Clomid | Clomiphene Citrate
Reading time 12 min 22 sec
Before considering this drug, I would first like to discuss the theoretical basics, without which it would be difficult for an uninitiated person to understand the essence and significance of antiestrogens, why they are needed, how they work and generally the importance of the PCT moment.
Therefore, no matter how boring it would be for someone, but please, for your own good, read everything.
The first thing I would like to dwell on is aromatization.
Aromatization is the natural process of converting testosterone to estradiol. In other words, the main male hormone in the main female sex hormone.
After the course of AAS, estradiol often rises, and testosterone decreases and continues to decline. Hormonal balance almost completely switches to female hormones.
It is this situation that requires the use of antiestrogens, one of which is Clomid.
ATTENTION! The use of Clomid during the course of AAS is not required.
Estradiol, by the way, has a very significant effect on the body and can not be reduced below the reference values. Even despite the fact that he generally by nature should not be located by the logic of things in the male body.
It also cannot be greatly increased, even though its increase stimulates the processes of lowering cholesterol. This is a rather confusing process. This is described in more detail in the special literature, or it can be read about in our blog or in the following articles specially devoted to aromatization, since the topic is really big.
That is why you should never trust sources that state anything unambiguously. You must understand that AAS is a lottery. And the more random it is, the less you focus on analysis and observation of the body.
Before gaining muscle mass on a course of anabolic steroids, it is necessary to minimize body fat. This will help reduce the likelihood of side effects and keep estradiol at reference values for a long time. A set of muscle mass in the presence of excess fat increases the accumulation of this fat in direct proportion to the available.
Each person has a different number of receptors that can bind to estradiol. In this regard, we can observe a very diverse picture. One on Dbol Cycle develops gynecomastia in 3 weeks, while the other in 1.5 years of Testosterone injections does not even have a hint of it.
Actually, aromatization itself occurs in receptors that tend to act with estradiol, and this conversion in the male body occurs directly in the testes, adipose tissue, liver tissue, and even some bone tissues. Aromatization occurs in different ways for everyone and the side effects that we observe in one person, we will not observe in another. It is because of the different distribution of receptors that can interact with estradiol.
Thus, it turns out that the thicker the person is (see above, it also occurs in fatty tissues), the higher is the level of estradiol. And it turns out that the higher the level of estradiol in a man, the easier it will be to gain excess fat, and this is again an increase in estradiol. The circle closed, a so-called vicious bond formed. Thus, obesity occurs.
You probably paid attention to the fact that the more “flatter” a person is, the more difficult it is to gain excess fat, and vice versa, if a person already has excess fat, then he is very easily gaining it.
Well, for example, if you take a thin person weighing about 70 kg (taking into account growth) and a person of the same height, weighing 105 – 110 kg, with the same strength indicators, then a person who weighs 110 kg at 2,000 calories based on carbohydrates, it can gain excess weight since the metabolism is slowed down and the level of glucose, estradiol and excess body fat are increased. All this in a compartment can give an increase in extra fat.
And a person who conditionally weighs 70 kg, with his physique and metabolism, on the same 2000 cal. at the same load, it will lose weight.
That’s the whole difference. Here, mostly, the main role is played by estradiol and, of course, insulin. These processes are quite complex and very much interconnected.
Prolactin is one of the hormones of the anterior pituitary gland.
Pituitary gland is the main organ of the endocrine system in the brain. Responsible for the regulation and production of all major hormones.
ATTENTION! Prolactin, as in the cases with estradiol, should not be reduced at the first excess of the reference values during the course of anabolic steroids.
In the female body, prolactin is responsible for milk production during lactation, but not only it. Of course, progesterone, estradiol, etc. are also involved in this, that is, the entire line of female hormones is involved.
In the male body, prolactin stimulates the activation of testosterone production. He is responsible only for the start of testosterone production, that is, indirectly gives the command for its production.
Therefore, greatly increasing it, you risk earning all the side effects that it carries with it along with estradiol. Without estradiol, it rarely rises, although this is in principle possible. By the way, if it increases without estradiol, the risk of side effects is significantly reduced, because both estradiol and prolactin in the male body are more referents, complement each other, enhancing the effect of side effects, thereby squeezing the entire male androgen system.
Thus, prolactin cannot be reduced uncontrollably, because the command that is given by the brain of the anterior pituitary gland to testosterone production may be disrupted. Despite the fact that it is considered a rudimentary hormone, that is, one that should not be in the male body, but as we see it has a certain value.
Gonadotropic hormones are hormones of the anterior pituitary gland that are responsible for the hormonal functioning of the sex glands. Consider the main three:
FSH (Follicle-stimulating hormone) – in the male body stimulates the development of sperm formation and division of Leydig cells in which testosterone is formed.
In the female body, it stimulates the development of follicles in which the egg matures.
LH (Luteinizing hormone) – in the male body, it stimulates Leydig cells to produce testosterone.
In the female body, he is responsible for the maturation of the egg.
Therefore, we often note that it is necessary to pass tests for FSH and LH because they are almost always crushed on the course. This means that the arc that is responsible for the connection of the hypothalamus-pituitary – testicles is broken.
Hypothalamus is a small organ that is located in the so-called midbrain, which is responsible for all neuroendocrine connections and homeostasis.
Homeostasis – the constancy of the environment. Balance.
If any hormone “jumped”, then the concept of homeostasis is their alignment or attempts to align them if you continue to push your body with hormones.
HCG (Human Chorionic Hormone) is the gonadotropin hormone of the placenta, which is responsible in women for the course of processes during pregnancy.
It is produced not by the anterior pituitary, like the previous two, but by the placenta in women and men by the testes. In men, it is responsible for stimulating the entire system of the pituitary gland – the hypothalamus – testicles. The human chorionic hormone is a more correct name, and not gonadotropin, as it is often called since gonadotropins are a class consisting of these three main hormones.
Now, after a small educational program on the hormonal system, we finally can go directly to the drug itself.
CLOMIFENE CITRATE / CLOMID
The drug is a class of “Antiestrogens.”
It interacts with receptors that are on the cell wall in the hypothalamus and testicles, blocks the action of estradiol.
It acts on all of the above-reviewed connections, that is, on the restoration of the arc. So that the levels of FSH and LH would start working again as they had previously worked and stimulated the production of Testosterone.
A team at William S. Merrell Chemical Company led by Frank Palopoli synthesized clomifene in 1956; after its biological activity was confirmed a patent was filed and issued in November 1959. Scientists at Merrell had previously synthesized chlorotrianisene and ethamoxytriphetol.
Clinical studies were conducted under an Investigational New Drug Application; it was the third drug for which an IND had been filed under the 1962 Kefauver Harris Amendment to the Federal Food, Drug, and Cosmetic Act that had been passed in response to the thalidomide tragedy. It was approved for marketing in 1967 under the brand name Clomid. It was first used to treat cases of oligomenorrhea but was expanded to include treatment of anovulation when women undergoing treatment had higher than expected rates of pregnancy.
The drug is widely considered to have been a revolution in the treatment of female infertility, the beginning of the modern era of assisted reproductive technology, and the beginning of what in the words of Eli Y. Adashi was “the onset of the US multiple births epidemic”.
The company was acquired by Dow Chemical in 1980, and in 1989 Dow Chemical acquired 67 percent interest of Marion Laboratories, which was renamed, Marion Merrell Dow. In 1995 Hoechst AG acquired the pharmaceutical business of Marion Merrell Dow. Hoechst, in turn, became part of Aventis in 1999, and subsequently a part of Sanofi. It became the most widely prescribed drug for ovulation induction to reverse anovulation or oligoovulation. (from Wikipedia)
Clomifene produces N-desmethylclomifene, clomifenoxide (clomifene N-oxide), and 4-hydroxyclomifene as metabolites. Clomifene has an onset of action of 5 to 10 days following the course of treatment and an elimination half-life about 5 days. Most clomifene metabolism occurs hepatically, where it undergoes enterohepatic recirculation. Clomifene and its metabolites are excreted primarily through feces (42%), and excretion can occur up to 6 weeks after discontinuation. (Wikipedia)
Application. Clomiphene is used in the treatment of female / male (indirect) infertility, menstrual irregularities. Able to increase estrogen in women. Increase sperm count in men.
Clomifene is marketed under many brand names worldwide, including Beclom, Bemot, Biogen, Blesifen, Chloramiphene, Clofert, Clomene, ClomHEXAL, Clomi, Clomid, Clomidac, Clomifen, Clomifencitrat, Clomifene, Clomifène, Clomifene citrate, Clomifeni citras, Clomifeno, Clomifert, Clomihexal, Clomiphen, Clomiphene, Clomiphene Citrate, Cloninn, Clostil, Clostilbegyt, Clovertil, Clovul, Dipthen, Dufine, Duinum, Fensipros, Fertab, Fertec, Fertex, Ferticlo, Fertil, Fertilan, Fertilphen, Fertin, Fertomid, Ferton, Fertotab, Fertyl, Fetrop, Folistim, Genoclom, Genozym, Hete, I-Clom, Ikaclomin, Klofit, Klomen, Klomifen, Lomifen, MER 41, Milophene, Ofertil, Omifin, Ova-mit, Ovamit, Ovinum, Ovipreg, Ovofar, Ovuclon, Ovulet, Pergotime, Pinfetil, Profertil, Prolifen, Provula, Reomen, Serofene, Serophene, Serpafar, Serpafar, Surole, Tocofeno, and Zimaquin. (Wikipedia)
The properties of Clomid and why it is used in sports.
After the start of taking AAS, FSH and LH are inhibited to one degree or another and prevent the further production of testosterone, which entails several side effects, such as aromatization.
Clomid is designed to contribute to the stimulation of gonadotropins, thereby stimulating the production of own testosterone, that is, restoring the arch of the pituitary gland – the hypothalamus – testicles. This is the same arc that we need to restore to whatever it gets up and as soon as possible immediately after finishing the course.
But, there is one interesting point about which few speak and write. Everyone is promoting Clomid as a wonderful tool, less dangerous and harmful than Tamoxifen. So, the so-called inhibition function of one’s own Testosterone, the inhibition function of gonadotropic hormones, is inherent in it. It occurs when the dosage of Clomid is exceeded, because you can not determine the amount of your estrogen receptors. Accordingly, for one person 50 mg of Clomid per day can serve as a full-fledged restoration of his arch, and for another person, such a dosage can inhibit his restoration of gonadotropin and delay the restoration of the reproductive system for long weeks.
That is why, there is such a tendency that PCT with the use of antiestrogens – not to do. And there is some truth in this, there is a certain logic.
ATTENTION! Clomid is capable of both restoring the secretion of gonadotropic hormones and inhibiting it. Which can delay your recovery and essentially extend the course.
Therefore, we kindly ask you to listen to our opinion and only by the results of analyzes, determine how much you need to use Clomid. Because if your FSH and LH are not significantly suppressed after a course of “working pharmacology”, and it should be working, to inhibit the levels of gonadotropic hormones, then, in this case, you should not use Clomid.
To prescribe it to everyone in a row, as most coaches do, who do not understand the essence of the processes taking place in the body and the subtleties of the hormonal system that we talked about above, working with estrogens is completely not logical and not right, as this can cause irreparable harm to health.
Before switching to PCT, it is necessary to take tests. Analyzes should be as follows:
Minimum list of analysis before applying CLOMID to the PCT:
- free testosterone;
- globulin binding sex hormones;
- estradiol and prolactin (optional).
This is the foundation of what helps you identify and choose the right PCT. Analyzes must be taken 1-2 weeks before the end of the course, so that you have time to purchase the necessary drugs during this time, as well as draw up schemes according to which you will take them or not.
ATTENTION! With significantly reduced levels of FSH, LH, free testosterone, increased SHBG, 25 mg is taken of Clomid per day before bedtime. After 10 to 12 days, the tests should be repeated.
The next property that Clomid possesses is a decrease in the level of estradiol and prolactin. These 2 hormones are mutually related. There can be no lactation from prolactin without exposure to estradiol. In other words, if, for example, you have increased prolactin, and estradiol is normal or slightly higher than referents, there may not be any formation of gynecomastia. Therefore, do not worry too much if a single value jumped. (By the way, prolactin gets off easier and is easier to act on than it is on estradiol).
The biggest side effect (IMHO) is recovery.
Therefore, if, according to the analysis of the tests, you do not need Clomid, then you do not need to use it. Accordingly, it is necessary to do tests on time to avoid the suppression of their hormones. Do not use dosages of 100 to 150 mg per day on an ongoing basis. Yes, you can 100 mg in the first 3 -5 days, as in the diagram, and then go on 50 and 25 mg, and if you have an arch pituitary- hypothalamus-testicles.
1 – 5 day:
Clomid 100 mg. + Zincteral 3 tabs + Vitamin C – 1000 mg. + Aevit 4 tabs + Yohimbine 10 mg.
6 – 15 day:
Clomid 50 mg. + Zincteral 3 tabs + Vitamin C – 2500 mg. + Aevit 3 tabs + Yohimbine 5 mg.
16 – 25 day:
Clomid 25 mg + Zincteral 2 tabs + Vitamin C – 3000 mg.
ATTENTION! This PCT scheme was compiled for a client who provided the results of his work on diet and analysis.
It is not recommended to test it in your courses without knowledge of the details.
It is not universal and is not suitable for everyone. This is an example of a specific scheme that has been applied to a specific person.
In our opinion, the main side effect, it is also the worst. Because, after sitting on the course for half a year and restoring your arc in 20 days, you might think that you have restored it, but in fact, you will delay the restoration, and there the next course is on its way, but you haven’t recovered from the previous one. And without passing tests before the course, as many do, you will begin a new course with an unrestored hormonal system after the previous one. And this is a direct path to infertility.
It is because of those people who are irresponsible to their health, who do not control the processes that need to be controlled and legends and myths that steroids cause impotence and infertility go.
The following side effects, which are presented in the table below, are individual and, unlike the above, may not occur in all.
- headaches of a migraine type;
- violation of libido;
- subjective feeling of heaviness in the testicles;
- “prostate tremor”;
- dry lips (in the morning);
- drying of the mucous membranes;
- violation of the heart rhythm;
- impaired renal activity;
ATTENTION! Side effects are not limited to this table. All that is not included in it, practically do not appear.
For the first time, libido can be suppressed, as some hormones have already recovered, while others have not yet recovered. When estradiol begins to decline, at this point the balance of Testosterone – estradiol can be completely disturbed. Testosterone is suppressed, estradiol levels begin to fall, exogenous testosterone also begins to fall, and against this background, libido also begins to decline. Therefore, for about 4 to 5 weeks from the start of PCT, there is a tendency for a drop/increase in libido. This happens quite often.
All other side effects do not occur in everyone, they do not always occur and may not occur at all.
When using oral steroids, in most cases, Clomid is not needed. It also happens that some “athletes” will use Stanozolol for 6 weeks, and then begin PCT with Clomid. With this unprofessional approach, various troubles can begin. Therefore, it is always necessary to take tests.
Clomid can suppress the production of gonadotropic hormones (FSH and LH), therefore, without fail, to be sure whether to use it or not, it is necessary to take tests.
Clomid is not required after courses of oral AAS for 2 – 2.5 months. Moreover, it is not required after courses for 4 weeks.
Clomid should be taken only after long courses of oral preparations, if the arc is crushed and then no more than 25 days. If more, then this can play against you. An arc may begin to oppress. In other words, 25 days, this is the time during which you give an incentive to the pituitary gland to produce your own Testosterone, to normalize gonadotropic hormones. Further, you can stimulate with yohimbine, zinc preparations, etc.
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