I am looking into other drugs to inhibit aromatization. Most of what I find online is from aas forums. Has anybody here had luck, or tried anything other than arimidex? It seems to be the gold standard. I am up to 1 mg a day to keep symptoms of high e2 away and I am feeling very good. But I cannot imagine this dose is sustainable due to its side effects. Any feedback would be greatly appreciated. Thanks!
Aromatase inhibitors other than arimidex?
- Thread starter tmckenzie
- Start date
Gene Devine
Super Moderator
That's pretty much your only option other then changing injection protocol to lower dosages and more frequent injections to eliminate the higher peaks in serum levels that increases aromatase synthesis.
Most men on daily transdermals who absorb well don't need an AI as well.
OTC options simply don't work.
Most men on daily transdermals who absorb well don't need an AI as well.
OTC options simply don't work.
Well, I am on twice weekly sub q, I doubt going to three shots will help. I tried Tds and e was high then too. I am not fat, just the way my body is. The reason the arimidex is not working is I have to take pain meds too. But doing ten times better on 1 mg a day. I feel like I am on trt. I get my e check Saturday to see where I am after 10 days of 1 mg a day. What about aromasin?
GettingAnswers
Member
I have read that many prefer aromasin. I have no experience with it but perhaps some others will chime in.
Nelson Vergel
Founder, ExcelMale.com
Aromasin (exemestane) stays in the body for a shorter time than anastrozole and needs to be given daily. Unlike anastrozole, it is an androgen-like molecule that can have some of the side effects of anabolic steroids. You can see below the molecules of the three most commonly used aromatase inhibitors used in breast cancer:
Now, look at how similar exemestane looks like dehydrotestosterone (DHT), a metabolite of testosterone that is responsible for some of its androgenic effects:
There is published study on the use of Aromasin and testosterone replacement.http://www.ncbi.nlm.nih.gov/pubmed/14671195
The following table was taken from a review paper comparing the latest 3 AIs in the treatment of breast cancer. It shows that at the high doses used for breast cancer, exemestane is a weaker blocker of estradiol. I am not completely sure that is a bad thing since excessive estradiol decreases can be a bad thing for men's sexual and brain function and body composition as reported in some older studies.
Source:http://onlinelibrary.wiley.com/doi/10.1002/cncr.10908/full
The following table shows how exemestane can lower high density lipoprotein (HDL- the "good" cholesterol) and triglycerides much like anabolic steroids (and DHT) do.
Like oral androgen products, exemestane may also increase liver enzymes:http://livertox.nih.gov/Exemestane.htm
Like oral androgen-like products, it has also been reported to improve lean mass in women treated for breast cancer: http://www.ergo-log.com/exemestane.html
Some bodybuilding forums speculate that Aromasin is better than anastrozole since it completely deactivates the estrogen receptors. The table above does not support that statement. However, I am curious to see sexual function data comparing TRT plus anastrozole or exemestane to see if the androgen-like nature of exemestane makes a difference at all. However, the HDL and liver enzyme issues make me worry.
I welcome a study using 12.5-25 mg per day of exemestane versus 0.5-1 mg per week of anastrozole in men on testosterone replacement with estradiol (by ultrasensitive testing) over 35 pg/ml to see the effects on not only estradiol but on the liver, HDL cholesterol, bone density, sexual function and body composition. We may never see a study like this one!
Now, look at how similar exemestane looks like dehydrotestosterone (DHT), a metabolite of testosterone that is responsible for some of its androgenic effects:
There is published study on the use of Aromasin and testosterone replacement.http://www.ncbi.nlm.nih.gov/pubmed/14671195
The following table was taken from a review paper comparing the latest 3 AIs in the treatment of breast cancer. It shows that at the high doses used for breast cancer, exemestane is a weaker blocker of estradiol. I am not completely sure that is a bad thing since excessive estradiol decreases can be a bad thing for men's sexual and brain function and body composition as reported in some older studies.
Source:http://onlinelibrary.wiley.com/doi/10.1002/cncr.10908/full
The following table shows how exemestane can lower high density lipoprotein (HDL- the "good" cholesterol) and triglycerides much like anabolic steroids (and DHT) do.
Like oral androgen products, exemestane may also increase liver enzymes:http://livertox.nih.gov/Exemestane.htm
Like oral androgen-like products, it has also been reported to improve lean mass in women treated for breast cancer: http://www.ergo-log.com/exemestane.html
Some bodybuilding forums speculate that Aromasin is better than anastrozole since it completely deactivates the estrogen receptors. The table above does not support that statement. However, I am curious to see sexual function data comparing TRT plus anastrozole or exemestane to see if the androgen-like nature of exemestane makes a difference at all. However, the HDL and liver enzyme issues make me worry.
I welcome a study using 12.5-25 mg per day of exemestane versus 0.5-1 mg per week of anastrozole in men on testosterone replacement with estradiol (by ultrasensitive testing) over 35 pg/ml to see the effects on not only estradiol but on the liver, HDL cholesterol, bone density, sexual function and body composition. We may never see a study like this one!
Last edited:
Nelson Vergel
Founder, ExcelMale.com
Pharmacokinetics and Dose Finding of a Potent Aromatase Inhibitor, Aromasin (Exemestane), in Young Males
The Journal of Clinical Endocrinology & Metabolism Volume 88, Issue 12
Abstract
Suppression of estrogen, via estrogen receptor or aromatase blockade, is being investigated in the treatment of different conditions. Exemestane (Aromasin) is a potent and selective irreversible aromatase inhibitor. To characterize its suppression of estrogen and its pharmacokinetic (PK) properties in males, healthy eugonadal subjects (14–26 yr of age) were recruited. In a cross-over study, 12 were randomly assigned to 25 and 50 mg exemestane daily, orally, for 10 d with a 14-d washout period. Blood was withdrawn before and 24 h after the last dose of each treatment period. A PK study was performed (n = 10) using a 25-mg dose. Exemestane suppressed plasma estradiol comparably with either dose [25 mg, 38% (P ≤ 0.002); 50 mg, 32% (P ≤ 0.008)], with a reciprocal increase in testosterone concentrations (60% and 56%; P ≤ 0.003 for both). Plasma lipids and IGF-I concentrations were unaffected by treatment. The PK properties of the 25-mg dose showed the highest exemestane concentrations 1 h after administration, indicating rapid absorption. The terminal half-life was 8.9 h. Maximal estradiol suppression of 62 ± 14% was observed at 12 h. The drug was well tolerated. In conclusion, exemestane is a potent aromatase inhibitor in men and an alternative to the choice of available inhibitors. Long-term efficacy and safety will need further study.
The Journal of Clinical Endocrinology & Metabolism Volume 88, Issue 12
Abstract
Suppression of estrogen, via estrogen receptor or aromatase blockade, is being investigated in the treatment of different conditions. Exemestane (Aromasin) is a potent and selective irreversible aromatase inhibitor. To characterize its suppression of estrogen and its pharmacokinetic (PK) properties in males, healthy eugonadal subjects (14–26 yr of age) were recruited. In a cross-over study, 12 were randomly assigned to 25 and 50 mg exemestane daily, orally, for 10 d with a 14-d washout period. Blood was withdrawn before and 24 h after the last dose of each treatment period. A PK study was performed (n = 10) using a 25-mg dose. Exemestane suppressed plasma estradiol comparably with either dose [25 mg, 38% (P ≤ 0.002); 50 mg, 32% (P ≤ 0.008)], with a reciprocal increase in testosterone concentrations (60% and 56%; P ≤ 0.003 for both). Plasma lipids and IGF-I concentrations were unaffected by treatment. The PK properties of the 25-mg dose showed the highest exemestane concentrations 1 h after administration, indicating rapid absorption. The terminal half-life was 8.9 h. Maximal estradiol suppression of 62 ± 14% was observed at 12 h. The drug was well tolerated. In conclusion, exemestane is a potent aromatase inhibitor in men and an alternative to the choice of available inhibitors. Long-term efficacy and safety will need further study.
This may be something to try. I will update here on my bloodwork. Should have this week. I am feeling better everyday on 1 mg a day of arimidex. I feel like maybe most guys who are on trt with arimidex may not be getting the benefits due to like me, other medications they are on. It has been a long time since I felt this good.
Nelson Vergel
Founder, ExcelMale.com
tmckensie: 1 mg per day of Arimidex? That is why too high and frequent of a dose. Do you really want to tank out your estradiol? Are you sure you are not going through a placebo effect?
Read what happens when you decrease estradiol to low levels: https://www.excelmale.com/forum/thr...trozole-(Arimidex)-What-Every-Man-Should-Know
Read what happens when you decrease estradiol to low levels: https://www.excelmale.com/forum/thr...trozole-(Arimidex)-What-Every-Man-Should-Know
According to the pharmacist my body is not getting all of the pill due to the pain meds I am on. The Dr. Agreed with him. So even though I am taking 1 mg a day, I am not getting 1 mg a day. Feels like I must be getting the right amount. I do get bloodwork done today to see where I am. No placebo effect, my breasts have shrunken back, they were so swollen and itchy, I was bloated bad as well, I had went up a couple pants sizes. Back in 33's now. The pharmacist also had a theory that since it really got bad just recently, I am on t compounded with dhea. He said the dhea might be causing me to aromatise more.
Nelson Vergel
Founder, ExcelMale.com
As Table 3 shows above, cortisol and aldosterone response may be decreased. I am not sure if this will translate into less stamina or water retention issues.
Gene Devine
Super Moderator
Nelson Vergel
Founder, ExcelMale.com
Damian, I am not too crazy about Exemestan's lowering effect on HDL, higher dose required and potential liver enzyme elevations.
Dug up, interested in the effects of Aromasin vs Anastrazole.
Ive been on 3mg/week of Anastrazole with 51 pg/ml E2s assay (high over 35pg/ml) with ~30mg of Clomid/week. Also SHBG has come in consistently in the upper quartile.
Tired, moody and defintely efficient at aromatizing. If Aromasin can knockdown Aromatase, lower E2 and SHBG to a normal range I would definitely consider it.
Any experienced users out there willing to share HDL/Enyzme labs? Thanks!
Ive been on 3mg/week of Anastrazole with 51 pg/ml E2s assay (high over 35pg/ml) with ~30mg of Clomid/week. Also SHBG has come in consistently in the upper quartile.
Tired, moody and defintely efficient at aromatizing. If Aromasin can knockdown Aromatase, lower E2 and SHBG to a normal range I would definitely consider it.
Any experienced users out there willing to share HDL/Enyzme labs? Thanks!
Whether someone in the meantime tried Aromasin instead of Arimidix ?
I'm reading users experience these days , and I like It's positive effect on mood, libido (based on coments) and I will try it instead of Arimidex. Friend of mine is also using it on TRT, and he said, he feels more powerful on it....
Nelson said it is bad for lipids, but at all other places (forums, articles) I read about its neutral effects on lipids....
I will try 12.5mg E3.5D and report here about my mood, libido, and bloodwork compared to 0.25mg Arimidex E3.5D.
"Exemestane, sold under the name Aromasin® by Pfizer, is an orally available suicidal aromatase inhibitor. <This sentence describes exactly why exemestane is the king of anti-e's for bodybuilding purposes.
Because exemestane is steroidal this gives it a favorable estrogen suppression profile and confers a few really awesome benefits over other anti-estrogens both on paper and in real experience. Steroidal anti-estrogens have the benefit of being lipid-friendly and they all lower sex hormone binding globulin which increases the ratio of free to bound testosterone, which as many experienced BB'ers know can have a relatively profound positive impact on gains.
I think it is important to understand how drugs work in order to properly dose them, exemestane is a suicidal aromatase inhibitor, this means that it binds with aromatase enzymes and as it does so permanently disables the enzyme and destroys it. Hence the "suicidal" this chemical is like a kamikaze pilot out to destroy your aromatase enzymes which is what makes it so special.
Exemestane's half life in the male body is actually very short (~9 hours) and it is quickly eliminated, however, since as soon as it enters your bloodstream it quickly destroys 80-90% of the aromatase enzymes present in your body, it is effective in maintaining significant reductions in estrogen for up to 72 hours after a single 25mg dose. Estrogen levels only begin to rise again after your body has begun to make new aromatase enzymes to replace the ones destro by exemestane.
There is a great study on the pharmacokinetics of exemestane in men which found the following:
-24 hours after one 25mg dose estrogen levels are reduced by 70-80%
-72 hours later estrogen levels are still 40% below baseline even though the drug itself is almost completely eliminated
-120 hours after initial dose estrogen levels return to baseline (without rebounding)
this means that you can find the timing and dosage that works for you, i've seen some guys recommend between 25mg ed and 12.5mg e4d, and you can see why both are effective while providing different levels of estrogen suppression, and it is this flexibility that makes exemestane such a versatile anti-e.
BUT WAIT, there's more. Aromasin is also a badass post cycle therapy (pct) drug! In males exemestane was found to increase total testosterone by ~60% after 10 days @ 25mg/day, however the same study found that while it increased total testosterone by 60% free testosterone was increased by over 100 percent! that's right, it DOUBLES bio-available testosterone (natty of course).
I can tell you this much, when I take Aromasin for post cycle therapy (pct) the results are dramatic, honestly my libido is never absent at any point during post cycle therapy (pct) and I absolutely feel great within a matter of days, and this is taking 12.5mg ed, the only side effect i notice is stiff joints and other stiff areas
the good:
-powerful aromatase inhibitor capable of stopping gynecomastia completely on its own (for aromatizing compounds)
-has powerful bloat-reduction effects
-lowers sex hormone binding globulin , increasing free test & makes all other anabolic steroids more bio-available (read: more gains)
-can actually boost libido on and off cycle
-increases IGF-1
-NO adverse changes in lipid profiles for men (granted if you are using it on cycle this may be different)
-is NOT liver toxic
-no estrogen rebound
the bad:
-typical aromatase inhibitor issues here include stiff joints and possibly lethargy
-more difficult to come by than a-dex or letro
Appropriate uses for Exemestane:
#1) on cycle estrogen control - that's right, any and all estrogen related problems can and should be corrected with this compound, from gynecomastia to acne to bloat exemestane is a panacea, run it at 12.5mg e4d for gynecomastia protection and bloat control, or run it at 25mg ed for pre-contest or for gynecomastia sensitive individuals or moon face. the beauty of Aromasin is it's okay to use preventatively and not just as spot treatment for gynecomastia as it doesn't hurt gains nearly to the degree that other anti-e's do, i'd still recommend using anti-e's only if you need them, but if you must use one throughout your cycle, you couldn't pick a better compound to use.
#2) post cycle therapy (pct). Aromasin is the premier post cycle therapy (pct) drug in my experience... honestly post cycle therapy (pct) is kind of fun with Aromasin (maybe that's a stretch) but it's a breeze compared to Clomid/nolva and significantly better than a-dex (more powerful and fewer sides) it works excellently with hcg and keeps the extra aromatization from the hcg injects at bay (you can even run higher dosages of hcg above 500iu/inject) and another bonus is since it's safe and comfortable to run for longer periods of time, you can stretch your post cycle therapy (pct) out to 6 or 8 weeks for suppressive cycles to make sure you get everything back in full working order
#3) gynecomastia reversal - in conjunction with a selective estrogen receptor modulator (raloxifene or Tamoxifen) and/or a dihydrotestosterone derived compound Aromasin can be effective in reversing/reducing existing gynecomastia
#4) off cycle testosterone boost - sometimes if i dont feel like running a cycle but still want a little extra kick i'll take 25mg EOD for 4-6 weeks, gains aren't improved all that greatly but significantly, but i do it more for the libido/mental effects anyways.
#5) hypogonadism - so you're getting older, you've been cycling since you were 21 and your natty test levels just never get back in the good range, but you don't wanna go HRT??? Aromasin will get you back in the game without having to take the plunge for HRT."
Source: http://www.steroidology.com/forum/t...e-aromasin-eod-like-arimidex.html#post2699581
I'm reading users experience these days , and I like It's positive effect on mood, libido (based on coments) and I will try it instead of Arimidex. Friend of mine is also using it on TRT, and he said, he feels more powerful on it....
Nelson said it is bad for lipids, but at all other places (forums, articles) I read about its neutral effects on lipids....
I will try 12.5mg E3.5D and report here about my mood, libido, and bloodwork compared to 0.25mg Arimidex E3.5D.
"Exemestane, sold under the name Aromasin® by Pfizer, is an orally available suicidal aromatase inhibitor. <This sentence describes exactly why exemestane is the king of anti-e's for bodybuilding purposes.
Because exemestane is steroidal this gives it a favorable estrogen suppression profile and confers a few really awesome benefits over other anti-estrogens both on paper and in real experience. Steroidal anti-estrogens have the benefit of being lipid-friendly and they all lower sex hormone binding globulin which increases the ratio of free to bound testosterone, which as many experienced BB'ers know can have a relatively profound positive impact on gains.
I think it is important to understand how drugs work in order to properly dose them, exemestane is a suicidal aromatase inhibitor, this means that it binds with aromatase enzymes and as it does so permanently disables the enzyme and destroys it. Hence the "suicidal" this chemical is like a kamikaze pilot out to destroy your aromatase enzymes which is what makes it so special.
Exemestane's half life in the male body is actually very short (~9 hours) and it is quickly eliminated, however, since as soon as it enters your bloodstream it quickly destroys 80-90% of the aromatase enzymes present in your body, it is effective in maintaining significant reductions in estrogen for up to 72 hours after a single 25mg dose. Estrogen levels only begin to rise again after your body has begun to make new aromatase enzymes to replace the ones destro by exemestane.
There is a great study on the pharmacokinetics of exemestane in men which found the following:
-24 hours after one 25mg dose estrogen levels are reduced by 70-80%
-72 hours later estrogen levels are still 40% below baseline even though the drug itself is almost completely eliminated
-120 hours after initial dose estrogen levels return to baseline (without rebounding)
this means that you can find the timing and dosage that works for you, i've seen some guys recommend between 25mg ed and 12.5mg e4d, and you can see why both are effective while providing different levels of estrogen suppression, and it is this flexibility that makes exemestane such a versatile anti-e.
BUT WAIT, there's more. Aromasin is also a badass post cycle therapy (pct) drug! In males exemestane was found to increase total testosterone by ~60% after 10 days @ 25mg/day, however the same study found that while it increased total testosterone by 60% free testosterone was increased by over 100 percent! that's right, it DOUBLES bio-available testosterone (natty of course).
I can tell you this much, when I take Aromasin for post cycle therapy (pct) the results are dramatic, honestly my libido is never absent at any point during post cycle therapy (pct) and I absolutely feel great within a matter of days, and this is taking 12.5mg ed, the only side effect i notice is stiff joints and other stiff areas
the good:
-powerful aromatase inhibitor capable of stopping gynecomastia completely on its own (for aromatizing compounds)
-has powerful bloat-reduction effects
-lowers sex hormone binding globulin , increasing free test & makes all other anabolic steroids more bio-available (read: more gains)
-can actually boost libido on and off cycle
-increases IGF-1
-NO adverse changes in lipid profiles for men (granted if you are using it on cycle this may be different)
-is NOT liver toxic
-no estrogen rebound
the bad:
-typical aromatase inhibitor issues here include stiff joints and possibly lethargy
-more difficult to come by than a-dex or letro
Appropriate uses for Exemestane:
#1) on cycle estrogen control - that's right, any and all estrogen related problems can and should be corrected with this compound, from gynecomastia to acne to bloat exemestane is a panacea, run it at 12.5mg e4d for gynecomastia protection and bloat control, or run it at 25mg ed for pre-contest or for gynecomastia sensitive individuals or moon face. the beauty of Aromasin is it's okay to use preventatively and not just as spot treatment for gynecomastia as it doesn't hurt gains nearly to the degree that other anti-e's do, i'd still recommend using anti-e's only if you need them, but if you must use one throughout your cycle, you couldn't pick a better compound to use.
#2) post cycle therapy (pct). Aromasin is the premier post cycle therapy (pct) drug in my experience... honestly post cycle therapy (pct) is kind of fun with Aromasin (maybe that's a stretch) but it's a breeze compared to Clomid/nolva and significantly better than a-dex (more powerful and fewer sides) it works excellently with hcg and keeps the extra aromatization from the hcg injects at bay (you can even run higher dosages of hcg above 500iu/inject) and another bonus is since it's safe and comfortable to run for longer periods of time, you can stretch your post cycle therapy (pct) out to 6 or 8 weeks for suppressive cycles to make sure you get everything back in full working order
#3) gynecomastia reversal - in conjunction with a selective estrogen receptor modulator (raloxifene or Tamoxifen) and/or a dihydrotestosterone derived compound Aromasin can be effective in reversing/reducing existing gynecomastia
#4) off cycle testosterone boost - sometimes if i dont feel like running a cycle but still want a little extra kick i'll take 25mg EOD for 4-6 weeks, gains aren't improved all that greatly but significantly, but i do it more for the libido/mental effects anyways.
#5) hypogonadism - so you're getting older, you've been cycling since you were 21 and your natty test levels just never get back in the good range, but you don't wanna go HRT??? Aromasin will get you back in the game without having to take the plunge for HRT."
Source: http://www.steroidology.com/forum/t...e-aromasin-eod-like-arimidex.html#post2699581
Nelson Vergel
Founder, ExcelMale.com
This is what I said:
"However, I am curious to see sexual function data comparing TRT plus anastrozole or exemestane to see if the androgen-like nature of exemestane makes a difference at all. However, the HDL and liver enzyme issues make me worry.
I welcome a study using 12.5-25 mg per day of exemestane versus 0.5-1 mg per week of anastrozole in men on testosterone replacement with estradiol (by ultrasensitive testing) over 35 pg/ml to see the effects on not only estradiol but on the liver, HDL cholesterol, bone density, sexual function and body composition. We may never see a study like this one!"
"However, I am curious to see sexual function data comparing TRT plus anastrozole or exemestane to see if the androgen-like nature of exemestane makes a difference at all. However, the HDL and liver enzyme issues make me worry.
I welcome a study using 12.5-25 mg per day of exemestane versus 0.5-1 mg per week of anastrozole in men on testosterone replacement with estradiol (by ultrasensitive testing) over 35 pg/ml to see the effects on not only estradiol but on the liver, HDL cholesterol, bone density, sexual function and body composition. We may never see a study like this one!"
Nelson Vergel
Founder, ExcelMale.com
I think there is something to Aromasin since the molecule is so close to what an androgen looks like. My estradiol is always low so I have never needed to use an AI even when I was cycling larger doses in the past.
Have you tried just letting go of the anastrozole for a while to see if your libido improves?
Have you tried just letting go of the anastrozole for a while to see if your libido improves?
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