Profile (History, Chemical Structure, Characteristics) 

History

Cabergoline was developed in the 1980s. The most popular brand name drug - Dostinex, produced in the United States and many other countries by the world pharmaceutical giant Pharmacia. Dostinex has retained exclusive rights on the marketing of cabergoline in the U.S. for many years, but between 2005 and 2007, the FDA approved several universal versions for the sale, including products of companies Barr, Ivax and Par Pharm.

Chemical structure

  • Cabergoline - ergotamine derivative with the chemical formula 1 - [(6-beta allilergolin-8-yl) carbonyl] -1- [3- (dimethyl amino) propyl] -3-etilurea.
  • The main mechanism of cabergoline action is the activation of D2 receptors that are located on lactophrys pituitary cells. Stimulation of the dopamine receptors in this area leads to a decrease in the secretory function of cells, which are producing prolactin.
  • In addition, it was found interaction with other receptors: D3, D4, 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, α2B. Antagonism with α2B receptors further explains the positive effect on erectile function (the process of expanding corpus cavernosum).

Effects

When the men have low prolactin level.

Low prolactin together with high level of testosterone gives strong confidence in themselves and in their abilities, make a person completely polygamous, unable to compromise and make concessions. Low level of prolactin makes a man more stable mentally, independent of public opinion. Also, the recovery time between sexual acts significantly reduced and generally sexual life improves. Low Prolactin also influences the genital organs enlargement, particularly the testicles and penis.

Side effects

A research, during which 200 patients with Parkinson's disease took high doses of cabergoline (0.5 mg daily) reported the following side effects:

 

  • Digestive system (most often): nausea, constipation, dry mouth, dyspepsia
  • Nervous system: insomnia, dizziness, depression, distorted consciousness
  • Cardiovascular system: drop in blood pressure, peripheral edema, rhythm disturbance, valves damage, pericarditis
  • Immune system: rarely - hypersensitivity reactions, skin rashes.
  • Hematopoietic system: Infrequent - rodonalgia.
  • Respiratory system: often - shortness of breath, rarely - pleural effusion, lung fibrosis, nasal bleeding.

 

If you are using low doses side effects are rare. People most commonly report about depressed mood and loss of appetite.

Dosages and Uses

Dosage: 0.25 mg

The frequency of dosing: every 4th (the best rate), or every 2nd day (intensive course)

To suppress prolactin the drug is taken in a dose of 500mkg weekly by dividing it into one or more doses for a week. The dose can be increased up to 1 mg per week, in some cases up to 4.5mg. Therapy lasts 4-6 weeks after the course.

Cycles (Courses)

Using experience showed that the optimal scheme of cabergoline use to decrease prolactin is constructed as follows:

  • During the course of progestin anabolic steroids (nandrolone, trenbolone): 0.25 mg (half or whole tablet) is taken every 7-21 days, beginning with the third or fourth week of the course, when the concentration of the ACC is close to the maximum. The optimal dose and frequency of using are chosen according to the examination of prolactin level, as far as the effect of the drug varies depending on the individual features of the organism.
  • When the  prolactin level is above the allowable measure, the frequency of use increases: 0.25 mg every 4 day. Comparison examination of prolactin is desirable to do after two doses with the following correction schemes.

The drug is advisable to be taken with food, the time of the day does not matter. The appointment is made only under medical supervision.

In bodybuilding, it is most often used with courses in which there are nandrolones or trenbolone. Classic regimen: 0.25 mg every 4 day if prolactin level is high, then take 0.25 mg every 2 days until it will no longer need it, then again use the first option until the end of the course. In the course of these steroids cabergoline, among other things, will also help to remove the swelling of the face and muscles. The most common form of cabergoline in bodybuilding is dostineks.

It is also practiced to use cabergoline in bodybuilding without a progestin activity, to get better results from the course and improve the quality of life. Then take 0.5 mg once per 10 days.

Also, athletes take cabergoline if they want to increase their activities without resorting to AAS, in this case, of course, the dosage will be much less.