Arimidex

[FittGrrl27]

So I have a question...

This is what I understand, and please if I am incorrect let me know!

Nolvadex- blocks estrogen from binding to the receptors, so your body would still produce estrogen but its effects would not be exerted (as much) because it is being blocked.

Arimidex- works by preventing the conversion of steroids made by the adrenal glands into estrogen- so it limits the amount of estrogen the body produces (estrogen that is created when aromatase converts testosterone into estradiole).

HOWEVER- if I am understanding this correctly, Arimidex would then have no effect on the estrogen that is produced by women's ovaries?

From Wikipedia:
Since most of the circulating estrogen is produced by the ovaries, not by conversion of androgens to estrogen, blocking the enzyme aromatase does not significantly decrease the production of estrogen. When aromatase inhibitors are used in premenopausal women, the decrease in estrogen activates the hypothalamus and pituitary axis to increase gonadotropin secretion, which in turn stimulates the ovary to increase androgen production. This counteracts the effect of the aromatase inhibitor.

Im just wondering if it makes sense then for me to be using Arimidex?

Previously I was on 30mg of Nolva per day... Pharmaceutical grade, still getting my period.

If it matters I am also running 10mg Winny, 40mg Anavar, 2IU GH per day, 75mcg T3.

Just wondering if anyone has any thoughts or can shed some light on this for me please

[bubba289]

"Aromatase: An enzyme involved in the production of estrogen that acts by catalyzing the conversion of testosterone (an androgen) to estradiol (an estrogen). Aromatase is located in estrogen-producing cells in the adrenal glands, ovaries, placenta, testicles, adipose (fat) tissue, and brain.

The growth of some breast cancers is promoted by estrogens. For example, the drug letrozole (brand name: Femara) is an antiestrogen sometimes used to treat such estrogen-dependent tumors. The drug acts by inhibiting the enzyme aromatase which lowers the level of the estrogen, estradiol."

since a-dex is an aromatase inhibitor i'm assuming it will inhibit all aromatase without regard to location. i dont think the drug was made with the intention of using it with aromatizable (<not sure if thats even a word) steroids, just to lower the total amount of estrogen in the body.

if that doesnt make sense maybe i'm not clear on what you're asking.

[FittGrrl27]

Originally Posted by bubba289

"Aromatase: An enzyme involved in the production of estrogen that acts by catalyzing the conversion of testosterone (an androgen) to estradiol (an estrogen). Aromatase is located in estrogen-producing cells in the adrenal glands, ovaries, placenta, testicles, adipose (fat) tissue, and brain.

The growth of some breast cancers is promoted by estrogens. For example, the drug letrozole (brand name: Femara) is an antiestrogen sometimes used to treat such estrogen-dependent tumors. The drug acts by inhibiting the enzyme aromatase which lowers the level of the estrogen, estradiol."

since a-dex is an aromatase inhibitor i'm assuming it will inhibit all aromatase without regard to location. i dont think the drug was made with the intention of using it with aromatizable (<not sure if thats even a word) steroids, just to lower the total amount of estrogen in the body.

if that doesnt make sense maybe i'm not clear on what you're asking.

No that makes perfect sense!!! THANK YOU

From what I was reading, the drug is given to POST menopausal women b/c of how it works- and that since Im PRE menopausal that it wouldnt affect the estrogen that is produced by my ovaries... only the estrogen produced from the conversion of testosterone to estradiol.... Im just trying to understand how it works and if it will work- theres not a lot of info for women out there!!!

Also- is 0.5mg every day an ok dose? I was reading that you can take it EOD, just wondering what people think about that?

[bubba289]

Originally Posted by FittGrrl27

No that makes perfect sense!!! THANK YOU

From what I was reading, the drug is given to POST menopausal women b/c of how it works- and that since Im PRE menopausal that it wouldnt affect the estrogen that is produced by my ovaries... only the estrogen produced from the conversion of testosterone to estradiol.... Im just trying to understand how it works and if it will work- theres not a lot of info for women out there!!!

Also- is 0.5mg every day an ok dose? I was reading that you can take it EOD, just wondering what people think about that?

well i really have no experience with women and AI's so i wouldnt feel comfortable saying. i know the beginning dosage for a man is .25mg EOD though, i never see guys using anything more than .5mg ED. .25 mg EOD is just to keep gyno away and to keep bloat down, not to help dry out for a show or anything which is why i'm assuming you're using it.. i'd ask Vadim for dosage ideas, he has experience with women and gear/serms/AI's

its a shame SSB went down, they had alot of good info for women there!

[FittGrrl27]

Ssb?

[CognitiveNutrition]

Originally Posted by FittGrrl27

No that makes perfect sense!!! THANK YOU

From what I was reading, the drug is given to POST menopausal women b/c of how it works- and that since Im PRE menopausal that it wouldnt affect the estrogen that is produced by my ovaries... only the estrogen produced from the conversion of testosterone to estradiol.... Im just trying to understand how it works and if it will work- theres not a lot of info for women out there!!!

Also- is 0.5mg every day an ok dose? I was reading that you can take it EOD, just wondering what people think about that?

1. Letrozole (name Femara) is a type 2.

Letrozole has shown to reduce estrogen levels by 98 percent while raising testosterone levels. The anti-estrogen action of letrozole is preferred by bodybuilders for use during a steroid cycle to reduce bloating due to excess water retention and prevent the formation of gynecomastia related breast tissue that is a side effect of some anabolic steroids. Usage above 2.5 mg/day is known to potentially temporarily kill sex drive. Above 5mg/day for extended periods may cause kidney problems.

2. Vorozole (yet to be approved) is a type 2.

3. Exemestane (Aromasin) is a type 1.

Exemestane is an irreversible, steroidal aromatase inactivator, structurally related to the natural substrate androstenedione. It acts as a false substrate for the aromatase enzyme, and is processed to an intermediate that binds irreversibly to the active site of the enzyme causing its inactivation, an effect also known as "suicide inhibition." In other words, the Exemestane, by being structurally similar to the target of the enzymes, permanently binds to those enzymes, thereby preventing them from ever completing their task of converting androgens into estrogen.

The estrogen suppression rate for exemestane varies from 85% to 95%.

4. Anastrozole (Arimidex) is a type 2.

While officially indicated for women, this drug has proven effective in the off-label use of reducing estrogens (in particular and more importantly, estradiol) in men. Excess estradiol in men can cause benign prostatic hyperplasia, gynecomastia, and symptoms of hypogonadism. Some athletes and body builders will also use anastrozole as a part of their steroid cycle to reduce and prevent symptoms of excess estrogens; in particular, gynecomastia and water retention.

Study data currently suggests that dosages of 0.5mg to 1mg a day reduce serum estradiol by about 50% in men

[FittGrrl27]

Originally Posted by uniquenutrition

1. Letrozole (name Femara) is a type 2.

Letrozole has shown to reduce estrogen levels by 98 percent while raising testosterone levels. The anti-estrogen action of letrozole is preferred by bodybuilders for use during a steroid cycle to reduce bloating due to excess water retention and prevent the formation of gynecomastia related breast tissue that is a side effect of some anabolic steroids. Usage above 2.5 mg/day is known to potentially temporarily kill sex drive. Above 5mg/day for extended periods may cause kidney problems.

2. Vorozole (yet to be approved) is a type 2.

3. Exemestane (Aromasin) is a type 1.

Exemestane is an irreversible, steroidal aromatase inactivator, structurally related to the natural substrate androstenedione. It acts as a false substrate for the aromatase enzyme, and is processed to an intermediate that binds irreversibly to the active site of the enzyme causing its inactivation, an effect also known as "suicide inhibition." In other words, the Exemestane, by being structurally similar to the target of the enzymes, permanently binds to those enzymes, thereby preventing them from ever completing their task of converting androgens into estrogen.

The estrogen suppression rate for exemestane varies from 85% to 95%.

4. Anastrozole (Arimidex) is a type 2.

While officially indicated for women, this drug has proven effective in the off-label use of reducing estrogens (in particular and more importantly, estradiol) in men. Excess estradiol in men can cause benign prostatic hyperplasia, gynecomastia, and symptoms of hypogonadism. Some athletes and body builders will also use anastrozole as a part of their steroid cycle to reduce and prevent symptoms of excess estrogens; in particular, gynecomastia and water retention.

Study data currently suggests that dosages of 0.5mg to 1mg a day reduce serum estradiol by about 50% in men

Thats fine but you totally didnt answer my question! I dont care what it does for men- Im a WOMAN!!!

[CognitiveNutrition]

Originally Posted by FittGrrl27

Thats fine but you totally didnt answer my question! I dont care what it does for men- Im a WOMAN!!!

LOL sorry. Letrozole in low doses I think is better than Anastrozole. But either one should work to lower estrogen levels by preventing T interconversion, thus increasing T levels.

[Vadim Beliaev]

That still does not apply to women.

I should have an answer to this question tomorrow, as i will be talking to an endocrinologist who also worked some time in oncology, and is familiar with prescribing AI's to women suffering from breast cancer.

[FittGrrl27]

Originally Posted by Vadim Beliaev

That still does not apply to women.

I should have an answer to this question tomorrow, as i will be talking to an endocrinologist who also worked some time in oncology, and is familiar with prescribing AI's to women suffering from breast cancer.

Thank you!

Wow Ive got people stumped!!! That was a good question

I really appreciate everyone taking the time to answer this, esp Vadim for going the extra step and actually speaking to an endocrinologist

[FittGrrl27]

So Ive been reading...

What Ive learned is that Arimidex is proven effective in the off-label use of reducing estrogens (in particular and more importantly, estradiol)... and that during the reproductive years, most estradiol in women is produced by the granulosa cells of the ovaries by the aromatization of androstenedione (produced in the theca folliculi cells) to estrone, followed by conversion of estrone to estradiol by 17β-hydroxysteroid reductase. Smaller amounts of estradiol are also produced by the adrenal cortex, and (in men), by the testes.

Sooo, I think I have answered my own question, although not as thoroughly as I would have liked and I still am looking forward to more info!

Thanks

[Vadim Beliaev]

It seems that you were correct. What the endo told me was that AI's (arimidex, femara and aromasin specifically) were ineffective in premenopausal women, just for the reasons that you've outlined. Of course estrogen levels will be lowered, but not significantly.
Not to despair though, there are other alternatives which should prove very effective. Look into fulvestrant (costly), which is a non-selective (meaning it blocks ALL estrogen receptors in the body) pure estrogen receptor antagonist (there are NO estrogenic effects when this binds to a receptor, contrary to tamoxifen, which is a very weak estrogen). Another option is Cytadren/Orimeten (aminoglutethemide), this is very interesting because it will stop the formation of ALL steroid hormones from cholesterol (estrogen included, as well as cortisol) - its use can be dangerous, if you are interested i can give you a lot of insight on how to use it effectively.