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  #1  
Old 03-31-2011, 03:05 AM
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Anastrozole - Arimidex Profile

Anastrozole/Arimidex Profile

Pharmaceutical Name: Anastrozole
Drug Class: Aromatase Inhibitor
Active Life: 48 hours


Anastrozole is an aromatase inhibitor. Aromatase inhibitors prevent the conversion of androgens into estrogen in fat, muscle, breast, and brain (1). The medical use of anastrozole is primarily to inhibit the progression and growth of breast cancer in women by blocking the aromatase enzyme. It has also been used by some doctors to try and treat low testosterone production in men, as well as being used in conjunction with testosterone replacement therapy.

For bodybuilders and strength athletes, anastrozole is used to minimize the aromatization of anabolic steroids, and to a lesser extent for it's ability to raise testosterone levels in users. By reducing the amount of estrogen in a steroid user's body he will be able to avoid estrogen related side effects such as water retention, gynocomastia, etc (2). Obviously this is something that users should be hoping to limit as much as possible.

Interestingly, in addition to decreasing estrogen it has been demonstrated that anastrozole can also increase testosterone levels by up to 58%, along with also raising levels of lutenizing hormone (3). This is quite significant especially when one considers that anastrozole can be used in conjunction with other compounds during a user's post cycle therapy to raise natural testosterone levels once administration of anabolics steroids is completed via the hypothalamic testicular pituitary axis.


Use/Dosing

In the majority of users, .5mgs per day should be enough to prevent any estrogen related side effects related to anabolic steroid use. Even when doses were increased to 1 mg per day there was no change in the amount of estrogen that was able to be reduced as compared to doses of .5mgs per day (3). This would seem to indicate that raising your dosage will show no further results if estrogenic side effects continue to be a problem at a dosage of .5mgs. If symptoms persist the user may have to try a more potent compound such as femara (4).

Having said all of this however, most users will be able to reduce any water retention that they may have, or other estrogen related side effects, with dose less than .5mgs per day. Anecdotally users have reported that doses in the range of .25mgs per day or .5mgs every other day are enough to acheive this result. It is possible to administer anastrozole every other day due to it's active life of 48 hours.

For users using anastrozole during their post cycle therapy the same dosages should apply. There is no need to increase or decrease dosages. It can be run throughout the post cycle period with no ill effects.

Blood levels of the compound should stabilize and reach their peak at about 7-10 days after first administering the drug (5). Therefore it is unlikely that a user would need to frontload with anastrozole or begin taking it before they start administering the anabolics that they plan on taking.


Side Effects/Risks

Anastrozole is seemingly very mild on blood lipids (cholesterol) and has not been shown to affect them adversely (6,7). However it should be noted that in theory if one was to consistently suppress your natural estrogen levels for a long period of time, this would negatively impact your health (including you cholesterol). Despite this there is no scientific evidence that anastrozole can be dangerous for healthy individuals to use, even for extended periods of time.

It would seem then that anastrozole has little in the way of negative side effects associated with it's use. It is by far one of the safest compounds that an athlete can use.

~ By Aboot

References

1. Preclinical pharmacology of "Arimidex" (anastrozole: ZD1033)--a potent, selective aromatase inhibitor. J Steroid Biochem Mol Biol 1996 Jul;58(4):439-45

2. The ATAC Trialists Group. The ATAC (Arimidex, Tamoxifen, Alone or in Combination) adjuvant breast cancer trial in post-menopausal women with early breast cancer. Lancet 2002; 359: 2131-39

3. Mauras N, O'Brien KO, Klein KO, Hayes V. "Estrogen suppression in males: metabolic effects." J Clin Endocrinol Metab. 2000 Jul;85(7):2370-7.

4. Leder BZ, et al. "Effects of aromatase inhibition in elderly men with low or borderline-low serum Testosterone levels." J Clin Endocrinol Metab. 2004 Mar;89(3):1174-80.

5. Taxel P, et al. "The effect of aromatase inhibition on sex steroids, gonadotropins, and markers of bone turnover in older men. J Clin Endocrinol Metab 2000 86:2869—2874

6. Dougherty RH, et al. "Effect of aromatase inhibition on lipids and inflammatory markers of cardiovascular disease in elderly men with low Testosterone levels." Clin Endocrinol (Oxf). 2005 Feb;62(2):228-35.

7. Hayes FJ, et al. "Aromatase inhibition in the human male reveals a hypothalamic site of estrogen feedback." J Clin Endocrinol Metab. 2000 Sep;85(9):3027-35.
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  #2  
Old 03-31-2011, 03:07 AM
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Arimidex (anastrozole)
Anastrozole is an anti estrogenic drug developed for the treatment of advanced breast cancer in women. Specifically, this agent is the first in a newer class of third generation selective oral aromatase inhibitors. It acts by blocking the enzyme aromatase, subsequently blocking the production of estrogen in the body. Since many forms of breast cancer cells are stimulated by estrogen, reducing levels of this hormone in the body may retard the progression of the disease. This is also the fundamental use of tamoxifen citrate (Nolvadex), except nolvadex blocks the action of estrogen at the receptor, not its actual endogenous production. The effects of anastrozole can be very substantial, with a daily dosage of 1mg capable of production estrogen suppression greater than 80% in treated patients. With the powerful effect this drug has on hormone levels, it is usually only prescribed to post menopausal women. Anastrozole was developed by Zeneca Pharmaceuticals, and approved for use in the United States at the end of 1995. The drug was developed as a new adjunct treatment for operable breast cancer in postmenopausal female patients, an area of medicine that had a long history of nolvadex use. Substantial date was needed to shit prescribing trends away from such an established medication treatment.

Most commonly called Arimidex, this substance is a true aromatase inhibitor which works by blocking the aromatase enzyme in the body, thus limiting the amount of estrogen buildup that takes place. This compound has obvious benefits to bodybuilders who use aromatizing steroids such as testosterone. These individuals might face estrogen related side effects such as water bloat and "gyno", but by taking Arimidex while on cycle, the chance of any of these sides are greatly reduced. In studies that have been done, Arimidex has been shown to reduce estrogen in the body by roughly 50%. This is a good balance for bodybuilders , because some estrogen is needed in order for the full anabolic benefits of the steroids being taken to be achieved. These results are typically the same with a dosage of .5 mg a day as they are with a dosage of 1 mg a day, meaning that in most cases, a half tablet a day will be sufficient for estrogen control throughout cycle. Typically, bodybuilders using Arimidex will begin taking it the day they start their cycle, and will run it throughout the duration of steroid administration. It is also important to point out Arimidex’s ability to increase testosterone in the body. Some studies have shown that natural testosterone levels have increases as much as 60% after the use of this substance for 7 days. Because of this, bodybuilders find this drug extremely effective during PCT where as they are trying to elevate natural levels as much as possible in order to avoid a post cycle "crash".

When used to mitigate the estrogenic side effects of anabolic/androgenic steroid use, male athletes and bodybuilders will commonly take a dose of .5mg to 1mg of anastrozole per day. In some instances a half of a tablet taken every other day is sufficient to mitigate the buildup of estrogen. When used with readily aromatizing androgens such as methandrostenolone or testosterone, gynecomastia and water retention are often effectively blocked. Additionally, the use of anastrozole may decrease fat mass, which can also be tied to estrogen levels. The result can be a harder and much more defined look to the muscles and physique, which makes this agent of interest for dieting and cutting purposes as well.

author???
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Old 05-24-2014, 03:16 PM
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aromatase inhibitors

are you sure anastrazole is active in the body for only 48 hrs.?
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Old 05-24-2014, 03:25 PM
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Quote:
Originally Posted by mikestevens View Post
are you sure anastrazole is active in the body for only 48 hrs.?
Pharmacokinetics and pharmacodynamic... [J Clin Endocrinol Metab. 2009] - PubMed - NCBI
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Old 11-15-2014, 02:57 PM
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Arimidex (Anastrozole)

Arimidex seems to have somewhat become the holy grail of anti-estrogens. Due to its limited availability, high price and extreme effectiveness, its become a much desired product on the black market. The compound anastrozole is indeed a revolution in the treatment of breast cancers. It's a new generation of aromatase blocker. Up until recently the main product for this purpose was the androgenic steroid Mesterolone (Proviron). But the problem here was that Proviron was not particularly strong and in the required doses of 50 to 100 mg per day, androgenic side-effects were not uncommon. Proviron is after all a DHT derivative. It could also never be used longer than the cycle lasted, because to some extent (despite readily being deactivated) it was suppressive of natural testosterone production.

Anastrozole seems to do the job more efficiently. In clinical trials a single tab daily proved to have a profound effect. In steroid circles, mostly due to the high cost, experimentation with half and quarter tabs proved it to be almost unbelievably strong. So much, that really half a tab per day suffices for most users.

Anastrozole operates by blocking the aromatase enzyme, the primary enzyme for the conversion of testosterone to estrogen. A steroid that is altered by this enzyme is referred to as an aromatizing steroid, and such steroids can cause estrogen build-up. This has several potential side-effects such as water retention, fat gain and lets not forget gynocomastia (the growth of breast tissue in men). To prevent such effects anti-aromatase products can be used. Often times during a cycle most will want to allow for some estrogen, since it heavily promotes strength and gains as well (increases GH, upgrades the androgen receptor, improves glucose utilization). These people will generally opt for an estrogen receptor antagonist such as Nolvadex (tamoxifen) or Clomid (Clomiphene). These products do not stop the formation of estrogen, but stop the estrogen from exerting its effects by competitively taking up the receptors for this hormone. This allows them to stop any problems dead in their tracks, acting very fast, but upon discontinuation allowing for immediate influx of estrogen again as well. This has the benefit that they can be used as soon as problems arise, and discontinued when they subside, thereby only reducing estrogen-mediated gains for the time-span of the occurring problem (mostly gyno).

Aromatase blockers like arimidex and proviron on the other hand are more useful for those seeking to eliminate estrogen from a cycle of aromatizable steroids all together. People who are willing to settle for slower gains, in an attempt to stay lean throughout, or for those who are truly sensitive to estrogen and do not want to take the risk of problems occurring. And arimidex is the clear weapon of choice here, at least to those who can afford it.

Things one needs to note while using arimidex is that the benefits of estrogen become non-existent as well. First of all that means gains can be drastically reduced. They will be leaner and more qualitative, but they will nonetheless be seriously reduced.
A second problem is that estrogen seems to have a positive effect on cholesterol levels. Since estrogen is reduced, the use of arimidex may have a profound impact on HDL to LDL ratio's in your cholesterol profile. In this aspect the use of Nolvadex is more user-friendly, because despite its anti-estrogenic effects in most tissues, it seems to exert positive estrogenic effects in the liver and promote a better cholesterol profile.

Lastly, the major problem with arimidex is the cost. I've seen people who were willing to fork over 250 dollars for a 28 tablet box of legit arimidex. That's the price of fame. Of course these prices are rididculous, but most people don't really know where to look. I've found the generic anastrozole tabs for as low as 2.2 dollars per tab, which is less than half the average street price. So it all comes down to shopping around a bit. Its not that anastrozole is that expensive to make, just that its patented. Which means that besides legit arimidex, all versions in existence are generics. This also means they could be slightly off on content or impure, if trustworthy at all. So be sure to check this with someone who has tried them or had them tested before buying a generic. The liquidex sells legit for not that much more, Around 3 to 4 bucks per gram and is generally a good buy as well, although content may be off. Since few will be investing in this to mess around with low doses and will generally opt to take 1 mg a day (1/4 cc), this shouldn't be a problem. The anastrozole powder is a real buy at merely 2-3 dollars per mg, but obviously no one will ship that for less than 100 mg orders.

Use:

As mentioned, arimidex is an ancillary that is supposed to be stacked with aromatizing steroids in order to stop all formation of estrogen. Its seemingly very potent, so doses of 0.5 to 1 mg are enough. Some claim that 0.25 mg is enough, but for anyone doing any sort of serious cycle, I would not advise less than 0.5. These steroids are, without exception testosterone, nandrolone, norethandrolone, boldenone and methandrostenolone. And all of their derivatives as well. The drug oxymetholone (anadrol) has estrogenic effects as well, but they seem to be the result of oxymetholone's acidic A-ring activating the estrogen receptor by itself, rather than by conversion to estrogen. So Nolvadex would be more advisable in that case. To understand the whole story, I refer you to my profile on Anadrol.

Although it does block gains, aromatase blockers are generally used for the extent or a certain duration on a cycle, whereas receptor antagonists are used mostly to solve problems. Because it takes some time for an aromatase blocker to take effect (even when aromatase is blocked, there is still a level of circulating estrogen) and again some time to bring estrogen back upon discontinuation (new estrogen needs to be made again), acute problems are best solved with Nolvadex or clomid.

When an aromatase blocker is used, Arimidex is the best choice by far. Proviron may be more apt when using with testosterone, due to its other characteristics and positive benefits on testosterone, but for all other intents and purpose arimidex should be preferred in these instances
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