basskiller
08-03-2014, 03:13 AM
Estrogen on Cycle: The Good, The Bad, and The Proper Management of Both
The next progression in Estrogen management is the use of Aromatase Inhibitors to control overall Estrogen levels. This has been a huge advancement in the management of estrogen. Aromatase Inhibitors act upon the Aromatase enzyme. This is the enzyme responsible for the conversion of testosterone to estrogen within the body. Aromatase Inhibitors prevent the binding of Aromatase to testosterone so the process of Aromatozation of test to Estrogen cannot take place. This sounds like the ultimate solution to the problem of Estrogen Management on cycle and too a large degree it is. However there are different Aromatase Inhibitors that may make one a more prudent choice than the other for certain situations or individuals. Also the value of Serms and their role in estrogen management cannot be dismissed just yet.
So we see we have 2 categories of compounds that can be of use to us in properly managing Estrogen or its side effects, Serms and AIs. Let''s take a look at our options in categories, their differences and potential interactions with one another, and how they might be used together to accomplish our goal.
First we will look at AIs as in my opinion they are the core of our Estrogen Management program. We essentially have 2 types of AI''s to choose from. Type 1 AIs like Exemestane and Type 2 AI''s such as letrozole or Anastrozole (arimidex). The difference in these types is as follows. A Type 1 AI like Exemestane binds permanently to the site on the Aromatase Enzyme where it binds to testosterone allowing its conversion to Estrogen. This permanent binding renders the Aromatase totally and permanently inactive. In contrast Type 2 AIs temporarily bind to this site on the Aromatase Enzyme rendering it inactive as long as the AI is being used. Onçe use of type 2 AI stops the aromatase will reactivate. So whats the difference in these Ai types for our purposes? Well Due to the '"reactivation" if you will of existing Aromatase with a Type 2 AI, when you stop using it a spike in Estrogen (often referred to as rebound) will occur due to the sudden increase availability of Aromatase Enzyme. Another important distinction when it comes to Type 1 and Type 2 AI''s. A Type 1 AI like Exemestane remains unaffected by the introduction of a serm into your Estrogen management program. Type 2 AIs like letrozole and Arimidex suffer a reduced in blood levels and effectiveness with the introduction of some serms. I will touch more on why we may need to introduce a serm a little farther on in this article.
When it comes to the strength of these AI''s letrozole would be the strongest followed by Arimidex and then by Exemestane. Now people might be up in arms saying Exemestane is stronger than Arimidex however when one looks and compare data from studies done on MALES the order of strength is exactly as I stated it, quite often much confusion comes in to play when people recite data on AI's taken from studies on women. The fact is AI's behave differently in males, they are less effective in males, and for our purposes it is only prudent to compare data gathered from studies on males to portray an accurate picture.
The next aspect to be considered when looking at AIs are the effects they indirectly illicit in other areas. We stated the positive effects of Estrogen, we must realize by lowering Estrogen via Ai use some of these positive effects may be compromised. It is important to look at the various AI options available and possibly use the data to help pick which AI we use. letrozole is an extremely potent AI and its effects demonstrate this as would be expected. letrozole has an adverse effect on lipid profile and somewhat on IGF levels. On the other hand Arimdex has a small impact in the area of IGF and depending upon which studies you cite a small adverse impact on lipids to no adverse impact on lipids. Exemestane seems to have no clinical impact on either IGF or lipids.
It is important to realize that it may seem like Exemestane shines as a clear cut winner when it comes to choice of AI, however I do not necessarily believe this to be the case for everyone. In some cases or maybe better said in some people, an extremely powerful AI like letrozole must be used to manage Estrogen properly. Some may respond better to Arimidex than Exemestane. I believe there is a place for all 3 of these. That being said, if possible my personal first choice of AI is Exemestane due to its lack of interaction with other compounds we may need to introduce such as certain serms, its positive effects on IGF and Lipids over other options, and also its lack of potential "rebound"(although I think that is an overstated issue quite often).
Regardless of which AI you choose for the vast majority of us our goal can be accomplished of maintaining Estrogen levels in the normal range while on cycle. It might seem like the discussion is over. Why do we even need to look at Serms? Read on:
So we have our Estrogen levels managed, all should be good. Well yes in most cases it will be but what if it isn't? What if you start to get sensitive, itchy or painful nipples? What if you get a lump around your nipple area? What if you are so predisposed to gyno you still get symptoms using an AI? It shouldnt happen but if it does your immediate solution should be a serm.
So we know what serms do. As stated above they bind to the Estrogen receptor in breast tissue, preventing Estrogen from eliciting its effects, which in this case is undesired breast development and tissue growth. However all serms are not created equal for this purpose. I am of the opinion that Raloxifene and tamoxifen are the 2 best suited serms for this purpose.
Raloxifene is the serm with the highest binding affinity to the Estrogen receptor in breast tissue. tamoxifen would be second. This means Raloxifene is the most effective serm available for gyno treatment and or prevention. Another point that bears mentioning, when using a Type 2 AI like Arimidex or letrozole, tamoxifen reduces blood levels of both of these AI's. Raloxifene on the other hand has no effect on blood levels of these AI's, allowing them to be run in conjunction with Raloxifene with no decrease in AI effectiveness. As was mentioned above any serm can be run with Exemestane (a Type 1 AI) with no impact on Exemestane's effectiveness.
tamoxifen is the serm with probably the most clinical data supporting its use for gyno prevention and treatment, in all likelihood due to the age of the drug. It is very effective for this purpose and very versatile as it is equally if not more effective in the area of PCT as well, meaning often it is likely on hand so it is readily available for most to use in the case of gyno symptoms.
So let's begin to put this all together. An AI should be the core of your Estrogen management program; the goal should be Estrogen levels in the clinically normal range even while on cycle. Id say between 25-30. I cannot emphasize enough the importance of blood work as a management tool. It really is the only effective means of proper Estrogen management (hormone profile management for that matter).
All AI''s can effectively manage Estrogen. My preference in order for this purpose would be Exemestane , then Arimidex , then letrozole however as stated earlier they all have their place. If Exemestane works well for you you have the luxury of the least amount of undesirable side effects and the most versatility as far as combining with a serm should the need arise for gyno prevention and treatment.
The logical question is why do even need to worry about a serm if I mange Estrogen with an Ai? Well hopefully you don't however in some cases it may become necessary due to predisposition, preexisting gyno , very high dosages of aromatizing steroids and so on. For this purpose Raloxifene is in my opinion the top choice offering no reduction in effectiveness of any AI you are running and the most powerful protection against gyno due to its binding affinity to the E receptor in brest tissue. tamoxifen is also a very solid option especially if running Exemestane as your Ai. If you are running letrozole or arimidex a corresponding increase in the dosage of Ai may be required due to tamoxifen reducing blood levels and effectiveness of these 2 AIs.
Bringng it to theReal World:
1- Manage Estrogen levels with an AI: Exemestane offers the most versatility with fewest adverse effects.
2- Have a Serm on hand in case of Gyno flare up. Raloxifene is most effective and has no adverse interactions with any AIs.
Run a low dose AI with your cycle to try to keep estrogen in the clinically normal range so you can reap the benefits and reduce the deleterious effects. Have a serm on hand just in case gyno rears its head. If it does start a serm immediately. At this point you NEED blood work so you can properly assess your situation and possibly adjust AI dosage up which may allow discontinuation of serm. It may not. You may need to run a serm and AI in conjunction on cycle but it is very unlikely. An Ai should be able to manage Estrogen properly for the vast majority of us. If you do need to run a serm and AI together I cannot emphasize enough that you need to reevaluate your situation. Elevated estrogen has some serious effects as I mentioned above. You should consider this option as I would encourage many too do anyway. Reduce the amount of aromatizing steroids in your cycle and replace them with non-aromatizing compounds. I cannot emphasize this enough. For example a lower test dose will allow for easier estrogen management. This is probably the single biggest thing any of us can do to help ensure proper estrogen management (besides blood work', which again is essential).
One more topic I want to touch on is Gyno. Gyno is considered the worst side effect of elevated estrogen but the fact is it is far from it. There are many much more serious issues going on inside of you if you start growing breasts. That being said when it does occur or start to occur we want to stop it. So often I see people recommend letrozole to treat gyno. This is a horrible idea in my opinion. letrozole works to treat gyno by lowering overall Estrogen levels so much there is no circulating Estrogen to bind to the Estrogen receptor in breast tissue. If you paid attention above you saw the beneficial effects of Estrogen. Some aren't even beneficial, they are essential. I think to eliminate estrogen to this point throughout your entire body is foolish. Introduce a serm such as raloxifene, block the Estrogen receptor in the breast. The gyno then cannot grow. Then again using blood work adjust your AI dose to MANAGE estrogen levels while taking the serm to prevent the continuation of the gyno.
The above is an interesting topic. I hope this info proved useful to some and I would love to discuss it further.
JimiThing
The next progression in Estrogen management is the use of Aromatase Inhibitors to control overall Estrogen levels. This has been a huge advancement in the management of estrogen. Aromatase Inhibitors act upon the Aromatase enzyme. This is the enzyme responsible for the conversion of testosterone to estrogen within the body. Aromatase Inhibitors prevent the binding of Aromatase to testosterone so the process of Aromatozation of test to Estrogen cannot take place. This sounds like the ultimate solution to the problem of Estrogen Management on cycle and too a large degree it is. However there are different Aromatase Inhibitors that may make one a more prudent choice than the other for certain situations or individuals. Also the value of Serms and their role in estrogen management cannot be dismissed just yet.
So we see we have 2 categories of compounds that can be of use to us in properly managing Estrogen or its side effects, Serms and AIs. Let''s take a look at our options in categories, their differences and potential interactions with one another, and how they might be used together to accomplish our goal.
First we will look at AIs as in my opinion they are the core of our Estrogen Management program. We essentially have 2 types of AI''s to choose from. Type 1 AIs like Exemestane and Type 2 AI''s such as letrozole or Anastrozole (arimidex). The difference in these types is as follows. A Type 1 AI like Exemestane binds permanently to the site on the Aromatase Enzyme where it binds to testosterone allowing its conversion to Estrogen. This permanent binding renders the Aromatase totally and permanently inactive. In contrast Type 2 AIs temporarily bind to this site on the Aromatase Enzyme rendering it inactive as long as the AI is being used. Onçe use of type 2 AI stops the aromatase will reactivate. So whats the difference in these Ai types for our purposes? Well Due to the '"reactivation" if you will of existing Aromatase with a Type 2 AI, when you stop using it a spike in Estrogen (often referred to as rebound) will occur due to the sudden increase availability of Aromatase Enzyme. Another important distinction when it comes to Type 1 and Type 2 AI''s. A Type 1 AI like Exemestane remains unaffected by the introduction of a serm into your Estrogen management program. Type 2 AIs like letrozole and Arimidex suffer a reduced in blood levels and effectiveness with the introduction of some serms. I will touch more on why we may need to introduce a serm a little farther on in this article.
When it comes to the strength of these AI''s letrozole would be the strongest followed by Arimidex and then by Exemestane. Now people might be up in arms saying Exemestane is stronger than Arimidex however when one looks and compare data from studies done on MALES the order of strength is exactly as I stated it, quite often much confusion comes in to play when people recite data on AI's taken from studies on women. The fact is AI's behave differently in males, they are less effective in males, and for our purposes it is only prudent to compare data gathered from studies on males to portray an accurate picture.
The next aspect to be considered when looking at AIs are the effects they indirectly illicit in other areas. We stated the positive effects of Estrogen, we must realize by lowering Estrogen via Ai use some of these positive effects may be compromised. It is important to look at the various AI options available and possibly use the data to help pick which AI we use. letrozole is an extremely potent AI and its effects demonstrate this as would be expected. letrozole has an adverse effect on lipid profile and somewhat on IGF levels. On the other hand Arimdex has a small impact in the area of IGF and depending upon which studies you cite a small adverse impact on lipids to no adverse impact on lipids. Exemestane seems to have no clinical impact on either IGF or lipids.
It is important to realize that it may seem like Exemestane shines as a clear cut winner when it comes to choice of AI, however I do not necessarily believe this to be the case for everyone. In some cases or maybe better said in some people, an extremely powerful AI like letrozole must be used to manage Estrogen properly. Some may respond better to Arimidex than Exemestane. I believe there is a place for all 3 of these. That being said, if possible my personal first choice of AI is Exemestane due to its lack of interaction with other compounds we may need to introduce such as certain serms, its positive effects on IGF and Lipids over other options, and also its lack of potential "rebound"(although I think that is an overstated issue quite often).
Regardless of which AI you choose for the vast majority of us our goal can be accomplished of maintaining Estrogen levels in the normal range while on cycle. It might seem like the discussion is over. Why do we even need to look at Serms? Read on:
So we have our Estrogen levels managed, all should be good. Well yes in most cases it will be but what if it isn't? What if you start to get sensitive, itchy or painful nipples? What if you get a lump around your nipple area? What if you are so predisposed to gyno you still get symptoms using an AI? It shouldnt happen but if it does your immediate solution should be a serm.
So we know what serms do. As stated above they bind to the Estrogen receptor in breast tissue, preventing Estrogen from eliciting its effects, which in this case is undesired breast development and tissue growth. However all serms are not created equal for this purpose. I am of the opinion that Raloxifene and tamoxifen are the 2 best suited serms for this purpose.
Raloxifene is the serm with the highest binding affinity to the Estrogen receptor in breast tissue. tamoxifen would be second. This means Raloxifene is the most effective serm available for gyno treatment and or prevention. Another point that bears mentioning, when using a Type 2 AI like Arimidex or letrozole, tamoxifen reduces blood levels of both of these AI's. Raloxifene on the other hand has no effect on blood levels of these AI's, allowing them to be run in conjunction with Raloxifene with no decrease in AI effectiveness. As was mentioned above any serm can be run with Exemestane (a Type 1 AI) with no impact on Exemestane's effectiveness.
tamoxifen is the serm with probably the most clinical data supporting its use for gyno prevention and treatment, in all likelihood due to the age of the drug. It is very effective for this purpose and very versatile as it is equally if not more effective in the area of PCT as well, meaning often it is likely on hand so it is readily available for most to use in the case of gyno symptoms.
So let's begin to put this all together. An AI should be the core of your Estrogen management program; the goal should be Estrogen levels in the clinically normal range even while on cycle. Id say between 25-30. I cannot emphasize enough the importance of blood work as a management tool. It really is the only effective means of proper Estrogen management (hormone profile management for that matter).
All AI''s can effectively manage Estrogen. My preference in order for this purpose would be Exemestane , then Arimidex , then letrozole however as stated earlier they all have their place. If Exemestane works well for you you have the luxury of the least amount of undesirable side effects and the most versatility as far as combining with a serm should the need arise for gyno prevention and treatment.
The logical question is why do even need to worry about a serm if I mange Estrogen with an Ai? Well hopefully you don't however in some cases it may become necessary due to predisposition, preexisting gyno , very high dosages of aromatizing steroids and so on. For this purpose Raloxifene is in my opinion the top choice offering no reduction in effectiveness of any AI you are running and the most powerful protection against gyno due to its binding affinity to the E receptor in brest tissue. tamoxifen is also a very solid option especially if running Exemestane as your Ai. If you are running letrozole or arimidex a corresponding increase in the dosage of Ai may be required due to tamoxifen reducing blood levels and effectiveness of these 2 AIs.
Bringng it to theReal World:
1- Manage Estrogen levels with an AI: Exemestane offers the most versatility with fewest adverse effects.
2- Have a Serm on hand in case of Gyno flare up. Raloxifene is most effective and has no adverse interactions with any AIs.
Run a low dose AI with your cycle to try to keep estrogen in the clinically normal range so you can reap the benefits and reduce the deleterious effects. Have a serm on hand just in case gyno rears its head. If it does start a serm immediately. At this point you NEED blood work so you can properly assess your situation and possibly adjust AI dosage up which may allow discontinuation of serm. It may not. You may need to run a serm and AI in conjunction on cycle but it is very unlikely. An Ai should be able to manage Estrogen properly for the vast majority of us. If you do need to run a serm and AI together I cannot emphasize enough that you need to reevaluate your situation. Elevated estrogen has some serious effects as I mentioned above. You should consider this option as I would encourage many too do anyway. Reduce the amount of aromatizing steroids in your cycle and replace them with non-aromatizing compounds. I cannot emphasize this enough. For example a lower test dose will allow for easier estrogen management. This is probably the single biggest thing any of us can do to help ensure proper estrogen management (besides blood work', which again is essential).
One more topic I want to touch on is Gyno. Gyno is considered the worst side effect of elevated estrogen but the fact is it is far from it. There are many much more serious issues going on inside of you if you start growing breasts. That being said when it does occur or start to occur we want to stop it. So often I see people recommend letrozole to treat gyno. This is a horrible idea in my opinion. letrozole works to treat gyno by lowering overall Estrogen levels so much there is no circulating Estrogen to bind to the Estrogen receptor in breast tissue. If you paid attention above you saw the beneficial effects of Estrogen. Some aren't even beneficial, they are essential. I think to eliminate estrogen to this point throughout your entire body is foolish. Introduce a serm such as raloxifene, block the Estrogen receptor in the breast. The gyno then cannot grow. Then again using blood work adjust your AI dose to MANAGE estrogen levels while taking the serm to prevent the continuation of the gyno.
The above is an interesting topic. I hope this info proved useful to some and I would love to discuss it further.
JimiThing