E2 with arimidex and aromasin
Posted: Mon Jun 22, 2020 1:07 pm
Gynecomastia Mechanics
First of all there are three different types of Gynecomastia (Gyno): Estrogen induced, Progesterone induced and Prolactin induced. Of course, you can avoid all three types of Gyno by keeping Estrogen (E2) within the normal range (unless using a 19-nor). The precursor to any type of Gyno is almost always Estrogen! Once you let Estrogen build up you signal to your brain that you have conceived, it doesn’t matter if you are a man or woman, your body at this point will have to go through certain processes to prepare you for lactation. Firstly your body will rush to use that Estrogen and build up breast tissue (which will form a lump) which is mandatory for the lactation process. Once this stage has been completed and you have let Estrogen still high your Progesterone will increase (Estrogen can still remain high) which is an attempt from your body to make the tissue larger and also make your aerolas bigger (puffy and enlarged nipples) again to get them ready for lactation. Last stage of Gyno is Prolactin lactation, all previous stages were preparing the body for this moment at this point your Progesterone and Estrogen will drop and your Prolactin will spike, this is when someone starts lactating.
Estrogen (E2)
Estrogen is commonly referred to as “E2”. Estrogens are made up of Estrone (E1), Estradiol (E2), and Estriol (E3) (though the one we’re concerned with is E2 specifically). It is fine to simply refer to these as Estrogen, but it’s more important that you know how to control your own and have a basic understanding of the topic.
The mechanisms through which E2 interacts with sexual reproductive organs and other hormones in the male body is actually much more complex than in a woman’s body. This is mainly because we have so little E2 compared to our female counterparts. The same can be said of Testosterone in women; a slight change in levels can trigger huge changes. A lot of people know the term “aromatase” or “aromatization”, but do people know exactly what it is?
The most challenging hormone for the steroid user is Estrogen by far. It is the cause of any changes in your nipple/pecs (gyno), mood, libido, hardness, bloat, skin, prostate, appetite – you name it, when you feel off 90% of the time is due to low/high Estrogen levels.
When you hit your sweet spot you will know, you can’t miss it. You will feel happy, content, you will sex like a champ, eat like a champ and train like a champ and to top it off everybody around you will be happy as well.
Here is an indicators of low/high Estrogen levels:
Low Estrogen Sides
Dry skin/lips
Feeling of dehydration
Loss of libido
Erectile Dysfunction
Loss of sensitivity
Dry glans (penis)
White glans
Loss of girth
Irritability/Mood swings
Crying for no reason
DHT rage (aggression you take out on others)
Dull orgasm
Hesitation just before urinating
Night sweats
Loss of appetite
Constant fatigue
Lethargy
Constipation (due to dehydration)
Diuretic effect (pissing more water than you are consuming)
Itchy scalp
Obsessive thoughts
Low and high Estrogen sides are very alike, the more experienced you get the easier it is to differentiate between them, but it will always be tricky. The best way to tell is always to get your Estradiol (E2) checked though blood work.
High Estrogen Sides
Acne
Loss of libido
Water retention (Bloat)
Moon face
Small testicles
Scrotum hanging too high
Soft testicles
Extreme oiliness all over
Moodiness (Aggression, depression, increased irritability)
Lethargy
Insomnia
Soft erections
Extreme cravings for sugar/chocolate
High BP
BP spikes
Enlarged prostate
Pressure in lower abdomen when urinating
Thin stream when urinating
Constipation (from water retention)
Itchy nipples
Gynecomastia
When you get one side effect, it is just an indication use this list to potentially make a full picture. Never go by one side only, being bloated only means nothing, having dry skin only means nothing again. Again, the best way to tell is always to get your Estradiol (E2) checked though blood work.
Aromatase
Aromatase is an enzyme that converts testosterone to estradiol and androstenedione to estrone. Similarly, 17-ketosteroid reductase is an enzyme that is capable of converting androstenedione to testosterone and estrone to estradiol. Aromatase is named based upon the fact that it removes a methyl group on the 19th carbon and rearranges ring A into an aromatic ring, hence it aromatizes the testosterone molecule.
Aromatase is found in many different cells in the body, however it is primarily found in adipose tissue. The liver, skin, and testes are also primary sites of aromatization. In the testes, you have two different cells that respond to the gondaotropic hormones (LH and FSH). Leydig/interstitial cells respond to LH and initiate the synthesis of testosterone. Sertoli/sustentacular cells respond to FSH and initiate and support spermatogenesis. Sertoli cells do not produce testosterone but they contain FSH-dependent aromatase. The estradiol produced in Sertoli cells binds to E2 receptors in Leydig cells and the estradiol will suppress the Leydig cell’s response to LH stimulation. Aromatase activity in other cells are not FSH-dependent. Much of the brain contains aromatase, except the pituitary gland.
Aromatase Regulation
Aromatase is decreased endogenously by prolactin and anti-Mullerian hormone, although AMH is irrelevant and concentrations are almost non-existent in adult males. It is also decreased exogenously by aromatase inhibitors, nicotine, zinc, vitamin E, and resveratrol. The enzyme is increased endogenously by gonadotropins, insulin, testosterone, and androstenedione. Increased adipose tissue increases quantity of aromatase in body.
Aromatase Inhibitors (AIs)
Keep in mind Estrogen is good for you in many ways (libido, mood, skin quality, hair, nails etc). But, most importantly, Estrogen is good for your lipids. I am sure you have heard how Arimidex and Letrozole are bad for your lipid values while Aromasin is ‘better’, in reality all AI’s are as bad as each other for your liver values. The more you lower Estrogen, the worse your liver values will get – it doesn’t matter which AI you use, all that matters is how much you are lowering your Estrogen. If you lower your Estrogen by 10 pg/mL you won’t notice much difference. If you crash your Estrogen down to single digits I guarantee you that your HDL/LDL will be completely out of whack no matter which AI you used.
Suicidal AI vs. Non-Suicidal/Binding AI
Arimidex and Letrozole are non-suicidal AI’s, all they do is bind any Estrogen you convert directly on your aromatase enzyme. Each AI binds a different percentage of Estrogen, Letrozole binds more than Arimidex of course. The problem with binding AI’s is that once you cease use, all of the Estrogen that had accumulated when you were using that AI suddenly gets released – this process is called "Estrogen rebound" and I am sure you know it can be far worse than Estrogen while on a cycle since normally when you drop your AI you either cruise with a low dose of Test or PCT. In both cases you have far less Test in you and once all that Estrogen is released you got a much higher chance of getting Gyno and of course you are going to be bloated and feel soft for weeks till your Estrogen comes down to normal levels.
Aromasin is the new generation of AI and it is suicidal, the difference between Aromasin and the other AI’s is Aromasin will actually destroy/kill a certain percentage of your aromatase enzyme so by doing so it also 'kills' any estrogen that was attached to that enzyme. This means when you stop using Aromasin you won’t rebound at all like you would with the binding AI’s. If anything, you will have to wait for a while for your body to start producing more aromatase (very bad if you crashed your Estrogen comparing to using the other AI’s). Each person is different in the rate they create new aromatase; it can take one to three weeks.
Arimidex (Anastrozole)
Arimidex (Adex) will lower your Estrogen by about 50-60%. Of course, if you keep taking it that percentage accumulates so you lower 50% by another 50% and so on, you can easily end up with your Estradiol in the singles if you take it for long enough at a high enough dose and you aren’t converting much Estrogen from aromatizing gear (using low dose of Test and high dose AI). Arimidex is a good for new steroid users as if they overestimate their dosing for AI and get symptoms of low E2, they will bounce back back up fairly quickly and adjust as needed.
Dosage on cycle: dosing is user dependent and you should get blood work to dial in your dose, but MOST users will find .5 mg of Arimidex E3D or E3.5D to be a good starting dose for 500-600 mg Testosterone (just for a reference). Some may need more frequent (EOD) dosing or some may even need less than E3.5D; this is really something that varies person-to-person too much and without blood work there is no way to know for sure what dosage you need.
Aromasin (Exemestane)
Aromasin (Asin) is an orally available suicidal aromatase inhibitor. Because Aromasin is steroidal this gives it a favorable Estrogen suppression profile and confers a few really awesome benefits over other anti-estrogens both on paper and in real experience. Steroidal anti-estrogens have the benefit of being lipid-friendly and they all lower SHBG which increases the ratio of free to bound Testosterone, which as many experienced bodybuilders know can have a relatively profound, positive impact on gains.
It is important to understand how drugs work in order to properly dose them, Aromasin is a suicidal aromatase inhibitor, this means that it binds with aromatase enzymes and as it does so permanently disables the enzyme and destroys it. Hence the “suicidal” this compound. Just beware, if you crash your estrogen on Aromasin, it can take a long time waiting for your E2 to rise again (compared to the non-suicidal AIs), which will have a negative impact on lipid profile, joint integrity, mental health, libido and overall gains.
Aromasin’s half life in the male body is actually very short (~9 hours) and it is quickly eliminated, however, since as soon as it enters your bloodstream it quickly destroys the aromatase enzymes present in your body, it is effective in maintaining significant reductions in estrogen for up to +72 hours after a single 25mg dose. Estrogen levels only begin to rise again after your body has begun to make new aromatase enzymes to replace the ones destroyed by Aromasin.
There is a great study on the pharmacokinetics of Aromasin in men which found the following:
24 hours after one 25mg dose estrogen levels are reduced by 58 ± 21%
3-6 days after initial dose estrogen levels return to baseline (without rebounding)
This means that you can find the timing and dosage that works for you; this flexibility is what makes Aromasin such a versatile Anti-E.
BUT WAIT, there’s more. In males, Aromasin was found to increase total testosterone by ~60% after 10 days @ 25mg/day, however the same study found that while it increased total testosterone by 60%, free testosterone was increased by over 100 percent! that’s right, it DOUBLES bio-available testosterone (in naturals of course). With all this said, it is an option to be ran into PCT like the study, when utilizing HCG right before or the first couple week of PCT.
The Good:
Lowers SHBG, increasing free test & makes all other anabolic steroids more bio-available (i.e. more gains)
Increases IGF-1
No adverse changes in lipid profiles for men (unless you crash estrogen - studies were also not on cycle and may be different)
Is not liver toxic
No Estrogen rebound
The Bad:
Typical aromatase inhibitor issues here, include stiff joints and possibly lethargy if E2 gets too low
If you crash your E2 levels, it will remained crashed until your body makes more aromatase at it's own rate.
Typically more expensive than Arimidex or Letrozole
Alopecia. The other two AI’s have hair loss/hair thinning as a side effect, but not full blown Alopecia.
Dosage on cycle: dosing is user dependent and you should get blood work to dial in your dose, but MOST users will find 12.5 mg of Aromasin E3D or E3.5D to be a good starting dose for 500-600 mg Testosterone (just for a reference). Some may need more frequent (EOD) dosing or some may even need less than E3.5D; this is really something that varies person-to-person too much.
First of all there are three different types of Gynecomastia (Gyno): Estrogen induced, Progesterone induced and Prolactin induced. Of course, you can avoid all three types of Gyno by keeping Estrogen (E2) within the normal range (unless using a 19-nor). The precursor to any type of Gyno is almost always Estrogen! Once you let Estrogen build up you signal to your brain that you have conceived, it doesn’t matter if you are a man or woman, your body at this point will have to go through certain processes to prepare you for lactation. Firstly your body will rush to use that Estrogen and build up breast tissue (which will form a lump) which is mandatory for the lactation process. Once this stage has been completed and you have let Estrogen still high your Progesterone will increase (Estrogen can still remain high) which is an attempt from your body to make the tissue larger and also make your aerolas bigger (puffy and enlarged nipples) again to get them ready for lactation. Last stage of Gyno is Prolactin lactation, all previous stages were preparing the body for this moment at this point your Progesterone and Estrogen will drop and your Prolactin will spike, this is when someone starts lactating.
Estrogen (E2)
Estrogen is commonly referred to as “E2”. Estrogens are made up of Estrone (E1), Estradiol (E2), and Estriol (E3) (though the one we’re concerned with is E2 specifically). It is fine to simply refer to these as Estrogen, but it’s more important that you know how to control your own and have a basic understanding of the topic.
The mechanisms through which E2 interacts with sexual reproductive organs and other hormones in the male body is actually much more complex than in a woman’s body. This is mainly because we have so little E2 compared to our female counterparts. The same can be said of Testosterone in women; a slight change in levels can trigger huge changes. A lot of people know the term “aromatase” or “aromatization”, but do people know exactly what it is?
The most challenging hormone for the steroid user is Estrogen by far. It is the cause of any changes in your nipple/pecs (gyno), mood, libido, hardness, bloat, skin, prostate, appetite – you name it, when you feel off 90% of the time is due to low/high Estrogen levels.
When you hit your sweet spot you will know, you can’t miss it. You will feel happy, content, you will sex like a champ, eat like a champ and train like a champ and to top it off everybody around you will be happy as well.
Here is an indicators of low/high Estrogen levels:
Low Estrogen Sides
Dry skin/lips
Feeling of dehydration
Loss of libido
Erectile Dysfunction
Loss of sensitivity
Dry glans (penis)
White glans
Loss of girth
Irritability/Mood swings
Crying for no reason
DHT rage (aggression you take out on others)
Dull orgasm
Hesitation just before urinating
Night sweats
Loss of appetite
Constant fatigue
Lethargy
Constipation (due to dehydration)
Diuretic effect (pissing more water than you are consuming)
Itchy scalp
Obsessive thoughts
Low and high Estrogen sides are very alike, the more experienced you get the easier it is to differentiate between them, but it will always be tricky. The best way to tell is always to get your Estradiol (E2) checked though blood work.
High Estrogen Sides
Acne
Loss of libido
Water retention (Bloat)
Moon face
Small testicles
Scrotum hanging too high
Soft testicles
Extreme oiliness all over
Moodiness (Aggression, depression, increased irritability)
Lethargy
Insomnia
Soft erections
Extreme cravings for sugar/chocolate
High BP
BP spikes
Enlarged prostate
Pressure in lower abdomen when urinating
Thin stream when urinating
Constipation (from water retention)
Itchy nipples
Gynecomastia
When you get one side effect, it is just an indication use this list to potentially make a full picture. Never go by one side only, being bloated only means nothing, having dry skin only means nothing again. Again, the best way to tell is always to get your Estradiol (E2) checked though blood work.
Aromatase
Aromatase is an enzyme that converts testosterone to estradiol and androstenedione to estrone. Similarly, 17-ketosteroid reductase is an enzyme that is capable of converting androstenedione to testosterone and estrone to estradiol. Aromatase is named based upon the fact that it removes a methyl group on the 19th carbon and rearranges ring A into an aromatic ring, hence it aromatizes the testosterone molecule.
Aromatase is found in many different cells in the body, however it is primarily found in adipose tissue. The liver, skin, and testes are also primary sites of aromatization. In the testes, you have two different cells that respond to the gondaotropic hormones (LH and FSH). Leydig/interstitial cells respond to LH and initiate the synthesis of testosterone. Sertoli/sustentacular cells respond to FSH and initiate and support spermatogenesis. Sertoli cells do not produce testosterone but they contain FSH-dependent aromatase. The estradiol produced in Sertoli cells binds to E2 receptors in Leydig cells and the estradiol will suppress the Leydig cell’s response to LH stimulation. Aromatase activity in other cells are not FSH-dependent. Much of the brain contains aromatase, except the pituitary gland.
Aromatase Regulation
Aromatase is decreased endogenously by prolactin and anti-Mullerian hormone, although AMH is irrelevant and concentrations are almost non-existent in adult males. It is also decreased exogenously by aromatase inhibitors, nicotine, zinc, vitamin E, and resveratrol. The enzyme is increased endogenously by gonadotropins, insulin, testosterone, and androstenedione. Increased adipose tissue increases quantity of aromatase in body.
Aromatase Inhibitors (AIs)
Keep in mind Estrogen is good for you in many ways (libido, mood, skin quality, hair, nails etc). But, most importantly, Estrogen is good for your lipids. I am sure you have heard how Arimidex and Letrozole are bad for your lipid values while Aromasin is ‘better’, in reality all AI’s are as bad as each other for your liver values. The more you lower Estrogen, the worse your liver values will get – it doesn’t matter which AI you use, all that matters is how much you are lowering your Estrogen. If you lower your Estrogen by 10 pg/mL you won’t notice much difference. If you crash your Estrogen down to single digits I guarantee you that your HDL/LDL will be completely out of whack no matter which AI you used.
Suicidal AI vs. Non-Suicidal/Binding AI
Arimidex and Letrozole are non-suicidal AI’s, all they do is bind any Estrogen you convert directly on your aromatase enzyme. Each AI binds a different percentage of Estrogen, Letrozole binds more than Arimidex of course. The problem with binding AI’s is that once you cease use, all of the Estrogen that had accumulated when you were using that AI suddenly gets released – this process is called "Estrogen rebound" and I am sure you know it can be far worse than Estrogen while on a cycle since normally when you drop your AI you either cruise with a low dose of Test or PCT. In both cases you have far less Test in you and once all that Estrogen is released you got a much higher chance of getting Gyno and of course you are going to be bloated and feel soft for weeks till your Estrogen comes down to normal levels.
Aromasin is the new generation of AI and it is suicidal, the difference between Aromasin and the other AI’s is Aromasin will actually destroy/kill a certain percentage of your aromatase enzyme so by doing so it also 'kills' any estrogen that was attached to that enzyme. This means when you stop using Aromasin you won’t rebound at all like you would with the binding AI’s. If anything, you will have to wait for a while for your body to start producing more aromatase (very bad if you crashed your Estrogen comparing to using the other AI’s). Each person is different in the rate they create new aromatase; it can take one to three weeks.
Arimidex (Anastrozole)
Arimidex (Adex) will lower your Estrogen by about 50-60%. Of course, if you keep taking it that percentage accumulates so you lower 50% by another 50% and so on, you can easily end up with your Estradiol in the singles if you take it for long enough at a high enough dose and you aren’t converting much Estrogen from aromatizing gear (using low dose of Test and high dose AI). Arimidex is a good for new steroid users as if they overestimate their dosing for AI and get symptoms of low E2, they will bounce back back up fairly quickly and adjust as needed.
Dosage on cycle: dosing is user dependent and you should get blood work to dial in your dose, but MOST users will find .5 mg of Arimidex E3D or E3.5D to be a good starting dose for 500-600 mg Testosterone (just for a reference). Some may need more frequent (EOD) dosing or some may even need less than E3.5D; this is really something that varies person-to-person too much and without blood work there is no way to know for sure what dosage you need.
Aromasin (Exemestane)
Aromasin (Asin) is an orally available suicidal aromatase inhibitor. Because Aromasin is steroidal this gives it a favorable Estrogen suppression profile and confers a few really awesome benefits over other anti-estrogens both on paper and in real experience. Steroidal anti-estrogens have the benefit of being lipid-friendly and they all lower SHBG which increases the ratio of free to bound Testosterone, which as many experienced bodybuilders know can have a relatively profound, positive impact on gains.
It is important to understand how drugs work in order to properly dose them, Aromasin is a suicidal aromatase inhibitor, this means that it binds with aromatase enzymes and as it does so permanently disables the enzyme and destroys it. Hence the “suicidal” this compound. Just beware, if you crash your estrogen on Aromasin, it can take a long time waiting for your E2 to rise again (compared to the non-suicidal AIs), which will have a negative impact on lipid profile, joint integrity, mental health, libido and overall gains.
Aromasin’s half life in the male body is actually very short (~9 hours) and it is quickly eliminated, however, since as soon as it enters your bloodstream it quickly destroys the aromatase enzymes present in your body, it is effective in maintaining significant reductions in estrogen for up to +72 hours after a single 25mg dose. Estrogen levels only begin to rise again after your body has begun to make new aromatase enzymes to replace the ones destroyed by Aromasin.
There is a great study on the pharmacokinetics of Aromasin in men which found the following:
24 hours after one 25mg dose estrogen levels are reduced by 58 ± 21%
3-6 days after initial dose estrogen levels return to baseline (without rebounding)
This means that you can find the timing and dosage that works for you; this flexibility is what makes Aromasin such a versatile Anti-E.
BUT WAIT, there’s more. In males, Aromasin was found to increase total testosterone by ~60% after 10 days @ 25mg/day, however the same study found that while it increased total testosterone by 60%, free testosterone was increased by over 100 percent! that’s right, it DOUBLES bio-available testosterone (in naturals of course). With all this said, it is an option to be ran into PCT like the study, when utilizing HCG right before or the first couple week of PCT.
The Good:
Lowers SHBG, increasing free test & makes all other anabolic steroids more bio-available (i.e. more gains)
Increases IGF-1
No adverse changes in lipid profiles for men (unless you crash estrogen - studies were also not on cycle and may be different)
Is not liver toxic
No Estrogen rebound
The Bad:
Typical aromatase inhibitor issues here, include stiff joints and possibly lethargy if E2 gets too low
If you crash your E2 levels, it will remained crashed until your body makes more aromatase at it's own rate.
Typically more expensive than Arimidex or Letrozole
Alopecia. The other two AI’s have hair loss/hair thinning as a side effect, but not full blown Alopecia.
Dosage on cycle: dosing is user dependent and you should get blood work to dial in your dose, but MOST users will find 12.5 mg of Aromasin E3D or E3.5D to be a good starting dose for 500-600 mg Testosterone (just for a reference). Some may need more frequent (EOD) dosing or some may even need less than E3.5D; this is really something that varies person-to-person too much.
