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Testosterone serves as the foundation for most anabolic steroid cycles. When using this compound, we inevitably encounter the effects of aromatization. Aromatase is an enzyme in the human body that converts testosterone into estradiol (E2) and estrone (E1). This group of hormones is called estrogens and is considered female sex hormones, although they are also present in men, but in much smaller quantities.
WHAT ARE ESTROGENS
Estrogens are a group of steroid hormones that play a key role in regulating the reproductive system and secondary sexual characteristics, mainly in women. The primary types of estrogens include estradiol, estrone, and estriol. Estradiol is the most active and prevalent of these hormones in the body.
Although estrogens are traditionally associated with the female body, they are also present in the male body and perform several important functions. In men, estrogens are produced in small quantities, primarily from testosterone via the enzyme aromatase. They play a crucial role in maintaining the balance between testosterone and estrogen, which is important for regulating libido, mood, and bone density. Estrogens also participate in the metabolism of fats and carbohydrates, helping to maintain a healthy weight and energy levels.
Additionally, they contribute to cardiovascular health and skin health. A deficiency or excess of estrogens in men can lead to various medical issues, such as osteoporosis, metabolic disorders, and other endocrine problems.
Aromatization
Aromatization is the process of converting androgens, such as testosterone, into estrogens, such as estradiol, through the action of the aromatase enzyme. This enzyme is present in various tissues of the body, including adipose tissue, the liver, and muscles. Aromatization plays a vital role in hormonal balance, regulating the levels of estrogens and testosterone in the male body. Under normal conditions, aromatization helps maintain a certain level of estrogens, which is necessary for bone health, lipid metabolism regulation, and cognitive functions.
However, excessive aromatization can lead to elevated estrogen levels, causing various adverse effects in men. One of the most noticeable symptoms is gynecomastia, the enlargement of breast tissue, which can be accompanied by pain and discomfort. Additionally, high estrogen levels can cause reduced libido, erectile dysfunction, and emotional changes, such as increased irritability or depression. Excessive aromatization can also affect metabolism, leading to increased fat mass and fluid retention. Controlling the level of aromatization is essential for maintaining overall hormonal health, and in some cases, medical intervention may be necessary to correct this process.
EXCESS ESTRADIOL WHEN USING TESTOSTERONE
In the case of excess estradiol, which often occurs due to the high doses of testosterone that inevitably convert into estradiol, athletes begin to experience a range of side effects. These include a decrease in emotional well-being, gynecomastia, increased fat deposits in a female pattern, edema, decreased libido, and others. Irritability and hysterical behavior in athletes can result not only from high androgen levels but also from elevated estradiol. Excessive emotionality may also occur. It might sound humorous, but if you start shedding tears while watching a melodrama with your girlfriend, it could be a sign that it's time to check your estradiol levels.
For these reasons, athletes try to avoid very high levels of estradiol. To reduce estradiol levels, aromatase inhibitors are used. These medications block the conversion of testosterone into estradiol, thereby maintaining higher testosterone and lower estrogen levels in the blood.
Monitoring estradiol levels
One of the crucial rules in structuring a steroid cycle is controlling estradiol levels before any side effects become apparent. There are numerous side effects that we might only recognize when it's too late. Often, beginners think that if they don't have visible signs of gynecomastia, they don't need to use aromatase inhibitors, but this is not true. It's not always wise to rely solely on your sensations. The best approach is to monitor estradiol levels through blood tests. Only with an estradiol test can you understand the actual level and, by comparing it with your symptoms, decide what to do next.
Avoiding too low estradiol levels
You should also avoid extremely low estradiol levels. This can be even more harmful than high estradiol levels: it can lower cholesterol levels, reduce bone density, decrease anabolism, and reduce libido since low estradiol levels negatively affect sexual desire just as much as excessively high levels. Therefore, using aromatase inhibitors without determining estradiol levels is also an incorrect approach. If you are administering testosterone injections, remember that if you want to achieve maximum results in bodybuilding with minimal health risks, you need to continuously monitor your hormone levels.
Controlling estradiol through body fat reduction
Adipose tissue plays a significant role in the aromatization process in men, as it is the main site of action of the aromatase enzyme, which converts testosterone to estradiol. The more fat a man has, the more active aromatase enzymes, which leads to an increased conversion of testosterone into estrogens. This can lead to an increase in estradiol levels in the blood, which, in turn, can cause undesirable side effects such as gynecomastia, fluid retention, decreased libido and accumulation of female-type fat mass. Therefore, reducing fat mass can help in controlling estradiol levels and reducing the risks associated with its excess. The less body fat you have, the easier it is to control estradiol levels.
SIDE EFFECTS OF HIGH ESTRADIOL LEVELS
High levels of estradiol in men can lead to a range of side effects affecting various aspects of health. Estradiol, the primary type of estrogen, although crucial for normal body function, can cause the following problems when present in elevated concentrations:
- Gynecomastia: High levels of this hormone often lead to gynecomastia. This can be avoided by constantly monitoring your estradiol levels and maintaining them within ranges suitable for you (these ranges can vary between individuals). Many inexperienced athletes begin to react only when they notice itching or pain in the nipples, indicating a prolonged high level of estradiol. Don't take chances with this, because if you don't act quickly to reduce estradiol, your breast tissue will start to enlarge, and soon you may develop gynecomastia, which can only be corrected surgically.
- Reduced libido and erectile dysfunction: High levels of estradiol can disrupt the balance of sex hormones, leading to decreased libido and erectile problems.
- Emotional changes: Excess estradiol can affect mood, causing depression, irritability, and increased emotionality.
- Fat accumulation: High estradiol levels promote fat accumulation, especially in the abdominal area, hips, and buttocks.
- Fluid retention: Elevated estradiol levels can lead to fluid retention in the body, manifesting as swelling, particularly in the lower extremities. This condition can cause discomfort and increased blood pressure.
- Excess bile and digestive issues: High levels of estrogens, including estradiol, can affect liver function and bile production processes. This can lead to excess bile, which in turn can cause abdominal discomfort, impaired fat digestion, and bloating. Disruption in bile acid metabolism can also contribute to gallstone formation.
- Increased cancer risk: Long-term elevated estradiol levels may be associated with an increased risk of developing certain types of cancer, such as prostate cancer. Estrogens can stimulate cell proliferation in prostate tissue, which in some cases can contribute to carcinogenesis.
- Gallstone disease: Changes in bile acid metabolism and lipid metabolism at high estradiol levels can promote the formation of gallstones, which can cause pain and require medical intervention.
- Immunological changes: High levels of estrogens can modulate the immune system, leading to changes in inflammatory processes. This can increase susceptibility to infections or, conversely, contribute to the development of autoimmune diseases.
- Tendency to thromboembolism: Estrogens can increase the risk of thrombosis by affecting blood coagulation. This is especially relevant for men with existing risk factors for cardiovascular diseases.
MANAGING HIGH ESTRADIOL LEVELS
To combat the side effects of high estradiol levels in men, various medicinal methods are used. One of the primary methods is the use of aromatase inhibitors. These drugs reduce the activity of the aromatase enzyme, decreasing the conversion of testosterone into estradiol and thus lowering the level of estrogens in the body. This helps reduce symptoms of gynecomastia, fluid retention, and other estrogen-related issues. Additionally, selective estrogen receptor modulators (SERMs), such as tamoxifen, can be used in some cases to block the action of estrogens on receptors in specific tissues, preventing their stimulatory effects.
Aromatase inhibitors
Aromatase inhibitors are a group of medications that suppress the activity of the aromatase enzyme, thereby reducing the conversion of androgens (e.g., testosterone) into estrogens. These drugs play a crucial role in treating various conditions associated with elevated estrogen levels. In men, aromatase inhibitors are often used to control symptoms caused by increased aromatization, such as gynecomastia, reduced libido, and other hormonal imbalances.
There are several types of aromatase inhibitors, which can be divided into steroidal and non-steroidal inhibitors. Steroidal inhibitors, such as exemestane, bind to aromatase and cause its irreversible inactivation. Non-steroidal inhibitors (reversible), such as Anastrozole and Letrozole, act differently by temporarily binding to the enzyme and preventing its function without causing permanent damage. Reversible inhibitors can be displaced by androgens, leading to the restoration of aromatase activity. Exemestane, being an irreversible inactivator, binds to the catalytic site of aromatase, causing a complete loss of its enzymatic function and is not displaced by androgens.
Both types of inhibitors effectively lower estrogen levels in the body, helping to reduce symptoms associated with their excess.
Aromatase inhibitors dosages
For comparison, 1 mg of Anastrozole is approximately equivalent to 1 mg of Letrozole or 25 mg of exemestane. This way, you can determine the equivalent dose regarding your impact on lowering estradiol levels, but keep in mind that the effect of all medications on the body is highly individual, so dose adjustment may be required depending on the drug used.
Sometimes one drug works better for some athletes, while another works better for others. Also, side effects may occur when using an aromatase inhibitor, in which case the drug causing them is replaced with another.
Sometimes, the aromatase response to exogenous testosterone is so great that estradiol cannot be reduced with usual doses. In this case, you should select a dosage under the supervision of a specialist that suits you in this particular case.
Anabolic steroids that reduce estradiol
Anabolic steroids such as Boldenone and Methenolone are also known to lower estrogen levels and are used in combination with Testosterone, though the exact mechanism is not fully understood.
The dosage of an aromatase inhibitor will depend on the testosterone-to-estradiol ratio and is determined by blood test results for estradiol.
The higher your testosterone dosage, the higher your estradiol level, and consequently, the higher the dosage of aromatase inhibitors. Start taking the medication only after obtaining blood test results. Your subsequent dosage will depend on these results. After 7-10 days of using any aromatase inhibitor, a follow-up estradiol level check should be conducted to determine the dose that suits you best for specific testosterone dosages. After a few tests, you will determine your dosage, and subsequent estradiol tests should be conducted every few months to monitor and adjust dosages.
SERMs
Selective estrogen receptor modulators (SERMs) are a class of drugs that act on estrogen receptors in various tissues, exerting both agonist and antagonist effects. At high estradiol concentrations in men, SERMs such as Tamoxifen, Raloxifene, and Clomiphene can be used to block the action of estrogens at the tissue level, especially in the breast. This can be helpful in reducing symptoms of gynecomastia, as SERMs block the binding of estradiol to receptors in breast tissue, preventing the stimulatory action of estrogens.
However, using SERMs to control high estradiol levels in men is an incorrect approach compared to aromatase inhibitors. SERMs do not reduce the amount of estrogen in the body but only block their action in certain tissues. This means that estrogen levels, including estradiol, remain elevated in the bloodstream, which can continue to affect other aspects of health, such as bone density and lipid profile. For example, the risk of cardiovascular diseases associated with impaired lipid metabolism may persist.
In contrast, aromatase inhibitors lower estrogen levels and, therefore, can be more effective in addressing the root cause of excessive aromatization. Thus, for proper management of high estradiol levels in men, it is preferable to use aromatase inhibitors rather than SERMs, as they more specifically address excessive estrogen production.
SIDE EFFECTS OF LOW ESTRADIOL LEVELS
Low levels of estradiol in men can also lead to several negative consequences. Despite estrogens traditionally being associated with female physiology, estradiol, as an important component of hormonal balance, plays a significant role in the male body. Its deficiency can manifest as follows:
- Osteoporosis and decreased bone density: Estradiol has a protective effect on bone tissue, helping to maintain bone density. Low levels of estradiol can lead to an increased risk of osteoporosis and fractures due to impaired bone mineralization. This condition is particularly relevant for older men whose hormone production decreases.
- Reduced libido and sexual dysfunction: While testosterone is primarily responsible for maintaining sexual desire and function, estradiol is also important for normal libido and erectile function. A deficiency in estradiol can cause decreased libido and erectile problems, thereby worsening quality of life.
- Cardiovascular risks: Low levels of estradiol can negatively impact the cardiovascular system. Studies show that estradiol helps maintain vascular health by improving elasticity and reducing inflammation. A deficiency in this hormone can contribute to the development of atherosclerosis, increasing the risk of heart attack and stroke.
- Changes in lipid profile: Estradiol affects lipid metabolism by promoting higher levels of "good" cholesterol (HDL) and lowering levels of "bad" cholesterol (LDL). Reduced estradiol levels can worsen the lipid profile, thereby increasing the risk of cardiovascular diseases.
- Mood and cognitive function problems: Estradiol has a neuroprotective effect and influences mood and cognitive functions. A deficiency in this hormone can lead to depression, irritability, memory deterioration, and reduced concentration.
- Muscle weakness and loss of mass: Estradiol also participates in maintaining muscle mass and strength. Low levels of this hormone can lead to reduced muscle mass and increased fat mass, ultimately affecting physical performance.
- Skin and hair problems: A deficiency in estradiol can cause skin dryness and reduced elasticity due to collagen loss. Hair condition may also deteriorate, manifesting as thinning and hair loss.
- Endocrine system disruptions: Estradiol is involved in regulating the hormonal balance, influencing the production of testosterone and other hormones. Its deficiency can cause overall hormonal imbalance, leading to various metabolic disorders.
ESTRADIOL LEVELS FOR DIFFERENT GOALS
To determine which doses of aromatase inhibitors you should use (and whether you need them at all), you need to get a blood test for estradiol, and then, based on your goals, adjust it to the level that suits you. How do you determine which estradiol level is right for you? First, we need to understand two things – both very high levels of estradiol (twice the upper limit of the normal range) and very low levels (below or at the lower end of the normal range) will negatively affect your body, and you are likely to experience side effects. Therefore, we avoid very low and very high values.
Bulk and strength growth
If your goal is maximum muscle mass growth, we recommend keeping estradiol at the upper end of the normal range or even slightly higher, but not more than 1.5 times the upper limit of normal. Estradiol itself is an anabolic hormone and has several positive properties, such as controlling the production of synovial fluid, which helps your joints lift heavy weights. Of course, estradiol above normal will retain some fluid, which may affect the aesthetics of your body, but it will promote better muscle mass growth and increased strength.
If you are a powerlifter or strongman, we also recommend keeping your estradiol at the upper end of the normal range or higher, as long as you do not show signs of gynecomastia, reduced libido, or mood deterioration. Fluid retention can also increase your blood pressure. This should be taken into account, and if your blood pressure is high, we recommend using medications to lower it, such as Telmisartan.
If you aim for maximum muscle mass and strength growth, you need to balance high estradiol levels with the side affects you may experience. Weigh all the pros and cons of this decision. You must monitor your estradiol levels and not allow them to become excessively high. The maximum allowable level can be considered 1.5 times the upper limit of normal.
Clean bulk or fat loss/cutting
A high level of estradiol can negatively affect your appearance due to fluid retention, making you look more bloated. Some people may have a round face due to this fluid retention, which might not be noticeable in the mirror but becomes clear when you look at old photos from times of high estradiol levels.
Additionally, estradiol is a hormone that increases the amount of subcutaneous fat, especially in the hips and buttocks (in a female pattern), meaning that if you want to burn fat, your estradiol level should be relatively low.
If your libido and mood are sufficiently high with average estradiol levels, stick to these values if your goal is clean bulking or cutting.
WHAT ESTRADIOL LEVEL IS RIGHT FOR YOU
Above, we described general trends in the effects associated with different estradiol levels, and you should use these as a guide when setting specific goals. However, the most important aspect of this process is your subjective experience, which should be compared with blood test results.
This means that despite some generally accepted standards, you should always listen to your body. For example, if your goal is clean bulking, you might aim to keep your estradiol level in the mid-normal range, but due to individual differences, this level might not be enough to maintain a high libido. In such a case, you may need to find a more suitable, probably higher, estradiol level.
Another example could be if you are a powerlifter seeking maximum fluid retention from high estradiol levels. If you start developing gynecomastia, you will likely want to lower your estradiol to avoid surgery. Alternatively, you might try using Raloxifene, which blocks estrogen receptors in breast tissue while allowing estradiol to act in other tissues.
High blood pressure is another visible side effect; in this case, we recommend not taking risks and lowering estradiol or using Telmisartan to manage blood pressure.
Recommended levels
Generally, the optimal levels of this hormone are mid-normal or slightly above (if you are a powerlifter, aim for the upper-normal range or slightly above up to 1.5 times the upper limit). It is important that your testosterone levels are also high. If you aim to keep estradiol above normal, your testosterone should be approximately double the upper limit. If your estradiol is 1.5 times the normal upper limit and your testosterone is only at the upper normal limit or lower, the results will likely be disappointing.
From mid-normal to 1.5 times the upper limit is the recommended range for estradiol, provided you feel good and have no issues with libido or mood.
Professional bodybuilders who compete often lower their estradiol to the lower end of the normal range in the final phase of preparation to avoid even minimal fluid retention. However, we do not recommend this outside of competitive sports.
- Below mid-normal values (but within the normal range): This is suitable for stage preparation or photoshoots to enhance muscle definition at very low body fat percentages.
- Mid-normal values: This is typically the optimal range for getting the most benefit from your cycle. You won't have excessive fluid retention that ruins your appearance or high blood pressure. Suitable for clean bulking and cutting.
- Upper-normal values: A good choice for bulking due to fluid retention in the body and anabolic response. Also suitable for good well-being, energy levels, and libido if mid-normal levels are insufficient.
- 1.5 times the upper-normal values: Similar to the previous estradiol level but potentially better for some individuals.
Non-recommended levels
There are athletes who do not reduce their estradiol level at all or maintain it at twice the normal range. We do not recommend this practice, as excessively high estradiol increases the long-term risk of cardiovascular diseases due to a higher risk of thrombosis, or more quickly – gynecomastia.
Similarly, estradiol levels below the normal range are definitely not suitable due to numerous side effects, such as worsening blood lipids, decreased bone density, mood issues, and libido problems.
ESTRADIOL CONTROL SCHEME STEP BY STEP
Here is an example of a step-by-step guide on how to find the appropriate estradiol level for you.
14 Days after the first injection
Approximately 14 days after your first Testosterone injection, you should take a blood test for estradiol. Fourteen days is a sufficient period for testosterone levels to stabilize, allowing us to obtain a sufficiently high estradiol reading.
Let's assume the result is 70 pg/mL, with a normal range for men being 10 to 50 pg/mL. Ideally, we want a consistent estradiol level between 20 and 40 pg/mL. This level is enough to feel good, protect the joint-ligament apparatus from unnecessary injury risks, maintain normal cholesterol levels, and avoid most side effects from estradiol such as fluid retention and decreased libido.
Our recommendation would be to start with the most popular drug – Anastrozole, at a minimal dose of 0.5 mg twice a week.
21 days after the first injection
Approximately 7 days later, take another blood test for estradiol.
If the estradiol level is within the desired range and you feel good, stick to these doses.
If the level is still high, for example, 50 pg/mL, and you want to lower it to 30-40 pg/mL, slightly increase the dose of Anastrozole, for example, to 0.5 mg three times a week.
28 days after the first injection
Another blood test should be conducted approximately 7 days later. If you have achieved the desired result, the next test should be in about 4 weeks (assuming there are no negative side effects indicating too low or high estradiol levels).
56 days after the first injection
Perform a control test to ensure everything is in order. These adjustments are ongoing until a stable and consistent estradiol level is achieved. If you change the dosage of Testosterone or other aromatizing steroids during the cycle, adjust the dose of aromatase inhibitors accordingly and retest to achieve the desired result.
SUMMARY OF STEPS
By following these steps, you can effectively manage and maintain your estradiol levels within the optimal range for your specific goals and needs.
14 days after first injection
- Take a blood test for estradiol.
- Analyze results and start with Anastrozole at 0.5 mg twice a week if needed.
21 days after first injection
- Take another blood test for estradiol.
- Adjust dose if necessary (e.g., increase to 0.5 mg three times a week).
28 days after first injection
- Take another blood test to check progress.
- Maintain the current dose if the desired level is reached.
56 days after first injection
- Perform a control test to ensure stability.
- Continue monitoring and adjusting doses as needed.
Adjust dosages
If changing testosterone or aromatizing steroid doses, adjust aromatase inhibitor doses and retest as necessary.
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