Caberlon

Cabernon is a new generation drug whose action is directed to the treatment of parkinsonism - a syndrome of the gradual defeat of the entire nervous system of man.

Our organism, including body movements, is controlled by the nervous system, which also includes the work of the brain and spinal cord. A person who develops parkinsonism, over time, loses the ability to control his movements and control the body. The disease is manifested by such symptoms as trembling, slowness of movements (bradykinesia), general decrease in activity, the appearance of pains of different etiology, changes in speech, increased muscle tone, chronic depression.

In general, the disease affects people (both men and women) at the age of 55-60 years, but in 10% of cases the insidious disease develops at a fairly young age - even before the age of forty. In this case we are talking about so-called. "Juvenile parkinsonism." Unfortunately, at a late stage in the course of this disease, the quality of life and patient activity are significantly reduced. Because of prolonged immobility, death most often occurs, which is caused by additional factors: pressure sores, swallowing dysfunction leading to exhaustion of the body, and various respiratory disorders. Among the causes of Parkinson's disease can be noted the aging process of the body, genetic predisposition, negative effects on the body of toxic substances, as well as atherosclerosis, viral infections, severe craniocerebral trauma.

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Indications Caberlon

Cabernon is used in medicine as a drug of auxiliary therapy in the treatment of Parkinson's disease in patients who suffer from various disorders of motor activity. Often, such patients experience involuntary movements and trembling of the limbs. Before starting treatment with the drug it is important to examine the patient for possible pathologies of the valvular apparatus of the heart. It is recommended to determine ESR, conduct a chest X-ray, determine the indicators of kidney function and perform pulmonary tests.

Indications for use Caberlone: the drug is used at an early stage of Parkinson's disease as a monotherapy, or in combination with an inhibitor of dopa decarboxylase and levodopa; it belongs to a group of dopaminergic agents, dopamine agonists.

1 tablet contains 1 or 2 mg of this substance. As auxiliary substances, lactose, magnesium stearate (E 572) and L-leucine were used. Therefore, patients with severe galactose intolerance or lactase deficiency this drug is contraindicated.

Cabergoline is a derivative of ergot alkaloids. It stimulates certain receptors of the pituitary gland, thereby causing prolonged oppression of the secretion of prolactin - the hormone of the anterior lobe. The substance is able to have a therapeutic effect in the presence of hyperprolactinaemia, reducing such manifestations as galactorrhea, infertility, impotence, menstrual irregularity, decreased libido.

Caberlon is prescribed by mouth, preferably - during meals, to exclude negative reactions to the drug from the gastrointestinal tract. It is necessary to take into account the fact that the cabergoline is able to lower blood pressure, thus affecting the rate of response of the patient. Therefore, when taking the drug, patients are advised to refrain from managing motor transport, as well as working with complex mechanisms and requiring increased attention.

Release form

Modern medicines are produced in various forms, depending on the composition, the characteristics of the effect of the substance on the body, and the ways of its administration. Tablets refer to solid dosage forms of drugs. They include the main active ingredient and all kinds of auxiliary components (starch, sugar, talc, etc.), which serve to improve taste and give the drug volume.

Nowadays it is important to know what a medical product looks like to prevent the risk of acquiring its counterfeit.

Cabernon is available in tablets of 1 or 2 mg (in both versions - 30 tablets in a glass bottle). Each bottle with tablets is packed separately.

Form of issue:

• tablets of 1 mg white, oval, biconvex, with notches and labeling "CBG" and number "1" from different sides;
• tablets of 2 mg of white color, capsular, biconvex, with notches and labeling "CBG" and number "2" from different sides.

This form of release facilitates convenient storage and easy transportation of the drug.

The drug Caberlon is released on prescription. Manufacturer: IVAX Pharmaceuticals sro (AYVEX Pharmaceuticals sro).

Pharmacodynamics

Cabernon has an effect on the human body that does not correlate with the therapeutic effect, it only affects the reduction of blood pressure.

Pharmacodynamics Caberlon: the maximum level of the hypotensive effect of the active substance - cabergoline, is achieved during the first 6 hours after taking the drug in a single dose and is dose-dependent with respect to frequency and maximum reduction.

Cabergoline is a dopaminergic derivative of ergoline and has the properties of a potent agonist of dopamine D2 receptors. During the test, in rats given cabergoline orally, the drug decreased the secretion of prolactin at a dosage of 3-25 mg / kg. This was due to the action of the pituitary cells on dopamine D2 receptors. In addition, the drug has a dopaminergic effect through the stimulation of D2 receptors in doses that exceed doses to reduce serum prolactin levels. Animals showed improvement in motor disorders, when the oral dose was 1-2.5 mg / kg for rats, and intramuscular dose 0.5-1 mg / kg for monkeys.

In volunteers who did not have health problems, when taking cabergoline in a dose of 0.3-2.5 mg, there was a pronounced decrease in serum prolactin level, which is dose-dependent.

Cabernon acts quickly (within 3 hours after administration) and has a lasting effect (7-28 days).

Pharmacokinetics

Cabernon has a fairly high level of absorption. After oral administration, this drug quickly enters the bloodstream through passage and absorption through the gastrointestinal tract. The maximum level of its concentration in the blood plasma is reached in 30 minutes - 4 hours after ingestion. At the same time, food intake does not affect the absorption and further distribution of the active substance (cabergoline).

Pharmacokinetics Caberlon: according to the results of medical research, it is known that with cabergoline it is able to bind by plasma proteins at concentrations of 0.1-10 ng / ml at 41-42%. As for the metabolic process, the main metabolite that was identified in the urine of the subject is 6-allyl-8ß-carboxy-ergoline. It was 4-6% of the dose. The number of other metabolites is less than 3% of the dose. According to the results of medical studies in vitro, their activity in inhibiting the secretion of prolactin is much lower than the active substance - cabergoline.

Following the above information, we can conclude about a fairly long half-life of the drug Cabernon from the body. In patients with hyperprolactinemia, it reaches 79-115 hours. Even after 10 days after the last administration of this drug, up to 18% of the dose in urine is detected (2-3% in the original form) and up to 72% of the dose in feces.

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Use Caberlon during pregnancy

Caberlon was tested on animals. In particular, the results of studies have shown its ability to penetrate the placental barrier in rats. Whether such an effect exists in humans is unknown.

The use of Caberlon during pregnancy has not been sufficiently studied. In experiments on rats there was no effect of the drug on reproductive function and no teratogenic effect was observed. According to the results of clinical studies, taking this medication does not increase the risk of congenital fetal disease, premature birth, interruption of pregnancy, or the occurrence of other problems associated with the reproductive function of the female body.

Because of insufficient clinical experience, as well as a long period of excretion of the drug Cablon from the body, women planning pregnancy, it is recommended to stop taking it one month before the desired conception. This will prevent the possible effect of the drug on the fetus. If the pregnancy occurred during the period of taking the drug, it must be urgently canceled in order to prevent any effect on the fetus.

The ability of cabergoline and its metabolites to penetrate into milk in rats is proved. According to some assumptions, when taking Caberlon, lactation can be delayed or suppressed because the drug has the properties of a dopamine agonist.

Due to the lack of any data on the effect of cabergoline on lactation, it is recommended that women stop breastfeeding if there are any symptoms of the drug's effect, in particular, delay or suppression of lactation.

Contraindications

Cableron is not recommended to be used concomitantly with antibiotics and antipsychotic drugs due to increased bioavailability of cabergoline and the severity of its side effects. It should be noted that after the administration of Caberlone, symptomatic hypotension may occur.

Contraindications to the use of Caberlon:

• serious heart disease and malfunction of the cardiovascular system;
• dysfunction of the liver and kidneys;
• the patient has stomach ulcer (including peptic ulcer) and duodenal ulcer;
• the occurrence of gastrointestinal bleeding;
• Raynaud's syndrome;
• serious mental disorders in the anamnesis;
• lung diseases in the anamnesis (in particular, fibrosis, pleurisy), in the treatment of which dopamine agonists were used;
• arterial hypertension;
• eclampsia, preeclampsia.

It is necessary to adjust the dose of the drug to patients with severe impairment of liver function. With caution give Caberlon with simultaneous reception with drugs, the action of which is aimed at lowering blood pressure.

Patients who took dopamine agonists had signs such as hypersexuality, increased libido, risk appetite.

Information on the effect of alcohol on the tolerability of the drug is currently not available.

Side effects Caberlon

Cabernon, like any other drug of a similar action, has a number of side effects.

Side effects of the Cabernon are of a short-term nature and are manifested to a moderate extent. In this case, the withdrawal of the drug is observed only in very rare cases.

In general, when taking the drug, side effects arise from the nervous system and the gastrointestinal tract and manifest themselves as:

• hyperkinesia,
• dyskinesia,
• hallucinations,
• confusion of consciousness;
• nausea, vomiting, constipation;
• dyspepsia, gastritis development.

Less common side effects from the cardiovascular system. They are manifested in the form of frequent attacks of dizziness and arterial hypotension. There is also the development of inflammatory processes that can spread to the mucosa and fibrous membranes: pulmonary fibrosis, pleurisy, pericarditis, pleural fibrosis, pericardial effusion, pathology of the valvular heart apparatus.

It should be noted that in patients taking Caberlon, the occurrence of a pathology of heart valves, including regurgitation, as well as associated violations in the form of pericarditis and pericardial effusion, was very often observed. Other adverse reactions arose due to the vasoconstrictor properties of this drug and related to the development of angina pectoris, peripheral edema, erythromelalgia. However, during the treatment with Caberlon ECG and heart rate changes were not observed.

Violations of the functions of the stomach were more often observed in women than in men, and the side symptoms from the CNS - in elderly patients.

Reception of the drug may also be accompanied by drowsiness, less often - cases of sudden falling asleep.

With prolonged use of the drug, there may be deviations in the results of standard laboratory tests.

When taking high doses of dopamine agonists, including cabergoline, the patients developed symptoms of pathological risk appetite, as well as hypersexuality and increased libido, which were reversible upon discontinuation of treatment or dose reduction.

[3], [4]

Dosing and administration

Cabernon is recommended for long-term use. Its effectiveness, as well as side effects, is associated with individual sensitivity. According to clinical studies, the safety of the drug is confirmed for 24 months or more, however, in each individual case, the duration of treatment should be determined by the attending physician. 

Dosage and administration: The drug is intended for oral administration. The recommended therapeutic dose of Caberlon is 0.5-1 mg / day, its optimization is achieved by gradual titration of the initial dose (0.5 mg / day - for patients not taking dopamine agonists and 1 mg / day for patients taking L- admission). Gradually, it is possible to reduce the dose of levodopa applied in parallel, and, on the contrary, to increase the dose of cabergoline to obtain the optimal ratio. The maximum dose of the drug should not exceed 3 mg / day. The weekly therapeutic dose of Caberlon is usually 500 μg, if necessary, it is gradually increased by another 500 μg per week at intervals of 1 month.

In the case of treatment of patients with hyperprolactinemia, doses are selected individually. For the prevention of lactation, a single dose of 1 mg of Caberlone is recommended on the first postnatal day. To suppress the already available lactation in women, the drug is usually given in a dose of 250 micrograms every 12 hours for 2 days.

[5], [6]

Overdose

When used correctly at recommended doses, Caberlon does not cause any negative symptoms. However, in cases of overdose, signs such as abdominal pain, nausea, vomiting, constipation, dizziness may be noted. The patient who has taken a large dose of the drug may also have the following symptoms:

• a decrease in blood pressure,
• skin rash,
• impaired consciousness,
• drowsiness,
• psychomotor agitation,
• hallucinations.

Overdose happens for a number of reasons, among which most often can be noted a person's tendency to self-medication, which leads to dangerous consequences, uncontrolled treatment with disregard for the doctor's recommendations, as well as non-prescription drug release. Unfortunately, an overdose can be deliberate (in the case of a suicide attempt).

In any case, the first symptoms of an overdose of Caberlon require urgent medical attention. The severity of the condition at the same time depends on the age, sex, the patient's concomitant diseases and the general condition of the body.

Treatment for an overdose is symptomatic. In this case, drugs of the reverse action are introduced, and measures are taken, primarily aimed at maintaining the liver.

Interactions with other drugs

Cabernon acts on the human body by stimulating dopamine receptors. For this reason, this drug is not recommended for use in combination with dopamine antagonists (metoclopramide, butyrofenone, phenothiazine, thioxanthene).

The interaction of Caberlone with other drugs can cause a number of undesirable consequences. For example, with the combined use of Caberlone with macrolide antibiotics (in particular, erythromycin), the patient may experience an increase in the level of bromocriptine in the blood plasma. With particular caution, this drug should be taken in combination with other drugs, the action of which is aimed at lowering blood pressure.

If we take into account the current information on the metabolism of cabergoline, the pharmacokinetic interaction of the drug Caberlone with other drugs can not be provided in advance. In medical studies of patients with Parkinson's disease, the pharmacokinetic interaction of this drug with L-dopa and selegiline has not been observed.

As for the effect of alcohol on drug tolerance, there is no reliable information on this issue at the moment. However, given the negative impact of alcohol on medications in general, it can be assumed that the simultaneous intake of Caberlone with alcohol will have a pronounced negative effect.

[7], [8], [9], [10], [11], [12], [13], [14]

Storage conditions

Caberlon is recommended to store in the original packaging at an air temperature of no higher than 30 ° C. The storage area should be well protected from sunlight and moisture, and also inaccessible to small children. In this case, it is recommended not to remove a capsule of silica gel from the bottle with the preparation, intended for adsorbing moisture.

The storage conditions of Caberlon also depend on the general requirements for the storage of medicinal products. Following them, this drug should be kept away from the light, preferably in some dark place. To prevent moisture from entering the tablets, they should be stored in a dry place. Therefore, the bathroom or other room in which an unstable moisture level is observed is not suitable for this purpose.

It is forbidden to store the medicinal product in the open state, because this can lead to the absorption of volatile substances, and also cause its reaction with oxygen. Therefore, after taking the next dose of the drug, the bottle should be tightly closed. It is desirable to store the tablets in a sealed factory package, and do not pour into any other container.

It should be remembered that medicines for indoor and outdoor use are best kept separate. It is desirable in this case to put them on different shelves of the cabinet, or store in separate packages.

Shelf life

Cabernon refers to medicines, the storage frames of which are clearly marked. Shelf life of this medicine is 2 years.

By "expiry date" is meant the period of time during which the medications meet all the conditions and requirements of the relevant documentation, referring to which they were manufactured. The initial period of storage of the preparation is determined directly by the manufacturer. Then, after the registration of the medicinal product and the start of its industrial release, the manufacturer undertakes to continue the research work aimed at studying the level of stability of this medicine. Thus, confirmation or clarification of the indicated shelf life occurs.

It is not possible that the expiration date of the medication exceeds 5 years, even though the final results of studying its stability allow doing this.

The date of release of the drug Cabernon is the initial date for the counting of its useful life. During the storage of the drug, all the conditions prescribed in the instructions and on the labeling of the package must be observed.

At the end of the expiry date, any medicinal product is strictly forbidden to use. This is fraught with irreversible effects on health. Tablets should be stored in a "native" package, in a dry place and protected from moisture and sun.

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