One of the topics always in question is how to manage estrogen and prolactin levels on cycle. This thread should serve as an informational base to educate users further. This is probably one of the more important topics as the lack of attention to these categories can result in some serious complications. Before we get into managing E2 and prolactin, it’s really important that you understand exactly what they are, their purpose and how they become elevated. Once you have a clear understanding of their function, we will move onto managing them in a safe manner. Let’s get cranking…
Estrogen in Men: Explanation and Purpose
Also referred to as Oestrogens, is a group of hormones found in various areas in the body. The main purpose of estrogen in men is to aid in the maturing your sperm, and to help regulate your libido. It’s far more abundant in females and aids them in developing female characteristics. Some of these characteristics can develop in males should estrogen be found in excess. But there’s more purpose to estrogen that we’ll be discussing.
Estrogen is biosynthesized. Meaning, it is formed by another source in the body. It’s a product of testosterone conversion. Testosterone is converted into estrogen with the help of an enzyme called the “Aromatase”. The amount of aromatase enzymes in a body matters. Not everyone has the same amount. But it’s mostly found in fat cells. The more fat that you carry, the more you estrogen you will convert. One of many reasons not to cycle anabolic steroids when you’re overweight. Make sense now?
You probably heard different references to it. Such as E2 or estradiol. Estrogen, as a whole, is comprised of several sex hormones. These are as follows:
- Estrone (E1)
- Estradiol (E2)
- Estriol (E3)
You notice Estradiol or E2 is in bold above. This is because E2 is what matter in a male. E2 is 10 times more potent than E1, and 100 times more potent than E3. This is why males get an Estradiol test, or better yet; a Sensitive Estradiol assay. We will discuss the importance of these tests later in this article.
Your estrogen levels should be in range to maintain a healthy libido and avoid side effects. This is one of the most important things to factor into cycle management. Levels that are too low can cause problems for you. Levels that are too high can cause serious complications. So we need a balance here. Let’s have a look at the issues you’ll experience with the highs and lows of estrogen levels…
Low Estrogen Side Effects:
- Osteoporosis (weakened bones) ; (long-term low levels)
- Poor sex drive
- Skin quality diminishes
- Poor sense of wellbeing & poor quality of life
High Estrogen Side Effects:
- Anxiety & panic attacks
- Erectile dysfunction
- Water retention
- High blood pressure
- Loss of balance/instability/dizziness
- Respiratory related concerns
- Low libido
- Prostate related issues
- Crying like a little girl and being emotional all the time
So you see, neither high nor low are healthy. And since we’ve already established the fact that the more body fat you carry, the more aromatase enzymes you have; you now understand why it’s best to cycle when body fat is low. As you look at these side effects, you can use this list of concerns to self-diagnose the possibility of “out of range” estrogen levels. Hopefully that would trigger the need to have your blood levels checked. But keep reading because we’re going to discuss blood work later in this article.
How To Control Estrogen
First of all, while I listed the side effects above, which also serve as symptoms; I really don’t have a “lazy man’s guide” for controlling estrogen levels. Blood work is really the only way to accurately manage your E2 levels. Otherwise, we would simply observe symptoms and self diagnosis becomes a guessing game. A dangerous one at that. But before we get into blood testing, let’s talk about methods used to control estrogen while you’re on a steroid cycle with aromatizable compounds.
Aromatase Inhibitors (AI)
There are several inhibitors available for you to use. The main purpose for all of these drugs is to maintain a healthy level of estrogen. While they work in different ways, they all focus on lowering or maintaining estrogen levels. Since we just learned that the Aromatase enzyme is what synthesized estrogen, the name “Aromatase Inhibitor” suddenly makes sense, right? AI’s do exactly as their title suggests; Inhibits the aromatase activity in your body. Now we need to find out what inhibitors are available and how they work…
There are several inhibitors available on the market today. Not all of them are made equal.
Types of Aromatase Inhibitors:
- Non Selective
For our purpose, we only need to be using Selective compounds because Non Selective compounds such as Cytadren and Teslac work differently and are generally pretty weak. So to save time, we will not be discussing Non Selective inhibitors since they are not relevant to our purpose.
Types of Selective Inhibitors:
- Reversible inhibition
- Irreversible inhibition (aka suicide inhibitor)
Reversible inhibition means that the aromatase enzymes’ activity is blocked, but the enzyme remains alive and intact. Irreversible, or suicide inhibitors kill the enzyme. It no longer exists. Please remember, just because the enzyme is dead, does not mean you will not develop more enzymes. Contrary; you continue to develop aromatase enzymes. By either killing or blocking aromatase enzymes, the conversion of testosterone to estrogen is blocked. And if dosed properly, eventually your levels drop to a reasonable and healthy range.
Available and Popular Reversible AI’s:
- Anastrozole (Arimidex )
- Letrozole (femara)
- Formestane (Lentaron)
- Vorozole (Revizor)
Available irreversible AI’s (Suicide inhibitors):
- Exemestane (Aromasin )
So there you have it. These are generally your options for lowering your Estrogen levels and maintaining a healthy state in the E2 department. You could also use some over-the-counter products. Some have been proven to work well. Depending on the individual, as we all react differently to these drugs, you may need an extra boost with an over the counter product. Pill forms are hard to split up properly sometimes and the addition of OTC drugs can help with the balance without going overboard.
Natural Over The Counter AI’s:
- DIM (Diindolylmethane) - I use this with TRT, very effective.
- Resveratrol (pretty weak)
- Chrysin (better than Resveratrol, but still weak)
- Zinc (Decent, but an effective dose is also not healthy)
In my experience, it’s always been proven (through blood work) that DIM is the most effective natural OTC product available today. Coupled with an AI, it can do some good for you. My TRT protocol is now managed so well, that I don’t even use an AI, I use DIM solely. Works perfect for me.
Inhibitor Dosing & Information
I’ll only discuss the common ones that are available through our site sponsors. If you need additional info on any others please let me know and I will do my best to deliver more information. So for the purpose of accessibility and this article, we will discuss dosing with Arimidex, letrozole , Aromasin and DIM.
Dosing below are STARTING DOSES based on a basic 500 mg Testosterone Cycle. Once you get blood work mid-cycle, you should be able to confirm if that dose is working, or if it needs adjusting. Never ever reply on my word or anyone elses for that matter. Always look at blood work to confirm, but this has generally proven effective for most. So I’m merely sharing my personal experiences with you over the years.
Please remember: Everyone is different and doses may vary, only blood work can identify proper dosage.
Informative Data On Mentioned Inhibitors:
*** Anastrozole (Arimidex)
- Half Life: 50 hours
- Recommended dose: 0.25 mg Every Other Day. (for a basic 500mg Testosterone cycle)
- Common side effects: Hot flashes, joint discomfort, stomach discomfort, diarrhea, elevated cholesterol levels.
- Drug interactions: Lowers the effectiveness of DHEA. Double your dose of DHEA in the presence of Arimidex.
- Note: Drug interactions updated 08/16/2013. No adverse interaction between Arimidex & Nolvadex. Thanks to member: 100% for this study.
*** Exemestane (Aromasin)
- Half Life: 24 hours
- Recommended dose: 25 mg Every Day.
- Common side effects: Hot flashes, fatigue, insomnia, headache, depression, elevated bilirubin, elevated liver enzymes, alopecia, back pain, chest pain, constipation, lymphopenia .
- Drug interactions: Lowers the effectiveness of DHEA. Double your dose of DHEA in the presence of Aromasin.
*** Letrozole (Femara)
- Half Life: 48 hours
- Recommended dose: 50 mcg (micrograms) daily. Do not abuse this drug. Typical milligram doses are nonsense and likely underdosed gear.
- Common side effects: Hot flashes, fatigue, insomnia, headache, depression, cough, flu-like-symptoms, elevated bilirubin, vision disturbance, elevated chromium, loss of appetite, stomach discomfort. letro is one of the most powerful AI’s out there. Be cautious especially with this one. It’s power could be good but also could be bad as it can easily crash your E2 fairly quickly, rendering you useless. Blood work blood work!!
- Drug interactions: Lowers the effectiveness of both Nolvadex and DHEA. Double your dose of DHEA/Nolvadex in the presence of letrozole.
*** Diindolylmethane (DIM)
- Half Life: 7 hours
- Recommended dose: 150 mg Twice Daily (for a total of 300 mg daily).
- Common side effects: At the doses above, there really aren’t any side effects. But some are possible such as headaches and nausea.
- Drug interactions: No known drug interactions todate.
Prolactin in Men: Explanation and Purpose
First thing… there is no such thing as “prolactin-induced” gynecomastia. I’ve heard this one too many times and later in this segment you will understand why. Now, prolactin is another sex hormone and is secreted by the pituitary gland in your brain. Although it’s found in both males and females, it’s main purpose is for milk production for females. The fact is, males have no use for prolactin that we know of today. Why, God, why?? Anyway, while low levels are not harmful, high levels certainly are. So let’s take a look at the concerns with higher than normal prolactin levels in men…
Effects of High Prolactin Levels in Men:
- Adverse Testicular Interference
- Lowers natural testosterone
- Lower sperm count (to infertility levels)
- long term elevation can cause erectile dysfunction (sometimes short term)
- Low Libido
- Breast tenderness
- Male lactation
- Low ejaculate volume
19-Nortestosterone steroid such as nandrolone and Trenbolone can cause prolactin levels to become elevated MAINLY with the presence of excess estrogen. They are NOT a direct cause of high prolactin. While using prolactin inhibiting drugs will resolve issues, your first line of defense is controlling estrogen, as elevated estrogen can boost the effect of prolactin increase. It’s not uncommon to prevent prolactin increase with the use of an AI. But the doses of 19-Nor steroids today, may prove that is somewhat ineffective. Leading to the necessity of having a secondary (and direct) compound to combat the effects.
The way it works is entirely complicated and I couldn’t even think of a way to put it in laymans terms. But in short, 19-Nor interaction with the estrogen receptors will boost prolactin secretion. This is why it’s important to control estrogen first, and prolactin second. Also why I recommend that you have a secondary combat drug “on hand” and in some cases, used on cycle. You might wonder why I say “on hand”, since I earlier said that low prolactin is not harmful. Well, these drugs have some fairly heavy side effects and if not used properly can really affect your progress on cycle. So it’s OK to wait until needed for the sake of sanity. But I want to emphasize this again… if you have high prolactin and/or lactating, it’s a near 100% confirmation that you failed to control your estrogen levels.
How To Control Prolactin
To control prolactin, or elevated prolactin, we use drugs that activate dopamine. Dopamine is a chemical launched by cells in the brain with the purpose of signaling nerve cells. So these drugs we’re looking at are dopamine agonists. There are several things that affect prolactin but dopamine is the dominant one that makes the overall difference.
Dopamine works with the pituitary. They’re friends, you see. But sometimes the pituitary gets a little excited and out of control, so Dopamine pays a visit to the pituitary and binds to the Dopamine receptors and slows prolactin production down to a reasonable level. This is all done with internal communication. What a nice friend to have. Make sense, folks? What a spectacular system we have. Even more reason to respect your body.
Now that we know how prolactin elevates and how to fix the problem, let’s have a look at common drugs used for prolactin control. I’m getting kind of bored with this article so I’ll keep this short since I still have to cover progesterone.
Common “Anti-Prolactin” (dopamine agonist) drugs available:
- Pramipexole (Mirapex)
- Cabergoline (Dostinex)
- Bromocriptine (Parlodel)
- Pergolide (Permax)
Informative Data On Mentioned Inhibitors:
*** Pramipexole (Mirapex)
- Half Life: 8 hours
- Recommended dose: 0.25 mg Every Night. Take right before you fall asleep. If after 3 days you can handle the dose just fine, increase to 0.5 mg. Then again to 0.75 and finally to 1 mg. Rarely more than 1 mg is needed.
- Common side effects: Nausea, dizziness, vomiting, insomnia, constipation, confusion, visual disturbance, hallucinations, headaches, frequent urination, congestion, achiness.
- Drug interactions: Do not use alongside other dopamine agonists. Avoid antihistamines altogether as the combination will have adverse effects on your central nervous system.
- Half Life: 65 hours
- Recommended dose: 0.25 mg Every Third Day. If after 4 doses you feel good, increase to 0.5mg every third day.
- Common side effects: Same as Prami for the most part, but can also cause anxiety and compulsive behavior.
- Drug interactions: Avoid anorexiants (appetite suppressors) as the combo can cause severe levels of serotonin. also avoid other dopamine agonists. Avoid Codeine because the combination renders the drug ineffective and lowers blood pressure too much.
Progesterone in Men: Explanation and Purpose
Progesterone is another steroid hormone in our bodies. Most people think this is only useful to women, however, unlike prolactin, there are actual benefits to healthy levels of progesterone. It “counters” some of the adverse effects stemming from estrogen. For those of us off cycle, it’s also a precursor for testosterone. Also cortisone via the adrenal glands. It’s produced from cholesterol where it’s first pregnenolone and then progesterone. In fact, many men are prescribed progesterone-increasing drugs to elevate levels into the upper range for a more healthy state.
If it’s so great, why don’t we cause it to produce even more? Well, out of range levels can cause complications. This hormone is beneficial but only in healthy ranges. Beyond that, it becomes an enemy. So our goal is to keep progesterone in range so that it remains a “friendly” hormone so to speak. Now let’s have a quick look at the concerns we will face, as men, in the presence of elevated progesterone levels…
Side Effects Of High Progesterone Levels:
- Erectile Dysfunction
- Lower Libido
- Hair Loss
- Muscle Atrophy
You see how serious high levels are? We need to maintain a healthy level of progesterone for many reasons as outlined above. But I want to cover gynecomastia for a minute because I want you to understand the cause.
Progesterone increases because too many receptors are activated by progestins. Progestins are compounds that act on these receptors, such as Trenbolone and nandrolone or any 19-nor steroid. This is what causes progesterone to increase and why you see the increase when these steroids are introduced. You never need protection with other steroids because others are not progestins. Make sense?
Can you guess what I’m going to say next? That’s right. It’s worse in the presence of excess estrogen! Especially in the breasts as it acts to promote breast tissue alongside estrogen by increasing 1GF-1 in the breast. Also, progesterone directly stimulates estrogenic activity at the mammary tissues. So here we have a semi-direct influence. High progesterone increases estrogenic activity and results in gynecomastia. But once again I want to reiterate, your first line of defense is controlling estrogen!
Treating elevated progesterone levels can be done via Selective Progesterone Receptor Modulators (SPRM). For example, Asoprisnil; also known as J867. SPRM’s are quite aggressive and should only be used in extreme cases and under a doctor’s supervision. So I do not recommend them because they could easily cause your levels to plummet, causing other issues. So instead, I recommend that you use an AI to simply put an end to progesterone stimulating estrogenic activity. So even though this has a direct effect, the effect would lesson in the presence of less estrogen.
I highly recommend Aromasin as the AI of choice when running 19-Nor steroids.
Myth: Nolvadex may not be used with 19-Nor. FALSE! Nolva/Tamox is a mixed estrogen receptor agonist/antagonist. Some tissue (not all), upregulation of progesterone receptor can happen; for example in the mucous membrane because it’s estro-sensitive. But our concern is the breast. And Nolva blocks the estrogen receptor. Progesterone receptor is then synthesized. Blocked estrogen receptor = down regulated progesterone receptor.
Gynecomastia: Explanation and how to treat it
This is simply the enlargement of breast tissue in males. Your body is basically adopting female characteristics. As mentioned earlier, this is caused by excess estrogen and can be aggravated directly by excess progesterone. There are several proven methods to reverse gynecomastia. Some are more effective than others. I’ll mention the most common ones.
Gynecomastia reversing drugs (ordered by effectiveness):
Do you notice a common denominator? They’re all Selective Estrogen Receptor Modulators (SERM). But why have I not listed the other popular SERMs such as Clomiphene (clomid) and Toremifene? Well, although the similarities are abundant, these other SERMs do more stimulation at the pituitary (brain), where the SERMs I mentioned are much stronger and effective at the breast tissue. This is why they are to be used in gynecomastia reduction/reversing. I’ll discuss dosing for the compounds I’ve personally used.
Raloxifene: Dose Raloxifene at 60 mg, up to 80mg daily. Do not go up and down with the dose. Start with 60 mg for 6 weeks. If you do not notice much difference, increase to 80 mg and stay at 80 mg until gynecomastia is reversed.
Tamoxifen: Dose at 40 mg every day for 1 week. After that, drop dose to 20 mg and use that every day until gynecomastia is reversed.
About Reversing With letrozole: Yes, it can be done. However, I do not recommend this method. Letrozole is a fairly harsh compound and the protocols I’ve seen out there are wild. Multiple milligrams of this compound time after time is a surefire way to crush your E2 levels. Then you’re left miserable and hating life. Do not use this compound. However, if you are not convinced, please be super cautious with it. The milgram + suggestions are mind boggling to me, I don’t care how many people say it works for them. I promise you, most of these folks are not monitoring blood work and this entire deal is a guessing game.
First of all, if you insist on Letro, I would run letro at NO MORE than 100 mcg daily. Yes, that’s MICROgrams. Letro took me from 47 ng/dL to 2 ng/dL in 10 days. That’s how powerful and difficult to manage this compound is.
Final note regarding gynecomastia reversal… This process takes time. Too many things factor into this so giving you an estimate on how long it takes makes zero sense. Everyone is different and every gynecomastia case is different. Main factors are the level of estrogen present, body fat percentage and the age of your gynecomastia. All that would render an estimate of time to reverse it useless. You must however, have patients. This is not a quick process at all. Not even close. In some cases it can take up to 9 months, heck even longer. But… My experience was that I noticed a big difference around week 6, and was able to completely reverse it before the end of the 3rd month.
Blood Work For E2 and Gynecomastia Prevention
Obviously you’ve noted by now that controlling estrogen is the main key to any negative issues that surround gynecomastia. Since this is your first line of defense, you’ll need to have your E2 checked mid cycle to verify your AI doses are actually working and keeping you in range. Even with progestins, your chances of gynecomastia are near zero with estrogen levels in range. But even the slightest elevation can aggravate the issue in the presence of other compounds.
Now, lots of folks seem to order a simple Estradiol panel. This is OK but it’s really not accurate. Especially in the presence of high conversion from Testosterone to Estrogen. Women have very high estrogen levels and a simple Estradiol test will suffice for them. Men however, are very sensitive to estrogen related issues and require a more accurate result. That would be a Sensitive or Ultrasensitive E2 assay. Your Estradiol result is not as accurate. So while you might think you’re in range, you may in fact be above range. Slightly above range is not that big of a deal for a lot of folks, but some folks are super sensitive and are “Gyno Prone”, so if you’re not super experienced, get a sensitive panel.