How to use anti-estrogens and prolactin inhibitors during a steroid cycle?

Author: Yuri Klimishin - an iron enthusiast and veteran of the "chemical" front.
2014-12-09

Important! We do not advocate for the use of steroids and other potent substances. All information is provided so that those who still decide to take them can do so with minimal health risks.

Drugs from both groups will be very useful for users of anabolic steroids. This refers to people who thoughtfully approach the construction of their dream healthy body. However, using these helpers must be done correctly and in a timely manner, or they can easily turn from friends into foes.

Very often, enthusiasts seriously underestimate the hidden dangers of these medications. Meanwhile, the side effects of both types are far more dangerous and significant than the side effects of anabolic steroids themselves. But it's also impossible to completely avoid them. Thus, the only solution is to use them correctly.

What is Aromatization

Aromatization is the conversion of testosterone into estradiol (estrogen) or androstenedione into estrone. This process takes place both naturally during metabolism and through the use of medications that are prone to aromatization.

The following are subject to aromatization:

• Testosterone,
• Methyltestosterone,
• Methandrostenolone,
• Chorionic gonadotropin.
• Boldenone also converts into estradiol, but it does not pose side effects.
• Oxymetholone exhibits estrogenic activity on its own and can easily provoke a whole range of estrogen-related issues.

What are the consequences? It's simple. Gynecomastia, excessive fluid retention, accelerated fat accumulation in the most unexpected places—around the waist, hips, and buttocks. Unfortunately, even a rugged man can develop a flabby backside. And let's not forget about acne.

Causes of Aromatization

I won't discuss natural transformations, but let's talk about those provoked by steroid use. There may be three reasons:

The first is using excessive dosages of aromatizing steroids for a particular user. When starting with dangerous steroids, you must begin with minimal dosages and not increase them until they no longer produce the desired effect. If these steroids are taken for more than two months without interruption, aromatase inhibitors become necessary.

The second reason is an unhealthy liver. If you are doing everything right, but estrogenic side effects keep surfacing, go check your liver's condition.

The third reason is an elevated level of the aromatase enzyme in the body or a large number of estrogen receptors in the skin, fat layer, and breast tissue. This situation is special, and the only way to avoid problems here is to give up aromatizing steroids once and for all.

To combat estradiol, we have two classes of medications:

• Aromatase Inhibitors. They reduce the amount of estradiol in the body.
• Estrogen Receptor Blockers. They occupy estrogen receptors, preventing estradiol molecules from binding to them and activating.

Now let's get specific about the medications and how to use them correctly.

Aromatase Inhibitors

Mesterolone (Proviron) is a pure androgen. However, it doesn't perform its primary functions very effectively. At least, it is definitely not worth using it as an anabolic or anti-catabolic agent. On the other hand, it does a decent job of inhibiting (reducing) estradiol levels. Its purpose is to prevent an excessive increase in the female sex hormone during the use of testosterone in a cycle.

Depending on the sensitivity of the specific organism and the steroid dosages, the working dose of Proviron ranges from 25-50 mg per day. There is no point in taking more than 50 mg. If these doses do not work, then you need to switch to more powerful medications.

There is a misconception about the complete safety of Proviron. This is not true. Being a derivative of dihydrotestosterone, it can provoke acne, hair loss on the scalp, increased hair growth in other parts of the body, and issues with the prostate. That is why one should not be reckless with dosing. Remember: Proviron is used during the cycle and immediately after it to deal with excess estradiol. IT CANNOT BE USED DURING PCT (POST CYCLE THERAPY)! AS A STRONG ANDROGEN, IT WILL SIGNIFICANTLY INTERFERE WITH THE RECOVERY OF THE BODY'S SEXUAL FUNCTION.

Anastrozole is a new generation aromatase inhibitor. It is currently the best option available. It quickly and effectively eliminates excess estrogen molecules and is well tolerated by the body when the correct dose is followed. It should only be used during the cycle for prevention and immediately after its completion before beginning PCT.

Dosage: half a tablet every other day (0.5 mg). You can keep some in your cabinet and when the first signs of aromatization appear, take a tablet immediately, then half a tablet every other day until the unwanted symptoms disappear. Afterward, stop taking it until new issues arise. After the cycle, take half a tablet every other day for a period of one to two weeks, and only then start PCT.

Just keep in mind - if you go overboard with a rational dose, the side effects will come flooding in. Typically, these include depression, insomnia, loss of appetite, chest pain, decreased speed and quality of thinking, and memory deterioration. There may also be issues with libido, bone pain, and a sharp deterioration in the ratio of bad to good cholesterol. All of this is related to an excessive reduction of estradiol in the body. A certain amount of the female hormone is necessary for normal functioning in the male body. As soon as its level drops below the acceptable norm, muscle growth halts, bone tissue deteriorates, and the heart and nervous system suffer. Moreover, a man becomes dull and loses interest in the opposite sex.

Letrozole and Exemestane are like the siblings of Anastrozole. Aromatase inhibitors. However, their use by amateur men is not permitted. Their action is so powerful that it won't be easy to control. By acquiring them, you risk experiencing everything I've mentioned above in the side effects of anastrozole, but in a hypertrophied form.

Aminoglutethimide (Cytadren, Orimetene) is a powerful anti-catabolic on one hand, and an aromatase inhibitor on the other. With the advent of anastrozole, it has completely lost its relevance. Despite its strong action and high effectiveness, it carries a host of side effects. The most dangerous is the sharp reduction in the synthesis of pregnenolone—the precursor of all steroid (cholesterol) hormones. Simply put, it can trigger problems with the reproductive system and adrenal glands. Do you really need that?

Testolactone is a new creation from the pharmacological luminaries. A revolutionary product that combines gonadotropin’s stimulating effect on the testes with powerful aromatase inhibition. It can be used both during a cycle and after it before PCT. One downside is that it costs as much as an airplane wing. So for the average person, this is currently beyond reach.

And the most important thing to remember is the two rules.

The first - any aromatase inhibitors are used exclusively during the steroid cycle (for prevention) and immediately after it ends (to get rid of excess estradiol) before starting PCT. During PCT, ONLY estrogen receptor blockers (tamoxifen, clomiphene, and toremifene) should be used.

The second - if the dosages mentioned above are insufficient for you, then the problem lies either within you (liver or genetic features of the body), or (which is MUCH more common) you need to lower the dosages of aromatizing steroids. And also - if a lump has formed under one or both nipples, only tamoxifen can handle it. Other anti-estrogens may or may not help. This is already individual.

Estrogen Receptor Blockers

Tamoxifen, Clomid, and Toremifene are selective estrogen receptor modulators. They should ONLY be used during PCT. The exception may be tamoxifen—used to combat already formed lumps during the cycle. Those who continue to adhere to Soviet stereotypes (using them during a cycle) are making a grave mistake. To confirm my words, I recommend finding the side effects of any of these three substances and studying them closely. I will not list them here—it's just too long of a list. Times change—and to stay in the past is STUPID!

It should be noted separately about oxymetholone. It does not convert into estradiol, but instead activates estrogen receptors directly. Therefore, aromatase inhibitors are useless in its case. The only way to combat the phenomena of feminization when using it is to simultaneously take estrogen receptor blockers (tamoxifen, clomid, toremifene).

What are the dangers of excess prolactin?

Nandrolone, oxymetholone (there it is again) and trenbolone are steroids that exhibit progestogenic activity. There is also norethandrolone, but obtaining it is unrealistic, so we won't discuss it.

What are the consequences? The molecules of these steroids can bind to progestin receptors—this, in turn, triggers increased activity of several enzymes that inactivate the action of dopamine. And dopamine is the only controller of prolactin production in the pituitary gland.

Next, it's simple - the level of prolactin becomes too high. This leads to pronounced feminization effects (development of secondary sexual characteristics in a female pattern). It's the same as having an excessive amount of estradiol in the body. Gynecomastia, water retention, fat accumulation, and the most serious issue - the global suppression of the hypothalamus-pituitary-testis axis. An excess of prolactin can severely disrupt erectile function and cause problems with spermatogenesis (testicular atrophy and sperm sterility). The most unpleasant consequence is the prolonged recovery of the sexual axis (especially after nandrolone). Additionally, it's worth mentioning prolactin-induced gynecomastia. The primary target receptors for prolactin are located in the breast tissue. Estrogen receptors are also found there (not in everyone, but in many). Prolactin not only promotes fat accumulation in the chest area but also increases the sensitivity of estrogen receptors and the activity of estradiol molecules. This means we can end up with not just gynecomastia but monstrous gynecomastia, which will be very difficult to combat.

In a separate category is trenbolone. In its case, gynecomastia is extremely rare. Water retention and fat accumulation are virtually nonsensical for tren. However, it can provoke erectile dysfunction. Unfortunately.

Now let's talk about the medications that help deal with all of this nonsense.

Prolactin Inhibitors

Cabergoline (Dostinex) is a new generation prolactin inhibitor. It selectively stimulates D-2 dopamine receptors. This means it quickly and reliably reduces excess prolactin. The most important thing is that while cabergoline is active, the previously suppressed dopamine will recover. The reasonable dose of cabergoline is 250 mcg every four days (roughly one tablet containing 500 mcg per week). Now there are analogs of Dostinex available, and they can be used as well.

The side effects of this substance (when the indicated dose is adhered to) manifest as insomnia and suppressed appetite. Mood deterioration can occur but not in everyone, and it usually passes a few days after starting the drug.

Bromocriptine (Parlodel) is also a prolactin inhibitor and is very effective as well. Its action is similar to cabergoline, but unlike the latter, bromocriptine can somewhat suppress the production of growth hormone by the pituitary gland (this fact is not yet fully proven, but it should be considered). Another distinguishing feature is the pronounced side effects. Common side effects of this substance include: nausea, complete loss of appetite, and migraines. Occasionally, bromocriptine can cause episodes of low blood pressure (which exacerbates all the aforementioned side effects and provokes drowsiness and physical weakness).

The most tolerant way to take this drug is to start with half a tablet daily before sleep and over ten days increase the dose to two tablets daily. One before breakfast and the second before sleep. This refers to tablets containing 2.5 mg of the active ingredient.

And now the most important thing. Prolactin is a very necessary hormone in the male body. Besides regulating water and salt metabolism, it plays a role in sperm formation and orgasm achievement. Most importantly, it has immunomodulatory effects. Just slightly lowering the natural level of prolactin puts the immune functions of our beloved body at risk. Not only the overall immunity suffers, but the cellular immunity as well.

Conclusions

As you can see, one should not overdo it with aromatase inhibitors and prolactin. Otherwise, we may find that sports become the least of our concerns. The simplest way to control prolactin and estradiol levels is to have regular blood tests done. Before, during, and after a cycle. Unfortunately, the average amateur is not financially prepared for this. The costs exceed those of pharmacology and food.

What can be recommended to those who do not have a suitcase full of dollars in the attic?

1. Be very careful in selecting and increasing testosterone dosages.

2. Exclude Methandienone, Oxymetholone, and Nandrolone (I won’t even mention Methyltestosterone) and cautiously familiarize yourself with Trenbolone.

3. If you decide to cycle throughout life, always keep aromatase and prolactin inhibitors on hand. But use them only in the case of a real need. After all, in this case, going overboard is much more dangerous.

4. Monitor the condition of your liver. Do not start cycling until you've taken care of it.

5. AND ALWAYS conduct PCT before a long break in steroid therapy.