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Active Ingredient: Cabergoline.

Analogs of Cabgolin:Dostinex.

Chemical name
1 – [(6-Allylergolin-8beta-yl) carbonyl] -1- [3- (dimethylamino) propyl] -3-ethylurea.

Chemical properties
This substance is a fairly common dopaminomimetic, a derivative of ergot alkaloids. The tool is synthesized in the form of a white fine powder, which is highly soluble in ethanol, N, N-dimethylformamide and chloroform. The chemical compound is slightly soluble in 0.1 n hydrochloric acid, n-hexane. The product does not dissolve in water.

In medicine, drugs based on Cabergoline are used to treat hyperprolactinemia, and the substance is also used by athletes.

Cabergoline in bodybuilding
The medicine is used to reduce prolactin levels and eliminate unwanted side effects from taking progestin anabolics – trenbolone and nandrolone. During the treatment, athletes monitor the level of prolactin and continue taking the medicine, depending on the results of the tests. It is believed that the substance eliminates fluid retention in the tissues and accelerates the growth of lean muscle mass.

Pharmachologic effect

Pharmacodynamics and pharmacokinetics
Cabergoline is a long acting dopamine receptor antagonist. The drug acts mainly on D2-dopamine receptors, to a lesser extent – on D1-dopamine, serotonin, alpha2- and alpha1-adrenergic receptors.

Laboratory data show that the drug has a direct effect on the synthesis of prolactin by lactotrophs in rats, lactotrophs are located in the pituitary gland. Plasma prolactin levels are significantly reduced, especially in reserpine individuals.

The hypoprolactinemic effect of the drug was carefully studied in two independent, randomized, double trials involving a placebo-controlled and comparative group. The effect of the substance was studied on women suffering from hyperprolactinemia. The test results improved, and the normal menstrual cycle was restored in about 77% of women who took the drug 2 times in 7 days at a dosage of 0.5 mg. In 73% of the subjects, galactorrhea disappeared.

Pharmacokinetic parameters are directly proportional to the dosage of the drug. Eating does not affect the processes of assimilation, metabolism and excretion. After penetration into the digestive tract, the maximum concentration of a substance in the blood plasma was observed after 2-3 hours. With systematic administration of the drug, its equilibrium concentration is several times higher than the concentration with a single dose.

It is not completely known what bioavailability Cabergoline has, but it is unambiguously exposed to the effect of “first passage” through the liver tissue. The degree of binding of the agent to plasma proteins ranges from 40 to 42%, depending on the dose taken. The medicine and its metabolites are quickly and well distributed in tissues and organs, the highest concentration was found in the pituitary gland.

The substance is metabolized by hydrolysis reactions involving urea residues or an acylurea bond in the liver tissues. Cytochrome P450 takes part to a small extent in the biotransformation of the drug. The half-life of the drug is about 65 hours. The substance and its metabolites are completely eliminated from the body within 20 days, mainly through the intestines and urine.

Mild to moderate renal failure and mild to moderate hepatic failure do not require dosage adjustment. With serious violations in the liver, an increase in the concentration of the drug in the blood plasma and AUC is observed. For elderly patients, the drug can be prescribed in the same dosages as for young ones, however, special care must be taken, taking into account all the concomitant diseases and the state of the body as a whole.

The effect of taking the drug is observed after 3 hours, after taking the tablets, reaching its maximum within 48 hours. The duration of the drug is 14 days. Cabergoline does not affect the secretion of other hormones of the anterior pituitary gland or cortisol level. The substance does not have mutagenic activity, slightly reduces fertility.

Indications for use
The tool is prescribed:

  • for the treatment of idiopathic hyperprolactinemia;
    – with macro- and microadenoma of the pituitary gland;
    – patients with amenorrhea, anovulation, oligomenorrhea and
  • – galactorrhea according to indications;
    – to suppress or prevent lactation after childbirth;
    -as part of complex therapy or as a monotherapy for Parkinson’s disease.

  • Contraindications
    The medicine should not be taken:
  • in the presence of hypersensitivity reactions to the active component or – – derivatives of ergoalkaloids;
    – during lactation;
    – patients with uncontrolled hypertension;
    – pregnant women
    – with fibrotic changes in the heart muscle or respiratory system, which – caused disturbances in the functioning of the organs.

  • Caution is recommended to observe:

– with low blood pressure;
– if parallel therapy with dopamine receptor antagonists, antihypertensive – drugs;
– with eclampsia or preeclampsia;
– persons suffering from liver disease;
– with psychosis, including a history of;
– to children.

Side effects
Adverse reactions due to treatment with this substance are quite rare, and in mild or moderate severity.

During clinical trials, the following adverse reactions have been identified.

Most often occur: constipation, headache and dizziness, nausea, pericarditis, peripheral edema, pericardial effusion.

Often develop:

hallucinations, confusion, depression;
indigestion, gastritis, angina pectoris, vomiting;
heart palpitations, flushing and redness of the face;
a decrease in the level of hemoglobin, red blood cells or hematocrit in the blood;
shortness of breath, increased sexual activity, asthenia, pain in the chest and lower back;
weakness, drowsiness (sudden falling asleep in people with Parkinson’s disease).

Less commonly observed:

hyperkinesia, psychotic disorders, fainting, delirium;
malfunctioning of the liver, dyskinesia of the gallbladder and biliary tract, spasm of the vessels of the fingers and toes;
respiratory failure, nosebleeds;
allergic rashes, alopecia, increased levels of creatine kinase in the blood, cramps of the fingers and muscles on the calves;
pulmonary fibrosis, hemionopsia, erythromelalgia, pleurisy, edema (rarely).

Cabergoline, instructions for use (Method and dosage)

In order to prevent lactation in the postpartum period, the medicine is taken once, on the first day after birth, at a dosage of 1 mg. To stop the existing lactation, 250 μg of the drug is used, every 12 hours, 4 times. The duration of treatment, therefore, is 2 days.

The treatment of hyperprolactinemia is carried out in accordance with the recommendations of the attending physician.

As a rule, the initial dosage is 500 mcg per week at a time or distributed over 2 applications. If necessary, the dosage can be increased by 0.5 mg per week, for a month. If the likelihood of developing unwanted adverse reactions is increased, then treatment can begin with 250 mg per week.

The standard therapeutic dose is 1 to 2 mg in 7 days. The maximum amount of a drug that can be prescribed per week is 4.5 mg.

Patients with Parkinson’s disease during monotherapy are prescribed from 500 μg to 3 mg of the substance, 1 time per day. The duration of treatment is determined by the doctor.

In case of an overdose, the victim has nasal congestion, hallucinations, increased side effects, and fainting. As a treatment, supportive and symptomatic therapy is used.

It is better to avoid co-administration of this substance and ergot alkaloids (their derivatives).

The drug is not recommended to be combined with macrolide antibiotics, they increase its bioavailability, more often and more side effects are manifested.

The drug cannot be combined with dopamine receptor antagonists (phenothiazines, thioxanthene, butyrophenone, metoclopramide), this leads to a decrease in the effectiveness of the drug.

Cabergoline is better not to use along with medicines that lower blood pressure.

Storage conditions
Tablets are stored in the original packaging in a cool place.

Shelf life
2 years.

Special instructions
Extra care must be taken in the treatment of patients with cardiovascular diseases, gastric and duodenal ulcers, Raynaud’s syndrome, gastrointestinal bleeding, severe liver diseases (dosage must be adjusted).

The first few days of drug therapy, it is recommended to control the patient’s blood pressure. The drug may cause it to decrease. Also, once a month you need to determine the level of prolactin in the blood. After discontinuation of the drug, prolactin levels can remain at a normal level from 2 weeks to several months.

Before starting treatment, the patient must undergo an examination to identify possible pathologies of the heart valves, liver or kidneys. It is also recommended to do an ECG about 1 time per six months or once a year, in accordance with the doctor’s recommendations. If valve regurgitation worsens, the valve wall thickens, and the lumen narrows, the drug must be replaced.

If during the course of therapy with the agent new clinical symptoms of the respiratory system have appeared, an X-ray of the lungs must be taken. If a patient develops pleural effusion or fibrosis (accompanied by shortness of breath, cough, chest pain and rapid breathing), blood ESR levels increase, additional studies are also needed.

Before starting treatment, it is necessary to accurately determine the cause of the development of hyperprolactinemia in order to exclude the presence of a pituitary tumor.

If you are taking drugs based on Cabergoline, then you can not drive a car and perform potentially dangerous activities, it should be remembered that drugs can lower blood pressure.

For children
This substance, as a rule, is not used in pediatric practice.
With antibiotics
The medicine cannot be combined with erythromycin and some macrolide antibiotics.

During pregnancy and lactation
During pregnancy, the drug is used with extreme caution. Pregnant women can start or continue treatment with the drug only after consulting a specialist.

The drug and its metabolites were found in the milk of experimental rats; it is not known whether the substance is excreted in milk in women. Since the drug can have a negative effect on the infant, it is recommended to stop breastfeeding or replace the medicine.

With antibiotics
The medicine cannot be combined with erythromycin and some macrolide antibiotics.

During pregnancy and lactation
During pregnancy, the drug is used with extreme caution. Pregnant women can start or continue treatment with the drug only after consulting a specialist.

The drug and its metabolites were found in the milk of experimental rats; it is not known whether the substance is excreted in milk in women. Since the drug can have a negative effect on the infant, it is recommended to stop breastfeeding or replace the medicine.

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