Review of Sports Pharmacology by Yuri Bombela

Review of Sports Pharmacology by Yuri Bombela

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Author of books and publications on sports pharmacology and nutritional supplements

19/11/2025

Coming soon on Amazon

13/11/2025

Enclomifene (or enclomiphene) is a relatively new drug. Essentially, it is a typical selective estrogen receptor modulator, but it lacks most of the disadvantages inherent in SERMs. However, acquiring enclomifene may present considerable challenges, because... But let's take it one step at a time.
Important notice
Get ready: there will be a lot of information, including scientific data. Unfortunately, the latter is unavoidable: this data is necessary to understand how and why the idea of creating enclomifene came from. I promise to explain everything in simple terms and as concisely as possible, without getting bogged down in unnecessary details.
Oh, yes: I should note right away that everything I write is addressed to men — after all, enclomifene was created specifically for them. However, no one is stopping women from reading this article.
What is enclomifene?
Everyone knows about a drug called Clomid (clomiphene). And many men not only know about it, but also actively use it — during post-cycle therapy, for example. But few people realize that Clomid is, in fact, a mixture of two stereoisomers of this substance: 38% zuclomifene and 62% enclomifene.
And here's what's interesting: these stereoisomers have directly opposite properties. Zuclomifene exhibits estrogenic activity, while enclomifene exhibits anti-estrogenic activity. Zuclomifene suppresses the activity of luteinizing (LH) and follicle-stimulating (FSH) hormones, while enclomifene increases the activity of both.
It turns out that enclomifene is responsible for all the benefits of clomid for men, while zuclomifene only interferes with it. If we leave only the first one and remove the second one in some way, we will get a drug that stimulates testosterone production (LG is responsible for this) and also increases fertility (FSH solves this task). At the same time, it would be free of the side effects that clomid has in abundance.
The task turned out to be not so simple, but in the end it was solved, and Repros Therapeutics introduced the drug Androxal, which contained enclomifene citrate as its active substance. All that remained was to obtain permission for its widespread sale. However, things did not go as expected.
The unhappy adventures
In 2007, the US Food and Drug Administration (FDA) refused to approve enclomifene, citing a lack of data on the drug's effectiveness. Between 2009 and 2019, additional studies were conducted, confirming that:
the use of enclomifene is safe and does not cause serious side effects;
enclomifene is indeed capable of increasing testosterone levels and can be recommended for patients with secondary hypogonadism;
the increase in testosterone levels occurs through the stimulation of LH and FSH production and activity.
Despite this, neither the FDA nor the European Medicines Agency has recognized enclomifene as an effective drug and has not granted permission for its free sale in either the United States or the European Union. That would be fine, but thanks to these same agencies, drugs with clearly unproven effectiveness and a whole bunch of side effects appear in pharmacies every year.
One can only guess at the reasons for this particular dislike of enclomiphene. I would venture to suggest that certain major players in the pharmaceutical market, unwilling to face strong competition, may have been involved. This is not the first such case, and, unfortunately, it will not be the last...
Be that as it may, today we have a paradoxical situation: enclomifene is produced and actively used with considerable success in medical practice. However, it has never been widely available for sale. More precisely, it was not available until recently, when generics began to be produced.
Weighing the pros and cons
Contrary to tradition, I will start with the arguments against the use of enclomifene. The first is that some people may not like the fact that the drug is not officially approved in either the European Union or the United States. However, if you do not live in either of those places, why do you need official approval?
The second argument against it is skepticism about generics. Although I know from my own experience that in terms of quality and effectiveness, they are often not only on par with the original drugs, but even surpass them.
The only serious argument against it is that enclomifene can increase the risk of blood clots. Yes, the risk is very small, and yes, problems can only occur in people who already have cardiovascular disease, but this argument is definitely worth considering.
Nothing else comes to mind: enclomifene has only a minor effect on the liver, very rarely causes headaches, and even more rarely causes nausea. Overall, it can be considered a fairly safe drug.
The main argument in favor of enclomifene is that it is extremely effective. There has not been a single (!) case where this drug has failed to increase testosterone levels. It is noteworthy that estradiol levels do not increase as a result of its use — neither Clomid nor tamoxifen can boast of this.
An absolutely amazing feature of enclomifene is its ability to increase the level and activity of not only luteinizing hormone, but also follicle-stimulating hormone. In other words, it helps fight both hypogonadism and infertility.
This means that enclomifene can be used in the vast majority of cases as the sole means of recovery after a steroid cycle – at least when it comes to testosterone production and fertility.
How do you use it?
Finally, some practical advice. The recommended doses of enclomifene are 12.5 and 25 mg per day. The latter is remarkably effective: in less than a month, it can achieve higher testosterone levels than those achieved with regular use of a drug such as AndroGel.
Enclomifene, unlike Clomid, has a fairly short half-life of only 10 hours. So it is best to take the drug twice a day, regardless of meals.
Above, I wrote that enclomifene is suitable for men who are trying to restore testosterone production after using anabolic steroids, but that is not the only group of people who may need this drug.
My advice to you is this: if you do not suffer from heart disease, try enclomifene. It will definitely help you solve your testosterone and fertility problems, if you have them. No better remedy has yet been invented to solve these two problems at the same time.

20/10/2025

I am planning to publish a book on selective androgen receptor modulators and peptide drugs in 2026. As I work on it, I will gradually introduce you to its contents, posting about one chapter per month. This one is dedicated to a drug known as Acadin, AC-262, or AC-262536. It is particularly relevant because I have been receiving a lot of questions about this drug lately.
Necessary caution
When purchasing selective androgen receptor modulators (SARMs), you do so at your own risk. All of these drugs are experimental — none of them have yet been launched into commercial production. This means that you cannot be completely sure of the effectiveness or safety of the selective modulator you are purchasing.
What's more, since all SARMs are produced exclusively illegally, you cannot be sure of the quality of your purchase — that the product you bought contains exactly what you paid for, and in the quantity stated.
What is AC-262?
If none of this scares you, then let's get started! Let's find out what AC-262536 is: this is the official name of the drug, but I will use its abbreviated form — AC-262.
The drug was developed by Acadia Pharmaceuticals, hence the name Acadine (spelled with one «c»). It was created specifically to combat prostate cancer; AC-262 should also help in the treatment of Alzheimer's disease.
The drug is currently in the research stage — so far, it has only been tested on laboratory animals. Human trials are still a long way off, so the effectiveness and safety of AC-262 for humans can only be judged based on the personal experience of those who have taken it.
It can be said with absolute certainty that AC-262 has a relatively low affinity for androgen receptors (AR): it lies in the lower range (1-10 nanomoles) and is approximately 5 nM. However, even when bound to AR, the AC-262 molecule does not necessarily activate it: on average, 66% of molecules are capable of doing so (each testosterone molecule necessarily activates AR).
On the other hand, the drug does not activate any other receptors, does not convert to estradiol or dihydrotestosterone, and does not bind to AR in the prostate (in fact, this property was inherent in it from the outset), skin, seminal ducts, or nerve fibers. In other words, AC-262 has minimal side effects.
What can you expect from the AC-262?
Moderate increases in muscle mass: experience with AC-262 shows that by consuming sufficient amounts of protein and other supplements, as well as training properly, it is possible to increase muscle mass by 2-2.5 kg in eight weeks.
I tried comparing AC-262 with other SARMs, and here's what I found
In terms of muscle mass gain, the drug is significantly inferior to RAD140, but superior to LGD-4033.
In terms of strength, drive, and recovery speed, AC-262 is significantly inferior to S-23.
Don't expect outstanding results in fat loss either: AC-262 can only slightly increase the rate of metabolic processes, but it has no effect on lipolysis — it's not like Ostarine (MK-2866).
But when it comes to side effects, AC-262 surpasses all of the above drugs: it can be considered almost the safest SARM (perhaps with the exception of S-4).
Another positive feature of AC-262 is its ability to suppress cortisol activity and thus prevent protein breakdown. In this respect, it is better to compare it not even with SARMs, but with an anabolic steroid such as stanozolol.
Weighing the pros and cons
AC-262 has been found to have a rather unpleasant side effect: prolonged use can trigger a heart attack or even a stroke. Apparently, this is why the drug has not yet been tested on humans.
Another unpleasant effect associated with taking AC-262 is quite severe headaches. In addition, joint pain is possible, albeit mild. So, those who have old injuries or chronic joint problems are better off not taking AC-262.
The drug's minimal impact on the body's own testosterone production is a plus. So, you can use it during post-cycle therapy to fight muscle breakdown.
Finally, let's talk about AC-262 dosage. In any case, it is worth starting with 10 mg per day — this will reduce possible side effects to an absolute minimum. 20 mg per day is for those who know what to expect from AC-262; this dosage achieves the ideal balance between effectiveness and safety.
30 mg is for athletes who value effectiveness over safety. With this dosage of AC-262, you will definitely experience significant suppression of your own testosterone production.
In any case, you should not take the drug for more than 4-6 weeks in a row; eight weeks is the absolute maximum. I am talking about people who do not have serious health problems. Those who suffer from cardiovascular diseases should not even consider AC-262.

13/09/2025

I have probably never written such a short book before, and I doubt I ever will again. Nevertheless, working on it proved to be no less difficult than working on a substantial, voluminous work — I had no idea there would be so many difficulties.
First of all, the thing is that everyone understands the word «prohormones» to mean whatever they want it to mean. That's why drugs that are completely different in origin are lumped together — not to mention their properties, behavior, effects on the body, and so on.
Secondly, information — there is practically none. There are very few studies that can really be relied upon; most articles are written in collaboration with manufacturers of «prohormones» (I put this word in quotation marks for a reason) — which means they are not particularly truthful.
Thirdly, availability. Yes, some prohormones (I mean real prohormones) can be purchased, but, first of all, with much greater difficulty than, for example, SARMs or even anabolic steroids. Second, the price: when you look at it, the desire to even try androgen precursors noticeably weakens and then disappears altogether.
Difficulties, difficulties, difficulties... I tried to overcome them, and what I came up with can truly be called the most comprehensive guide to the use of prohormones. I tried to proceed systematically — from limiting the range of substances that can be considered prohormones, through the history of their creation, to the consideration of specific drugs.
We will talk about the effectiveness of prohormones and about drugs such as prosteroids. But let's start with the answer to this simple question: how does testosterone synthesis occur? And then we will move on to the formal definition of prohormones.
the book is available on Amazon:

https://www.amazon.com/dp/B0FQCM642J

09/09/2025

Coming soon on Amazon!.

22/08/2025

What you are reading now is the most comprehensive guide to planning short steroid cycles. In fact, it is the only guide of its kind. So you definitely made the right choice by paying attention to it.
Why did I decide to write it? It's simple: many fans of the bulging muscles of athletes would love to try anabolic steroids — drugs that provide a significant advantage on the path to the desired physique. But fear holds them back, because there are so many unpleasant things said about steroids. If only it were completely safe...
So, it turns out that using anabolic steroids can be safe after all! Maybe not 100%, but definitely 99%. You just need to be smart about it and not go overboard. Short cycles are the best way to go for a sensible and balanced approach.
Interestingly, I didn't realize this right away: my first experience with short cycles was a complete disappointment. I even swore never to go back to them, only to break my vow a month later and try to figure out what could be improved.
A lot of time has passed since then, and I have completed countless short cycles; I have learned how to plan them correctly and get the most safety and effectiveness out of them. I want to share all this knowledge with you in this book.
And one more thing: in the first sentence, I wrote «steroid cycles». In fact, I am not going to limit you to the use of anabolic steroids alone — there are many other drugs that are not only suitable for use in short cycles, but even make them more effective.
Well, it's time to get down to business! This book will contain a lot of practical information — almost all of it, in fact. But I would still like to start with a theoretical explanation of short cycles.
Available on Amazon

https://www.amazon.com/author/yuri_bombela

25/07/2025

Estradiol Monitoring - What, How and Why_

We are used to thinking that men only need to monitor their estradiol levels during a steroid cycle — the rest of the time, it is within the normal range. In fact, this is not the case: many factors influence estradiol levels, so it can go beyond the acceptable range even without the help of anabolic steroids. I will definitely talk about these factors, but first, let's answer the question,
What is the danger of high estradiol levels?
Let me start with this: recently, there has been a noticeable decrease in the average testosterone level in young men. One of the reasons for this decrease is considered to be the relatively high level of estradiol — both hormones are interrelated.
In other words, an increase in estradiol levels will ultimately lead to a decrease in testosterone levels. This will immediately awaken a host of «demons», including low libido and erectile dysfunction, waistline gain, constant fatigue, mood swings, and even depression.
Estradiol generally has a beneficial effect on the cardiovascular system: women are less likely to develop cardiovascular diseases than men. However, excessively high (especially persistently elevated) levels of estradiol can be harmful, causing various complications. Yes, this applies to young men in particular.
Finally, excessively high levels of estradiol will lead to the development of gynecomastia, which occurs even in those who have never even heard of anabolic steroids. And, of course, there will be no muscle growth in this case.
What is an elevated level of estradiol?
Evaluating the level of estradiol in the blood of men on its own is a pointless exercise. It is necessary to look at the ratio of the levels of two hormones — testosterone and estradiol. And based on that, decide what to do.
(I am assuming that your testosterone levels are within the normal range — too low levels of this hormone are a separate issue).
So, the ideal situation is when testosterone levels exceed estradiol levels by 120-300 times. A ratio of 100:1 to 120:1 between the two hormones is also considered acceptable: it is worth being alert, but there is no need to intervene yet.
However, anything below a ratio of 100 to 1 should not only cause concern but also prompt specific steps to remedy the situation. We will look at these specific steps a little later, but for now, let's talk about
What can increase estradiol levels?
First and foremost, age. As the body ages, the activity of aromatase, an enzyme that converts testosterone into estradiol, increases.
Unfortunately, that's not all — the synthesis of enzymes called cytochromes P450, which are responsible for metabolizing estradiol and removing it from the body, also slows down. This means that as the body ages, more and more of this hormone accumulates in the blood.
The amount of cytochrome P450 in the blood decreases not only with age, but also with regular consumption of grapefruit juice, for example. Or with an unhealthy addiction to alcohol.
Some medications have a negative effect on P450: the antibiotic ciprofloxacin, the proton pump inhibitor omeprazole, the antihistamine cimetidine, the anticoagulant warfarin, and some others. Even a harmless supplement such as ginkgo biloba can disrupt enzyme synthesis, as can zinc deficiency.
Adipose tissue. Since testosterone is converted into estradiol mainly in adipose tissue, more fat under the skin means higher estradiol levels. All men who are overweight should be wary of this.
Xenoestrogens are chemical compounds that mimic the action of endogenous estrogens. Unfortunately, in today's world, they are everywhere: in plastic food packaging, insect repellents, perfumes, sunscreens, and even directly in food (these properties are inherent in some dyes and food preservatives).
Finally, there are plant estrogens, which are most abundant in soy products. Yes, they are much less dangerous and, unlike xenoestrogens, do not remain in the body for long. But with regular consumption, they can cause problems.
Eliminating the causes of increase
You should always start by eliminating the causes of the disease, rather than treating it. First of all, you should try to reduce the amount of fat under your skin by any means available. It is also worth eliminating phytoestrogens, i.e. avoiding foods containing soy. Just in case.
Xenoestrogens are more difficult to deal with, but there are some things you can do. First, do not use plastic packaging — either for storing food or for reheating it. Second, do not leave plastic containers with water in the sun; if they become very hot, they should be discarded.
Try not to eat farmed fish (tilapia, salmon, sturgeon; even shrimp are now farmed in the same unnatural conditions, so they should also be avoided). Use only olive or rice oil for frying, and add them to salads.
It is worth completely giving up fast food, as well as other foods that contribute to the accumulation of fat under the skin, such as cakes and pastries, mayonnaise, margarine, and foods that contain it, and so on.
The habit of eating right will even help you get rid of some fat deposits, and remember that it is in fatty tissue that testosterone is converted into estradiol. What else? Can you cut down on alcohol? Of course, if you try. Take supplements containing zinc? That shouldn't be a problem either.
You can replace P450-lowering medications and supplements — fortunately, there are plenty of alternatives. The only thing you can't do is stop aging.
Medicines for treating estradiol
However, there are remedies for this condition. They are called anti-estrogen drugs and are divided into two broad classes: aromatase inhibitors (arimistane, letrozol, exemestane) and selective estrogen receptor modulators (SERMs). I will not go into detail about how they work, their advantages and disadvantages, but I will say that only aromatase inhibitors are worth taking.
The single dose is one tablet, but the frequency of administration depends greatly on the «starting point». Usually, one tablet per week is sufficient, but if the estradiol level is significantly elevated, you can take one tablet every 3-4 days. If the level is very high, you can even take one every other day.
There is also a drug called Arimistane, which you can easily find online at a relatively affordable price. It should be noted that Arimistane is also an aromatase inhibitor, but it is very weak, so it is best to take it daily. Even so, you will not achieve the same effect as, for example, with letrozole.
What else is worth mentioning? Of course, Proviron. It is a common anabolic steroid with both SERM and aromatase inhibitor properties. It should be taken daily (preferably two tablets a day), and you should not expect any stunning effects from it. However, Proviron is guaranteed to increase libido.
There are other anabolic steroids with anti-estrogenic activity: drostanolone (Masteron), epistane, trenbolone... But drugs are a last resort. And you can take plain old vitamin D just for prevention: it's not an anti-estrogen on its own, but it can slow down the aromatization process when it gets out of control, so less testosterone turns into estradiol.
It is essential to know your s*x hormone levels; you should check them at least once every three months and take immediate action if any problems are detected. This will allow you to avoid a whole host of health problems and simply give you a much brighter and more fulfilling life.

16/07/2025

How can insulin sensitivity be improved?

Insulin sensitivity is the ability of body tissues to respond to insulin, one of the most important hormones in the human body. The opposite condition is insulin resistance, which can lead to many problems, the most serious of which is type 2 diabetes. In this article, I will list all the methods and techniques currently available that can help increase insulin sensitivity fairly quickly.
Why is this important?
I have already mentioned type 2 diabetes, but this disease does not develop immediately against a background of constantly reduced insulin sensitivity — it can take years. What will happen immediately, however, is difficulty in burning fat — insulin levels in the blood will be constantly elevated, and lipolysis is impossible in the presence of this hormone.
There will also be difficulties with increasing muscle volume: insulin sensitivity decreases primarily in muscle tissue, which means that muscles will receive fewer nutrients, primarily glucose. As a result, their glycogen stores will decrease, and with their decrease, your endurance will also decrease — you will not be able to train as much as you are used to.
How to check insulin sensitivity?
Insulin sensitivity is assessed using the HOMA-IR (Homeostatic Model Assessment for Insulin Resistance) index. It is calculated using the following simple formula:
HOMA-IR = fasting glucose (mmol/L) * fasting insulin (mIU/mL) / 22.5
Usually, if you have a blood test for glucose and insulin, your HOMA-IR index will be calculated automatically. If the laboratory did not do this, it will not be difficult for you to calculate it yourself.
How should you interpret the result? It's very simple: if you (or the laboratory) get a number lower than 2.7, then your insulin sensitivity is fine and there is no need to worry.
But if your HOMA-IR index is higher, you need to start increasing your insulin sensitivity. There are quite a few methods available to do this.
The simplest ways to improve insulin sensitivity
Although I have called these methods the simplest, some people may find them the most difficult. We are used to prioritizing taking various kinds of pills rather than making changes to our usual lifestyle.
But they need to be made, and the first changes should concern sleep. If you regularly don't get enough sleep, sleeping less than 7 hours a night, your insulin sensitivity will begin to decline quite quickly.
To make it easier to fall asleep and get a deeper sleep, take 3-5 mg of melatonin half an hour before going to bed. This advice is especially relevant in the summer, when most of us experience a disruption in our biological clock.
Try to go to bed early and take a brisk 15-20 minute walk in the fresh air after waking up — this will stimulate your body to fall asleep earlier.
The second change concerns stress — its amount must be reduced. You may say that this is not always possible, but I disagree. Yes, of course, you may not be able to reduce the number of stressful situations, but you can certainly change your reaction to them.
For example, by taking a combination of three simple supplements: vitamin C, ashwagandha, and Eurycoma longifolia extract (Tongkat Ali or Longjack). I have been taking it for about ten years, and it has helped me significantly increase my resistance to stress.
The third change in lifestyle is not only possible but necessary for everyone who is able to move independently. I have already mentioned a short walk immediately after waking up, but it is better not to limit yourself to that, but to walk for another half hour before going to bed.
In general, physical activity has about the same effect on insulin sensitivity as medication — its contribution to the fight against insulin resistance cannot be overestimated.
Strength training is particularly important, but if you are unable to go to a gym, don't worry. Just 5-7 minutes of simple push-ups, squats with your own body weight, or abdominal exercises 2-3 times a day 15 minutes before meals can work wonders, increasing your muscles' sensitivity to insulin to the sky.
Supplements and diet
I will start with the diet and, first of all, mention not what you should do, but what you should avoid. Surprisingly, you should avoid strict low-carb diets — if you regularly consume less than 100 grams of carbohydrates per day, your insulin sensitivity will begin to steadily decline after about a week and may drop to critical levels within a month.
However, intermittent fasting allows insulin sensitivity to increase quite quickly. One or two days of complete fasting per week, or at least a significant reduction in calorie intake to 30-40% of normal, will also help reduce insulin resistance.
If you don't want to follow any diet, just stick to these rules:
• Give up simple carbohydrates and trans fats.
• Use apple cider vinegar as a salad dressing — it greatly increases insulin sensitivity.
• Start each meal with protein and only then move on to carbohydrates.
• Eat more soluble fiber, which is found in beans, broccoli, Brussels sprouts, sweet potatoes, carrots, avocados, peaches, apricots, and figs.
• Take omega-3 fatty acids, but only those that are rich in docosahexaenoic acid (DHA).
Pharmaceuticals
There are many articles on the Internet devoted to increasing insulin sensitivity. But they all stop at the most interesting point — I have not seen a single one that mentions pharmaceuticals.
That's why I decided to write this article — to fill this glaring gap. Because apple cider vinegar and omega-3 fatty acids are good, but they are significantly less effective than medications.
There are not many drugs available to increase the body's sensitivity to insulin, but there are definitely some to choose from. The first one to mention is metformin — it can be called the most effective remedy.
Metformin deserves a separate article — it would be difficult to cover it in just two or three paragraphs. But I will try, providing only the basic information. So, metformin:
• primarily increases the sensitivity of muscle tissue to insulin
• slows down the absorption of glucose in the digestive tract, which means that it prevents blood sugar from rising too high even if you accidentally eat simple carbohydrates
• stimulates lipolysis, allowing you to get rid of fat deposits fairly quickly.
Metformin used to be prescribed only to patients with type 2 diabetes, but now it is commonly taken simply as a preventive measure — especially since this remarkable drug even helps to increase life expectancy.
Moxonidine, the active substance in Physiotens, comes in second place. However, the main purpose of moxonidine is not to increase insulin sensitivity — it is intended for the treatment of hypertension. This imposes restrictions on its use: moxonidine is definitely not suitable for people with normal or low blood pressure.
In third place is bromocriptine, a prolactin secretion inhibitor. Bromocriptine is capable of mimicking the action of the hormone leptin, which means it can help reduce insulin resistance. However, this drug is also not suitable for everyone: if your prolactin levels are within the normal range, it is best to avoid using bromocriptine.
The fourth worth mentioning is the anabolic steroid trenbolone. It significantly reduces the amount of visceral fat in the body, which also helps increase insulin sensitivity. However, anabolic steroids are not for everyone; trenbolone, in particular, is definitely not suitable for women.
Finally, there is growth hormone. It was previously believed that this drug even increases insulin resistance and contributes to the development of type 2 diabetes, but scientists later concluded that this is only true for high doses of synthetic somatotropin — 15-20 IU per day. However, if you do not exceed 15-20 IU per week, insulin sensitivity will actually increase.
That's about it. But before I go, I want to mention that I have a book called Insulin in Sports: A Comprehensive Guide. It contains a lot of interesting and useful information—not only about increasing insulin sensitivity, but also about how to make this wonderful hormone work for you, turning it into a reliable ally in your muscle-building efforts.

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