AROMASIN (EXEMESTANE) VS ARIMIDEX (ANASTROZOLE)

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RaW InStiNcTz • Thu, Aug 8th, ’13 17:02 • 54 replies, 11501 views
I remember reading this somewhere I liked it so much that I saved it, Hope you guys like it I found it very informative.

Some points to remember before you begin reading.

It’s equally important for those of you unfamiliar with Cholesterol to please familiarize yourself with the following link that outlines the clinical definition and differences between HDL and LDL. I’m certain this topic will invariably come up during the discussion of Arimidex , as this appears to plays a key role in the decision whether to choose Arimidex or Aromasin .

Cholesterol

Two important points to also bear in mind: Both Arimidex and Aromasin were originally developed to fight cancer cells in woman, and most importantly and often mistaken, both behave differently in men and woman. And having said this, I know that some of you may bring up the “Lancet” study and its results that were reported a few years back. Please keep in mind that this study and results were conducted on, and from, WOMAN.

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AROMASIN – Exemestane

Type-I Aromatase Inhibitor

Aromasin (Exemestane) is a Type-I aromatase inhibitor, or suicidal aromatase inhibitor. It’s called this because it lowers estrogen production in the body by attaching to the aromatase enzyme, and permanently deactivating it. It averages 90% rate of estrogen suppression, which equals a reduction in estradiol levels of about 50%, as well as significantly raising testosterone .(up to 60%)

Aromasin not only increases testosterone and lowers estrogen, but it also increases levels of insulin -like growth Factor (IGF). And Aromasin is not too harsh on lipid panel (cholesterol), unlike some of the other AIs’ like Letrozole .(Femara) Aromasin reaches steady blood plasma levels of after a week of administration, and this is also when we see it begin its maximal effect on reducing circulating estrogen levels. It has a terminal half life of 9 hours in MEN, so taking it once per day will build up blood plasma levels to a very effective level.

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Also, there have been some additional researches related to Aromasin in men in pharmacokinetics. The results of the research are the following:

24 hours after one 25mg dose, estrogen levels are reduced by 70-80%;

72 hours later estrogen levels are still 40% below the baseline;

120 hours after initial dose, estrogen levels return to baseline.

Additionally, the University of Florida conducted a study in healthy young men:

Pharmacokinetics and Dose Finding of a Potent Aromatase Inhibitor, Aromasin (Exemestane), in Young Males.

Nemours Children’s Clinic and Research Programs (N.M., J.L., A.R.), Jacksonville, Florida 32207; and University of Florida Health Sciences Center (D.P.) and Amersham Pharmacia Biotech (E.d.S., A.K., B.L.), Peapack, New Jersey 07977

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 Aromasin daily, orally, for 10 days with a 14 day washout period. Blood was withdrawn before and 24 hours after the last dose of each treatment period. A PK study was performed using a 25mg dose. Aromasin suppressed plasma estradiol comparably with either dose [25 mg, 38%; 50 mg, 32%], with a reciprocal increase in testosterone concentrations (60% and 56%; for both).

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The following observations were made:

Plasma lipids and IGF-I concentrations were unaffected by treatment.
The PK properties of the 25-mg dose showed the highest concentrations 1 h after administration, indicating rapid absorption.
Maximal estradiol suppression of 62 ± 14% was observed at 12 h.
The drug was well tolerated.
The terminal half-life was 8.9 hours in the male subjects.
In conclusion, Aromasin (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.

References and Supporting Data:

A predictive model for exemestane pharmacokinetics/pharmacodynamics incorporating the effect of food and formulation.Br J Clinical Pharmacology. 2005 Mar, 59(3):355-64.

Eur. J. Cancer. 2000, May;36(8):976-82

The Journal of Clinical Endocrinology & Metabolism Vol. 88, No. 12 5951-5956Copyright © 2003 by The Endocrine Society

Clin Cancer Res. 2003 Jan;9(1 Pt 2):468S-72S

Anticancer Res. 2003 Jul-Aug;23(4):3485

J Clin Endocrinol Metab. 2003 Dec;88(12):5951-6.

ARIMIDEX – Anastrozole

Type-II Aromatase Inhibitor

Arimidex binds reversibly to the aromatase enzyme through competitive inhibition. This suppresses the conversion of androgens into estrogen. Circulating plasma estrogen can be reduced by nearly 85% in women using Arimidex. A common misconception is that aromatase inhibition is similar in men and women. However in trials when males were administered 1mg of Arimidex daily, circulating estrogen was only reduced by about 50%. Anastrozole is rapidly absorbed orally (time to reach maximum concentration, 1 hour) with a slow apparent clearance of 1.54 liters/h and a terminal half-life of 46.8 h.

But unlike Aromasin, once you stop taking Arimidex, the aromatase enzyme is free to convert androgens (testosterone) into estrogen again. This is referred to as estrogen rebound.

Estrogen has been measured as much as 7 times higher than normal in men on steroids . This is excessive and can potentially cause water retention, gynecomastia or benign prostatic hyperplasia. Therefore, in order to avoid these side effects, estrogen must be controlled. Reduction in breast area and breast volume have been observed in young men treated for 6 months with Arimidex (1 mg daily). These subjects had recent pre-existing gynecomastia (less than one year). However boys with longstanding gynecomastia (more than one year) were unresponsive to 6 months of Arimidex treatment, possibly due to development of dense breast fibrosis. Therefore using Arimidex to treat recent gynecomastia is supported by the data.

From all the data available, 0.25-.50mg of Arimidex every other day is a good starting point on moderate doses of testosterone. If testosterone doses are raised, then an increase may be needed to control estrogen. Since either high and low estrogen can cause side effects, such as low libido, only labs can determine the appropriate dose of Arimidex. Arimidex not only lowers circulating estrogen but it also increases LH and FSH concentrations in addition to increasing testosterone by about 58% in men. In one study elderly men with mild hypogonadism were administered 1mg daily of Arimidex for 12 weeks. This treatment normalized serum testosterone levels in those men without adversely affecting lipids, precursors of cardiovascular risk or insulin resistance. Please see excerpt from ATAC study below.

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“Clinical Study – Cholesterol

During the ATAC 5 year trial (Arimidex, Tamoxifen , Alone, or in Combination) more patients receiving ARIMIDEX were reported to have an elevated serum cholesterol compared to patients receiving tamoxifen (9% versus 3.5%, respectively). A post-marketing trial also evaluated any potential effects of ARIMIDEX on lipid profile. In the primary analysis population for lipids (ARIMIDEX alone), there was no clinically significant change in LDL-C from baseline to 12 months and HDL-C from baseline to 12 months.

In secondary population for lipids (ARIMIDEX+risedronate), there also was no clinically significant change in LDL-C and HDL-C from baseline to 12 months. In both populations for lipids, there was no clinical significant difference in total cholesterol (TC) or serum triglycerides (TG) at 12 months compared with baseline.“

The difference in the elevated serums levels during the ATAC trial between patients receiving Arimidex and those receiving Tamoxifen were, (9% versus 3.5%, respectively) Only a 5.5% difference. Again, in this trial, treatment for 12 months with ARIMIDEX alone had a neutral effect on lipid profile. Combination treatment with ARIMIDEX and risedronate also had a neutral effect on lipid profile. Please see link for complete study: ARIMIDEX (ANASTROZOLE) TABLET [ASTRAZENECA PHARMACEUTICALS LP]

*So for average users of AAS who chooses to include Arimidex as their primary aromatase inhibitor, there is no cause for concern. However, monitoring your Cholesterol levels while using AAS, is recommended.

Other Clinical Studies

Effect of aromatase inhibition on lipids and inflammatory markers of cardiovascular disease in elderly men with low testosterone levels.

Dougherty RH, Rohrer JL, Hayden D, Rubin SD, Leder BZ.
Department of Medicine, Massachusetts General Hospital, Boston, MA 02114, USA.

Anastrozole is an oral aromatase inhibitor that normalizes serum testosterone levels and decreases oestradiol levels modestly in elderly men with mild hypogonadism. Thirty-seven elderly hypogonadal men were randomized to receive either anastrozole 1 mg daily, anastrozole 1 mg twice weekly, or daily placebo for 12 weeks in a double-blind fashion. Men aged 62-74 years with mild hypogonadism defined by testosterone levels less than 350 ng/dl. And although androgen replacement has been shown to have beneficial effects in hypogonadal men, there is concern that androgens may deleteriously affect cardiovascular risk in elderly men.

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Treatment with Arimidex did not significantly affect fasting lipids, inflammatory markers adhesion molecules or insulin sensitivity. There was, however, a positive correlation between changes in serum triglycerides and changes in serum oestradiol levels. And while short-term administration of Arimidex is an effective method of normalizing serum testosterone levels in elderly men with mild hypogonadism, it does not appear to adversely affect lipid profiles, inflammatory markers of cardiovascular risk or insulin resistance.

Note: These studies were summarized and showed Arimidex decreased Estradiol by about 50% while raising Testosterone by about 58% in males.

References

Effect of aromatase inhibition on lipids and inflammatory markers of cardiovascular disease in elderly men with low testosterone levels.
Estrogen suppression in males: metabolic effects.
Pharmacokinetics and pharmacodynamics of anastrozole in pubertal boys with recent-onset gynecomastia.
Influence of Neoadjuvant Anastrozole (Arimidex) on Intratumoral Estrogen Levels and Proliferation Markers in Patients with Locally Advanced Breast Cancer.
CONCLUSIONS:

To recap:

Aromasin takes a little longer to raise serum levels and has a shorter half life (10 hours), and is a suicide inhibitor. Recommend dose 12.5mg MIN – every day (ED)

Arimidex raises serum levels quicker yet has a longer half life (47 hours), and is a blocker type inhibitor. Recommended dose .25mg – every other day. (EOD)

After researching both compounds and reading the various studies available, i believe that Aromasin or Arimidex are both solid choices for an aromatase inhibitor used on cycle for the average AAS user. I equally believe that there is enough substantial data and evidence that suggests and supports the DAILY use of Aromasin as an aromastase inhibitor as a standard protocol. I no longer subscribe to the every other day (EOD) protocol when advising Aromasin as the primary AI.

And please remember that this article is NOT about which AI is better, rather it focuses on the fact that Arimidex is less invasive on lipids than previously thought by many of us here and elsewhere.

Please share your thoughts as I am interested in your opinions so we can continue to learn together.

COMMENTS
Bigdane82’s picture
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Bigdane82 6 months ago
I take 1mg 3x week of arimidex…..helps in so many ways. If anyone is thinking about trying it out as an AI, do it…..after years of just using Novla whenever gyno soreness started I switched to arimidex throughout and it helps maintain general performances all around, not just keep symptoms at bay.

shnickerdoodles’s picture
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shnickerdoodles 7 months ago
I’m gonna get myself some Aromaxyl now. Thank you

kibby’s picture
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kibby 7 months ago
Good info cheers mate

whoremoans’s picture
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whoremoans 8 months ago
Arimidex worked perfect at .5e3d. Estrodials were at 20 consistently throughout

kibby’s picture
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kibby 7 months ago @whoremoans
Hi mate,
What were you running?? Dosage ect. ..

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j223 8 months ago
Numbers mean nothing if a person individually does not tolerate one of the anti-estrogens. Personally aromasin gives me horrible side effects. Massive fluctuations in estrogen no matter the dose. Depression, ED, sensitive nips, hairloss, creaky joints etc.

For me Arimidex has hardly any side effects at all. It is my number one pick ALWAYS because it is reliable, has less side effects (or none at all !) and makes me feel 100% all the time. The same cannot be said about aromasin.

For example, Aromasin is generally ONLY prescribed in post menopausal women for a reason. That is because is has much more harsh androgenic side effects that only post menopausal women can tolerate. As for men it can also have more harsh side effects

What is my point? That both can be great drugs. Some people respond to one better than the other. It is PERSONAL PREFERENCE. Blood testing is important as well as trying out each for your own. Try each and see which works best for YOU. Forget statistics and studies because the only thing that matters is finding what works best for you!!!! After multiple cycles and trying each out you will find what works best for you and that is ultimately why starting new cycles with less compounds (test only) is important because finding the right balance of test and estrogen will have the biggest impact on success of future cycles and allow you to properly cycle, keep estrogen in check and get the most out of your cycles!

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Bigdane82 6 months ago @j223
I also use arimidex. Do you have any experience with Letro?

vhman’s picture
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vhman 8 months ago @j223
Great info (+2). Aromasin works great for me and I use it with my TRT regimen. I don’t get any noticeable side-effect with it. I tried Arimidex quite a while ago, and it worked fine for me during my cycle.
Like you said, people need to experiment with both to see what works best, and that includes taking bloods.

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j223 8 months ago @vhman
Right on it’s great to hear you love exemestane. It seems 50-50. Half the people I know love adex, half love aromasin!! I think it’s great you found what works best for you! It really only comes down to personal preference. Heck, I know guys that do best on letrozole !!!

numbere’s picture
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numbere 8 months ago
Wow, this whole post is plagiarized.

MickyKnox is the real author.

Here is a link to the original thread.

Aromasin (Exemestane) vs Arimidex (Anastrozole) Unraveled

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CBBurrr 8 months ago @numbere
I remember reading this somewhere I liked it so much that I saved it, Hope you guys like it I found it very informative.
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numbere 8 months ago @CBBurrr
Thanks, I saw that when I read the OP.

Just because one admits they are plagiarizing does not make it right.

A simple internet search would have shown OP who the original author.

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seoulcitydan 8 months ago
I’m unsure if tis experience has any bearing to this post but I do have a question of AI usage.

I did a pretty harsh cycle without the use of AI’s.
Luckily for me I never once had any gyno side effects.
I did get a lot of water retention as expected and of the 30lbs+ I gained, I lost 10 and kept 20.
I did a Pre PCT of HCG then PCT of Nolva, I know I did a lot of things wrong on my first cycle, in any case, I am well past 2 months of my PCT. I recently did a blood test and found that though my Testosterone levels have come back pretty well, unfortunately, my Estradiol level is way too high as well as my cortisol level.

My question is, can I and or should I go on an Aromasin or Arimidex therapy cycle to treat my high Estradiol level, or is it too late or futile at this point?

Thanks

numbere’s picture
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numbere 8 months ago @seoulcitydan
Gyno should be the least of your worries when not using an AI on cycle. Having high e2 is probably the most unhealthy thing that can happen on cycle. High e2 it terrible for your cardiovascular system. You can’t feel a blood clot forming.

If you aren’t taking exogenous test then you shouldn’t use an AI. You should know that men often read 10-20 points higher on a standard e2 assay because that specific test is geared towards women.

If you want to get an accurate e2 reading then you need a “sensitive e2” assay.

I think you should give it a few more weeks then have another blood test. If e2 is still high the consider taking 50-75 mg of zinc everyday for a month.

CBBurrr’s picture
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CBBurrr 2 years ago
Does an AI have any effect on existing estro, or does it just reduce further conversion by the aromatase enzyme?

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WhyNot 2 years ago @CBBurrr
An AI has no effect on existing Estrogen. The effect is in stopping the conversion of testosterone to estrogen, while your body metabolizes the existing estrogen.

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markymark 2 years ago
this should be a must read for all…great post!! im a big fan of exemestane
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tman5150 2 years ago
I appreciate the sharing of this information. I was hoping you’d know about the difference between aromasin and arimidex for PCT. Is arimidex a possible choice, even though aromasin might be the best.

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wimpy1 3 years ago
Excellent read!! This community and the people in it make this place #1. All the information a newbie + a long Time user ever needs is here. Glad I found eroids before jumping in head first into my cycle. This place has helped me out tremendously.

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BilMcbigballs 3 years ago
Very good read brother. +1
Aro works great for me while on cycle

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ash48 3 years ago
quick question guys… briefly read the aromasin part… its says it lowers estrogen, raises testosterone , igf1 levels…

so how does it cause u to crash as ive seen a few post claim now??

my concern about it is, I just took my first 12.5mg aromasin tonight, to control my estro (no gyno signs thou)….

hmmmm

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kibby 7 months ago @ash48
Hi buddy,
I’m not sure how it crashes estrogen but at the beginning of my cycle I underestimated the quality of my aromasin (Pfizer pharma grade) started running it to early and at 12.5mg eod was to strong a dose and definitely crashed it I felt awful. I got some advice from cd1 as this happend to him about 6 months ago I am starting to feel normal again and get bloods done this week

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RaW InStiNcTz 3 years ago @ash48
I believe crash levels happen with Adex rather than aromasin

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mechyeng 2 years ago @RaW InStiNcTz
what does crash level mean? is that like starting to early in a cycle and the AI builds in the system and you kill off to much estro?

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vhman 3 years ago @RaW InStiNcTz
You can crash your levels with both.

RaW InStiNcTz’s picture
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RaW InStiNcTz 3 years ago @vhman
Never had crashing levels with aromasin, butb have had with adex

j223’s picture
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j223 8 months ago @RaW InStiNcTz
That is a dosing issue, and has nothing to do with the drugs

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ash48 3 years ago @ash48
god this game is hard work…. u think even a simple cycle is easy… not for me paranoid

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CBBurrr 3 years ago @ash48
I hear you man! You should have seen me after I smoked some pot last night, I was worried about everything from the package I’m expecting in the mail, side effects, and even the bag of doobage I have a med card for.

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vhman 3 years ago @CBBurrr
You need to get a different strain of weed! Keep those paranoid thoughts at bay. In reality, you just need to take a deep breath, man up and start your cycle. It’s a good beginning cycle and you will be fine. Quit doubting yourself and your plan.

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