2):260-3). Unfortunately, it does this too well, and although it cleared up my minor gyno lumps, and has been shown to do this in animal studies as well (J Steroid Biochem Mol Biol. 2001 Dec;79(1-5):27-34. Aromatase overexpression transgenic mice model: cell type specific expression and use of letrozole to abrogate mammary hyperplasia without affecting normal physiology.). This got my gyno lumps to the point that they are totally gone now, prolonged use lowered my immune system and gave me joint problems (due to a lack of estrogen). It’s very strong, and maximum inhibition of aromatase in one study was found to happen in women at tiny 100mcg doses (J Clin Endocrinol Metab. 1995 Sep;80(9):2658-60.)If you aren’t on a cutting cycle, training for a contest, or trying to clear up some gyno, Letrozole is not for you. Still, it’s the most potent Aromatase Inhibitor on the market today, so I’ll cautiously give it a … Final Grade:B Buy research Letrozole Buy Pharmaceutical Grade Letrozole Find these and other research grade ancilliary drugs at AG-GUYS.COM. Find all of these and many more Pharmaceutical grade Post Cycle Therapy drugs at: eClenbuterol.com

To understand what happened to poor Billy, in this issue of EliteFitness.com News, we'll examine estrogen and its relationship to male use of anabolic steroids.

Also in this week's EFN, we'll look at drugs you can use to annihilate estrogen in a blinding burst of anabolic goodness! Read on, unless of course you actually want a career in the exotic dancing arts like our friend Billy.

Why Billy Has Breasts: The Story of Estrogen

Before we begin to talk about all the great benefits of anabolic steroids I think it is important to take a moment to talk about side effects and how to prevent them. The biggest source of steroid related side effects comes from the impact anabolic steroids have on your body's production of estrogen. So, here is a quick biochemical over-view of estrogen. Estrogens regulate the growth, differentiation, and functioning of diverse target tissues, both within and outside of the reproductive system. Most of the actions of estrogens appear to be exerted via the estrogen receptor (ER) of target cells, an intracellular receptor that is a member of a large super family of proteins that function as ligand-activated transcription factors, regulating the synthesis of specific RNAs and proteins. This process is almost identical to the action by which anabolic steroids affect protein synthesis.

Estrogen is also a steroid hormone, although not used for athletic enhancement. However, estrogen plays a key role in the use of AAS. Certain steroids, at high enough dosages, can convert via the enzyme aromatase into other hormones; in the case of testosterone-based steroids this other hormone is usually estrogen. Steroids with a dihydrotestosterone (DHT) base are not subject to aromatization; as a metabolite of testosterone its structure is not affected by the aromatase. Steroids with 17-alkylated structures generally convert into weaker estrogens. Some steroids, such as nandrolone (deca-durabolin) or trenbolone (parabolan, or in most people's cases Finaplex) convert into progesterone.

High dosages of steroids for prolonged periods also shut down the body's natural production of certain hormones (particularly testosterone) when steroid therapy is stopped the body attempts to establish homeostasis by adjusting hormonal levels. The average ratio of testosterone to estrogen in a healthy male is 100:1. When drugs increase the testosterone in the body, the body will respond by increasing the estrogen in the body. Additionally, estrogen circulates in the body bound to the protein SHBG (sex hormone binding globulin) as does the testosterone. SHBG is produced in the liver and use of steroids increases the production of this protein; which has a very high receptor affinity for testosterone. With more SHBG in the body, more testosterone is bound, becoming inactive as only free testosterone can activate an androgen receptor. SHBG, however, has poorer receptor affinity for estrogen and more active free estrogen circulates in the body, further altering the hormonal balance. These effects of steroids (i.e. the potential for conversion into estrogen, as well as the disruption of the hormonal balance in the body) can cause serious side effects in male users. Thus, steroid users seek ways to block this estrogen from affecting them.

That is all a very nice and formal way of saying that you need to be taking anti-estrogens when you are using steroids. See, without the anti-estrogens you get all sorts of pleasant side effects, not limited to a nice pair of breasts (with oh -so tender nipples) and extra body fat! Without anti-estrogens you will end up like poor Billy, shaking his titties in the face of wealthy Japanese businessmen. No, seriously, this chapter will explore how to effectively use anti-estrogens to prevent many of the side effects that accompany anabolic steroid usage.

The Drugs Are Your Friends

Oral clomiphene citrate (Clomid) is an ovulation stimulant used to treat ovulatory failure in women. Oral tamoxifen citrate (Nolvadex) belongs to a class of antineoplastics called antiestrogens. It is used to treat breast cancer. Body builders use both of these drugs. Why on earth would they do that?

The answer is that both of these drugs are anti-estrogens. The term anti-estrogen is a little inaccurate. This class of pharmaceutical does not engage in some sort of matter/anti-matter reaction, annihilating estrogen in a blinding burst of anabolic goodness. Rather, let us think of the classical anti-estrogen drugs (such as nolvadex and clomid) as estrogen receptor antagonists (ERA). These ERAs are chemicals that are close enough in structure to estrogen to fit into the estrogen receptor site; however these chemicals do not have the same chemical effect as estrogen. The result is that any estrogen produced by the body or exogenous estrogen cannot find an open receptor site to attach to. The free-floating estrogen then presents far less problems to homeostasis.

There is a lot of conflict over using nolvadex, clomid and other ERAs. The regulation of estrogen-induced cellular effects is a multi-step molecular process. The diversity of estrogen and anti-estrogen effects on cellular functions is also modulated by tissue and gene specificity. This diversity of reaction may be explained by different levels of molecular regulation, including the presence of two distinct estrogen receptor isoforms (ER alpha and ER beta), their binding to activator or co-repressor transcriptional proteins, and their affinity to different DNA binding domains of target genes (estrogen responsive element or API). These mechanisms may account for the specific responses to estrogens or anti-estrogens according to tissue, cell or gene level.

Therefore, in English, a drug like nolvadex, which targets breast tissues, is going to do a better job of preventing gynocomastia than is clomid. However clomid has the benefit of boosting the levels of follicle stimulating hormone, which helps restore the bodies natural testosterone levels and protects against testicular atrophy.

Many people stop using their ERA drugs when they end the cycle. That is a terrible idea. Clomid, as we have already discussed, helps immensely with your recovery processes. But remember, there is almost always an estrogen backlash to having been using testosterone drugs for so long. Therefore, many symptoms of high estrogen levels appear after the cycle. I would continue to use both Clomid and Nolvadex for up to 3 weeks after the last of the drugs have left your body. Remember, if on Friday you take 500 mg of a longer acting drug like Sustanon, then don't consider the following few weeks as truly off time. That is why it is important to know how long the drugs are effective in your body and yet another reason to switch to faster acting drugs in the last few weeks of a cycle.

Effective dosages of these two drugs are debated. I would recommend that the two drugs be used together, Nolvadex at 20 mg per day, and clomid at 50 mg per day. If Nolvadex is used by itself, 20-40 mg are sufficient. 50-100 mg of clomid can be used if clomid is the only ERA drug. Clomid should be used for two weeks after the last steroid injection to help return your body to its natural hormonal state. Nolvadex and Clomid are mildly expensive, but very available because they are not scheduled drugs and can be imported.

There is a second class of drug used to combat estrogen side effects from what is grandly called steroid therapy; there are aromatase inhibitors. As mentioned previously in this chapter, the body can convert testosterone into estrogen using the enzyme aromatase. This second group of drugs, which I will call the inhibitors, prevents this process from occurring at all. This class of medication is generally only prescribed for severe conditions and is generally more expensive then any of the ERA.

Teslac, (testolactone), has fallen out of favor for several reasons. First of all, almost one gram daily is needed to achieve sufficient estrogen synthesis inhibition. This makes this a very expensive drug to use. Also, it is currently a scheduled drug because it is a testosterone derivate.

Cytadren (aminoglutethimide) is a better choice, requiring dosages of between 250-500 mg per day to suppress estrogen synthesis. 250mg cytadren doesn't cause significant desmolase inhibition, so there would still be cortisol and other steroids, while estrogen is minimized! Cytadren is used therapeutically to combat Cushing's syndrome because it also interferes with the body's ability to synthesis cortisol. Sounds like fun, huh ... no cortisol, no estrogen. What a fantastic environment. Tell that to Andreas Munzer! Cytadren can cause cysts as well as effect things like blood clotting. It is reported that Munzer used 1-2g(!) of cytadren/day! Therefore cytadren use should be done with precision.
Arimidex (anastrozole) is a drug designed to combat second stage breast cancer. It is an extremely potent drug; one pill per day is sufficient to almost entirely inhibit estrogen in the body. However, the draw back is that this one pill per day can cost you around ten dollars.

The final conclusion about inhibitors is that these are far more powerful drugs then the ERA. All the drugs listed above effect a much wider hormonal spread then the anti-estrogens and they are also going to cost you a lot more. Of all the drugs mentioned, I think that arimidex is the most useful drug for the body builder. Duchaine helped promote cytadren, particularly because of its anti-catabolic ability to suppress cortisol. But, even he acknowledged the double-edged sword that this drug was. Too little cortisol is painful to the joints and in the end, extremely dangerous. I would not recommend the use of cytadren, but I have provided the moderate dosage schemes. The bottom line: These are not drugs to pop like M&Ms.

The Argument Against Our Little Friends

But these drugs decrease your gains right? Damn it. I hate hearing that phrase clutched to... you guessed it... peoples' breast like a mantra. First of all, there is no way of telling what your gains would have been like without nolvadex or clomid. The scientific evidence that gave rise to this whole dispute (which I believe Duchaine had a hand in too) is that in addition to its anti-estrogenic action requiring estrogen receptors (ER) and leading to growth arrest of breast cancers, studies have previously shown that the anti-hormone tamoxifen (nolvadex) is able to block EGF, insulin and IGF-I mitogenic activities in total absence of estrogens. Thus the excessive use of anti-estrogens will actually result in a loss of some of the most anabolic of hormones (insulin and insulin-like growth factor 1). Steroid antagonists can inhibit not only the action of agonist ligands of the receptors they are binding to, but can also modulate the action of growth factors by decreasing their receptor concentrations or altering their functionality.

Translation: Yes, you are probably compromising your anabolic state by using ERA. But does that mean they shouldn't be used? No. I have heard statements so ridiculous as "Don't use anti-estrogens, they cut into your gains and cost too much. Just get surgery". Lovely, just fucking brilliant. Sure, like surgery isn't going to cut into your workouts or your gains.

Anti-Estrogens

Lets consider the top drugs used to combat the estrogen based side effects of anabolic steroids.

Clomid

Taken daily during a cycle as an anti-estrogen, dosages range between 50-100 mg per day if used exclusively. If combined with Nolvadex, 50 mg per day is sufficient. For more information on this drug, see the chapter entitled Some Specific Drugs Considered.

Nolvadex

If used alone then 20-40 mg are needed. Some athletes, because of evidence that it negatively impacts various growth factors in the body, dislike this drug. If combined with clomid, 10-20 mg are sufficient. For more information on this drug, see the chapter entitled Some Specific Drugs Considered.

Proviron

This drug binds to androgen receptors but is also helps prevent excess testosterone from converting into estrogen. I consider this effective when stacked with either clomid or nolvadex. 1 pill will do if combined with either 50 mg of clomid or 20 mg or nolvadex. On its own, I suggest at least 2 pills.

Arimidex

This is a very potent drug that prevents the body from converting testosterone into estrogen. The drawback is that is very expensive. The minimum effective dosage is around between a quarter and a half of a milligram/day. This drug does not need to be combined with any other during the cycle; however I recommend you begin using arimidex two weeks prior to commencing your cycle so that the drug can effectively eliminate the enzyme that permits conversion of testosterone to estrogen. Clomid is still useful in the post cycle period. For more information on this drug, see the chapter entitled Some Specific Drugs Considered.

Remember, anti-estrogens are not scheduled. It is not against the law to import them and there are many online resources that do this with accuracy and reliability. Don't gamble with this aspect of your health and don't start until you have all that you need to cover yourself throughout the whole cycle. There is no excuse for not having plenty of clomid and nolvadex on hand.

So, back to our fiend Billy. If he had only taken a few simple precautions, he would not find himself in the predicament he is in now. What has Billy been up to lately? Well, when last I heard from him, he was working at the Hooters - and not in the kitchen I might add.

Here's some related threads to discuss on the EliteFitness.com Discussion Forums:

• Introducing the top Gynecomastia Surgeon in the country.
• another question....clearing gynecomastia while on cycle
• Treatment for Gynecomastia
• How long does it tak for clomid to kick in for a noticeable effect?
• Clomid & Nolvadex – The Dark Side
• Alternatives to Clomid??
• I don't get the benefits of hcg over clomid/nolva IF one's testes have NOT shrunk
• Clomid side effects?
• Will letrozole + nolvadex reverse Gyno?
• Use Nolvadex? Nipples Puffy
• arimidex vs nolvadex PCT
• Nolvadex Will Not Get Rid Of Gyno
• Is there a OTC Supp. Alternative to Proviron? Like something that does the same but doesn't have the same active ingredient as it?
• Proviron/Anavar/Primobolan cycle Comments
• Proviron as anti-estrogen - TRUTH or FALSE?
• Proviron - Your thoughts?

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