Often overlooked, particularly by those with little knowledge of steroids, is the importance of managing estrogen on cycle. Why is this? Depending on the type of compound used, use of aromatase inhibitors, and other factors, you may experience the following side effects.

Side effects of high estrogen:

• Skin and Physical Appearance
  • Acne
  • Water retention (Bloat) and;
  • Moon face (puffy face)
  • Gynecomastia (gyno) 
• Sexual Health
  • Low libido
  • Soft erections (Erectile Dysfunction)
  • Urinary Issues
• Mood and Mental Health
  • Moodiness (Aggression, depression, increased irritability)
  • Lethargy
  • Insomnia
• Other
  • Increased cravings for sugar/chocolate
  • Constipation 
  • High blood pressure and spikes 

Side effects of low estrogen:

• Skin and Physical Appearance
  • Dry skin/lips 
  • Feeling of dehydration
  • Dry glans (penis)  
  • Dry, achy joints  
• Sexual Health
  • Low libido
  • Soft erections (Erectile Dysfunction) 
  • Loss of sensitivity  
  • Weak orgasms
  • Urinary issues
• Mood and Mental Health
  • Irritability/mood swings – emotional instability – random urges to cry
  • Obsessive thoughts
• Other
  • Constipation
  • A diuretic effect 
  • Loss of appetite
  • Fatigue & lethargy
  • Night sweats

Clearly managing your estrogen levels is important. It appears estrogen-related side effects appear in a U shaped curve, with some similar side effects appearing with either low or high estrogen. It is important to keep in mind that having one of these side effects does not indicate your estrogen levels and blood work is the most effective way of determining your hormonal profile. Think of this list of side effects to be more as a profile of symptoms, with the more experienced the more likely it is they are related to high/low estrogen. 

Before diving into the methods of management it is important to understand the different types of estrogen. Estrogen is often referred to as E2 (Estradiol) as this is the active form of estrogen, whereas E1 (Estrone) and E3 (Estriol) are less-active forms. E2 is the primary point of concern for PED purposes. E2 is in lower levels in men’s bodies then womens, and plays a more complicated role, and on the other side of the coin Testosterone is found in low amounts in women’s bodies and plays a more complicated role. For the sake of simplicity, Estrogen will be referred to as an overarching term.

So how do Estrogen levels fluctuate on a cycle? Well when you increase Testosterone levels, through exogenous administration, more Testosterone will be converted into Estrogen via the enzyme aromatase then what would happen normally. Conversely, when you use a compound like Halotestin, which isn’t a substrate for aromatase (does not interact with aromatase), there is no conversions into an estrogenic metabolite, thus using a non-aromatising steroid by itself will lead to crushed estrogen levels.

How can you manage Estrogen levels? Through the use of compounds that alter aromatase activity. These can either be over the counter supplements or prescription medications – which are known as aromatase inhibitors. 

Before delving into those lets address the low hanging fruit of lowering Estrogen levels:

• Reducing body fat percentage: Aromatase enzyme expression is far higher in adipose tissue, so reducing the amount of adipose tissue will lower your Aromatase/Estrogen levels. BF being between 8-12% seems to be the sweet spot for most.
• Insulin resistance: Somewhat ties in with the last point, but chronically elevated insulin levels can lead to the overexpression of aromatase
• General poor dietary choices

Aromatase inhibitors: 

• Exemestane (Aromasin): Steroidal suicide inhibitor
• Arimidex (Anastrozole): Non-steroidal reversibly binding inhibitor 
• Letrozole (Femara): Non-steroidal reversibly binding inhibitor

Aromasin (Exemestane) is an oral, suicidal aromatase inhibitor. Due to its steroidal structure, it is better for lipid profiles, and increases the ratio of free-total testosterone by lowering SHBG.

Suicidal aromatase inhibitor, means it binds to aromatase enzymes and permanently disables them i.e. its name ‘suicidal’. This prevents an estrogen rebound seen by Arimidex (Anastrozole), and Letrozole (Femara). Aromasin has a short half life of ~9 hours, but maintains estrogen suppression up to 72 hours, from one 25mg dose.

Arimidex (Anastrozole) is a non-steroidal reversibly binding inhibitor. In studies 1mg Arimidex lowered Estradiol (E2) by 70% within 24, and then 80% after two weeks of administration, suggesting a build up of concentrations (similar dynamics to that of Finasteride). Studies found 0.5mg had comparable effects. The amount of Arimidex used depends on the dosage of anabolic steroid used, the type of anabolic steroid used, and other factors. Arimidex has a half life of ~48 hours. 

Letrozole appears to be the most nuclear option, being highly potent at crashing estrogen, and having more side effects reported anecdotally. 

To prevent estrogen rebounds seen by Arimidex and Letrozole it is particularly important you taper off the dosage. Remember the lowest effective dosage is always the best for your health, don’t follow arbitrary numbers. 

Another factor to consider is blood work. The most important part of managing Estrogen is getting regular blood work. This will establish a baseline, help see how your body reacts to both AAS and Aromatase Inhibitors, and allows you to determine how to address Estrogen-related side effects. 

Obviously choosing a specific dosage requires a personalised approach, but for those looking for a reference number, here are the accepted values. 0.5 mg Arimidex every 3 days (E3D) or bi-weekly (E3.5D) for 500-600 mg of Testosterone. 12.5 mg of Aromasin E3D or E3.5D for 500-600 mg of Testosterone. Obviously the dosage should depend on your bloodwork, Estrogen levels, and Aromatase activity. 

Over the counter supplements and compounds are most suitable for those who are low-aromatisers naturally, as they wont lower estrogen as significantly as aromatase inhibitors, but since you have naturally lower aromatase levels you don’t quite need high inhibition.

• Diindolylmethane (DIM): An arbitrary dosage to point to is 100 mg in the morning and 100 mg in the evening which may help balance estrone (E1) and estradiol (E2) levels. TRT leads to higher conversions to E2, and metabolism of E2 too E1 will help balance these levels – leading to less estrogenic burdens from elevated E2 levels. 

• Vitamin C (Ascorbic Acid): High doses (e.g, 2,000-5,000 mg daily) may inhibit aromatase enzymes due to its antioxidant effects, and it is also beneficial for collagen deposition.
• As mentioned before, Insulin resistance can lead to increased aromatase expression, so over the counter supplements/compounds that improve insulin sensitivity may indirectly lower Estrogen levels. These include Berberine, Cinnamon extract, Alpha Lipoic Acid, and fenugreek, with Berberine showing the most efficacy. However there is no direct evidence on their effects on Estrogen levels.
• Nicotine gum can act as a mild aromatase inhibitor
• Tadalafil at 5 mg daily can reduce serum estradiol levels and improve the ratio between total testosterone and estradiol
• It’s been known Metformin can lower Estradiol for some time now. However i’m yet to see anyone explain why this is. My theory is that since Metformin blocks Tumor necrosis factor-alpha it indirectly lowers Estrogen levels, as Tumor necrosis factor-alpha has been shown to increase aromatase gene expression in adipose tissue (SEE REFRENCES)
• Others include, Melatonin at 3mg daily, Zinc at 11 mg daily (indirectly) and Calcium D-Glucarate

5 Alpha Reductase Inhibitors (5ARI) – Finasteride or Dutasteride – also alter Estrogen levels. 5ARIs work by inhibiting the 5 Alpha Reductase enzyme, which would normally convert Testosterone into DHT. Having lowered 5 Alpha Reductase levels through the use of a 5ARI leads to an increase of Testerone levels, allowing more Testosterone to convert to Estrogen if Aromatase activity isn’t managed. 

Another consideration when it comes to 5ARIs is that DHT actually acts as a reversely binding aromatase inhibitor and blocks estrogen mediated Gene transcription, reducing or limiting estrogenic side effects even if Estradiol levels are moderately elevated. However since DHT levels are lowered by 5ARIs, you become more susceptible to estrogenic side effects. So not only does it elevate serum Estradiol levels, it also makes you more sensitive to the effects of Estrogen. 

Even when serum estradiol levels are somewhat elevated. so not only do five Alpha reductase Inhibitors increase serum estradiol levels they also make you more susceptible to estrogenic side effects

Where does prolactin fit into the equation?

Although referred to as the lactation hormone, Prolactin has a wide number of functions (>300). Contrary to popular belief, Prolactin doesn’t cause gynecomastia. This myth likely stems from the fact that prolactin-related nipple changes can resemble early-stage gynecomastia. People with Gynecomastia rarely have elevated Prolactin . Symptoms often attributed to prolactin, such as puffy, sensitive nipples with oily discharge, are more likely caused by the enlargement of Montgomery glands, which are sebaceous glands that lubricate the nipples. 

The prolactin-related effects on the nipples are temporary and separate from true gynecomastia (permanent hyperplasia and fibrosis of breast tissue). 

However prolactin can cause an individual to be more at risk to estrogenic side effects like gynecomastia. This is because Prolactin has been shown to increase estrogen receptor density within breast tissue, thereby making a person more sensitive to Estrogen levels, and increases the risk of Gynecomastia development, especially if Estrogen is not managed. The 19-nortestosterone derivatives – Nandrolone (Deca/NPP) + Trenbolone + Trestolone/MENT (less known for Prolactin increases) are well known to increase Prolactin levels. Prolactin may also increase body fat percentage by increasing the production of a specific protein called lipoprotein lipase (LPL). 

As you can see when it comes to managing estrogen, there is a direct need to consider Prolactin levels too. Additionally elevated Prolactin in general is very burdensome on your high body, and managing levels should be considered whether you believe you’re at a low risk of Estrogenic side effects. 

Primary Options to managing prolactin: 

• Vitamin B6
• Bromocriptine
• Vitamin E
• SAM-e

Secondary Options:

• Ginseng Extract
• Maca Powder

• Ashwagandha
• Mucuna Pruriens
• Zinc
• Ginkgo Biloba

Primary options detailed breakdown:

Vitamin B6 (Pyridoxine Hydrochloride & P5P) is an affordable and effective prolactin inhibitor. A single 300mg dose lowers prolactin through dopaminergic activity. How does a dopaminergic compound lower Prolactin levels? Dopamine plays a major role in controlling prolactin by lowering its production. It does this by binding to D3 receptors, which block prolactin release from lactotrophs (the prolactin-producing cells in the pituitary). Dopamine agonists mimic dopamine, tricking the body into sensing high dopamine levels. This either shuts down or reduces prolactin production, depending on the dose.

Regular 300 mg doses (twice daily) reduced prolactin and slightly increased growth hormone in women. It also combats opioid-induced hyperprolactinemia, and exercise-related prolactin spikes are reduced. 

• P-5-P (active B6): 50-200mg daily, divided doses.
• Regular B6: 300-1000mg daily, divided doses.

Side effects – May cause peripheral neuropathy (tingling/numbness). P5P (active form) is often used to avoid this side effect. Ensure you’re taking Pyridoxine Hydrochloride (not Pyridoxal Hydrochloride), as the latter doesn’t lower prolactin.

Bromocriptine is the most effective at lowering Prolactin but has many side effects.

Vitamin E effectively lowers prolactin, with additional fertility benefits. Studies show it reduces prolactin in hemodialysis patients and potentially combats adenomas related to prolactin.

300-400 IU daily, increasing if needed. However it may temporarily raise blood pressure.

Higher doses can deplete iron stores so eating iron-rich foods or supplements is an important consideration.

SAM-e SAM-e enhances dopamine, lowers prolactin, and boosts mood. Studies on depressed patients show significant prolactin reduction with SAM-e supplementation. 200-100mg daily, paired with Vitamin B6 and E. May cause nausea or overstimulation or other excessive dopaminergic side effects in certain users.

References:

 Dickson G. Gynecomastia. Am Fam Physician. 2012 Apr 1;85(7):716-22. PMID: 22534349.

 Hyun B, Shin S, Lee A, Lee S, Song Y, Ha NJ, Cho KH, Kim K. Metformin Down-regulates TNF-α Secretion via Suppression of Scavenger Receptors in Macrophages. Immune Netw. 2013 Aug;13(4):123-32. doi: 10.4110/in.2013.13.4.123. Epub 2013 Aug 26. PMID: 24009539; PMCID: PMC3759709.

Zhao Y, Nichols JE, Valdez R, Mendelson CR, Simpson ER. Tumor necrosis factor-alpha stimulates aromatase gene expression in human adipose stromal cells through use of an activating protein-1 binding site upstream of promoter 1.4. Mol Endocrinol. 1996 Nov;10(11):1350-7. doi: 10.1210/mend.10.11.8923461. PMID: 8923461.