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Old 10-21-2009, 06:15 PM
Rex
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Default Anti Estrogen compounds and how they work

Arimidex
Anastrozole
Arimidex (Anastrozole) is what we call an aromatase inhibitor (AI). In clinical use, itīs used to halt the progression of Breast Cancer in women. It works by blocking the aromatase enzyme, which is responsible for the production of estrogen. In athletics and bodybuilding, it is used as an ancillary compound to be added to a cycle of Anabolic Steroids. In this respect it is also used for its estrogen reducing properties, but it has the additional benefit of increasing testosterone levels, as weīll see...

Arimidex Side Effects
Many anabolic steroids aromatize (convert to estrogen via the aromatase enzyme), and this is responsible for many of the unwanted side effects found with anabolic steroid use (acne, gynocomastia, water-retention, etc...). In one study, both .5mg and 1mg doses of Arimidex were shown to decrease estrogen by roughly 50%. The 1mg/day dose also increased testosterone levels by 58% (1). In that same study, in both groups, LH and FSH also went up slightly.

Changes in testosterone and E2 concentrations in normal young men (15 22 yr old) before () and after 10 days of oral anastrozole at 0.5 and 1 mg.(1)

This would seem to suggest that for use during a cycle, a dose of .5mgs/day would be sufficient to combat estrogen-related side effects. It is, however, important to remember that some estrogen is necessary to obtain optimal muscle growth. The lower estrogen levels provided by īdex seems, anecdotally at least, to produce a more "hard" and "quality" look for bodybuilders who have experimented with itīs use in either a cutting or bulking cycle.

Iīd like to point out that the elevation in Testosterone provided by Arimidex is so large that it can be used as a "form" of testosterone replacement therapy for hypogonadal men (2). Clearly, this suggests its use in a post-cycle-therapy (as well as its previously discussed use within a cycle) to regain natural testosterone levels and full functioning of the HPTA (Hypothalamic-Testicular-Pituitary-Axis).

Literature provided by the original maker of Anastrozole (Arimidex, produced by Zeneca Pharmaceuticals) states that stable blood plasma concentrations of the compound are achieved after a mere 7 consecutive 1mg daily doses. Also, Arimidex is just over 80% effective at inhibiting aromatase (3). Thus, if you want to take it for the entire duration of a cycle of anabolic steroids, you can simply start taking it on the same day you begin your cycle. Those are some pretty good numbers, huh?

But can you use it for the entire duration of a cycle? Is it dangerous? Well, certainly reducing estrogen levels in your body is good from a body building point of view, as it reduces water-retention and the potential for gynocomastia (if thereīs no estrogen in your body, you canīt get gyno, regardless of how much progesterone is floating around)(5). Luckily this stuff is very mild on blood lipids (cholesterol) and doesnīt affect them adversely (2), in the studies Iīve seen.

Arimidex and Cholestrol
As previously mentioned, those lowered estrogen levels could possibly (eventually) adversely affect your cholesterol and possibly even your immune function. I am, however, very comfortable recommending Arimidex for relatively long-term use. This should be the ancillary compound of choice for those on long and heavy cycles, especially since it also doesnīt inhibit igf like some other ancillary compounds (insulin-like-growth-factor is an important component of anabolism)(4).


Aromasin
Exemestane
Aromasin (Exemestane) is a steroidal suicide aromatase inhibitor, which means that it lowers estrogen production in the body by blocking the aromatase enzyme, the enzyme responsible for estrogen synthesization. (1)(2)(3)

This stuff was developed to fight breast cancer in post-menopausal women, who need a particularly aggressive therapy, and for whom first line defenses such as SERMS (Tamoxifen) have not worked. This should be our first clue in inferring that this stuff is pretty strong, or at least stronger than some of the other compounds which are used to fight breast cancer.

Aromasin and Side Effects
Aromasin averages an 85% rate of estrogen suppression (4), so itīs clearly a very effective agent for bodybuilders and other athletes wanting to avoid estrogen related side effects such as gyno, acne, or water-retention brought on by aromatizing steroids. Specifically, Exemestane dose this by selectively inhibiting aromatase activity in a time-dependent and irreversible manner (hence the "suicidal" portion of itīs name, I guess).(7)

As with most of the compounds in this class, it also causes a reasonable rise in testosterone levels (6), and as you may have guessed, this rise in testosterone means that Exemestane can also cause androgenic sides(8)(9)(10). exemestane is very effective at both lowering estrogen (estradiol) and raising testosterone:
Estrogen and androgen plasma levels after 10 d of daily exemestane (25 or 50 mg) in healthy young males (mean ą SD; n = 9-11). To convert to Systeme International units: estradiol, picomoles per liter (x3.671); estrone, picomoles per liter (x3.699); androstenedione, nanomoles per liter (*0.003492); and testosterone, nanomoles per liter (x0.03467). (13)

So we can see that 25mgs is a very effective dose from that chart, right? As an added benefit, exemestane not only increases testosterone and lowers estrogen, but it also increases IGF levels (11).Additionally Worth noting is that Aromasin may possibly be less harsh on blood lipids (14)than some of the other (similar) compounds we use in the world of bodybuilding or athletics (other AIīs). It also has, at best no effect on IGF, and at worst could lower (13) it. AIīs are very tricky with regards to inconsistencies in IGF levels.

Unfortunately, you need to take Exemestane for a week to reach steady blood plasma levels of it, and exemestane has a ― life of 27 hours (12.).

The ability of exemestane to lower estrogen levels by the aforementioned 85% makes it a very nice choice for use in any cycle where aromatizing steroids are used. In addition, since itīs not too harsh at all on blood lipid profiles, itīs a very good choice for longer cycles. Itīs ability to raise both testosterone levels also seem to suggest that it would be a very nice addition to a Post-Cycle-Therapy (PCT).

Clomid
Clomiphine Citrate
Clomid is a drug given to women for use as a fertility aid. It is a SERM (Selective Estrogen Receptor Modulator) which acts by actually binding to the estrogen receptor and thereby blocking estrogen from doing the same. Clearly, this is advantageous when it binds to breast tissue, and prevents estrogen from binding there to cause gynocomastia (although it is not nearly as effective as nolvadex for this purpose). It also opposes the negative feedback loop that the body has with regards to estrogen and the HPTA (Hypothalamic-Pituitary-Testicular-Axis), and this in turn stimulates LH (Leutenizing Hormone) and FSH (Follicle Stimulating Hormone). LH and FSH, in turn stimulate the release of testosterone. Clearly this is advantageous to bodybuilders and athletes coming off of a cycle, and beginning their post-cycle-therapy. What we have in Clomid is essentially a drug that acts as a preventative measure against gynocomastia, as well as a drug that acts to raise endogenous (natural) testosterone levels. Usually, it is compared with another SERM, Nolvadex, for those reasons.

Clomid, however, is much weaker than nolvadex in a mg for mg comparison, with roughly 150mgs of clomid being equal to 20mgs of nolvadex (1).It should be noted, however, that 150mgs of clomid will still raise testosterone levels to approximately 150% of baseline value(1). You donīt have to use 150mgs, however; in my research, Iīve found that doses as low as 50mgs will show improvements and elevations in testosterone levels (4). In fact, my original Post-Cycle-Therapy regime (as suggested by Dan Duchaine in the original Underground Steroid Handbook) was 100mgs per day for a week and 50mgs/day for a week. Donīt laugh& for the late 90īs, when most anabolic steroid users didnīt even know how to use Clomid, it was considered a "state of the art" PCT routine. I suspect that Duchaine originally introduced this compound to the steroid using community.

Clomid, just like nolvadex, is very safe for long term treatment of lowered testosterone levels (2), with some studies showing its safety and efficacy for up to four months. And post-cycle, when steroid users are suffering form lowered testosterone levels, is when clomid is most effective.

I used to run Clomid for about 3 weeks post cycle, at 100-150mgs. Any more than that, and I experience emotional side effects (no, really) due to the excess amount of circulating estrogen I have in my body. All of that extra estrogen tends to make me moody, and it gets hard to squeeze workouts and cardio in-between reruns of "Sex & the City" (ok, Iīm exaggerating).

Clomid Side Effects
A problem arose during a very aggressive Clomid PCT routine once. I was taking pretty high doses (150mgs/day) of clomid for an extended time (over a month) and was having vision issues. When I looked into the subject more closely, this was a common occurrence with steroid.com members. Upon further investigation, I found out the optic neuropathy (a fancy way of saying "vision problems") was actually very common with clomid usage (5)(6).Since I already wear contact lenses, Iīve had to remove Clomid from my PCT routine.
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