Find out why bodybuilders use Cabergoline on an ongoing basis after a course of steroids and what benefits and dangers this unusual drug hides. Cabergoline belongs to the class of medications called dopamine mimetics. It is able to interact with dopamine-type receptors located in the pituitary gland. This leads to a significant suppression of the production of the hormone prolactin. In medicine, the agent is used during the treatment of a disease such as hyperprolactinemia. Cabergoline is also actively used in bodybuilding.
In addition, cabergoline can be effective for menstrual irregularities, galactorrhea, low sex drive, impotence. It is also used to prevent the suppression of the lactation process. In addition to the ability to interact with dopamine-type receptors, Cabergoline is a weak agonist of alpha-1 and alpha-2 adrenergic receptors.
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 for it.
Cabergoline is a very common drug 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 bergolac. It is quite obvious that the original drug has a higher cost in comparison with domestic counterparts.
Pharmacological effects of Cabergoline
As we said, cabergoline is a dopamine-type receptor agonist. The active ingredient of the drug is a dopaminergic substance derived from ergoline. This indicates that he has a strong prolactin-lowering activity. The mechanism of work of the drug is associated with the ability to act on dopamine receptors of the D2 type.
The use of the drug in doses exceeding therapeutic ones, allows you to reduce the concentration of prolactin, as well as achieve a strong dopaminergic effect. The prolactin level begins to fall within three hours from the moment of using the drug and is maintained at the required level for one to four weeks.
This applies to people without 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 respects, 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. After about six hours from the moment of application, the hypotensive effect begins to manifest itself, and its strength depends directly on the dosages used.
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 its high similarity with 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 agent is used in the treatment of hyperprolactinemia, hypersecretion of the hormone prolactin by the pituitary gland, as well as in 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 agent interacts with the D2 receptors. Thus, dopamine becomes negative feedback for prolactin release.
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, growth hormone, luteinizing, and thyroid stimulating hormones.
Prolactin is a member of the same group of hormones as growth hormone. It is a one-peptide substance, the molecule of which contains 199 amines. Although its size is slightly higher than that of growth hormone, prolactin is in many ways similar to growth hormone. 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 processes of breast milk production. The drug can also be used in the postpartum period with milk hypersynthesis 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, disputes between scientists about the last property of prolactin do 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 cabergoline is so popular in bodybuilding. Note that lactational gynecomastia is accompanied by the release of a small amount of fluid when the nipple is compressed. This ailment has the ability to accumulate, and this fact is known to many athletes. At the first signs of the development of gynecomastia, they make appropriate adjustments to their course of anabolic steroids.
Lactational gynecomastia is poorly understood and the reason for its development is considered to be an imbalance between prolactin, estrogens and androgens. Also, the disease can be the result of a genetic predisposition. To avoid all these troubles, it is necessary to use cabergoline in bodybuilding.
If you analyze the profile web resources, then athletes rarely remember an 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 speak eloquently about the inhibitory ability of some hormones against prolactin, for example, androgens. This gives us a reason to say that not only the increase in estrogen levels is the main reason for the development of lactational gynecomastia.
To date, quite a few studies have been carried out in this direction. Actually, there is nothing to be surprised at, because this ailment is almost always found only in athletes who actively use steroids. In ordinary men, the disease is rarely diagnosed.
However, we found the results of one experiment that investigated the effect of two testosterone esters (propionate and enanthate) on prolactin concentration. 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, the level of prolactin has reached almost those levels that are characteristic of the female body.
How to use 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 a time or divided into two or more doses. You can also increase the frequency of use of Dostinex for better results by applying 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 cases when the drug was used by men to achieve multiple orgasms during intercourse. This fact can be explained by the high rate of dopamine synthesis during sex. After the body, a strong release of prolactin is observed and all the accumulated dopamine is neutralized. This fact is related to the fact that after the body, the sexual arousal of men quickly disappears. If you block prolactin production with dostinex, then multiple orgasms become a reality. Sportswomen do not use cabergoline.
What side effects are possible when using Cabergoline?
In sports, the drug is considered safe, although some side effects are inherent in it. Headache (26 percent), nausea (27 percent), and vomiting were most common in the studies. The latter negative effect was recorded in only two percent of the subjects.
It should also be noted that other side effects are possible, but their manifestation is extremely unlikely. All the 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, if necessary, increase it.
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 for the treatment of certain diseases. Although the drug is considered safe, because when it is used in the recommended dosages, the risk of side effects is small, there are some contraindications to its use. We are talking about persons under 16 years of age, high sensitivity of the body to any ingredient of the drug. You should also be careful in its use in the presence of certain ailments.
More details about Cabergoline and its use in the following video:
