Rationale for the Use of Aromasin with Tamoxifen During
Post Cycle Therapy
Aromasin (Exemestane) is one of those weird
compounds that nobody
really knows what to do with. What we generally hear about
it makes it very uninteresting…It’s a third generation Aromatase
Inhibitor (AI) just like Arimidex (Anastrozole)
and Femera (Letrozole). Both of those two drugs are very efficient at
stopping the conversion of androgens into estrogen, and since we have
them, why bother with Aromasin? It’s a little harder to get than the
other two commonly used aromatase inhibitors, because
it’s not in high demand, and there’s never been a readily apparent
advantage to using it. And I mean…lets face
it: It’s awkward-sounding. Aromasin doesn’t have much of a ring to it,
and exemestane is even worse. Arimidex has a
bunch of cool abbreviations ("A-dex" or just ‘dex) and even Letrozole
is just "Letro" to most people. Where’s the cool
nickname for Aromasin?
Aromasin/exemestane? A-Sin? E-Stane? It just doesn’t work. It’s the
black sheep of AIs. And why do we even need it when
we have Letrozole, which is by far the most efficient AI for stopping
aromatization (the process by which your body converts testosterone
into estrogen)? Letro can reduce estrogen levels by 98% or greater;
clinically a dose as low as 100mcgs has been shown to provide maximum
aromatase inhibition (2)!
So, you like the way Arnold looks? Those big arms, that barrel chest,
those biceps that are unmatched to this day!
Let’s face it, Arnold was a god among men when it came to bodybuilding.
Small bones and small waist allowed him to compete at a tiny 220lbs.,
but look like he was 250lbs.+ The man was just amazing.
I was recently contacted by a girl I used to know, who was taking GH,
Steroids and Thyroid meds. It seems that she went to her
doctor, had a blood panel done, and her thyroid levels were as low as
the test could measure. And unfortunately, I was contacted to help her
fix this problem, out of the blue…
But what I uncovered in my research is going to become a part of
“Thyroid-PCT” for both men and women, and
it’s going to involve a compound that we’ve been using for (regular)
Post-Cycle Therapy (PCT) for years.
I’m talking about HCG (Human Chorionic Gonadotropin), oddly enough. And
dishearteningly, since she happens to do her
‘research’ at places that ubiquitously and powerfully advocate total
nonsense, she didn’t even know that
HCG is a medication indicated for females, not males; she’d only seen
it spoken about as an ancillary or PCT compound for men. I
will wager that most people who do know what HCG is commonly used for
typically wouldn’t ever suspect it could be used as a thyroid
function stimulator.
Now, the thyroid gland is quite resilient, and usually recovers its
function reasonably quickly…but since she had been using
several drugs, all of which affected her thyroid in one way or another,
her thyroid didn’t recover within the usual 6-8 weeks after
cessation of her thyroid meds. In fact, it didn’t do much of anything.
First, I’ll tell you a bit about how she got in this mess, and how the
thyroid gland functions. As is very common with women who
use anabolics, she didn’t’ do anything resembling traditional PCT after
her Thyroid/Steroid/GH cycle; she just stopped
taking everything and figured she’d recover. The first time she tried
that (on her first cycle, several months prior), severe
depression followed, as did some losing some of the gains she’d made.
This time, however, she was using quite a bit
more drugs, and her thyroid didn’t recover at all as a result. More
severe depression followed, which I thought at the time to
be a result of totally removing the androgens from her body (low
androgen levels are associated with depression). Now I believe it to be
from the psychological implications of the non-receptor mediated
effects of thyroid hormones (1). As usual, she had a look on the
various websites and forums on the internet looking for some kind of
solution…and predictably, knowing the various boards she
frequents (read: wastes) time on, she found no acceptable answers.
Luckily, she avoided listening to the usual Liturgy of Incompetence
that usually gives advice on the internet, and didn’t cause herself
further damage.
After explaining what the number in the test meant relative to her
thyroid function (“you’re screwed”), I
told her that the thyroid gland basically secretes two hormones:
thyroxine (T4) and triiodothyronine (T3). T3 is usually considered the
actual physiologically active hormone, while T4 is just thought to be
converted into T3 by deiodinase. Roughly 80% of T3 is generated from
this conversion. Secretion of T4 is regulated by Thyroid Stimulating
Hormone (TSH) which is produced by the pituitary gland. I’m
sure at this point, most people will see that something that acts on
the Hypothalamic-Pituitary-Testicular axis may also act on the thyroid,
since both are influenced by the pituitary. Anyway, TSH secretion is in
turn controlled through release of Thyrotropin Releasing Hormone (TRH)
which is produced in the hypothalamus (2).
But if the pituitary is involved with thyroid regulation, maybe certain
meds that we use to regulate and restore it for traditional PCT could
be used for Thyroid PCT? At first this seems like an off-the wall-idea,
perhaps even a bit weird or chaotic; but remember, I like theories (and
people for that matter) to be nice and logical, and to have some kind
of intelligence and integrity backing them. Thus, I have no stomach for
chaos or for anyone who does.
So now, by figuring out that much of the thyroid’s action is regulated
by the pituitary (and looking at compounds that could operate
in that nexus of effects), I found HCG; but, even though my logic
seemed sound (funny how it always does to me), I wanted to be 100% sure
about this. That’s when I ended up taking a close ‘molecular’ look at
HCG.
The HCG molecule actually ‘looks’ similar to a TRH molecule! In ‘real’
medical terms, HCG is a
glycoprotein hormone that has structural similarity to TSH (3). Right,
so if Human Chorionic Gonadotropin has structural similarity to TSH,
and TSH stimulates your thyroid, then couldn’t we use HCG to make your
body produce some T4; and then if T4 goes up, we should raise
T3 also. And if we’re getting our bodies to produce T3, then we’ve
fixed our thyroid! So there’s my theory: HCG
can kick-start your thyroid into eventually producing the thyroid
hormones, and ultimately T3.
So here’s what I dug up to support my theory that you can use HCG to
help your thyroid begin functioning again quickly after a cycle:
In one study, performed on rodents, HCG was found to induce expression
of a thyroid-cell growth-promoting gene (4) During pregnancy, excess
HCG can cause hyperthyroidism (5) through cross-talk with the TSH
receptor (6). In fact, at the time of peak HCG levels in normal
pregnancy, serum TSH levels fall, in an exact mirror to the rise of the
HCG peak. This reduction in TSH clearly suggests that HCG causes an
increased secretion of T4 and T3 (7), if we simply realize that this is
just a probable mechanism for maintaining thyroid homeostasis. Often,
Hypothyroidism is even seen as a possible result of the development
resistance to HCG (8); concomitantly, if your thyroid gets too high,
your body will begin to lower its sensitivity to HCG, to compensate and
attempt to lower thyroid levels (9). All of this clearly points to the
ability of HCG to stimulate the thyroid to begin producing T4 and
ultimately produce some T3 again, and getting your thyroid back to
normal.
Now, some of these studies were done on women, and men simply do not
have the high responsiveness to HCG that women do (remember, HCG is a
very important hormone in both conception and pregnancy for women).
Very large doses of HCG still produced definite thyroidal iodine
release (TIR) response in normal men, but it is only a weak thyroid
stimulator when thyroid function is normal (10). I am, however,
confident that if thyroid function is low, both men and women will find
HCG to be a very potent stimulator of their Thyroid Gland, and can use
it to quickly regain normal thyroid levels after use of thyroid
medication. As a quick jump-start for your thyroid, I would suggest
1,000 IU per day for 10 days to two weeks, to stimulate production of
T4 and to normalize your thyroid as quickly as possible.
So what happened to the girl who originally contacted me for help with
her thyroid? Well, I gave her a list of various supplements to use, and
some other advice for normalizing her thyroid. Hopefully this piece
finds its way into her hands somehow, because I think it’s the final
piece of the puzzle for her recovery; well, that and not frequenting
terrible boards.
References:
• Peptides. 2005 Nov 23; [Epub ahead of print]
• Human Anatomy and Physiology, 6th ed. Hole. WCB Press
• Res Clin Endocrinol Metab 2004 Jun;18(2):249-65
• Thyroid. 1992 Winter;2(4):315-9
• Endocrinol Metab Clin North Am. 1998 Mar;27(1):127-49
• Cell Mol Life Sci. 2001 Aug;58(9):1301-22
• Best Pract Res Clin Endocrinol Metab. 2004 Jun;18(2):249-65.
• J Endocrinol Invest. 2003 Nov;26(11):1128-35.
• Thyroid.2004;14 Suppl 1:S17-25.
• J Clin Endocrinol Metab. 1978 Oct;47(4):898-901
Clomid for Thyroid Recovery
After my article on using HCG to help repair the thyroid, I was asked
to go on the radio with Carl Lanore and speak on
that topic. Well, to make a long story short, I did go on the radio and
I didn't end up speaking on that topic at all. What happened is that
the host of the show called me, and we started discussing thyroid
repair and related topics…and I ended up e-mailing him about
five of my strongest articles, and he decided to take a different route
with the interview. He eventually interviewed me on anabolic steroids
and their various mechanisms of action, possible and impossible side
effects, and the media hype surrounding them.
But in the course of my interaction with him, he ended up e-mailing me
an abstract that was in-line with my original piece on thyroid repair.
I'm actually kind of annoyed with myself for not figuring it out
beforehand. If you recall, in that piece, I said:
…that much of the thyroid's action is regulated by the pituitary, and
looking at compounds that could operate in that nexus of
effects, I found HCG…but…even though my logic seemed sound (funny how
it always does to me), I wanted to be 100% sure
about this. That's when I ended up taking a close molecular look at
HCG... (1)
The question is: why didn't I go one step further, and move on to
examining other, similar compounds? I should have, honestly- because
then I might not have needed to have it pointed out to me. Clomid
(Clomiphene Citrate) is used for a very similar purpose as HCG is (to
augment fertility in women), so why can't we use it to help out our
thyroid after prolonged use of thyroid hormones? Well, the answer -as
you may have guessed from the title of this piece- is that we can!
Unfortunately, I lost track of the original study that was sent to me
where Clomid was found to stimulate thyroid hormone production, but I
managed to find quite a few on my own. Before we dive into that, a
brief refresher course on the thyroid gland and the hormones involved
in regulating thyroid function is probably in order.
First, lets find it…
Take your hands, and feel around, in front of your neck. If you're a
man, you can use your Adam's apple as a point of reference. Your
thyroid is just below that, and above the top edge of your breastbone.
If you're a woman and you are using your Adams apple as a point of
reference, then your career in professional bodybuilding has apparently
taken its toll on you.
Anyway, the thyroid gland is made up of two lobes (one on the right and
one on the left). These lobes are connected by a narrow band in the
middle, called the isthmus. From the isthmus, a thin band of tissue
called the pyramidal lobe extends upward. If you use your imagination,
it looks kind of like a butterfly with the left and right lobes being
the two “wings.” Alternately, it just looks like a
very detailed Rorschack blot to you. Anyway, the thyroid gland
partially wraps around your voice box (larynx) and windpipe (trachea),
both of which are found right by where your hand was a second ago (you
can put your hands down now). The “wings” of our
thyroid butterfly are kind of snuggled in behind your neck muscles, at
the top of your breast bone (2).
Now that we're on the same page concerning the location of the thyroid
gland, here's what it does: the thyroid gland secretes thyroxine
(typically referred to as T4) and triiodothyronine (typically referred
to as T3). T3 is the “active” hormone, with T4
being converted into T3 by an enzyme called deiodinase; about 80% of
your T3 comes from T4 being converted by this enzyme. T4 secretion is
regulated by Thyroid Stimulating Hormone (TSH), which is produced by
the pituitary gland. TSH is, itself, controlled primarily through
release of Thyrotropin Releasing Hormone (TRH), which is produced in
your hypothalamus (2).
So how does Clomid fit into this picture? And how can we use it as part
of our thyroid PCT?
Well, in one study I looked at, the researchers concluded that it is
evident from their investigation into the matter that Clomid must
either act via the hypothalamus or directly over the pituitary to
increase TSH secretion, which of course is then followed by increased
thyroid activity (3). Sounds promising for us, if are looking for a
drug to aid in a speedy recovery of normal thyroid function after
prolonged use of thyroid hormones. In fact, in some cases, Clomid is
actually used in conjunction with thyroid replacement for the treatment
of a luteal-phase defect in patients with subclinical hypothyroxinemia
(4).
I do need, however, to state at this point that this will probably be a
much more effective therapy for thyroid repair in women than it will in
men, as was the case when I introduced HCG for this purpose. In women,
body temperature is one of the indicators for ovulation and the various
stages of the menstrual cycle. This is because a specific temperature
range in a woman's BBT (Basal Body Temperature) is required for
successful reproduction.
All of this means that HCG is therefore going to be much more effective
at repairing a woman's thyroid then a man's, simply because their
bodies are much more sensitive to the compounds we're discussing here.
Does that mean that this method won't work for men as well as women?
Certainly not. As was the case with HCG, both of these compounds will
work to repair the thyroid - specifically, by increasing TRH output and
stimulating thyroidal activity.
And, as was the case with HCG, I can support my claim that it works for
men as well as women. In the final study I looked at, 100 mg of Clomid
was given once a day to two groups of healthy male volunteers for
either 5 or 12 straight days, respectively. In the 5-day group, on day
5, a slight increase in TSH was observed, although before that, there
was a slight decrease. In the 12-day group, the response of TSH to TRH
showed a slight (non-significant) increase after 5 days and a
significant increase after 12 days on Clomid. The researchers concluded
that the observed results indicate that Clomid exerts an [(in my eyes)
stimulatory] influence directly on thyroid function (5). But, keep in
mind that the effects didn't even start until day five, and increased
as Clomid therapy continued. I'd therefore recommend 100mgs/day of
Clomid for a minimum of 12 days, and even up to three to four weeks at
that dose, to speed up thyroid recovery.
So there you have it, an unplanned part two to my article on using HCG
to repair your thyroid. Clomid at 100mgs/day in either males or females
should help get thyroid function recovered as quickly as possible.
References
• Applied Anatomy and Physiology, 6 th ed. John W. Hole Jr.
Fareston is a Selective Estrogen Receptor Modulator (SERM), not unlike
its more popular cousins Nolvadex and Clomid. Just
as we see with Nolvadex, Fareston is used to treat breast cancer in
post-menopausal women. It does this by exerting estrogen antagonistic
effects in certain tissue, most notably, breast tissue. This is
actually the same mechanism of action found in Nolvadex. This is why
Nolvadex is often recommended to bodybuilders who are trying to avoid
gynocomastia (growth of breast tissue in males). SERMs, in addition,
have several other well known effects in men, which are not simply
limited to preventing the abnormal growth of breast tissue.
At the hypothalamus and pituitary, estrogen acts in cooperation with
the male body’s negative feedback loop to send a signal to
decrease the secretion of LH, and when LH secretion is lowered, so are
natural testosterone levels. SERMs, like Fareston, possibly act as an
estrogen antagonist in the hypothalamus and pituitary, in order to
increase testosterone production. Thus, although it hasn’t
been studied to any great degree, it’s highly likely that Fareston is
capable of increasing testosterone in the same way that
Nolvadex it, as it’s androgenicity:estrogenicity ratio is 5x that of
Nolvadex (1). It may also be better than Nolvadex for reasons
that are of particular interest to steroid using athletes and
bodybuilders.
Fareston differs from Nolvadex in several ways, however- even though
it’s very similar to it in others. Firstly, the risk of
certain side effects (although relatively rare with Nolvadex) is
actually quite a bit lower with Fareston. However unlikely these risks
are in the first place, the risk of stroke, pulmonary embolism, and
cataract is probably lower with Fareston than with Nolvadex. This is
going to be of interest to people who have issues with “floaters” in
their vision, which is sometimes caused by Nolvadex and Clomid, as this
product may represent
significantly less occular toxicity. It also differs slightly from
Nolvadex in its potent with regards to improving lipid (cholesterol)
profiles. In terms of improving bone mineral density, Fareston is
roughly equal to Nolvadex.(2)