akn
Musclechemistry Member
Letrozole is a non-steroidal selective third generation
aromatase inhibitor. The structure and activity of this
compound are very similar to that of Arimidex
(anastrozole), and it is prescribed for similar medical
purposes. More specifically, U.S. prescribing guidelines for
letrozole recommend it be used for the treatment of
postmenopausal women with estrogen receptor-positive
or estrogen receptor-unknown (unsure if the cancer is
responsive to estrogen) breast cancer. It is typically used as
a second line of treatment after an estrogen-receptor
antagonist like tamoxifen has failed to elicit a desirable
response, although it is sometimes initiated as the first
course of therapy depending on the circumstances. Male
bodybuilders and athletes find value in letrozole for its
ability to mitigate the estrogenic side effects associated
with the use of aromatizable anabolic/androgenic steroids,
such as gynecomastia, fat buildup, and visible water
retention.
Letrozole represents one of the newer achievements in a
long line of drugs targeting aromatase inhibition. It is
among the most potent estrogen-lowering drugs
developed to date, and has an effect significantly stronger
than non-selective first generation aromatase inhibitors
like Teslac and Cytadren. The dosage of each tablet of
Femara is 2.5 milligrams, which according to product
information was sufficient to lower estrogen levels by an
average of 780/0 during clinical trails. The drug, however,
appears to often remain quite effective in lower doses.The
package insert for the product itself comments that during
clinical studies doses as low as .1 and .5 milligrams
produced 75 and 78% estrogen inhibition, respectively in
many patients.The recommended dose, likewise, reflects a
level that seems to elicit a desired level of inhibition in
nearly all patients. A large number of people may,
therefore, respond well to lower doses of the drug.
History:
The U.S. Food & Drug Administration approved letrozole
for prescription sale in 1997, where it is sold by Novartis
under the Femara trade name. Novartis also extensively
markets the drug in other nations, and more than 70
nations now carry letrozole as an approved drug. The
Femara brand is by far the dominant preparation
worldwide, and is found in such nations as Argentina,
Australia, Belgium, Brazil, Canada, Chile, Czech Republic,
France, Germany, Greece, Hong Kong, India, Netherlands,
New Zealand, Italy, South Africa, Switzerland, and Russia.
Novartis also markets the drug under the Femar trade
name in some other nations including Finland, Denmark,Norway, and Sweden. Additionally, letrozole products can
also be found under such other brand names as Fempro
(India), Oncolet (India), Trozet (India), Insegar (Spain),
Aromek (Poland), Lametta (Poland), Cendalon (Argentina),
Fecinole (Argentina), and Kebirzol (Argentina). Given its
high level of efficacy and strong marketing support,
Femara, and Femar, remain the most popular letrozole
product currently available.
How Supplied:
Letrozole is most commonly supplied in tablets of 2.5 mg.
Structural Characteristics:
Letrozole is classified as a non-steroidal selective third
generation aromatase inhibitor. It has the chemical
designation 4,4'(1 H-1 ,2,4-Triazol-1ylmethylene)
dibenzonitrile.
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:
Letrozo,le is FDA approved for 1) adjuvant treatment of
postmenopausal women with hormone receptor positive
early breast cancer; 2) the extended adjuvant treatment of
early breast cancer in postmenopausal women who have
received 5 years of adjuvant tamoxifen therapy; 3) firstline
treatment of postmenopausal women with hormone
receptor positive or hormone receptor unknown locally
advanced or metastatic breast cancer; and 4) the
treatment of advanced breast cancer in postmenopausal
women with disease progression following anti-estrogen
therapy.The recommended dose of letrozole is one 2.5 mg
tablet administered once per day, without regard to
meals. When used (off-label) to mitigate the estrogenic
side effects of anabolic/androgenic steroid use or increase
muscle definition, male athletes and bodybuilders often
take 1.25 mg to 2.5 mg per day. In some cases a dosage of
a half of a tablet (1.25 mg) taken every other day is
sufficient to prevent the onset of estrogenic side effects.
Availability:
Letrozole is most commonly sold under the brand name
Femara by the international drug-manufacturing firm
Novartis.lt is widely available at the present time.
aromatase inhibitor. The structure and activity of this
compound are very similar to that of Arimidex
(anastrozole), and it is prescribed for similar medical
purposes. More specifically, U.S. prescribing guidelines for
letrozole recommend it be used for the treatment of
postmenopausal women with estrogen receptor-positive
or estrogen receptor-unknown (unsure if the cancer is
responsive to estrogen) breast cancer. It is typically used as
a second line of treatment after an estrogen-receptor
antagonist like tamoxifen has failed to elicit a desirable
response, although it is sometimes initiated as the first
course of therapy depending on the circumstances. Male
bodybuilders and athletes find value in letrozole for its
ability to mitigate the estrogenic side effects associated
with the use of aromatizable anabolic/androgenic steroids,
such as gynecomastia, fat buildup, and visible water
retention.
Letrozole represents one of the newer achievements in a
long line of drugs targeting aromatase inhibition. It is
among the most potent estrogen-lowering drugs
developed to date, and has an effect significantly stronger
than non-selective first generation aromatase inhibitors
like Teslac and Cytadren. The dosage of each tablet of
Femara is 2.5 milligrams, which according to product
information was sufficient to lower estrogen levels by an
average of 780/0 during clinical trails. The drug, however,
appears to often remain quite effective in lower doses.The
package insert for the product itself comments that during
clinical studies doses as low as .1 and .5 milligrams
produced 75 and 78% estrogen inhibition, respectively in
many patients.The recommended dose, likewise, reflects a
level that seems to elicit a desired level of inhibition in
nearly all patients. A large number of people may,
therefore, respond well to lower doses of the drug.
History:
The U.S. Food & Drug Administration approved letrozole
for prescription sale in 1997, where it is sold by Novartis
under the Femara trade name. Novartis also extensively
markets the drug in other nations, and more than 70
nations now carry letrozole as an approved drug. The
Femara brand is by far the dominant preparation
worldwide, and is found in such nations as Argentina,
Australia, Belgium, Brazil, Canada, Chile, Czech Republic,
France, Germany, Greece, Hong Kong, India, Netherlands,
New Zealand, Italy, South Africa, Switzerland, and Russia.
Novartis also markets the drug under the Femar trade
name in some other nations including Finland, Denmark,Norway, and Sweden. Additionally, letrozole products can
also be found under such other brand names as Fempro
(India), Oncolet (India), Trozet (India), Insegar (Spain),
Aromek (Poland), Lametta (Poland), Cendalon (Argentina),
Fecinole (Argentina), and Kebirzol (Argentina). Given its
high level of efficacy and strong marketing support,
Femara, and Femar, remain the most popular letrozole
product currently available.
How Supplied:
Letrozole is most commonly supplied in tablets of 2.5 mg.
Structural Characteristics:
Letrozole is classified as a non-steroidal selective third
generation aromatase inhibitor. It has the chemical
designation 4,4'(1 H-1 ,2,4-Triazol-1ylmethylene)
dibenzonitrile.
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:
Letrozo,le is FDA approved for 1) adjuvant treatment of
postmenopausal women with hormone receptor positive
early breast cancer; 2) the extended adjuvant treatment of
early breast cancer in postmenopausal women who have
received 5 years of adjuvant tamoxifen therapy; 3) firstline
treatment of postmenopausal women with hormone
receptor positive or hormone receptor unknown locally
advanced or metastatic breast cancer; and 4) the
treatment of advanced breast cancer in postmenopausal
women with disease progression following anti-estrogen
therapy.The recommended dose of letrozole is one 2.5 mg
tablet administered once per day, without regard to
meals. When used (off-label) to mitigate the estrogenic
side effects of anabolic/androgenic steroid use or increase
muscle definition, male athletes and bodybuilders often
take 1.25 mg to 2.5 mg per day. In some cases a dosage of
a half of a tablet (1.25 mg) taken every other day is
sufficient to prevent the onset of estrogenic side effects.
Availability:
Letrozole is most commonly sold under the brand name
Femara by the international drug-manufacturing firm
Novartis.lt is widely available at the present time.
