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Arimidex

Generic Name: Anastrozole

Arimidex

 
 

Arimidex is a very new drug developed for the treatment of advanced breast cancer in women. Specifically, Arimidex is the first in a new class of third-generation selective oral aromatase inhibitors. It acts by blocking the enzyme aromatase, subsequently blocking the production of estrogen. Since many forms of breast cancer cells are stimulated by estrogen, it is hoped that by reducing amounts of estrogen in the body the progression of such a disease can be halted.

Product
Price
 
Arimidex 1mg x 28 tablets by Astra Zeneca
$275.00

This is the basic premise behind Nolvadex, except this drug blocks the action and not production of estrogen. The effects of Arimidex can be quite dramatic to say the least. A daily dose of one tablet (1 mg) can produce estrogen suppression greater than 80 % in treated patients. With the powerful effect this drug has on hormone levels, it is only to be used (clinically) by post-menopausal women whose disease has progressed following treatment with Nolvadex (tamoxifen citrate). Side effects like hot flushes and hair thinning can be present, and would no doubt be much more severe in pre-menopausal patients.
It is important to note however, that this drug does not directly convert to estrogen in the body. Oxymetholone is a derivative of dihydrotestosterone, which gives it a structure that cannot be aromatized. As such, many have speculated as to what makes this hormone so troublesome in terms of estrogenic side effects. Some have suggested that it has progestational activity, similar to nandrolone, and is not actually estrogenic at all. Since the obvious side effects of both estrogens and progestins are very similar, this explanation might be a plausible one. However we do find medical studies looking at this possibility. One such tested the progestational activity; of various steroids including nandrolone, norethandrolone, methandrostenolone, testosterone and oxymetholone. It reported no significant progestational effect inherent in oxymetholone or methandrostenolone, slight activity with testosterone and strong progestational effect inherent in nandrolone and norethandrolone. With such findings it starts to seem much more likely that oxymetholone can intrinsically activate the estrogen receptor itself, similar to but more profoundly than the estrogenic androgen methandriol. Clearly if this is the case we can only combat the estrogenic side effects of oxymetholone with estrogen receptor antagonists such as Nolvadex or Clomid, and not with an aromatase inhibitor. The strong anti-aromatase compounds such as Cytadren and Arimidex would similarly prove to be totally useless with this steroid, as aromatase is uninvolved.

Description:

Anastrozole (Arimidex) is the aromatase inhibitor of choice. The drug is appropriately used when using substantial amounts of aromatizing steroids, or when one is prone to gynecomastia and using moderate amounts of such steroids. Arimidex does not have the side effects of aminoglutethimide (Cytadren) and can achieve a high degree of estrogen blockade, much moreso than Cytadren. It is possible to reduce estrogen too much with Arimidex, and for this reason blood tests, or less preferably salivary tests, should be taken after the first week of use to determine if the dosing is correct.
As an aromatase inhibitor, Arimidex's mechanism of action -- blocking conversion of aromatizable steroids to estrogen -- is in contrast to the mechanism of action of anti-estrogens such as clomiphene (Clomid) or tamoxifen (Nolvadex), which block estrogen receptors in some tissues, and activate estrogen receptors in others. During a cycle, if using Arimidex, there is generally no need to use Clomid as well, but (as mentioned in the section on Clomid) there may still be benefits to doing so.


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