The War on Estrogen

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.

Conclusion

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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