akn
Musclechemistry Member
Description:
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 thirdgeneration
selective oral aromatase inhibitors.826 It acts by
blocking the enzyme aromatase, subsequently blocking
the production of estrogen in the body. Since many for.ms
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 dose of 1mg (commonly 1
tablet) capable of producing 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. Side effects like hot flashes and
hair thinning can present themselves during therapy, and
would be much more severe in pre-menopausal patients.
For the steroid-using male athlete, anastrozole is applied to
minimize the side effects associated with elevated
estrogen levels secondary to anabolic/androgenic steroid
use. In comparison with traditional methods such as
Nolvadex and Proviron, anastrozole is significantly more
effective at controlling estrogen.
History:
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
tamoxifen use. Substantial data was needed to shift
prescribing trends away from such an established
medication treatment. Shortly after its release, anastrozole
was investigated as part of an extremely large multicenter
double blind trial based out of Rome (ATAC). The study
evaluated the use of anastrozole and tamoxifen, alone or in
combination, in 9,366 postmenopausal women following
breast cancer surgery. The results favored anastrozole over
tamoxifen at promoting disease regression and improving
overall survival rates. Upon publication of this trial in 2002,
anastrozole emerged as a new contender for the
adjunctive treatment of postmenopausal breast cancer.827
828 Around this same time the drug was also gained
popularity with male bodybuilders and athletes who
began taking notice of the strong estrogen suppression
caused by anastrozole, both in the anecdotal reports of
others and in clinical trials.
How Supplied:
Anastrozole is most commonly supplied in tablets of 1mg.
Structural Characteristics:
Anastrozole is classified as a selective non-steroidal
aromatase inhibitor. It has the chemical designation 1,3benzenediacetonitrile,
a,a,a',a'-tetramethyl-5-(1 H-1 ,2,4triazol-
1-ylmethyl).
Side Effects:
Common side effects associated with the use of an
aromatase inhibitor include hot flashes, joint pain,
weakness, fatigue, mood changes, depression, high blood
pressure, swelling of the arms/legs, and headache.
Aromatase inhibitors may also decrease bone mineral
density, which may lead to osteoporosis and an increase in
fractures in susceptible patients. Some individuals may also
respond to the medication with gastrointestinal side
effects including nausea and vomiting. Aromatase
inhibitors can harm the development of an unborn fetus,
and should never be taken or handled during pregnancy.
When taken by men (as an off-label use) to reduce
estrogenicity during prolonged periods of steroid
treatment, aromatase inhibitors may increase
cardiovascular disease (CVD) risk by retarding some
beneficial properties of estrogen on cholesterol values.
Studies have demonstrated that when an aromatizable
steroid such as testosterone enanthate is taken in
conjunction with an aromatase inhibitor, suppression of
HDL (good) cholesterol levels become significantly more
pronounced. Since the estrogen receptor
agonist/antagonist Nolvadex® generally does not display
the same anti-estrogenic (negative) effect on cholesterol
values, it is usually favored over aromatase inhibitors for
estrogen maintenance by male bodybuilders and athletes
concerned with cardiovascular health.
Administration:
Anastrozole is FDA approved for adjunctive treatment of
postmenopausal women with hormone receptor-positive early breast cancer, first-line treatment of
postmenopausal women with hormone receptor-positive
or receptor unknown locally advanced metastatic breast
cancer, and treatment of advanced breast cancer in
postmenopausal women with disease progression
following tamoxifen therapy. The dosage prescribed in all
instances is 1mg per day until disease progression has
halted. When used to mitigate the estrogenic side effects
of anabolic/androgenic steroid use, male athletes and
bodybuilders will commonly take .5 mg to 1mg of
anastrozole per day. In some instances a half of a tablet (.5
mg) 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
appearance to the muscles and physique, which makes
this agent of interest for dieting/cutting purposes as well.
It is of note that food does not appear to affect the
absorption of anastrozole, so the drug may be taken with
or between meals.
Availability:
Anastrozole is widely available in the U.S. and many other
nations as a prescription drug product. It is also found
readily on the black market.
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 thirdgeneration
selective oral aromatase inhibitors.826 It acts by
blocking the enzyme aromatase, subsequently blocking
the production of estrogen in the body. Since many for.ms
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 dose of 1mg (commonly 1
tablet) capable of producing 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. Side effects like hot flashes and
hair thinning can present themselves during therapy, and
would be much more severe in pre-menopausal patients.
For the steroid-using male athlete, anastrozole is applied to
minimize the side effects associated with elevated
estrogen levels secondary to anabolic/androgenic steroid
use. In comparison with traditional methods such as
Nolvadex and Proviron, anastrozole is significantly more
effective at controlling estrogen.
History:
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
tamoxifen use. Substantial data was needed to shift
prescribing trends away from such an established
medication treatment. Shortly after its release, anastrozole
was investigated as part of an extremely large multicenter
double blind trial based out of Rome (ATAC). The study
evaluated the use of anastrozole and tamoxifen, alone or in
combination, in 9,366 postmenopausal women following
breast cancer surgery. The results favored anastrozole over
tamoxifen at promoting disease regression and improving
overall survival rates. Upon publication of this trial in 2002,
anastrozole emerged as a new contender for the
adjunctive treatment of postmenopausal breast cancer.827
828 Around this same time the drug was also gained
popularity with male bodybuilders and athletes who
began taking notice of the strong estrogen suppression
caused by anastrozole, both in the anecdotal reports of
others and in clinical trials.
How Supplied:
Anastrozole is most commonly supplied in tablets of 1mg.
Structural Characteristics:
Anastrozole is classified as a selective non-steroidal
aromatase inhibitor. It has the chemical designation 1,3benzenediacetonitrile,
a,a,a',a'-tetramethyl-5-(1 H-1 ,2,4triazol-
1-ylmethyl).
Side Effects:
Common side effects associated with the use of an
aromatase inhibitor include hot flashes, joint pain,
weakness, fatigue, mood changes, depression, high blood
pressure, swelling of the arms/legs, and headache.
Aromatase inhibitors may also decrease bone mineral
density, which may lead to osteoporosis and an increase in
fractures in susceptible patients. Some individuals may also
respond to the medication with gastrointestinal side
effects including nausea and vomiting. Aromatase
inhibitors can harm the development of an unborn fetus,
and should never be taken or handled during pregnancy.
When taken by men (as an off-label use) to reduce
estrogenicity during prolonged periods of steroid
treatment, aromatase inhibitors may increase
cardiovascular disease (CVD) risk by retarding some
beneficial properties of estrogen on cholesterol values.
Studies have demonstrated that when an aromatizable
steroid such as testosterone enanthate is taken in
conjunction with an aromatase inhibitor, suppression of
HDL (good) cholesterol levels become significantly more
pronounced. Since the estrogen receptor
agonist/antagonist Nolvadex® generally does not display
the same anti-estrogenic (negative) effect on cholesterol
values, it is usually favored over aromatase inhibitors for
estrogen maintenance by male bodybuilders and athletes
concerned with cardiovascular health.
Administration:
Anastrozole is FDA approved for adjunctive treatment of
postmenopausal women with hormone receptor-positive early breast cancer, first-line treatment of
postmenopausal women with hormone receptor-positive
or receptor unknown locally advanced metastatic breast
cancer, and treatment of advanced breast cancer in
postmenopausal women with disease progression
following tamoxifen therapy. The dosage prescribed in all
instances is 1mg per day until disease progression has
halted. When used to mitigate the estrogenic side effects
of anabolic/androgenic steroid use, male athletes and
bodybuilders will commonly take .5 mg to 1mg of
anastrozole per day. In some instances a half of a tablet (.5
mg) 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
appearance to the muscles and physique, which makes
this agent of interest for dieting/cutting purposes as well.
It is of note that food does not appear to affect the
absorption of anastrozole, so the drug may be taken with
or between meals.
Availability:
Anastrozole is widely available in the U.S. and many other
nations as a prescription drug product. It is also found
readily on the black market.
