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  • Doss's picture
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  • AI: what are they and do you need them?

  • Doss   •   Wed, Mar 20th, '13 21:19   •   69 replies, 6583 views

As I browse through the forums, I am seeing more and more that some are keeping their AI on-hand in case of gyno flare ups or other sides. The majority – I hope – is aware of the necessity of AI’s on cycle, but I wanted to address this for the lesser informed.

What is an AI?

An AI is an aromatase inhibitor. Aromatase is an enzyme whose sole responsibility is to synthesize estrogen hormones – estrone and estradiol – from androgens via a process called aromatization. Because our bodies are physiologically programmed to maintain a state of balance – homeostasis – aromatase enzymes are synthesized in response to elevated androgen levels. Therefore and in general, the higher the level of adrogens, the higher the level of aromatase enzymes. The higher the level of enzymes, the greater the potential for hyperestrogenism (excess estrogen). AI’s act to inhibit the activity of the enzyme, thereby providing regulation of estrogen levels.

High Estrogen Symptoms

• Fluid retention and weight gain
• Fluctuations in body temperature
• Elevated BP
• Adult acne
• Depression, apathy, irritability and aggression due to a hormonal imbalance
• Decrease libido or impotence
• Prostate issues (inflammation or cancer)
• Gyno

Why an AI

Taking into consideration that our androgen levels are well in excess while on cycle, the fact arises that the potential for excess estrogen dramatically increases. By allowing estrogen levels to rise uncontrollably, we are opening ourselves up to a host of symptoms associated with high estrogen. Outside of the risks of gyno, there is also the concern of sexual dysfunction. How many times do we see comments or reviews where a lesser experienced user is claiming bunk gear due to decreased of libido? Often times digging a little deeper into the cycle log or history of this individual, we will find an improper cycle and AI issues. Although some of the symptoms are minor, with gyno and libido issues being the greatest concern, there is no need IMO to experience any of these sides if they can be avoided. Considering that once you have gyno, the only way to get rid of it is through surgical removal, we should realize that these sides are much easier to prevent than they are to reverse. The AI’s main role here is to achieve greater hormonal balance and provide control for the user so as to avoid the occurrence of sides.

One aspect that I want to add to this is the effects estrogen has on the gonadotropins – LH & FSH. Studies have proven that estrogen provides negative feedback towards the synthesis and secretion of both LH & FSH. This is detrimental to the overall objective of PCT, which is to reboot natty systems. These gonadotropins main role here is to stimulate production of testosterone. If estrogen levels are elevated and left unchecked, outside of the listed side effects, the suppression of the gonadotropins will compromise the goal of PCT. Therefore, it is imperative that balance be achieved in order to not only prevent side effects but to also allow for a proper PCT and reset.

Types of AI’s

There are two types of AI’s:

• Type 1 (irreversible steroidal inhibitors)
• Type 2 (non-steroidal inhibitors)

Type 1 inhibitors form a permanent and deactivating bond with the aromatase enzyme, so it never lets go even when the drug is discontinued or its active life expires. Type 2 inhibitors inhibit the synthesis of estrogen via reversible competition for the aromatase enzyme, which means that it binds reversibly. An example of an irreversible inhibitor would be Aromasin (exemestane). Examples of reversible inhibitors, or Type 2, would be Letrozole (Femara) or Anastrozole (Arimidex).

Below is an excerpt from another thread that does a great job of explaining the two types and their modes of action:

Aromatase Inhibitors come in 2 types. Type 1 and Type 2. First Type 1 AI's bind by a process called hydroxylation; this hydroxylation process produces an unbreakable covalent bond between the inhibitor and the enzyme protein. Now the enzyme is permanently blocked even after all of the inhibitor is removed and can only be resumed by new enzyme synthesis. Type 2 Inhibitors on the other hand function all the same in their ability to reduce the binding process of the enzyme and the receptor. Except once the drug is discontinued or the concentration of the drug is sparse enough it is possible for the enzyme to seperate itself from the Inhibitor and eventually will allow renewed competion between the Inhibitor and the Enzyme for the receptor site. Aromasin is a type 1 AI and once it does what it's purpose is we don't need to continue use. Letro and Adex are Type 2 Ai's and the success of those drugs are continigent on the Doses and protocol of which we use them. Once you stop them you expose yourself to an Estrogen rebound. Now having said all of that there are also many other reason to why Aromasin use is beneficial to a Bodybuilder. One is Arimidex/Anastrozole Decreases IGF-1 18% while Aromasin/Exemestane Increases IGF-1 28%. Another is Aromasin is also known to decrease estrogen between 90-95% while boosting Endogenous Testosterone 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.

The above quoted paragraph's credit goes to CarlosDanger aka GS, who is IMHO the pct guru.

How much AI?

This answer can be tricky, because some degree of trial and error must take place to find your individual “sweet spot”. In order to do this, the following recommended doses should be administered during your cycle, and then blood tests must be run to determine where your estradiol levels are presently. This data will guide you in determining what, if any, tweaks are appropriate.

Aromasin: 12.5mg EOD
Arimidex: 0.25mg E3D
Letro: see below

My personal preference is Aromasin. Adex will suffice in terms of controlling enzyme activity during cycle. Because the bond Adex forms is reversible, it can cause the bound enzymes to become released and renew competition once the drug has been discontinued or its active life has expired. For this reason, IMO, Adex should be tapered off and Aromasin introduced leading into PCT. I am also more fanatical about ED dosing of Aromasin vs EOD. With a drug half-life of 27 hrs, a lower dose of 6.25mg ED would IMO yield a more stable and better sustained level. Once again, blood tests are a must for confirming the individuals “sweet spot”.
Letro, once again, should be used in the case of an emergency such as gyno flares. Because estrogen is active in the breast tissue during your gyno flares, eradication of the hormone will cause suppression of the symptom. With this in mind, you can and should expect to experience the symptoms of low estrogen (see below). The following is an excerpt from a conversation between I and someone about letro:

There's no particular concrete method to determining doses for Letro. Like the other AI's it really depends on how ur body responds to it. Tapering up to and maintaining a concentration at which I have had guys run is 2.5mg, maintaing that dose until u see relief of symptoms is key and after a week of relief u should begin to taper down. I recommend a daily administration. There is a great link where I found this protocol.
http://www.basskilleronline.com/gynoprevention.shtml

Now, keeping all of this in mind, I arrive at my final point:

TOO MUCH AI IS DETRIMENTAL AS WELL!!

The goal with incorporating an AI is to regulate the enzyme’s activity so as to avoid hyperestrogenism, not completely suppress it. Some estrogen is needed for normal physiological functions. Just like too much estrogen can lead to a host of side effects, so too can too little estrogen. Following the recommended dosages and running your blood work is key to achieving balance in this regard.

Low Estrogen Symptoms:

• Fatigue
• Weight gain
• Hot flashes and night sweats
• Depression, apathy, irritability and aggression due to a hormonal imbalance
• Elevated BP
• Insomnia or restless sleep
• Headaches
• Low libido or impotence
• Stiffness or joint pain
• Anxiety
• Heart palpitations
• Adult acne

UPDATE

For the longest time, we've preached a 27h half life for aromasin. We came to this conclusion based on case studies available to us at that time. These studies involved test subjects undergoing treatment for breast cancer (women).

Recent studies, however, have been showing a different half life for men. Below is an excerpt from one of these studies:

The terminal half-life in the present study (8.9 h) was considerably shorter than the published value of 27 h (23). The reason for this difference is not clear, but may be related to a true gender dependency possibly involving the volume of distribution (lower in males than females) and plasma or tissue protein binding (respectively, higher and lower in males). This finding may also be due to the lower sensitivity of the analytical methodology used in the previous studies (14 pg/ml by HPLC/RIA) (21).

The case study is from the Journal of Endocrinology and Metabolism and can be read here:

http://m.jcem.endojournals.org/content/88/12/5951.long

Comments

  • Keez's picture
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  • Keez
  • 4 years ago

Hey bruva
Can I pm you?
I read ya piece on ai's. Well helpful! I want to know more about blood work

  • thahulk2014's picture
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  • thahulk2014
  • 6 years ago

Fr sent

  • Hustle28's picture
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  • Hustle28
  • 6 years ago

what would work better aromasin liquid ??? or tab??? also adex same question

  • Doss's picture
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Theoretically, tabs would provide more consistency with dosages. Fewer variables involved when you don't have to shake a suspension and draw before it settles.

  • jackarow's picture
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  • jackarow
  • 6 years ago

Forgive me bro if this has been covered elsewhere. Im doing a cycle of test prop and E and mast prop and E. I realize the antiestrogenic effects of masteron are not that great and I have aromisan for AI. Should I still use the aro at 12.5 eod or should the doseage be less because of the masteron. This is my second cycle and I will get bloods done but wanted help beforehand as to not have to find out ive crashed my e2 or anything. Im 35 about 190 previous cycle was test only. I figured Doss that youd be one of the best to seek info. Thanks bro.

  • Doss's picture
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Masteron will have an impact on your e2 levels. But to what extent? Only bloodwork can confirm if you have the right balance between it and your AI. If it were me, I'd cut the AI dose in half but have bloodwork done around weeks 5-7.

  • Denser's picture
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  • Denser
  • 6 years ago

Great info bro! +2

Does Aromasin work in such a way that the higher the dose, the more estrogen it kills?

  • Doss's picture
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Yes. It doesn't actually kill estrogen tho. It suppresses it by inhibiting enzyme activity. And the effects are dose dependent.

  • krakhedz's picture
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  • krakhedz
  • 7 years ago

Hey i'm sorry if this sounds stupid, i will be starting my first cycle of test e really soon, do you recommend i take 12.5mg of aromasin(before i find my sweet spot) every day or every week? Again i'm new to this try to take it easy on me. Also one more thing, should i use liquid or tab form?

  • vhman's picture
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Use the search function above (blue magnifying glass, top left) and you will find countless answers to your question. Aro is USUALLY dosed every other day (EOD). Again, search it out and you will find the answer.

  • Doss's picture
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Sorry for the late response... For the longest we've recommended eod dosing. For some that works and is a matter of gettin the dose strength matched. For others ed dosing was more appropriate. Lately, we've seeing patterns more and more with bloodwork that shows ed dosing to be more effective. In light of the study posted below, you can see why.

So, my advice is to dose ED and go with 6.25 to start. Don't just go off of feeling and personal recommendations. I can't emphasize enough about the importance of running bloodwork, especially for newer aas users like yourself.

  • vhman's picture
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Thanks for your response and your great original post. It's been very helpful to many. Agree completely regarding blood work and starting with 6.25.

  • Doss's picture
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You're welcome brother. That was meant for both you and the the gentleman you had replied to.

  • redNblue's picture
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  • redNblue
  • 7 years ago

Just got my E2 results back, 39.9 ng/l , to high, to low, I´m confused tbh.

  • Doss's picture
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That's not too bad bro. A slight increase in your AI or adjustment in frequency could drop it a few more points.

  • redNblue's picture
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Thank you for your reply, I´m really at a loss right now, I was happy it went from 200 to 39.9 but I´m more confused now, not sure if it´s to high or because I´m on AAS I could tolerate a higher number.
I´m willing to experiment for sure, currently taking Aromasin 6.25ed, should I bump it to 8.33mg ed or maybe keep the dose as it is but take it twice a day ?
I appreciate your advise.

Best regards !

  • Doss's picture
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If that's your sweet spot and holding you at 39, I'd consider how you feel at those numbers. If the libido is fine and acne is ok, I wouldn't adjust unless sides appear or you increase your test dose.

  • redNblue's picture
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Libido as been better, it´s ok but nothing comparing with a few weeks back, I wish I had gone for tests then but hey I´m a newb and still learning, acne is horrible mate tbh, all over my upper body, neck is the worse and my chest and back are bad also, the pimples are really small and bright red.
Also my upper chest and neck are very red.

  • Doss's picture
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Somehow I missed this post of yours. Sorry about that brother

  • Doss's picture
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  • Doss
  • 7 years ago

UPDATE

For the longest time, we've preached a 27h half life for aromasin. We came to this conclusion based on case studies available to us at that time. These studies involved test subjects undergoing treatment for breast cancer (women).

Recent studies, however, have been showing a different half life for men. Below is an excerpt from one of these studies:

The terminal half-life in the present study (8.9 h) was considerably shorter than the published value of 27 h (23). The reason for this difference is not clear, but may be related to a true gender dependency possibly involving the volume of distribution (lower in males than females) and plasma or tissue protein binding (respectively, higher and lower in males). This finding may also be due to the lower sensitivity of the analytical methodology used in the previous studies (14 pg/ml by HPLC/RIA) (21).

The case study is from the Journal of Endocrinology and Metabolism and can be read here:

http://m.jcem.endojournals.org/content/88/12/5951.long

  • MakaveliCD7's picture
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I definitely think it's also the structure of males metabolism vs women's that plays a factor too....I think in most cases that women's are more sensitive to hormones say than male for the fact that women require such a smaller dose of hormones to produce results than a male....I feel it have everything to do with our genetic wiring and most certainly our metabolic make up.... So in effect I think that the conversion rates will differ as well which supports this study

Excellent post Dossy again!!! +1 my nooka

  • Doss's picture
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I can't take full credit here. This youngster and I were having a debate on this topic. Standing firm on my 27h half life I went lookin for a reference link outside of Wikipedia. Lol. When this study popped up. Trust me, my arrogant ass don't like admitting I'm wrong, since I rarely am lmao, but this def is worth posting IMO. Now i just gotta revise this thread topic...

  • Sparkayy's picture
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  • Sparkayy
  • 7 years ago

thanks for this bro!

  • RoidyNoob's picture
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  • RoidyNoob
  • 7 years ago

Rich Piana said in one of his videos with Ric drasin, that Adex reduces good cholesterol level. Whats your take on this?
+1

  • j223's picture
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Adex is prescribed 1mg per day in women with breast cancer for many many years sometimes the rest of their lives.

Even then the HDL decrease isn't drastic. Your diet can help increase it though. Aromasin on the other hand does put some stress on the liver. So both drugs have their ups and downs. Still need to take an AI

  • RoidyNoob's picture
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  • RoidyNoob
  • 7 years ago
  • @j223

Thanks dude, and obviously will always use an AI.

  • Doss's picture
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That is prolly the most neutral post of yours yet regard aromasin. Lol ;)

  • Doss's picture
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Unsure bro. Never compared lipid panels for AI's

  • anon
 
  • Anonymous
  • 7 years ago

That dude in quotes is a smart mofo;) Great post bro. Love all the info u have posted up here. Hope the newer guys read it all

  • Doss's picture
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He sho is. Lol. It's guys like him that make this site what it is