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Using Aromasin with Tamoxifen During Post Steroid Cycle Therapy

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Using Aromasin with Tamoxifen During Post Steroid Cycle Therapy

Dear Friend and Fellow Athlete,

Today's EliteFitness.com News article Using Aromasin with Tamoxifen During Post Steroid Cycle Therapy is brought to you by AG-Guys.com - home to all your research chemical needs. The article is by my friend Anthony Roberts. Anthony is the author of Beyond Steroids - about how you can discover and learn to use all the world's newest, rarest and most effective bodybuilding drugs... The ones that really work, but have never before been written about... And Beyond Steroids will show you new and radical ways to combine the new stuff with the "classic anabolic steroids" in ways most Pro Bodybuilders don't even understand. Here's a link to go Beyond Steroids.

And a little further down in the right sidebar, we have an article from my friends at Ziegler Labs. It's all about the invention of the anabolic steroid Dianabol and how athletes have used it over the years to achieve superior performance - so, I'm passing it along to you. I'm sure you'll find it interesting.

Using Aromasin with Tamoxifen During Post Steroid Cycle Therapy

Aromasin (Exemestane) is one of those weird compounds that nobody really knows what to do with. What we generally hear about it makes it very uninteresting... It’s a third generation Aromatase Inhibitor.

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My friends at Ziegler Labs sent me the following article about the invention of the anabolic steroid Dianabol and how athletes have used it over the years to achieve superior performance - so, I'm passing it along to you. I'm sure you'll find it interesting.

In 1959 the physician John Ziegler fancied himself as a researcher who was on a quest to merge science and sports. He experimented on some pills, later called Dianabol, made of a derivative of the hormone testosterone. Produced in the testicles in males, testosterone not only has the power to turn a boy into a man, but it also sends messages to those primal areas in the brain that trigger strength. Every legitimate athletic goal has been shadowed by a parallel universe of counterfeit Olympic Gold and hormonal home runs.

Scientists in GermanyScientists in Germany first isolated testosterone in the 1930s by distilling urine from German police officers. They later synthesized it in their labs. German soldiers have proven to have been injected by physicians with testosterone during World War II. Following World War II the Soviet Union applied the German science to its Olympic athletes, male same as female, as part of Stalin’s crusade to prove communist superiority.

Molecular Structure D-BLADE:
Dianabol
Molecular Structure DIANABOL:
image

John ZieglerAnd that’s where John Ziegler showed up, desperately looking for a counter-weapon in a Cold War competition against a Russian enemy that no longer existed. Ziegler watched as the Soviets were pumping iron. He found their physics extremely hairy and outsized.

As a team doctor Ziegler discovered at the 1954 World Games in Vienna that the Soviets were using testosterone to boost their strength. Smart enough Ziegler invited the USSR’s team doctor to a local tavern. After a while the Soviet revealed that his lifters were building their muscles with testosterone.

1950 allies To beat the Russians with their own weapons Ziegler found allies who provided him with lab-made testosterone as well as literature on German research. The result was Dianabol.

Actually Dianabol did not pump up muscles as seen in the movies. In the chemistry of the body testosterone sends messages to muscle cells. In combination with a high protein diet and addicted workouts Dianabol acted like a high-powered amino acid.

superhumanIn addition it cut down recovery times. Ziegler Labs went ahead to follow these studies and finally came up with the first true sublingual equivalent to Dianabol, D-Blade.

The results were so spectacular that D-Blade is now proven to enable man to achieve physical performances to be considered SUPERHUMAN!

LIST OF olympic MEDAL WINNERS between 1954 and 1976:

medal winners
Number of Medals Winner Nations
161 Medals USSR and GDR
404 Medals for remaining 17 Nations
This corresponds to 28.48 % for only 2 nations (USSR and GDR)
SCIENTIFIC FACTS OF D-BLADE:
  • The active substance DIANABOL was developed by Dr. Ziegler in the sixties as the best oral steroid (proportion anabol-androgen) to date. It was used by ZIEGLER Labs as the basis for the development of D-Blade!

  • By integrating the active substance in a substance grid, which is 100% embedded in the membrane system, the efficiency of the substance is enhanced by a factor of 10!

  • The 17 AA loses its significance and is converted into a novel, synthetic subperitrophic membrane ester (17 M - hybrid - 17a-M-hybrid-17b-hydroxy-1.4-androstadien-3-one, (M-hybrid = palmitic acid myricyl ester) that simulates the human organism!

  • Due to the super-sublinguality thanks to this special structure, immediate flooding into the organism and 100% absorption into the bloodstream are effected!

  • There is no inactivation of the active substance, it can thus unfold its full effect over a longer period of time. So far no other oral steroid, pro-hormone, etc. has been able to achieve this goal!

  • With the C-14 myristic acid present in the membrane this absolutely new and patented administration form enables a very high level of plasma-protein binding of almost 98% whereby this mechanism creates a timed release effect that results in the active substance being metabolised by the organism very slowly, thus producing both, a constant, very high active substance level and anabolism!

  • RESULT: Strength of the muscle-building effect and the level of power enhancement are increased by a factor of 5 (500%) compared with conventional substances!

If you have no success with D-Blade, you’ll have no success with anything! Here's a link to learn more about D-Blade.

(AI) just like Arimidex (Anastrozole) and Femera (Letrozole). Both of those two drugs are very efficient at stopping the conversion of androgens into estrogen, and since we have them, why bother with Aromasin? It’s a little harder to get than the other two commonly used aromatase inhibitors, because it’s not in high demand, and there’s never been a readily apparent advantage to using it. And I mean... lets face it: It’s awkward-sounding. Aromasin doesn’t have much of a ring to it, and exemestane is even worse. Arimidex has a bunch of cool abbreviations ("A-dex" or just 'dex) and even Letrozole is just "Letro" to most people. Where’s the cool nickname for Aromasin/exemestane? A-Sin? E-Stane? It just doesn’t work. It’s the black sheep of AIs. And why do we even need it when we have Letrozole, which is by far the most efficient AI for stopping aromatization (the process by which your body converts testosterone into estrogen)? Letro can reduce estrogen levels by 98% or greater; clinically a dose as low as 100mcgs has been shown to provide maximum aromatase inhibition (2)!

So why would we need any other AIs? Well, first of all, estrogen is necessary for healthy joints (3) as well as a healthy immune system (4). So getting rid of 98% of the estrogen in your body for an extended period of time may not be the best of ideas. This may be useful on an extreme cutting cycle, leading up to a bodybuilding contest, or if you are particularly prone to gyno, but certainly can’t be used safely for extended periods of time without compromising your joints and immune system.

That leaves us with Arimidex, which isn’t as potent as Letrozole, but at .5mgs/day will still get rid of around half (50%) of the estrogen in your body. Problem solved, right? Use Arimidex on your typical cycles, and if you are very prone to gyno or are getting ready for a contest, use Letro.

But what about Post Cycle Therapy (PCT)?

I think at this point most people are sold on the use of Nolvadex (Tamoxifen Citrate) instead of Clomid for post cycle therapy (PCT), since both compete estrogen at the receptor site, both increase serum test levels, and both drugs may also alter blood lipid profiles favorably (6). But since 20mgs of Tamoxifen is equal to 150mgs of clomid for purposes of testosterone elevation, FSH and LH, but Tamoxifen doesn’t decrease the LH response to LHRH (6) I think most people agree to Nolvadex’s superiority for PCT.

Aromasin with Nolvadex

I’ve always been in favor of using Nolvadex during PCT, along with an AI, because reducing estrogen levels has been positively correlated with an increase in testosterone (7) so in my mind, it’s be beneficial to increase testosterone by as many mechanisms as possible while trying to recover your endogenous testosterone levels after a cycle. SO which AI do we use? Letro or A-dex? Well, why don’t we just keep using whichever one we used during the cycle, and add in some Nolvadex? Unfortunately, Nolvadex will significantly reduce the blood plasma levels of both Letrozole as well as Arimidex (8). So if we choose to use one of them with our Nolvadex on PCT, we’re throwing away a bit of money as the Nolvadex will be reducing their effectiveness.

This, of course, is where Aromasin comes in, at 20-25mgs/day.

Aromasin, at that dose, will raise your testosterone levels by about 60%, and also help out your free to bound testosterone ratio by lowering levels of Sex Hormone Binding Globulin (SHBG), by about 20% (12)... SHBG is that nasty enzyme that binds to testosterone and renders it useless for building muscle. But what about using it along with Nolvadex for PCT?

Difference Between Type-I and Type-II Aromatase Inhibitors

To understand why Aromasin may be useful in conjunction with Nolvadex while both Letro and A-dex suffer reduced effectiveness, we’ll need to first understand the differences between a Type-I and Type-II Aromatase Inhibitor. Type I inhibitors (like Aromasin) are actually steroidal compounds, while type II inhibitors (like Letro and A-dex) are non-steroidal drugs. Hence, androgenic side effects are very possible with Type-I AIs, and they should probably be avoided by women. Of course, there are some similarities between the two types of AIs…both type I & type II AIs mimic normal substrates (essentially androgens), allowing them to compete with the substrate for access to the binding site on the aromatase enzyme. After this binding, the next step is where things differ greatly for the two different types of AI’s. In the case of a type- I AI, the noncompetitive inhibitor will bind, and the enzyme initiates a sequence of hydroxylation; this hydroxylation produces an unbreakable covalent bond between the inhibitor and the enzyme protein. Now, enzyme activity is permanently blocked; even if all unattached inhibitor is removed. Aromatase enzyme activity can only be restored by new enzyme synthesis. Now, on the other hand, competitive inhibitors, called type II AI’s, reversibly bind to the active enzyme site, and one of two things can happen: 1.) either no enzyme activity is triggered or 2.) the enzyme is somehow triggered without effect. The type II inhibitor can now actually disassociate from the binding site, eventually allowing renewed competition between the inhibitor and the substrate for binding to the site.

This means that the effectiveness of competitive aromatase inhibitors depends on the relative concentrations and affinities of both the inhibitor and the substrate, while this is not so for noncompetitive inhibitors. Aromasin is a type-I inhibitor, meaning that once it has done its job, and deactivated the aromatase enzyme, we don’t need it anymore. Letrozole and Arimidex actually need to remain present to continue their effects. This is possibly why Nolvadex does not alter the pharmacokinetics of Aromasin (11).

Conclusion

Before we close the book on Aromasin, it’s worth noting that you can (and should) still use one of the non-steroidal AIs during your cycle to reduce estrogen, if necessary. When you are ready for PCT, you can then switch over to Aromasin and still experience the full effects of an AI, since there is no cross-over tolerance experienced between steroidal and non-steroidal AIs (9). Since Aromasin is about 65% efficient at suppressing estrogen (10), it’s certainly a very powerful agent, especially considering you won’t experience reduced effectiveness because of your concurrent use of Nolvadex or from any sort of tolerance developed by using other AIs on your cycle(9). There is also a decent amount of preclinical data suggesting that Aromasin has a beneficial effect on bone mineral metabolism that is not seen with non-steroidal agents, and it may also have beneficial effects on lipid metabolism that are not found in the non-steroidal Letro and A-dex (9).

Finally, as we’re going to be using Nolvadex for PCT anyway, and we ought to be using an AI with it for maximum recovery... I think

Aromasin- considering it’s compatibility with Nolvadex and beneficial effects on bone mineral content and lipid profile, has finally stopped being the black sheep of AIs and found a home in our cycles.

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References:

1. Clin Cancer Res. 2005 Apr 15;11(8):2809-21.

2. 2. J Clin Endocrinol Metab. 1995 Sep;80(9):2658-60.

3. [Clinical aspects of estrogen and bone metabolism] Clin Calcium. 2002 Sep;12(9):1246-51. Japanese.

4. Science, Vol 283, Issue 5406, 1277-1278 , 26 February 1999

5. J Clin Endocrinol Metab 2000 Jul;85(7):2370-7, "Estrogen Suppression in Males"

6. Fertil Steril. 1978 Mar;29(3):320-7

7. J Clin Endocrinol Metab. 2004 Mar;89(3):1174-80

8. .J Steroid Biochem Mol Biol. 2001 Dec;79(1-5):85-91.

9. The Oncologist, Vol. 9, No. 2, 126–136, April 2004

10. Zilembo N., Noberasco C., Bajetta E., Martinetti A., Mariani L., Orefici S. Endocrinological and clinical evaluation of exemestane, a new steroidal aromatase inhibitor. Br. J. Cancer, 72:

1007-1012, 1995

11. Clinical Cancer Research Vol. 10, 1943-1948, March 2004

12. The Journal of Clinical Endocrinology & Metabolism Vol. 88, No. 12 5951-5956

Copyright © 2003 by The Endocrine Society

Yours in sport,

George Spellwin

George Spellwin