Page 1 of 6 123456 LastLast
Results 1 to 40 of 211
Like Tree5Likes

Thread: *Aromasin (Exemestane) vs Arimidex (Anastrozole) Unraveled*

  1. #1
    MickeyKnox is offline Banned
    Join Date
    Dec 2011
    Location
    CANADA
    Posts
    13,200

    *Aromasin (Exemestane) vs Arimidex (Anastrozole) Unraveled*

    Some points to remember before you begin reading.

    I have gathered information from several studies that were relevant, and have attempted to streamline whenever I could so that key points of these articles would not be obscured from the importance of their effects on AAS use.

    I feel 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.





    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.

    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).

    The following observations were made:

    1. Plasma lipids and IGF-I concentrations were unaffected by treatment.
    2. The PK properties of the 25-mg dose showed the highest concentrations 1 h after administration, indicating rapid absorption.
    3. Maximal estradiol suppression of 62 14% was observed at 12 h.
    4. The drug was well tolerated.
    5. 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:

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

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

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

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

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

    6. 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.

    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.

    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

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



    MY 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.

    *This following is an important link to my friend JimmyInk'dUp's thread entitled, "Aromasin - The Underdosed AI." Please take the time to read it - it is well written and offers a slightly different protocol.

    Aromasin - The Underdosed AI

    http://forums.steroid.com/anabolic-s...ml#post6493560
    Last edited by MickeyKnox; 04-25-2013 at 08:40 AM.

  2. #2
    lovbyts's Avatar
    lovbyts is offline Knowledgeable Member
    Join Date
    Apr 2008
    Posts
    29,390
    Thanks for all that and making it clear. I have done a fare amount of reading on both and this helps clear some things us such as why my Exemestane was not as effective as it should have been or basically was not at all. I knew it was mostly my fault but didnt realize your levels went back to normal after 3 days. I wast TRYING to use it eod but usually it was every 3 days, sometime 4. This time I had decided (looks like the right choice) to just use it every day to be safe and so I wont forget. Looks like that's the best way to go anyways.

    One of the reasons I went with Exemestane was also due the cholesterol issues. I'm glad I did.

  3. #3
    MickeyKnox is offline Banned
    Join Date
    Dec 2011
    Location
    CANADA
    Posts
    13,200
    Quote Originally Posted by lovbyts View Post
    Thanks for all that and making it clear. I have done a fare amount of reading on both and this helps clear some things us such as why my Exemestane was not as effective as it should have been or basically was not at all. I knew it was mostly my fault but didnt realize your levels went back to normal after 3 days. I wast TRYING to use it eod but usually it was every 3 days, sometime 4. This time I had decided (looks like the right choice) to just use it every day to be safe and so I wont forget. Looks like that's the best way to go anyways.

    One of the reasons I went with Exemestane was also due the cholesterol issues. I'm glad I did.
    Not sure if i understand this correctly, LB. Is this because you believe there are cholesterol issues with Adex? Or some other reason?

  4. #4
    lovbyts's Avatar
    lovbyts is offline Knowledgeable Member
    Join Date
    Apr 2008
    Posts
    29,390
    Quote Originally Posted by MickeyKnox View Post
    Not sure if i understand this correctly, LB. Is this because you believe there are cholesterol issues with Adex? Or some other reason?
    Yes that was one of my original reasons besides reviewing a lot of personal reviews on both and people seemed to like how Exemestane worked long term. My understanding before was Exemestane had no effect on Cholesterol and people though Adex did. The study shows significant change but still better safe than sorry.

  5. #5
    MickeyKnox is offline Banned
    Join Date
    Dec 2011
    Location
    CANADA
    Posts
    13,200
    Quote Originally Posted by lovbyts View Post
    Yes that was one of my original reasons besides reviewing a lot of personal reviews on both and people seemed to like how Exemestane worked long term. My understanding before was Exemestane had no effect on Cholesterol and people though Adex did. The study shows significant change but still better safe than sorry.
    Ahh ok. Yeah, that's the impression i was under for awhile too. But the clinical clearly supports the fact the Adex is NOT that hard on lipids after all.

    Personally, i will be using Arimidex from now on because the transparent truth is, it's a LOT easier to maintain stable serum levels, imho. And quite frankly, its cheaper - thats a win win for me.

  6. #6
    Turkish Juicer's Avatar
    Turkish Juicer is offline Knowledgeable Member
    Join Date
    Feb 2011
    Location
    Istanbul
    Posts
    2,984
    Great post Mickey!

  7. #7
    snowblowjoe's Avatar
    snowblowjoe is offline Senior Member
    Join Date
    Apr 2012
    Posts
    1,267
    Blog Entries
    1
    But Adex doesn't cut down on estrogen nearly as effective as the others and you also have to worry about an estrogen rebound just like letrozole if I was reading that correctly... So with this being said why not just go exemestane and have letrozole on hand for backup?

  8. #8
    snowblowjoe's Avatar
    snowblowjoe is offline Senior Member
    Join Date
    Apr 2012
    Posts
    1,267
    Blog Entries
    1
    Sticky material

  9. #9
    lovbyts's Avatar
    lovbyts is offline Knowledgeable Member
    Join Date
    Apr 2008
    Posts
    29,390
    Quote Originally Posted by MickeyKnox View Post
    Ahh ok. Yeah, that's the impression i was under for awhile too. But the clinical clearly supports the fact the Adex is NOT that hard on lipids after all.

    Personally, i will be using Arimidex from now on because the transparent truth is, it's a LOT easier to maintain stable serum levels, imho. And quite frankly, its cheaper - thats a win win for me.
    The other nice thing about adex from what I understand is it does not take a week for things to level out or control Estrogen but works immediately.

    I'm sticking with Exemestane, because I already have several. lol
    Last edited by lovbyts; 03-03-2013 at 01:34 AM.

  10. #10
    kronik420's Avatar
    kronik420 is offline Anabolic Member
    Join Date
    Feb 2012
    Location
    Australia
    Posts
    6,257
    good info, thank you Mr Knox

    on adex currently, and it seems to be doing it's job, no sides yet..

  11. #11
    MickeyKnox is offline Banned
    Join Date
    Dec 2011
    Location
    CANADA
    Posts
    13,200
    Quote Originally Posted by snowblowjoe View Post
    But Adex doesn't cut down on estrogen nearly as effective as the others and you also have to worry about an estrogen rebound just like letrozole if I was reading that correctly... So with this being said why not just go exemestane and have letrozole on hand for backup?
    I honestly think that all three are so close, likely within 10% of each other, that it really is insignificant. Adex and Letro are both competitive type blockers, so the only clinical difference that separates them would be the the percentage of aromatase they each are responsible for preventing from attaching to the receptors.

    Although, the only caveat i can think of here, is that many folks appear to experience bad sides from Letro, ie..feeling like crap. (when daily doses are administered properly)

  12. #12
    lovbyts's Avatar
    lovbyts is offline Knowledgeable Member
    Join Date
    Apr 2008
    Posts
    29,390
    Quote Originally Posted by MickeyKnox View Post
    I honestly think that all three are so close, likely within 10% of each other, that it really is insignificant. Adex and Letro are both competitive type blockers, so the only clinical difference that separates them would be the the percentage of aromatase they each are responsible for preventing from attaching to the receptors.

    Although, the only caveat i can think of here, is that many folks appear to experience bad sides from Letro, ie..feeling like crap. (when daily doses are administered properly)
    And with Letro you have the possibility of rebound if you dont taper off it.

  13. #13
    MickeyKnox is offline Banned
    Join Date
    Dec 2011
    Location
    CANADA
    Posts
    13,200
    Quote Originally Posted by lovbyts View Post
    And with Letro you have the possibility of rebound if you dont taper off it.
    Adex is no different - they're both competitive type blockers. The only difference is Letro is stronger.

  14. #14
    OdinsOtherSon's Avatar
    OdinsOtherSon is offline Knowledgeable Member
    Join Date
    Sep 2012
    Posts
    2,518
    Excellent as always Mickey! I'm subbed.

  15. #15
    Lunk1's Avatar
    Lunk1 is offline aka "JOB"
    Join Date
    Mar 2012
    Location
    METHAMERICA
    Posts
    16,392
    letro is substantially stronger imo and can be difficult to dose! I believe it to be very effective but to a degree too effective and one could risk E2 crash more easily then with Aro or Adex

    Doesn't letro work on diff receptors as well????

  16. #16
    MickeyKnox is offline Banned
    Join Date
    Dec 2011
    Location
    CANADA
    Posts
    13,200
    Quote Originally Posted by Lunk1 View Post
    letro is substantially stronger imo and can be difficult to dose! I believe it to be very effective but to a degree too effective and one could risk E2 crash more easily then with Aro or Adex

    Doesn't letro work on diff receptors as well????
    How much stronger? If you mean mg for mg, i agree with you 100%. But when both are dosed accordingly, whats the difference? 8%,10%? Show me some numbers.

    And what does "too effective" mean in terms of AAS? Again, if dosed properly according to the strength mg for mg.

    I do agree that both Adex or Letro can crash your E2 quicker and likely easier, but only because they tend to saturate serum levels faster than Aromasin .

    EDIT: I forgot to include that Letro's half is much longer than the other two, but its strength is similar to Aromasin on paper.
    Last edited by MickeyKnox; 03-03-2013 at 11:30 AM.

  17. #17
    ChiveOn's Avatar
    ChiveOn is offline Senior Member
    Join Date
    Dec 2012
    Location
    SoCal USA
    Posts
    1,404
    Nice post! I've always used adex, but for no real reason over aromasin . However, this gives some actual information and I think ill be sticking to my plan. But ill have a reason why finally haha

  18. #18
    redz's Avatar
    redz is offline Knowledgeable Member
    Join Date
    Nov 2007
    Location
    GTA
    Posts
    13,880
    I've used both and im currently running adex. I think it's mostly a personal preference as long as they are dosed correctly.

  19. #19
    MickeyKnox is offline Banned
    Join Date
    Dec 2011
    Location
    CANADA
    Posts
    13,200
    Quote Originally Posted by redz View Post
    I've used both and im currently running adex. I think it's mostly a personal preference as long as they are dosed correctly.
    This is what i believe as well.

    This article is certainly not trying to suggest one over the other, but rather allow the reader to make an informed decision based on facts, not hearsay. They are both excellent choices for use as an AI, imho.

  20. #20
    GhostOfRome is offline Junior Member
    Join Date
    Feb 2013
    Posts
    65
    Great post brother!

  21. #21
    clarky.'s Avatar
    clarky. is offline MONITOR
    Join Date
    Sep 2012
    Location
    Scotland
    Posts
    16,400
    Great read mate.

  22. #22
    MickeyKnox is offline Banned
    Join Date
    Dec 2011
    Location
    CANADA
    Posts
    13,200
    Bump..

  23. #23
    Knockout_Power's Avatar
    Knockout_Power is offline "Even sexier than Siggy"
    Join Date
    Oct 2006
    Location
    R.I.P My friends
    Posts
    15,015
    My intial research pointed me in the direction of Aromasin and its what I keep on hand at all times... thank you for this write up, I like a more in depth explanaition.

  24. #24
    MickeyKnox is offline Banned
    Join Date
    Dec 2011
    Location
    CANADA
    Posts
    13,200
    Quote Originally Posted by Knockout_Power View Post
    My intial research pointed me in the direction of Aromasin and its what I keep on hand at all times... thank you for this write up, I like a more in depth explanaition.
    Good choice KP.

    The beauty of this article is that it proves you can't go wrong with either one as a solid AI.

  25. #25
    noon's Avatar
    noon is offline Senior Member
    Join Date
    Jul 2012
    Location
    In hiding
    Posts
    1,271
    Very helpful to me just starting to learn all of this
    Thanks for the solid read

  26. #26
    Knockout_Power's Avatar
    Knockout_Power is offline "Even sexier than Siggy"
    Join Date
    Oct 2006
    Location
    R.I.P My friends
    Posts
    15,015
    Quote Originally Posted by MickeyKnox View Post
    Good choice KP.

    The beauty of this article is that it proves you can't go wrong with either one as a solid AI.
    exactly... everyone has their opinion on which one is better and often forget that both work well. Its just nice to have this info around to show options cause IMO Letro is too harsh but its still pushed by a lot of people. I have never had gyno or noticable ERSE so maybe Letro has its place, but I will not make the effort to keep it around.

  27. #27
    Buster Brown's Avatar
    Buster Brown is offline Knowledgeable Member
    Join Date
    Feb 2012
    Location
    Proud Bostonian
    Posts
    4,722
    Awesome post, should be a sticky!

  28. #28
    MickeyKnox is offline Banned
    Join Date
    Dec 2011
    Location
    CANADA
    Posts
    13,200
    Bump.

  29. #29
    Buster Brown's Avatar
    Buster Brown is offline Knowledgeable Member
    Join Date
    Feb 2012
    Location
    Proud Bostonian
    Posts
    4,722
    Bump

  30. #30
    snowblowjoe's Avatar
    snowblowjoe is offline Senior Member
    Join Date
    Apr 2012
    Posts
    1,267
    Blog Entries
    1
    I wanna get off my ai now. .. I don't want to get letrozole estrogen rebound so how long should I run my exemestane?

  31. #31
    MickeyKnox is offline Banned
    Join Date
    Dec 2011
    Location
    CANADA
    Posts
    13,200
    Quote Originally Posted by snowblowjoe View Post
    I wanna get off my ai now. .. I don't want to get letrozole estrogen rebound so how long should I run my exemestane?
    Please keep the questions related the thread topic. Post your own thread in the Q&A Forum. Thanks.

  32. #32
    Far from massive's Avatar
    Far from massive is offline Knowledgeable Member
    Join Date
    Sep 2010
    Location
    No Sources Given
    Posts
    5,389
    Quote Originally Posted by MickeyKnox View Post
    Some points to remember before you begin reading.

    I have gathered information from several studies that were relevant, and have attempted to streamline whenever I could so that key points of these articles would not be obscured from the importance of their effects on AAS use.

    I feel 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 .

    http://my.clevelandclinic.org/health...olesterol.aspx

    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.





    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.

    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).

    The following observations were made:

    1. Plasma lipids and IGF-I concentrations were unaffected by treatment.
    2. The PK properties of the 25-mg dose showed the highest concentrations 1 h after administration, indicating rapid absorption.
    3. Maximal estradiol suppression of 62 14% was observed at 12 h.
    4. The drug was well tolerated.
    5. 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:

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

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

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

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

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

    6. 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.

    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: http://dailymed.nlm.nih.gov/dailymed...l1231180697883

    *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.

    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

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



    MY CONCLUSIONS:

    To recap:

    Aromasin takes a little longer to raise serum levels and has a shorter half life (47 hours) , and is a suicide inhibitor. Recommend dose 10mg - every day (ED)

    Arimidex raises serum levels quicker yet has a longer half life (10 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.
    Great post, However in case it gets stickied, as it should... There may be a couple of typo's, see underlined sections, Are the half lives reversed? Also you said suicide where I believe you meant to say suicidal.

  33. #33
    MickeyKnox is offline Banned
    Join Date
    Dec 2011
    Location
    CANADA
    Posts
    13,200
    Thanks FFM.

    "Suicide inhibitor" is correct. Any others?

  34. #34
    lovbyts's Avatar
    lovbyts is offline Knowledgeable Member
    Join Date
    Apr 2008
    Posts
    29,390
    bump

  35. #35
    MickeyKnox is offline Banned
    Join Date
    Dec 2011
    Location
    CANADA
    Posts
    13,200
    Ttt..

  36. #36
    songdog's Avatar
    songdog is offline ARs TOP DOG ~ MONITOR ~
    Join Date
    Jun 2009
    Posts
    13,532
    Good job Mickey

  37. #37
    slumchop is offline New Member
    Join Date
    Feb 2013
    Location
    central PA
    Posts
    40
    Quote Originally Posted by redz View Post
    I've used both and im currently running adex. I think it's mostly a personal preference as long as they are dosed correctly.
    I agree 100%

  38. #38
    MickeyKnox is offline Banned
    Join Date
    Dec 2011
    Location
    CANADA
    Posts
    13,200
    Thanks SD.

    Shameless bump..

  39. #39
    kelkel's Avatar
    kelkel is offline HRT Specialist ~ AR-Platinum Elite-Hall of Famer ~ No Source Checks
    Join Date
    Sep 2010
    Location
    East Coast Dungeon
    Posts
    28,962
    Nice MK!
    -*- NO SOURCE CHECKS -*-

  40. #40
    emp
    emp is offline Junior Member
    Join Date
    Feb 2013
    Posts
    106
    Great read!

Page 1 of 6 123456 LastLast

Thread Information

Users Browsing this Thread

There are currently 1 users browsing this thread. (0 members and 1 guests)

Posting Permissions

  • You may not post new threads
  • You may not post replies
  • You may not post attachments
  • You may not edit your posts
  •