Know Thy Enemy

Estrogen. It's definitely not a hormone we bodybuilders want circulating in our bodies. If it were up to us, there wouldn't be a damn drop of that stuff around. I mean, after all, it's to blame for everything wrong with a man's world. Lost your big promotion after grabbing the receptionist's ass? It was estrogen. Couldn't convince that drunk girl to come over last night? Estrogen was behind it! Did your favorite football team get spanked Monday night? Yep, someone must've spiked their Gatorade with estrogen!

Okay, okay, so maybe I'm exaggerating just a little. And sure, we need just a smidgen of that crap in order to function properly. Still, with all of estrogen's negative effects – lowering of GnRH, LH and Testosterone; decreasing lean body mass; increasing fat mass; Richard Simmons, etc. – it's no wonder why we hate the stuff so much.(1,2)

The increasing fat mass, in turn increases aromatase activity, which in turn causes further depression of Testosterone levels and a preferential storage of abdominal fat, eventually leading to a state of hypogonadism.(3) Yikes! Even worse, estrogen has recently been implicated in both benign prostate hypertrophy and prostate cancer! It's possible that the correlation between increased Testosterone and prostate cancer occurs because of the simple fact that more T is being aromatized to estrogen, not because of Testosterone itself.(4, 5, 6)

Speaking of aromatase, this should be a very real worry to you. Why? Well, as you age, levels of this particular enzyme can start to increase and cause a general decrease in both free and total Testosterone. Not only this, but you become less responsive to the effects of LH. These particular changes cause the usual decrease in lean body mass and increase in fat mass (stemming from a decrease in oxidation of fat) that you see with older guys, despite their efforts in the gym. These guys may also complain of sagging libido, loss of energy, decreased cognitive function and strength, and can just plain turn into grumpy bastards! (7, 8, 9, 10, 11)

Hence, the idea of Testosterone replacement. It works to reverse these problems, but the solution is only temporary and you must be administered Testosterone for the rest of your life. I could handle that, but some guys find it rather troublesome and expensive. So what to do? Well, I'll give you the answer in a little bit, but first, I have to get the younger guys a reason to be interested, as well as give the older guys even more of a reason to worry about their estrogen and Testosterone levels. Warning: This next part could be frightening!

Xeno: The Warrior Princess

What's the big commotion about? What's the cause of all this stress? They're called xenoestrogens. Think of them as an ex-girlfriend who goes around telling everyone that you have a tiny penis after a bad breakup. These Sci-fi Channel-sounding substances are actually hormone-like chemicals found throughout the environment. They can mimic the effects of estrogen in your body and antagonize the effects of Testosterone and other hormones. They can also disrupt the synthesis and metabolism of hormones.(12) This can lead to an increase in estrogen levels in men and a decrease in T levels. In fact, it has! (13,14,15,16,17,18)

This suppression of Testosterone can have detrimental effects such as decreased strength, decreased muscle mass, and increased fat tissue, even in young men.(2) The effects are even worse for older men, as they have to deal with their already decreasing T levels. Xenoestrogens have even been implicated in certain cancers, including prostate and testicular cancer, as well as benign prostate hypertrophy.

In short, xenoestrogens can have the same negative effects as estrogen.(19, 20) The only difference is that they can be easily absorbed into your body. Unlike natural estrogens, these suckers aren't easily broken down, remain intact in the environment for years, and can accumulate in the fat tissue of humans.(21, 22, 23)

The Enemy is Everywhere!

The biggest problem, besides their effects, is that these chemicals are lurking throughout your environment. We get them through the food we eat, household products, lubricants, pesticides, plastics, detergents, and many other sources. Some of these chemicals have been banned, yet are still readily found in the environment, even after 20 years of discontinued usage! A few examples are pesticides, like DDT, endosulfan, methoxychlor, kepone, and toxafene.

Bisphenol A is used worldwide in the manufacturing of polycarbonate plastics found in storage containers and baby bottles. It also happens to be a very potent estrogen agonist. Even pharmaceuticals like cimetidine and birth control pills may play a role in terms of estrogen mimicking. Ordinary household products like detergents, surfactants, and paints have breakdown products called nonylphenol and octylphenol that have estrogenic effects. The spermicide and lubricant called nonoxynol may be metabolized into nonylphenol. However, before you throw out your Trojans, nonylphenol is an extremely rare exception, as it may act as a slight androgen agonist. Still, be careful.

Polychlorinated biphenyls, or PCB's, stem from adhesives, fire retardants, and certain waxes. These are also very potent estrogen agonists. A lot of these chemicals find their way into our bodies by ingestion of food, drinking water, or simple inhalation. In terms of inhalation, chemicals like Benzo[a]pyrene and 3,9-dihydroxy-dmba are both resultants of fossil fuel combustion.

What's even worse is the fact that these chemicals are agonists at the alpha receptor subtype.(24,25,26,27,28,29,30,31) These xenos may even act synergistically with one another.(32)

Oh yeah, and for you "herb" lovers out there, tetrahydrocannabinol, or THC, the active ingredient in marijuana, is also estrogenic.(24) Damn! There goes my lunch break with the guy in the mailroom who likes to listen to the Grateful Dead!

Oh, and although, this doesn't technically fit under the xenoestrogen category, guard your balls with your life! There's some evidence that testicular trauma may increase estradiol levels.(33) So, wear a nut cup the next time you decide to use your classic pick up line of, "Hey, baby, it's cold in here. Can I use your thighs as earmuffs?"

Breaking Out the Artillery!

Now that we know what the enemy is and what it's capable of doing, it's time to arrange a strike force of our own. We must either prepare to do battle or live the rest of our lives locked in a protective bubble (not a plastic one, of course!). So what can we do to minimize the effects of these chemicals? I know a lot of people would suggest using something like tamoxifen or clomiphene, since they're considered to be estrogen antagonists. Well, in terms of preventing estrogen itself from binding to certain alpha receptor sites in areas like the breast, this is great! However, what people need to understand is that these two – tamoxifen more so – are also estrogen agonists in certain tissues as well.

Tamoxifen can even activate the alpha receptor in specific tissues.(34,35,36) Now, I don't know anyone who's gained fat just from using tamoxifen, but then again, rarely is anyone using tamoxifen by itself. Don't get me wrong, though, it's a great help in preventing gyno as well as increasing LH (as is clomiphene) in order to get your testes functioning again.

So, clomiphene and tamoxifen won't be of much benefit since they both increase estrogen levels significantly and don't have an effect on aromatase levels.(10,11) If the goal is to simply increase endogenous LH and Testosterone, then I'm all for them. However, in aging guys, these two compounds won't do as much. In fact, they don't respond to the Testosterone boosting effects of clomiphene to the same degree as younger guys do.

When young men were given clomiphene, their total and free Testosterone increased by 100% and 304% on average. Yet the older men only had an increase of 32% and 8% of total and free T.(10) The antagonism of estrogen still doesn't help in young men exposed to estrogen increasing xenos either.

So what's the solution? Well, it would seem that the solution would be to decrease estrogen itself. The way to accomplish this would be to use some sort of aromatase inhibitor. Cytadren, or aminoglutethimide, used to be the choice drug because of its ability to inhibit the production of estrogen. Unfortunately, it also suppressed the production of corticosteroids as well; thus, it's also referred to as a non-selective aromatase inhibitor. Good for a little while, but when the person stops taking in the drug, cortisol levels would rebound quickly and lead to an accumulation of fat and a general "puffy" look.

Formestane was found to be more potent in terms of decreasing estrogen levels and, unlike aminoglutethimide, it was selective. The only problem is that you have to inject around 250 mg every two weeks just to get a reduction of around 60-70% of estrogen. It has a short duration of action and has now been surpassed by what is the current "big dawg" in aromatase inhibitors. The best drug is Arimidex (anastrozole). This newer, selective aromatase inhibitor has been found to decrease estrogen by as much as 21% more than formestane and only has to be taken one time per day in a little 1-mg tablet. It has a long half life of around 50 hours.(37, 38)

Don't try the "more is better" thing either, as there was no significant difference shown between 1 mg and 10 mg of Arimidex in terms of estrogen suppression. (Also note that food may interfere with its absorption to a slight extent.) It's also been shown to significantly increase Testosterone and LH as a result of the estrogen suppression. Not only that, but it could reduce prostate size. It's also possible that it'll reduce fat mass in areas where estrogen would bind.(39,40) So, Arimidex seems to have all of the benefits that we're looking for. We may not be able to stop the xenos themselves, but we can sure as hell negate their effects on our bodies!

To help give you an idea of their potency, note the following comparison of the ability of the various aromatase inhibitors to inhibit the aromatase enzyme in vitro.(41)

  • Aminoglutethimide (Cytadren) 1
  • Formestane 60
  • Exemestane 60
  • Anastrozole (Arimidex) 200
  • Letrozole 200
  • Vorozole 1000

So, for instance, Arimidex is 200 times more potent than Cytadren in terms of aromatase inhibition. I should note, however, that in vivo, the triazole compounds haven't shown much of a difference in terms of estrogen suppression. So, even though vorozole may appear to be the most potent, it hasn't been shown to surpass the effects of Arimidex. At least, I haven't seen any evidence that points to that, anyway.

Both anastrozole and vorozole have been shown to lower estrogen levels to the point where estrogen can barely be detected, if at all. If vorozole were shown to be more potent than anastrozole, it would be overkill anyhow. Vorozole also has a very short half-life of around 8 hours.

What might work even better would be a combination of clomiphene and anastrozole. This could be a great combo for those with problems in terms of higher estrogen and lower Testosterone levels. This wouldn't be very cheap by any means, however. Over a period of 12 to 16 weeks, the increased T and decreased estrogen levels could produce a rather noticeable increase in muscle size and strength. You could also see other mood boosting and cognitive enhancing effects of increased T, as well as a decrease in fat mass.


Well, hopefully I've convinced you to never wear rubbers, stay in a non-plastic bubble, and hold your breath when you're forced to come out to use the bathroom. Oh, and don't forget, never use any air freshening agents, plastic food containers or detergents. Nah, just joking!

Seriously though, if you can, try to minimize your exposure to these agents and perhaps give Arimidex a try if lab tests indicate that your estrogen levels are the cause of your diminishing progress in the gym. Try that along with the other possible Testosterone enhancing actions, like eating a good amount of monounsaturated fats, getting plenty of protein and fiber, and minimizing your consumption of alcohol. Ditch that lunch break date with Mary Jane, too.

Don't forget, you could also combine clomiphene and/or Tribex-500 with Arimidex. Anything to get that precious T up and beat down that bitch estrogen! Be careful, it's a war out there!


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