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Cabergoline (active ingredient) – suppresses the secretion of prolactin, in addition increases libido and erection, significantly reduces the recovery time between sexual acts, and lowers blood pressure. Cabergoline refers to the derivatives of ergot alkaloids, the mechanism of action is an agonist of dopamine (D2) receptors. It is a more modern and safe analogue of bromocriptine.
The drug can almost completely eliminate the main side effects of such steroids as Deca (deca-dick) and Trenbolone. One of the effects caused by a decrease in prolactin concentration is a decrease in fluid retention in tissues, which gives an increase in more dry muscle mass.
Developed cabergoline in the 80’s. Produced in the US and many countries around the world by the giant company Pharmacia, widely known as Dostinex (Dostinex). It still has original rights to marketing cabergoline in the US for a long time, despite this, in 2005-2007, the FDA approved for sale several universal versions, including products of Barr, Ivax and Par Pharm. Cabergoline in tablets is very common in the world market, it can be purchased in more than 30 countries. It should be noted that even outside the US borders, the Dostinex brand continues to lead in many markets, it can be found in such countries as Argentina, Australia, Austria, Belgium, Brazil, Canada, Chile, Czech Republic, Denmark, Finland, France, Germany, Greece , Hong Kong, Ireland, Israel, Italy, Malaysia, Mexico, Netherlands, Norway, New Zealand, Poland, Portugal, Russia, South Africa, Singapore, Spain, Sweden, Switzerland, Turkey, United Kingdom and Venezuela. Cabergoline has a lot of names (more than 10) (in Russia it is known as Bergolak and Agalates, the American analogue is more expensive than the domestic one).
Mechanism of action
The main mechanism of action of cabergoline is the activation of D2 receptors, which are located on the lactotrophic cells of the pituitary gland. The excitation of dopamine receptors in this region leads to a decrease in the secretory function of cells that produce prolactin.
In addition, interaction with other receptors has been established: D3, D4, 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, α2B. Antagonism with α2B receptors further explains the positive effect on erectile function (expansion of cavernous bodies occurs).
The experience of application showed that the optimal scheme of application of cabergoline for the decrease of prolactin is constructed as follows:
During the course of progestin anabolic steroids (nandrolone, trenbolone): 0.25 mg (whole or 1/2 tab.) Every 7-21 days, starting from the third or fourth week of the course, when the ACC concentration approaches the maximum. The optimal dose and frequency of reception is selected under the control of prolactin levels, because the effect of the drug is different and depends on the individual characteristics of the organism.
With an increase in the level of prolactin above the allowable frequency of reception increases: 0.25 mg, every 4 days. It is desirable to perform a control analysis of prolactin after two procedures with subsequent correction of the regimen.
The drug is taken with food, and on an empty stomach.
Admission (for men)
In medicine, in order to inhibit the secretion of prolactin, cabergoline tablets are recommended first 500 μg per 7 days. The dose can be taken as at one time, and divided into two, or more. It can also be increased to 500 μg in 3-4 days in order to achieve the desired physiological response. The most common dose is 1 mg in 7 days, but sometimes it is fashionable to use 4.5 mg. When taking the drug by athletes in order to suppress prolactin release (as well as in the case of lactating gynecomastia), doses of the lower level of the therapeutic range are most often taken. The athlete usually starts with a dose of 250 micrograms per meal (1/2 tablet) twice per 7 days. The drug is taken for a month, then, if necessary, the dose can be increased to 1 mg per week. In clinical medicine, the drug can be taken for half a year, even longer, or longer, but athletes usually adhere to a 4-6 week course of therapy (combining with different modes of taking steroids). It is worth noting that sometimes men take Cabergoline in order to get multiple orgasms during sex. This fact is explained very simply, during sexual intercourse, sexual desire and desire in men is caused by increased production of dopamine in certain areas of the brain. At the time of orgasm, there is a sharp release of prolactin, which “extinguishes” the entire volume of dopamine, which is developed, so the men’s sexual desire quickly disappears. During the experiments, it was concluded that men blocking the production of prolactin continue to experience orgasms, but dopamine is not “discharged” and it turns out that sexual attraction does not disappear after orgasm, in connection with this, a multiplicity of orgasms becomes possible.
Admission (for women)
For medical reasons, 0.25 mg (1/2 tablet) is taken 2 times per 24 hours for 2 days (total dose is 1 mg) in order to suppress the steady lactation. To reduce the risk of orthostatic hypotension in lactating women, a single dose of Kabergoline should not exceed 0.25 mg.
To treat violations associated with hyperprolactinemia, the drug is taken for 0.5 mg in 7 days in 1 (1 tablet) or 2 doses (1/2 tablet, for example, on Tuesday and Friday). Increase the weekly dose is carried out gradually – by 0.5 mg with an interval of 4 weeks before the optimal therapeutic effect. The optimal therapeutic dose is 1 mg per week, but it can range from 0.25 to 2 mg per week. The maximum dose for patients with hyperprolactinemia is 4.5 mg in 7 days.
Depending on the tolerability of the drug in patients, a weekly dose can be taken at a time, or divided into 2 or more doses in 7 days. The split of a weekly dose into several doses is recommended if the drug is prescribed in a dose of more than 1 mg per week.
Side effects of Cabergoline
A study of 200 patients with Parkinson’s disease using high doses of cabergoline (0.5 mg every day) reports the following side effects:
- Digestive system (most often): nausea, constipation, dry mouth, indigestion
- Nervous system: insomnia, dizziness, depression, distortion of consciousness
- Cardiovascular system: falling of arterial pressure, peripheral edemas, disturbance of a rhythm, damages of valves, pericarditis
- From the immune system: infrequently – a hypersensitivity reaction, a skin rash.
- From the hemopoietic system: infrequently – erythromelalgia.
- On the part of the respiratory system: often – shortness of breath, infrequently – pleural effusion, lung fibrosis, epistaxis.
- When using low dosages side effects are rare or completely absent. On the forums most often reported on the depressed mood and loss of appetite.
It is not recommended to take more than one pill per week (exception – a very high level of prolactin).
Contraindications to medical use
Children and adolescents under 16 years of age (safety and efficacy have not been established); increased sensitivity to cabergoline or any components of the drug, and to any ergot alkaloids. Cabergoline is administered with extreme caution in such conditions and / or diseases: hypertension that has developed during pregnancy, for example, preeclampsia or postpartum arterial hypertension (Cabergoline is used only if the potential benefit of taking the drug is significantly greater than the potential risk); severe cardiovascular diseases, Raynaud’s syndrome; peptic ulcer, gastrointestinal bleeding; severe hepatic insufficiency (it is recommended to use lower doses); severe psychotic or cognitive impairment (including anamnesis); symptoms of cardiac and respiratory failure after fibrotic changes or the presence of such conditions in the anamnesis; simultaneous use with drugs that have antihypertensive effects (because of the risk of developing orthostatic hypotension).
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