Universal reference book for medicines
Product name: CABERGOLINE (CABERGOLINE)

Active ingredient: cabergoline

Type: Dopamine receptor agonist.
Prolactin secretion inhibitor
Producer: Obninsk Chemical and Pharmaceutical Company (Russia)
Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..

PHARMACHOLOGIC EFFECT
The derivative of ergot alkaloid ergolin, a dopamine D 2 receptor agonist.
Stimulating these receptors of the pituitary gland causes a pronounced and prolonged inhibition of the secretion of the hormone of the anterior lobe - prolactin. Has a therapeutic effect in hyperprolactinaemia, reducing the severity of such manifestations as disorders of the menstrual cycle (oligomenorrhea, amenorrhea), infertility, galactorrhea; impotence, decreased libido. Prevents and suppresses physiological lactation.
At doses higher than those required to inhibit the secretion of prolactin, cabergoline causes a central dopaminergic effect due to stimulation of dopamine D 2receptors.
The action is dose-dependent. Cabergoline reduces daily motor fluctuation in patients with Parkinson's disease who are treated with a combination of levodopa / carbidopa. Cabergoline has selective activity without affecting the basal secretion of other pituitary and cortisol hormones.
The pharmacodynamic effects of cabergoline, not related to therapeutic activity, include only a decrease in blood pressure.
With a single admission, the maximum hypotensive effect occurs within the first 6 hours and is dose-dependent.
PHARMACOKINETICS
After oral administration, cabergoline is rapidly absorbed from the digestive tract.
C max in blood plasma is achieved in 0.5-4 hours. Food does not affect the absorption or distribution of cabergoline. Pharmacokinetics has a linear character up to a dose of 7 mg / day.
The binding of cabergoline (at a concentration of 0.1-10 ng / ml) with plasma proteins is 41-42%.

In the urine, cabergoline metabolites are found: 6-allyl-8-carboxy-ergoline in an amount of 4-6% of the dose taken, as well as three other metabolites with a total content of less than 3%.
All metabolites to a much lesser extent (in comparison with cabergoline) inhibit the secretion of prolactin. Cabergoline has a long T 1/2 . T 1/2in healthy volunteers is 63-68 hours, T 1/2 in patients with hyperprolactinemia is 79-115 hours. With such a T 1/2, the equilibrium state is reached after 4 weeks. In urine and feces 18% and 72% of the dose, respectively, were detected. The content of unchanged cabergoline in urine is 2-3%.
INDICATIONS
Hyperprolactinemia (macro- and microadenomas of the pituitary gland, idiopathic hyperprolactinemia).
Disorders associated with hyperprolactinemia (including functional disorders such as amenorrhea, oligomenorrhea, anovulation, galactorrhea). Prevention or suppression of physiological lactation in the postpartum period.
For the treatment of diseases and symptoms of Parkinson's disease, as monotherapy in patients with newly diagnosed symptoms or as a combination therapy, when the use of other drugs is not effective.

DOSING MODE
Intended for oral administration.
To prevent lactation - once on the first day after childbirth at a dose of 1 mg. To suppress the already available lactation - for two days to 250 mcg every 12 h. In the treatment of hyperprolactinemia, doses are selected individually. The initial dose is usually 500 μg per week, usually in a single dose (sometimes in the form of two divided doses). In the future, if necessary, the dose is gradually increased - by 500 μg per week at intervals of 1 month. Usually the therapeutic dose is 1-2 mg per week, in some cases it can be increased to 4.5 mg per week. If the weekly dose exceeds 1 mg, then it is recommended to divide it into 2 divided doses. In some cases, an effective dose of 250-500 μg per week is effective.
In parkinsonism, the dose is set individually, depending on the treatment regimen, and is 0.5-3 mg 1 time / day.

SIDE EFFECT
From the nervous system: very often - dizziness, dyskinesia;
often - hallucinations, sleep disorders, confusion, headache, drowsiness, depression; infrequently - hyperkinesia, delirium, psychotic disorder, sudden onset of sleep, fainting; rarely - hemiopia. Excessive drowsiness during the day and episodes of sudden falling asleep, especially in patients with Parkinson's disease, are possible.
From the side of the digestive system: very often - nausea;
often - constipation, dyspepsia, gastritis, vomiting; infrequently - violations of the liver, dyskinesia biliary tract.
From the cardiovascular system: very often - peripheral edema, cardiac valvulopathy (including regurgitation) and related disorders (pericarditis and pericardial effusion);
often - postural hypotension, angina pectoris, palpitations, redness of the face; infrequently - spasm of the vessels of the fingers; rarely erythromelalgia.
On the part of the hematopoiesis system: often - reduction of hemoglobin, hematocrit and / or erythrocytes (> 15% compared to the baseline level).

On the part of the reproductive system: often - increased libido.

From the respiratory system: often - shortness of breath;
infrequently - impaired breathing, respiratory failure; rarely - pleurisy, pulmonary fibrosis, nosebleeds.
Dermatological reactions: infrequent - rash, alopecia.

On the part of the musculoskeletal system: infrequently - spasms of the calf muscles, an increase in CK in the blood.

Common reactions: often - asthenia, fatigue, chest pain, back pain;
infrequently - hypersensitivity reactions; rarely - swelling, fatigue.
Other: rarely - fibrosis, cramps in the fingers.

CONTRAINDICATIONS
Severe liver function abnormalities, pregnancy, preeclampsia, eclampsia, history of psychosis, risk of postpartum psychosis, postpartum hypertension, breastfeeding period, uncontrolled hypertension, symptoms of cardiac and respiratory failure due to fibrotic changes, or history of such symptoms;
damage to the valves of the heart due to prolonged therapy with cabergoline, confirmed by echocardiography; children and adolescents under 18; increased sensitivity to cabergoline and ergot alkaloids.
PREGNANCY AND LACTATION
Contraindicated in pregnancy and during breastfeeding.

Cabergoline restores ovulation and fertility in women with hyperprolactinemic hypogonadism.
Because pregnancy can occur before the resumption of menstruation, pregnancy tests are recommended during the amenorrhea period, and after the recovery of the menstrual cycle - in all cases, their delay is more than 3 days. Women who do not plan pregnancy are recommended to use non-hormonal contraceptives during treatment with cabergoline and after its termination. Women planning pregnancy, it is recommended to conceive not earlier than 1 month after the abolition of cabergoline.
APPLICATION FOR FUNCTIONS OF THE LIVER
Use with caution in patients with impaired renal function.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in severe violations of liver function.

SPECIAL INSTRUCTIONS
They are used with caution in patients with cardiovascular diseases, Reynaud's syndrome, peptic ulcer of the stomach and duodenum, gastrointestinal bleeding, impaired renal function, severe hepatic insufficiency (recommended use in lower doses), serious mental illness in the anamnesis, and on the background of treatment with antihypertensive drugs.

Cabergoline can cause symptomatic arterial hypotension, especially when taken together with drugs that lower blood pressure.
It is recommended to regularly measure blood pressure in the first 3-4 days after the start of treatment.
With long-term use of cabergoline and other ergot derivatives, which are active against serotonin 5-HT 2B receptors, the risk of fibrotic and serous inflammatory diseases such as exudative pleurisy, pleural fibrosis, pulmonary fibrosis, pericarditis, damage to one or more valvular heart valves (aortic, mitral, tricuspid), retroperitoneal fibrosis.
The abolition of cabergoline in the case of the development of this pathology led to an improvement in signs and symptoms.
Before the onset of long-term therapy with cabergoline, all patients must undergo a complete examination to detect cardiac valve lesions, to determine the functional state of the lungs and kidneys to prevent worsening of the course of concomitant diseases.

When new clinical symptoms appear on the part of the respiratory system, fluoroscopy of the lungs is recommended.
In patients with pleural effusion / fibrosis, there was an increase in ESR, therefore, with an increased ESR without obvious clinical signs, an X-ray examination should also be performed.
With prolonged therapy with cabergoline, gradual development of fibrotic disorders is possible, therefore, the appearance of symptoms such as shortness of breath, shortness of breath, coughing, chest pain, back pain, swelling of the lower limbs, signs of retroperitoneal fibrosis, heart failure should be monitored during treatment.

After the initiation of cabergoline therapy for the prevention of fibrotic disorders, the condition of the heart valves should be monitored and an ECG examination should be carried out within 3-6 months.
Further, the frequency of ECG monitoring is set by the doctor individually for each patient, but at least once every 6-12 months. In the case of appearance or deterioration of valvular regurgitation, narrowing of the lumen or thickening of the valve wall, cabergoline therapy should be discontinued.
The need for the patient in other types of clinical examination is established by the doctor on an individual basis.

Hyperprolactinaemia in combination with amenorrhea and infertility can be associated with pituitary tumors, so before starting treatment with cabergoline it is necessary to find out the cause of hyperprolactinaemia.

It is recommended to check the content of prolactin in the blood serum every month, tk.
after achieving an effective therapeutic regimen, the normal level of prolactin persists for 2-4 weeks. After the withdrawal of cabergoline, hyperprolactinaemia usually occurs again. However, in some patients there is a persistent decrease in prolactin concentration for several months.
Impact on the ability to drive vehicles and manage mechanisms

Cabergoline lowers blood pressure, which can disrupt the reaction rate in some patients.
This need to be taken into account by patients who drive vehicles and other activities that require a high concentration of attention and speed of psychomotor reactions.
DRUG INTERACTION
It is not recommended to apply simultaneously with antibiotics macrolides (including with erythromycin), t.
the bioavailability of cabergoline and the severity of its side effects increase.
The mechanism of action of cabergoline is associated with direct stimulation of dopamine receptors, so it should not be used in combination with dopamine receptor antagonists (phenothiazines, butyrophenones, thioxanthenes, metoclopramide).

Combination with ergot alkaloids and their derivatives is not recommended.

Given the pharmacodynamics of cabergoline (hypotensive effect), it is necessary to take into account the interaction with drugs that reduce blood pressure.

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