Cabergoline
Cabergoline: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Cabergoline
ATX code: G02CB03
Active ingredient: cabergoline (cabergoline)
Producer: Obninsk Chemical-Pharmaceutical Company, CJSC (Russia)
Description and photo update: 2018-26-10
Prices in pharmacies: from 299 rubles.
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Cabergoline is a dopaminergic drug, a dopamine receptor agonist.
Release form and composition
Dosage form of Cabergoline - tablets: flat-cylindrical, oblong, beveled on both sides, on one side - dividing risk, almost white or white (2, 8 or 10 pcs. In blister strip packaging, in a cardboard box 1, 2 or 3 packages; 2 or 8 pcs. In polymer cans, in a cardboard box 1 can).
Composition for 1 tablet:
- active substance: cabergoline - 0.5 mg;
- auxiliary ingredients: leucine - 3.6 mg; anhydrous lactose - 75.9 mg.
Pharmacological properties
Pharmacodynamics
The active ingredient of the drug is cabergoline, a dopaminergic derivative of ergoline, characterized by a pronounced and long-term prolactin-lowering efficacy due to direct stimulation of DRD2 (dopamine D2 receptors) of pituitary lactotropic cells. The consequence of taking higher doses of cabergoline in comparison with those required to lower plasma levels of prolactin in the blood is the central dopaminergic effect of the substance as a result of stimulation of DRD2.
The concentration of prolactin in plasma decreases within 3 hours from the moment of taking the pills and remains for 1-4 weeks in healthy people and patients with hyperprolactinemia and up to 2-3 weeks in the postpartum period.
Cabergoline has a strictly selective effect, does not affect the basal secretion of other hormones (pituitary gland, cortisol). The prolactin-lowering effect of the drug directly depends on the dose taken, both in terms of the severity of the action and its duration.
Another pharmacodynamic effect of cabergoline, not associated with a therapeutic effect, is a decrease in blood pressure (blood pressure). Due to a single dose of the drug, the maximum antihypertensive effect is observed during the first 6 hours and is dose-dependent.
Pharmacokinetics
- absorption: after oral administration from the gastrointestinal tract (gastrointestinal tract), cabergoline is rapidly absorbed; its maximum level in plasma is reached after ½ – 4 hours, 41–42% binds to blood proteins;
- distribution: on the 11th day after administration, it is found in urine ~ 18%, and in feces ~ 72% of the dose taken; the proportion of unchanged cabergoline in the urine is 2 to 3%. The absorption and distribution of cabergoline does not depend on the patient's regimen and diet;
- metabolism: the main metabolite of cabergoline is 6-allyl-8b-carboxy-ergoline, its concentration in urine from the dose taken varies in the range of 4-6%, and the content of the other three metabolites does not exceed 3%. Metabolic products have a significantly less inhibitory effect on prolactin secretion in comparison with cabergoline;
- excretion: the substance is excreted by the kidneys, the half-life (T 1/2), estimated by the rate of elimination, is 63–68 hours in healthy volunteers, and 79–115 hours in patients with hyperprolactinemia. The result of a long half-life is the achievement of a state of equilibrium concentration after 4 weeks.
Indications for use
Indications for the use of Cabergoline are:
- the need to prevent physiological lactation after delivery;
- suppression of already established postpartum milk secretion;
- amenorrhea, oligomenorrhea, anovulation, galactorrhea, other disorders associated with hyperprolactinemia (for therapy);
- macro- and microprolactinomas (prolactin-secreting pituitary tumors): syndrome of "empty sella turcica" in combination with hyperprolactinemia, idiopathic hyperprolactinemia.
Contraindications
Absolute:
- violations of respiratory function and cardiac activity as a result of fibrotic changes in the pericardium, lungs, heart valves, retroperitoneal space, as well as the presence of data on such conditions in the anamnesis;
- anatomical indicators of pathological changes in the valve apparatus of the heart (thickening of the leaflet, narrowing of the lumen, mixed anomaly - narrowing and stenosis of the valve) during long-term therapy, confirmed by an echocardiogram (EchoCG) performed before treatment;
- an increased risk of developing postpartum psychosis;
- lactation (breastfeeding);
- children and adolescents under 16 years of age;
- rare hereditary diseases: lactase deficiency, lactose intolerance, glucose-galactose malabsorption;
- hypersensitivity to any ergot alkaloids, cabergoline, and other components of the drug.
Relative contraindications for which Cabergoline, like other ergot derivatives, should be used with caution:
- hypertensive disease that developed during pregnancy (preeclampsia or arterial hypertension in the postpartum period); cabergoline is used after a careful assessment of the ratio of the potential benefits from the use of the drug with the possible risks;
- severe liver failure;
- renal failure;
- severe cardiovascular disease, Raynaud's disease;
- arterial hypotension;
- Parkinson's disease;
- psychotic and cognitive disorders of severe degree, as well as the presence of data on such conditions in the anamnesis;
- gastrointestinal bleeding, peptic ulcer;
- use simultaneously with antihypertensive drugs (increased risk of orthostatic hypotension).
Instructions for the use of Cabergoline: method and dosage
Cabergoline is intended for oral administration, tablets are recommended to be taken simultaneously with food.
Dosing regimen according to indications:
- prevention of physiological lactation: once 1 mg (2 tablets of 0.5 mg) for 1 day after delivery;
- suppression of already established postpartum milk secretion: 2 days in a total dose of 1 mg (2 tablets of 0.5 mg), every 12 hours ½ tablet (0.25 mg); to reduce the likelihood of orthostatic hypotension in women who are breastfeeding, a single dose of cabergoline should be ≤ 0.25 mg;
- therapy of disorders associated with hyperprolactinemia: the initial dose is 1 tablet (0.5 mg) once a week at a time or divided into two doses, for example, on Tuesday and Friday, ½ tablet (0.25 mg). The weekly dose should be increased gradually, by 0.5 mg per month, until the optimal therapeutic dose is reached, which is usually 1 mg per week, but may vary within 0.25–2 mg; the maximum permissible weekly dose for hyperprolactinemia is 4.5 mg.
A weekly dose of the drug is taken once or divided into several doses (2 or more), depending on the tolerance and dose. More than 1 mg per week is recommended to be taken several times.
To reduce the risk of side effects with increased sensitivity to dopaminergic drugs, treatment with cabergoline is started at a lower dose (once a week, 0.25 mg) with a gradual increase until the optimal therapeutic effect is achieved. In case of severe adverse reactions, in order to improve the tolerability of cabergoline, a temporary decrease in the dose is possible with a gradual increase (for example, by 0.25 mg per week every 2 weeks) in the future.
Side effects
According to clinical studies, when taking Cabergoline to terminate physiological lactation (at a dose of 1 mg once) and to suppress the steady secretion of milk (0.25 mg once every 12 hours for 2 days), adverse reactions were recorded in about 14% of cases.
Taking pills for six months, 1-2 mg per week, divided by 2 times, for the treatment of disorders associated with hyperprolactinemia, caused side effects in 68% of patients. Basically, negative reactions were observed during the first 2 weeks of admission and were mostly transient (disappeared in the course of continuing the course or a few days after the withdrawal of cabergoline). Typically, side effects were mild or moderately dose-dependent. Severe side effects were noted once in at least 14% of patients, and discontinuation of therapy was required in about 3% of cases.
Side effects from systems and organs, registered in the range from 1 to 10%:
- cardiovascular system: angina pectoris, palpitations, increased hypotensive effect due to prolonged use (in some cases, orthostatic arterial hypotension is possible), asymptomatic decrease in blood pressure in the first 3-4 days after delivery (systolic - more than 20 mm Hg, diastolic - more than 10 mm Hg);
- nervous system: tremor, increased fatigue, dizziness / vertigo, headache, depression, drowsiness, asthenia, fainting, paresthesia, anxiety, nervousness, impaired concentration, insomnia, impulse control disorder (irresistible passion for shopping in the store, bulimia, uncontrollable waste of money);
- digestive system: nausea / vomiting, epigastric pain, gastritis, dyspepsia, abdominal pain, dryness of the oral mucosa, toothache, diarrhea / constipation, flatulence, irritation of the pharyngeal mucosa;
- respiratory system, chest and mediastinal organs: pleurisy;
- other reactions: dysmenorrhea, mastodynia, rhinitis, nosebleeds, transient hemianopsia, flushing of the face, spasms of the capillaries of the fingers, cramps of the muscles of the lower extremities (cabergoline, like other ergot derivatives, has a vasoconstrictor efficacy), flu-like symptoms, visual impairment, malaise, periorbital / peripheral edema, pruritus, acne, anorexia, joint pain;
- laboratory data: due to prolonged treatment, deviation of standard laboratory parameters from the norm was rare; in patients with amenorrhea, a decrease in hemoglobin level was observed for several months after the restoration of the menstrual cycle.
Side effects associated with taking cabergoline, registered in post-marketing studies: alopecia, dyspnea, mania, fibrosis, abnormalities in liver function and abnormalities, increased blood CP (creatine phosphokinase) activity, rash, hypersensitivity reactions, respiratory disorders, respiratory failure, painful addiction gambling, valvulopathy, pericarditis, increased libido, hypersexuality, psychotic disorders, aggressiveness, bouts of uncontrolled sudden falling asleep, nasal congestion, weight loss or increase.
Overdose
Symptoms of a cabergoline overdose are: nausea / vomiting, dyspeptic disorders, psychosis, confusion, hallucinations, orthostatic hypotension.
For the treatment of the condition, it is recommended to carry out measures aimed at extracting the remnants of the drug that have not been absorbed into the gastrointestinal tract by washing the stomach. If necessary, blood pressure should be maintained within the normal range. Dopamine antagonists may be needed.
special instructions
When cabergoline is prescribed for the treatment of diseases associated with hyperprolactinemia, a complete examination of the pituitary gland is required. It is also necessary to assess the state of the heart and blood vessels, including echocardiography, to identify pathologies of the function of the valve apparatus, which are asymptomatic.
Long-term use of cabergoline, like other ergot derivatives, may contribute to the development of pleural effusion / fibrosis and valvulopathy. Sometimes these patients have received prior therapy with ergotonin dopaminomimetics. In connection with such a reaction to cabergoline, it is not recommended to prescribe it to patients with existing clinical symptoms and / or signs of impaired cardiac and respiratory functions associated with fibrotic changes, or with anamnestic data on such conditions.
If signs of the appearance / deterioration of blood regurgitation, narrowing of the lumen or thickening of the valve leaflets are detected, the drug should be discontinued. According to observations, it was found that ESR (erythrocyte sedimentation rate) increases due to the development of pleural effusion / fibrosis. If there is an unexplained increase in ESR, a chest x-ray should be taken. Plasma creatinine studies and an assessment of renal function are also important to make a correct diagnosis.
In the presence of valvulopathy, pleural effusion / fibrosis, symptoms improved upon completion of cabergoline therapy. There are no reliable data on the deterioration of the condition of patients with signs of blood regurgitation while taking cabergoline.
The drug is not prescribed when fibrotic changes in the heart valve apparatus are detected.
It should be borne in mind that fibrotic changes can develop asymptomatically, and therefore requires regular monitoring of the following symptoms in patients receiving long-term treatment with cabergoline:
- pleuropulmonary disorders: shortness of breath, difficulty breathing, persistent cough, chest pain;
- obstruction of the ureters, renal failure, obstruction of the abdominal organs: edema of the lower extremities, pain in the side or in the lumbar region, any swelling or pain on palpation in the abdomen (retroperitoneal fibrosis may develop);
- pericardial effusion, fibrosis of the cusps of the heart valves: manifested by the main signs of heart failure, in connection with which it is necessary to exclude the further transition of fibrosis of the cusps of the heart valves to constrictive pericarditis at the first signs of heart failure.
It is necessary to regularly monitor the condition of patients for the appearance and development of fibrotic changes. For the first time, echocardiography is performed 3-6 months after the start of cabergoline. Further, the study is carried out depending on the clinical assessment of the patient's condition, paying special attention to the symptoms listed above, at least once every 6-12 months of continuous treatment.
The need to examine patients by other methods, such as physical monitoring, including auscultation of the heart, radiography, computed tomography, is determined in each case individually.
Dose titration of cabergoline is carried out under medical supervision to establish the minimum effective dose that produces a therapeutic effect. After selecting an effective dosing regimen, it is recommended to regularly (once a month) determine the plasma concentration of prolactin. Normalization of prolactin levels is usually observed within 2-4 weeks of taking the drug.
After the withdrawal of cabergoline, a relapse of hyperprolactinemia usually occurs, but in some patients a persistent decrease in prolactin levels is recorded over several months. In most patients, ovulatory cycles persist for at least six months after completion of therapy.
Cabergoline helps restore ovulation and fertility in hyperprolactinemic hypogonadism. Considering that pregnancy can occur before the menstrual cycle settles and before the first menstruation after a break, it is recommended that pregnancy tests be carried out at least once every four weeks throughout the entire period of amenorrhea, and after the restoration of the cycle - with each delay of menstruation by more than three days. When pregnancy is not desirable, barrier contraceptives are required during cabergoline therapy and after its withdrawal until anovulation recurs. With the onset of pregnancy, close medical supervision is necessary for the timely diagnosis of symptoms of an enlarged pituitary gland, since pregnancy can increase the size of already existing pituitary tumors.
The use of the drug causes drowsiness, and in Parkinson's disease, dopamine receptor agonists can cause sudden sleep. In such cases, the dose of the drug is recommended to be reduced or interrupted.
Influence on the ability to drive vehicles and complex mechanisms
It is recommended to refrain from performing potentially dangerous types of work, including driving vehicles, since cabergoline affects the speed of psychomotor reactions and the ability to concentrate.
Application during pregnancy and lactation
Controlled clinical studies in pregnant women with the use of cabergoline have not been conducted, therefore, its appointment is possible only when absolutely necessary, after a thorough assessment of the ratio of the expected benefits to potential risks to the mother and the fetus.
In the event of pregnancy on the background of cabergoline therapy, its intake should be discontinued immediately, but only after a careful assessment of the benefit / risk ratio.
According to monitoring data, taking cabergoline in a weekly dose of 0.5 to 2 mg for the treatment of disorders associated with hyperprolactinemia is not accompanied by an increase in the frequency of multiple pregnancies, miscarriages, premature births, and congenital malformations of the child.
There is no information on the penetration of the drug into breast milk, but if cabergoline is not effective to prevent / suppress lactation, breastfeeding should be abandoned. For the treatment of disorders associated with hyperprolactinemia, patients planning breastfeeding are not prescribed cabergoline.
Pediatric use
The safety and efficacy of Cabergoline in children and adolescents under 16 years of age have not been established, and therefore it is contraindicated for them to prescribe the drug.
With impaired renal function
According to the instructions, Cabergoline is prescribed with caution to patients with impaired renal function.
For violations of liver function
In severe hepatic impairment of class C on the Child-Pugh scale, in patients who are shown a long course of therapy, Cabergoline is recommended to be used in lower doses. As a result of a single dose of the drug at a dose of 1 mg, there was an increase in the area under the concentration-time curve (AUC) compared with patients with less severe hepatic impairment or with healthy volunteers.
Use in the elderly
Studies on the use of the drug in elderly patients for the treatment of disorders associated with hyperprolactinemia have not been conducted. Based on the available data, it can be concluded that there is no specific risk of such treatment.
Drug interactions
- other ergot alkaloids: there is no information on the interaction with cabergoline, and therefore it is not recommended to use them simultaneously during prolonged therapy with cabergoline;
- phenothiazines, butyrophenones, thioxanthenes, metoclopramide and other dopamine antagonists: can weaken the effectiveness of cabergoline, aimed at reducing the concentration of prolactin, so their combined use is contraindicated;
- erythromycin and other macrolide antibiotics: may increase the systemic bioavailability of cabergoline (simultaneous use is contraindicated).
Analogs
The analogues of Cabergoline are Agalates, Bergolak, Dostinex, etc.
Terms and conditions of storage
Store at 25 ° C. Keep out of the reach of children.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Cabergoline
There are few reviews about Cabergoline, but almost all of them are positive. Patients note the affordable cost of the drug, its effectiveness and the almost complete absence of adverse reactions. Those who received drug therapy are strongly advised not to take it without the appointment of a specialist.
Complaints are caused by the small size of the tablets, since they often have to be divided, which is not very convenient.
Price for Cabergoline in pharmacies
Estimated price for Cabergoline tablets 0.5 mg for 2 pcs. in the package is 270-300 rubles., for 8 pieces. in the package - 687-775 rubles.
Cabergoline: prices in online pharmacies
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Drug name Price Pharmacy |
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Cabergoline 0.5 mg tablets 2 pcs. 299 r Buy |
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Cabergoline 0.5 mg tablets 8 pcs. 908 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
