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