Cabergoline

$75 $69
Cabergoline is a derivative of ergot. It acts as a dopamine receptor agonist, characterized by its strength, longevity, and selectivity, with high affinity for the D2 receptor. Its effects and clinica

Performance

antiprolactin：

★★★★★

Muscle Gain：

★★★★★

Reduce Fat/Water：

★★★★★

Side Effects：

★★★★★

Sustained Effects：

★★★★★

SKU：

0.5mg/tablet × 8 tablets/bottle

Package：

capsule

Appearance：

oral

Dosage：

0.5–1 mg/week

Cycle：

Throughout the cycle

    Introduction:

Cabergoline is a selective dopamine receptor agonist with a highly specific action, possessing strong affinity for dopamine D2 receptors and lower affinity for serotonin 5-HT2 receptors. Its primary clinical use is to treat hyperprolactinemia, or symptoms of excessive anterior pituitary prolactin secretion (commonly caused by pituitary tumors). It is also used in treating Parkinson's disease. By mimicking the action of dopamine on D2 receptors, cabergoline effectively inhibits prolactin secretion (dopamine acts as a negative feedback for prolactin release). As a targeted dopamine D2 receptor agonist, cabergoline does not affect other pituitary hormones such as growth hormone (GH), luteinizing hormone (LH), adrenocorticotropic hormone (ACTH), or thyroid-stimulating hormone (TSH).


Prolactin is a growth hormone, of the same class as human growth hormone (GH). It is a single peptide hormone composed of 199 amino acid chains, which makes its structure similar to (although slightly larger than) growth hormone, which is composed of 192 amino acids. However, any similarity between these two hormones ends at their structure. Prolactin is not an anabolic steroid (at least not for skeletal muscle) but rather a lactogenic hormone. Its primary physiological value is in females, becoming more evident during pregnancy, as it aids in lactation. If there is a specific medical need, cabergoline is used to inhibit postpartum lactation. In males, the therapeutic value of prolactin, such as whether high levels of prolactin are related to impotence, infertility, or sometimes even gynecomastia, is still unknown (whether it has a pathogenic effect remains a topic of much debate).


Although prolactin has almost no association with males, in reality, high levels of prolactin are associated with galactorrhea in gynecomastia in athletes using steroids, though this is a very small proportion. The characteristic of this disease becomes more evident through the discharge of a small amount of fluid from the nipples when pressed. Although the situation may worsen, the first signs are often enough to deter these athletes from their current steroid regimen. Male breast development is not automatically (or typically) associated with lactation, making this a rare phenomenon. It may be caused by an abnormal hormone imbalance (androgens, estrogens, and progestogens can all participate and play different roles), or it may be due to specific individual sensitivity to this disease. However, when it does occur, cabergoline has been used as a remedy for this potentially embarrassing situation.


In athletes using steroids, there are no regular records of high prolactin levels (related to the need for cabergoline), further illustrating the relatively rare nature of this disease. We know that estrogen plays a stimulating role here, and it is likely the key to the increase in male prolactin secretion. However, other studies suggest that other hormones, including androgens, also have a suppressive effect on prolactin. This might explain why hormonal dysregulation leads to lactating male gynecomastia, rather than high estrogen alone. Consultation with medical literature reveals only a few studies on prolactin levels and steroid use, with few definitive conclusions. One study analyzed the effects of testosterone and its esters on men, noting a significant increase in prolactin four days after injection. Another study noted that in five athletes, estrogen increased by seven times (typical for females), but had no consistent effect on prolactin secretion. A third study on athlete self-administration and a fourth clinical study with nandrolone failed to show an increase in prolactin levels.


History:

Cabergoline was developed in the 1980s. The most popular brand name for this drug is Dostinex, produced by the pharmaceutical giant Pharmacia in the United States and many other countries. Dostinex monopolized the U.S. market for cabergoline for many years, but between 2005 and 2007, the FDA approved several generic versions, including those from Barr, Ivax, and Par Pharm. Cabergoline is widely used internationally and can be found in over thirty countries. Outside the United States, the Dostinex brand still dominates, available in Argentina, Australia, Austria, Belgium, Brazil, Canada, Chile, the Czech Republic, Denmark, Finland, France, Germany, Greece, Hong Kong, Ireland, Israel, Italy, Malaysia, Mexico, the Netherlands, Norway, New Zealand, Poland, Portugal, Russia, South Africa, Singapore, Spain, Sweden, Switzerland, Turkey, the United Kingdom, and Venezuela. In addition to Dostinex, cabergoline is available under at least a dozen other brand names.


Specifications Offered:

Cabergoline is most commonly available in 500 mcg tablets.


Structural Characteristics:

Cabergoline is an ergot derivative, chemically named as 1-[(6-allylergoline-8-yl)carbonyl]-1-[3-(dimethylamino)propyl]-3-ethylurea.


Side Effects:

The most common side effects of cabergoline include headaches, nausea, and vomiting, which occurred in 26%, 27%, and 2% of patients, respectively, during a clinical trial. Other potential side effects include (but are not limited to) constipation, dry mouth, abdominal pain, diarrhea, dizziness, fatigue, anxiety, anorexia, discomfort, depression, insomnia, hot flashes, palpitations, low blood pressure, breast pain, and acne, with nausea and headaches being the most prominent side effects. Many side effects are dose-related, further warranting the reason for starting at the lowest therapeutic dose. Prescription information does not mention death as an apparent consequence of overdose, but it does list hallucinations, low blood pressure, and nasal congestion. Note that patients who overdose may need to take measures to increase their blood pressure.


Usage Guidelines:

In medical settings, cabergoline is administered at an initial dose of 500 mcg per week to suppress prolactin secretion. This can be taken in a single dose or split into two or more doses on different days. The dose can be increased by 500 mcg weekly at monthly intervals until the desired physiological response is reached. The dose is typically maintained at 1 mg per week, although doses as high as 4.5 mg may be used in some cases. When athletes/bodybuilders use it to suppress prolactin secretion (e.g., for lactating male gynecomastia), the lower end of the therapeutic range is most commonly used. Patients typically take one dose (half a tablet) of 250 mcg twice per week. This is the dosage for the first four weeks, at which point, if necessary, the dose can be adjusted upwards to a full tablet (1 mg per week). In clinical medicine, the drug may be taken for 6 months or longer, although athletes/bodybuilders find that a 4-6 week treatment regimen is most appropriate (combined with intelligent cycling of toxic drugs).

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