The drug appeared in the 80s and has been a leader in the sports medicine market since then. In our market it is sold under such trade names as “Bergolak”, “Dostinex” and from Fominsky Pharm. enterprises. The most popular brand is Dostinex. There are many analogues of this drug. Italy, in addition to Dostinex, offers the cheaper Cabaser. The Czech Republic produces Agaltex and Alakting. The medicine can be produced in dosages of 0.25 g, 0.5 g and 1 g. Its effect is identical and does not depend on the brand and price.
A brief history of the creation of Cabergoline
The drug was developed in the eighties by the American company Pharmacia.
It is produced in many countries around the world and is also known as Dostinex. It was under this name that the drug was first registered and the developer company has patent rights to it. Cabergoline is a very common medication and is used in many countries around the world. Despite the fact that the rights to the Dostinex trademark still belong to Pharmacia. It is under this name that it is most often sold. However, the drug has a lot of names and, for example, in Russia it is also known as agalates and bergolak. It is quite obvious that the original drug has a higher cost compared to domestic analogues.
Pharmacological effects of Cabergoline
As we have already said, cabergoline is a dopamine-type receptor agonist.
The active component of the drug is a dopaminergic substance derived from ergoline. This indicates that it has strong prolactin-lowering activity. The mechanism of action of the drug is associated with the ability to act on dopamine type D2 receptors. Using the drug in doses exceeding therapeutic doses can reduce prolactin concentrations and also achieve a strong dopaminergic effect. Prolactin levels begin to fall within three hours from the moment of using the drug and are maintained at the required level for one to four weeks.
This applies to people who do not have pathologies, as well as women with hyperprolactomy. After childbirth, the drug is able to maintain the required level of prolactin for two to three weeks. In many ways, the prolactin-lowering properties of the drug depend on the dosage used, which also affects the duration of the dopamine mimetic.
It is important to note that Dostinex works selectively and is not able to influence the production of other hormones synthesized by the pituitary gland, including cortisol. The drug has, among other things, several effects that are not closely related to the therapeutic effect. Among them, we note the ability to reduce blood pressure. Approximately six hours after use, the hypotensive effect begins to appear, and its strength depends directly on the dosages used.
Ways to suppress aromatization
We will not pay much attention to this section, but we will briefly go over the most popular drugs and methods.
Clomid acts on estrogen receptors in the pituitary gland and ovaries. Binds estrogen receptors in the pituitary gland. Clomid breaks the negative feedback mechanism, that is, if usually estrogens, acting on the pituitary gland, reduce the production of FSH and LH by the latter, then this does not happen when taking Clomid. Clomid does not affect the level of estrogen in the blood itself, nor does it affect the level of estrogen in the blood, since its mechanism of action comes down to blockade of different types of estrogen receptors, including in the pituitary gland. Quite a toxic drug. Tamoxifen also increases the number of progesterone receptors.
Aromatase inhibitors (letrozole, anastrozole, exemestane) are a class of medications designed primarily to reduce the concentration of estrogen in the blood. Unlike tamoxifen and Clomid, it does not block estrogen receptors and acts directly on aromatization, suppressing it. It is also used to increase the level of your own testosterone and gonadotropic hormones.
Reducing the amount of adipose tissue . Do not neglect the condition of having a large or moderately large amount of subcutaneous fat. After all, the more obese the person, the stronger the aromatization. Reducing the percentage of subcutaneous fat will significantly reduce aromatization. Also, as a rule, on low-carbohydrate/no-carbohydrate diets, there is a decrease in the conversion of testosterone to estradiol.
Cabergoline in bodybuilding: positive properties
The drug is a selective agonist of dopamine-type receptors and at the same time works quite specifically.
It should be noted that it is highly similar to D2 receptors, but the drug interacts weakly with adrenergic (alpha-1 and alpha-2) and serotonin (5-HT1, 5-HT2) receptors. For therapeutic purposes, this drug is used in the treatment of hyperprolactinemia, hypersecretion of the hormone prolactin by the pituitary gland, as well as Parkinson's disease. The drug has a high ability to inhibit prolactin synthesis and it is for this reason that cabergoline is very popular in bodybuilding. At the same time, the drug interacts with D2 receptors. Thus, dopamine becomes a negative feedback for the release of prolactin.
We have already said that an important feature of the drug is its inability to influence the processes of synthesis of other hormonal substances synthesized by the cellular structures of the pituitary gland - corticotropin, somatotropin, luteinizing, and thyroid-stimulating hormones.
Prolactin is a representative of the same group of hormones as somatotropin. This is a single-peptide substance whose molecule contains 199 amines. Although its size is slightly larger than that of growth hormone, prolactin is in many ways similar to somatotropin. However, as soon as the conversation turns to the structure of these substances, all similarities immediately disappear.
Prolactin is not capable of exhibiting anabolic properties, but is intended to stimulate lactation processes. This fact suggests that Dostinex is very important for women because of its physiological properties. This is most noticeable during pregnancy, because it allows you to speed up the production of mother's milk. The drug can also be used in the postpartum period during hypersynthesis of milk to suppress this process.
At the moment, scientists do not know the therapeutic value of prolactin in relation to the male body. It has been established that a high concentration of this hormonal substance can cause the development of impotence, infertility and gynecomastia. However, the debate between scientists about the last property of prolactin does not stop, and not all of them believe that this is possible.
Gynecomastia is quite rare in ordinary men, but not uncommon in AAS users. This is one of the reasons why cabergoline is a big success in bodybuilding. Note that lactation gynecomastia is accompanied by the release of a small amount of fluid when the nipple is compressed. This disease has the ability to accumulate, and many athletes know this fact. At the first signs of the development of gynecomastia, they make appropriate adjustments to their course of anabolic steroids.
Lactational gynecomastia is poorly studied and the cause of its development is considered to be an imbalance between prolactin, estrogens and androgens. The disease can also be a consequence of genetic predisposition. To avoid all these troubles, it is necessary to use cabergoline in bodybuilding.
If we analyze specialized web resources, athletes rarely remember the increased concentration of prolactin. At the same time, the need to use Dostinex depends on this. It has been established that estrogens stimulate the growth of prolactin levels and this is probably the main reason for the development of lactational gynecomastia.
But there are research results that eloquently speak about the inhibitory ability of some hormones in relation to prolactin, for example, androgens. This gives us reason to say that not only an increase in estrogen levels is the main reason for the development of lactational gynecomastia.
To date, little research has been carried out in this direction. Actually, there is nothing to be surprised here, because this disease almost always occurs only in athletes who actively use steroids. In ordinary men, the disease is diagnosed extremely rarely.
However, we did find results from one experiment that examined the effects of two testosterone esters (propionate and enanthate) on prolactin concentrations. A significant increase in the concentration of this female hormone was observed already on the fourth day of the course. In the second experiment, a sevenfold increase in hormone levels was noted after using AAS. As a result, prolactin levels reached almost those levels that are typical for the female body.
Flavoring
Under the influence of the aromatase enzyme, testosterone is able to convert into estradiol, hence the process called aromatization. Interestingly, the molecules of testosterone and estradiol differ only slightly, namely in the absence of one methyl group and several hydrogen atoms. In the male body, estradiol is a derivative of testosterone. This means that, as a rule, increased estradiol is a consequence of increased testosterone, excluding individual special cases, which are not the rule.
In excess amounts, estradiol harms a man, turning him into a woman.
Let's figure out what estradiol is and why we need it. Estradiol, as we defined at the beginning, belongs to the group of female sex hormones, estrogens. This hormonal substance in a man’s body performs a number of important functions, for example: active participation in the process of ejaculate secretion, improving oxygen metabolism, regulating the functioning of the nervous system, increasing blood clotting, stimulating metabolism, etc. It is believed that in excess quantities the hormone can lead to to such side effects as female-type fat deposition, nervousness, decreased libido and erectile dysfunction, gynecomastia, etc. In other words, to simplify, we can say that in excess estradiol harms a man, turning him into a woman.
Testosterone norm for men Estradiol (E2) 3–70 pg/ml
So, we found out that excess and deficiency of estradiol are harmful, a golden mean is necessary.
Instructions for using Cabergoline in bodybuilding?
In medical practice, the drug is used by men to suppress the production of prolactin in an amount of 0.5 grams per week.
The dosage can be used at once or divided into two or more doses. You can also increase the frequency of using Dostinex to get better results, using 0.5 grams every third or fourth day. Cabergoline in bodybuilding is used during AAS courses, which include steroids with progestogenic activity (trenbolones, oxymetholone or trenbolone). The dosage is 0.25 grams every third day. The duration of the Dostinex course is one month, after which it is used as needed.
There are known cases where the drug was used by men to achieve multiple orgasms during sexual intercourse. This fact can be explained by the high rate of dopamine synthesis during sex. After the body, there is a strong release of prolactin and all accumulated dopamine is neutralized. This fact is related to the fact that after the body the sexual arousal of men quickly disappears. If you use Dostinex to block the production of prolactin, then multiple orgasms become a reality. Athletes do not use cabergoline.
Main goals of post-cycle therapy
Androgenic anabolic steroids (AAS) place a lot of stress on the hormonal system. These are generally very capricious comrades. After taking them, the goals are:
- establish a healthy hormonal balance;
- reduce rebound and maintain the maximum of gained muscle mass;
- prevent the appearance of effeminate breasts in men;
- save the testicles from “drying out”;
- return sexual activity;
- improve blood composition;
- protect the liver and avoid the occurrence of liver diseases;
- lower the level of the hormone cortisol.
Therefore, never give up on PCT. After steroids, she is needed like air.
Reduce muscle loss on PCT
We already wrote above that the muscles begin to break down at the end of the course. They may suffer greatly or only slightly. It is clear that any muscleman wants to keep his “guns”.
To do this, it is imperative to restore testosterone levels. PCT preparations include various components that enhance the production of male sex hormones. By taking them, you can defeat the laws of physiology
.
Restoring hormone balance
Your own testosterone does not begin to be produced until the amount received from outside is reduced to a minimum. It will not be possible to ensure the natural production of the hormone right away - you need to wait until the reserves of the artificial one run out. Here you will have to delve into the concept of “decay period”. Some steroid supplements disintegrate quickly, while with others you have to wait two or even three weeks.
Prolactin and estradiol also put a spoke in the wheels of testosterone. It happens that their concentration on the course increases sharply. Until they decrease, normal testosterone production will not be restored. PCT drugs make it possible to put everything in its place.
What side effects are possible when using Cabergoline?
In sports, the drug is considered safe, although it has some side effects.
The most common symptoms reported in the studies were headache (26 percent), nausea (27 percent), and vomiting. The latter negative effect was recorded in only two percent of subjects. It should also be noted that other side effects are possible, but they are extremely unlikely. All negative properties of Dostinex are directly related to the dosages used. This suggests that you should start taking the drug with a minimum dose and increase it if necessary.
Reasons for increasing the amount of prolactin in the body
Before considering the benefits of taking cabergoline, you should understand the reasons for the increase in prolactin.
They can be divided into two categories: related or not related to taking drugs for athletes.
Let's start with the reasons not related to taking steroids:
- diseases of the pituitary gland and hypothalamus;
- thyroid problems;
- kidney disease;
- liver diseases;
- lupus erythematosus, arthritis and other autoimmune diseases;
- low content of vitamin B6 in the body;
- a large amount of progesterone, estradiol;
- frequent stress.
It should be noted that due to the presence of congenital diseases, an increase in prolactin is not observed .
Among bodybuilders, the cause of such problems, in most cases, is illiterate use of steroids.
Indications and contraindications for the use of Cabergoline
If we talk about sports, the drug is primarily used to suppress the progestogenic activity of several AAS.
In medicine, the drug is indicated for use by women to treat certain diseases. Although the drug is considered safe, because when used in recommended dosages the risk of side effects is low, there are some contraindications to its use. We are talking about persons under 16 years of age whose body is highly sensitive to any ingredient of the drug. You should also be careful in using it if you have certain ailments. More details about Cabergoline and its use in the following video:
