Aromatase Inhibitors Posted on 10 Apr 20:57 , 0 comments

[caption id="attachment_319" align="alignnone" width="300"]The degree of shredded is thanks to Aromatase inhibition! My degree of shredded is thanks to Aromatase inhibition! Cuts through my nipples! No Gyno here![/caption]

By Todd Lee M.D.
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Around 2003 the World Changed

Breast Cancer awareness was very strong and most people knew that breast cancer was often treatable by using estrogen blockers.  This of course didn't stop women from getting uterine cancer from the estrogen binding to the endometrium though.  That was the big downfall of the main treatment at the time, the SERM tamoxifen. Tamoxifen seemingly caused one cancer by curing another.  But that's not the truth.  By stopping and inhibiting breast growth by binding to the estrogen receptor on the breast there was just that much more estrogen in circulation to bind to the uterus!

So how did the world change? Aromatase inhibitors (AIs) were developed.  Now, instead of just gumming up the receptor like a bandaid, we now can stop the body from MAKING estrogen from testosterone.  

[caption id="attachment_692" align="alignnone" width="500"]Notice in both Breast cancer treatment algorithms the SERMS or the AIs are both first and second? Because they are COMPLETELY different but work synergistically together. Notice in both Breast cancer treatment algorithms the SERMS or the AIs are both first and second? Because they are COMPLETELY different but work synergistically together. Additionaly notice it says "tamoxifen" not "SERMs"? It's because Clomid is garbage![/caption]

Aromatase Inhibitors

[caption id="attachment_693" align="alignnone" width="524"]At the bottom right it shows how Aromatase converts Testosterone to estrogen. Blocking that enzyme results in more testosterone and less estrogen. At the bottom right it shows how Aromatase converts Testosterone to estrogen. Blocking that enzyme results in more testosterone and less estrogen.[/caption]

Aromatase Inhibitors and Bodybuilding

So how does this affect you, a guy?  A.I.’s can stop testosterone from converting to estrogen. This means neither your natural testosterone, anabolic steroids nor prohormones will be broken down into the ‘anti-test’ estrogen when you're on an A.I.

Why is this important? Estrogen not only counteracts the effects of testosterone, it stops your body from making test!

[caption id="attachment_695" align="alignnone" width="467"]Details the relationship of Visceral fat converting testosterone to estrogen and estrogens inhibition on testosterone production: as you gain fat you start to become a little bitch Details the relationship of Visceral fat converting testosterone to estrogen and estrogens inhibition on testosterone production: as you gain fat you start to become a little bitch[/caption]

The main point of a man using an A.I. post cycle is to stop estrogen from stopping testosterone production. By stopping your body from making estrogen through using an A.I., you stop the estrogen from turning off your testosterone production. Now, using the estrogen blocker Tamoxifen (a SERM NOT an A.I.), you will give the opposite signal of normal estrogen on the pituitary and turn ON testosterone production (as a secondary effect of LH release)!  

So Which Do I Use?

[caption id="attachment_696" align="alignnone" width="482"]This table shows you the order the Aromatase Inhibitors were created This table shows you the order the Aromatase Inhibitors were created, and how they inhibit aromatase. If you were going to use 2, you would use one irreversible one and a reversible one for fine tuning.  That's why I use 35 androsta and 7,8 benzo in Thor's Hammer [/caption]

Like the SERMs, A.I.s are prescription drugs and thus illegal.  

Of the three illegal aromatase inhibitors, I think Arimidex (Anastrazole) is the best and here is why:

Arimidex and Exemestane only take 7 days to reach steady state, letrozole takes 60!

This is weird because the half lives are 48 hours, 60 hours and 27 hours respectively. So I don't get how it takes 60 days for Letrozole to reach steady state when it should take 4 days with a 27 hour half life.

Arimidex had no negative effect on HDL and thus LDL, nor did it inhibit cortisol. Exemestane and Letrozole did. In case you're new here let me explain.  Estrogen is good for some stuff. One of which is it stimulates HDL production, which clears up LDL (the 'bad’ cholesterol).  By stopping all estrogen from forming in the body you're basically telling your body NOT to make HDL and thus your LDL gets sky high. This is how bodybuilders die usually. Not the liver or kidneys despite what you hear.

SO, if Arimidex somehow DOES NOT lower HDL, despite that making no sense, then you’ll live longer if you use Arimidex than if you use Exemestane or Letrozole.

Remember how Tamoxifen does the opposite of estrogen at the pituitary? It turns on, not off, testosterone production?  Well, it does the SAME thing as estrogen on the liver; it stimulates HDL production just like estrogen!  Yeah Tamoxifen! Way to kick some major ass!

[caption id="attachment_697" align="alignnone" width="462"]Chart showing who the boos is, Not arimidex! BUT arimidex doesn't hurt your HDL so in theory you can run it forever, staying lean year round! Chart showing who the boss is, Not Arimidex! BUT Arimidex doesn't hurt your HDL so in theory you can run it forever, staying lean year round![/caption]

Arimidex (Anastrazole) offers 97% inhibition of Aromatase, Letro 98%+ and Exemestane 98%.  Do what most guys do and use 1 mg Arimidex every 3 days instead of every day. This way you get the HDL benefits of Arimidex.

Legal Alternatives

Androsta

Androsta-3,5-diene-7,17-dione (Androsta) is a metabolite of 7-Keto-DHEA, which is a very potent suicide aromatase inhibitor. Like Exemestane, the other suicide inhibitor, it destroys the aromatase enzyme so there is no rebound in estrogen after you stop using it like Letrozole or Arimidex cause. It is a natural occurring compound, produced by metabolism of the prohormone DHEA and it’s used in a wide array of supplemental stacks. It is so powerful that even the World Anti-doping Agency (WADA) has it on its banned list of anabolic agents, meaning Olympians will fail a drug test if it shows up in the blood. This does not make it illegal, they have everything on that list from asthma medication to creatine to even CAFFEINE! Ridiculous!! I have included Androsta in the Thor's Hammer Combo Pack! 

7,8 Benzo

7,8 Benzoflavone is a synthetic flavone derivative, which is a potent aromatase inhibitor. It is known as alpha-naphthoflavone and it shouldn’t be confused with 5,6 benzo, known as, beta-naphthoflavone, which is an inducer of detoxification enzymes and is not an aromatase inhibitor at all.

I am also including this A.I. in Thor’s Hammer combo pack!

Summary

Arimidex has no downsides and is almost as effective as letro but it’s active so much earlier that for the first 60 days Arimidex is stronger. Since no PCT is 60 days long…. Arimidex is king. Now, keep in mind that this is comparing 2.5 mg of letro a day to 1 mg Arimidex.  In my PCT article I show the study that proves 2.5 mg letro a WEEK is better than 2.5 mg letro a DAY for purposes of PCT.  Likewise, normal use of Arimidex in bodybuilders is 1 mg Arimidex every 2 to 3 days not every day.

If you would rather not break the law, use Thor’s Hammer combo pack to get as close as legally possible to Arimidex and Tamoxifen, and to get as close as legally possible to Viagra and HCG. I pulled no punches, and I designed the best shit on earth!

Click Here to get THOR'S HAMMER COMBO PACK!!

References

Letrozole

Buzdar AU, Robertson JF, Eiermann W, Nabholtz JM: An overview of the pharmacology and pharmacokinetics of the newer generation aromatase inhibitors anastrozole, letrozole, and exemestane. Cancer. Nov 1;95(9):2006-16, 2002

  1. Haynes BP, Dowsett M, Miller WR, Dixon JM, Bhatnagar AS: The pharmacology of letrozole. J Steroid Biochem Mol Biol. Oct;87(1):35-45, 2003
  2. Buzdar AU: Pharmacology and pharmacokinetics of the newer generation aromatase inhibitors. Clin Cancer Res. Jan;9(1 Pt 2):468S-72S, 2003
  3. Chen S, Masri S, Wang X, Phung S, Yuan YC, Wu X. What do we know about the mechanisms of aromatase inhibitor resistance? J Steroid Biochem Mol Biol. 102(1-5):232-40, 2006
  4. Miller, WR; O′Neill, J. The importance of local synthesis of estrogen within the breast. Steroids. 50:537–548, 1987

Arimidex

  1. Buzdar AU: Pharmacology and pharmacokinetics of the newer generation aromatase inhibitors. Clin Cancer Res. Jan;9(1 Pt 2):468S-72S, 2003
  2. Riepe FG, Baus I, Wiest S, Krone N, Sippell WG, Partsch CJ: Treatment of pubertal gynecomastia with the specific aromatase inhibitor anastrozole. Horm Res. 62(3):113-8. Epub 2004 Jul 20, 2004

Exemestane

  1. Buzdar AU: Pharmacology and pharmacokinetics of the newer generation aromatase inhibitors. Clin Cancer Res. Jan;9(1 Pt 2):468S-72S, 2003
  2. Lonning PE: Exemestane: a review of its clinical efficacy and safety. Breast. Jun;10(3):198-208, 2001
  3. Mauras N, Lima J, Patel D, Rini A, di Salle E, Kwok A, Lippe B: Pharmacokinetics and dose finding of a potent aromatase inhibitor, aromasin (exemestane), in young males. J Clin Endocrinol Metab. Dec;88(12):5951-6, 2003

Disclaimer

Nothing in this article or on this site should be considered medical advice or as an endorsement to violate any law of the country in which you reside.  The information given is for fun and entertainment purposes only.  All claims are 100% dependent upon proper diet and exercise.  Please consult a medical practitioner prior to any diet and exercise program.