Caberlon

Caberlon is a new generation drug, the action of which is aimed at treating Parkinsonism - a syndrome of gradual damage to the entire human nervous system.

Our body, 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 eventually loses the ability to control their movements and control their body. The disease manifests itself with symptoms such as tremors, slowness of movement (bradykinesia), general decreased activity, the occurrence of pain of various etiologies, changes in speech, increased muscle tone, chronic depression.

The disease mainly affects people (both men and women) aged 55-60 years, but in 10% of those affected, the insidious disease develops at a fairly young age - before the age of forty. In this case, we are talking about the so-called "juvenile Parkinsonism". Unfortunately, at a late stage of the disease, the quality of life and activity of patients are significantly reduced. Due to prolonged immobility, death most often occurs, which is caused by additional factors: bedsores, swallowing dysfunction leading to exhaustion of the body, and various respiratory disorders. Among the causes of Parkinson's disease, one can note the aging process of the body, genetic predisposition, negative impact on the body of toxic substances, as well as atherosclerosis, viral infections, severe traumatic brain injuries.

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Indications Caberlon

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

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

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

Caberlogin is an ergot alkaloid derivative. It stimulates certain pituitary receptors, thereby causing prolonged suppression of prolactin secretion, a hormone of the anterior lobe. The substance is capable of exerting a therapeutic effect in the presence of hyperprolactinemia, reducing its manifestations such as galactorrhea, infertility, impotence, menstrual irregularities, and decreased libido.

Caberlon is prescribed orally, preferably during meals, to exclude negative reactions to the drug from the gastrointestinal tract. It is necessary to take into account the fact that caberlogin is able to reduce blood pressure, thus affecting the patient's reaction speed. Therefore, while taking the drug, patients are advised to refrain from driving vehicles, 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 particular effects of the substance on the body, and the routes of administration. Tablets are solid dosage forms of medicines. They contain the main active ingredient and all sorts of auxiliary components (starch, sugar, talc, etc.), which serve to improve the taste and give the drug volume.

Nowadays, it is important to know what a particular medical drug looks like in order to avoid the risk of purchasing a counterfeit.

Caberlon is available in tablets of 1 or 2 mg (both versions contain 30 tablets in a glass bottle). Each bottle of tablets is packaged separately.

Release form:

• 1 mg tablets, white, oval, biconvex, with notches and markings "CBG" and the number "1" on different sides;
• 2 mg tablets, white, capsule-shaped, biconvex, with notches and markings "CBG" and the number "2" on different sides.

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

The drug Caberlon is available on prescription. Manufacturer: IVAX Pharmaceuticals sro (IVAX Pharmaceuticals s.r.o.).

Pharmacodynamics

Caberlon has an effect on the human body that does not correlate with the therapeutic effect; it only concerns the reduction of blood pressure.

Pharmacodynamics of Caberlon: the maximum level of the hypotensive effect of the active substance - caberlogine, is achieved within the first 6 hours after taking the drug as a single dose and is dose-dependent in terms of frequency and maximum reduction.

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

In healthy volunteers, when taking cabergoline at a dose of 0.3-2.5 mg, a pronounced decrease in serum prolactin levels was observed, which was dose-dependent.

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

Pharmacokinetics

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

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

Based on the above information, we can conclude that the half-life of the drug Caberlon in the body is quite long. In patients with hyperprolactinemia, it reaches 79-115 hours. Even after 10 days from the last administration of this drug, up to 18% of the dose is found in the urine (2-3% in its original form) and up to 72% of the dose in the feces.

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Dosing and administration

Caberlon 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, but in each individual case, the duration of treatment should be determined by the attending physician.

Method of administration and dosage: 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-dopa). The parallel dose of levodopa can be gradually reduced, and the dose of cabergoline, on the contrary, can be increased until the optimal ratio is achieved. The maximum dose of the drug should not exceed 3 mg/day. The weekly therapeutic dose of Caberlon is usually 500 mcg, if necessary, it is gradually increased by another 500 mcg per week at intervals of 1 month.

In the case of treating patients with hyperprolactinemia, doses are selected individually. In order to prevent lactation, a single dose of 1 mg of Caberlon is recommended on the first postpartum day. To suppress existing lactation in women, the drug is usually prescribed in a dose of 250 mcg every 12 hours for 2 days.

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Use Caberlon during pregnancy

Caberlon has been tested on animals. In particular, the results of studies have shown its ability to penetrate the placental barrier in rats. Whether this effect occurs in humans is unknown.

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

Due to insufficient clinical experience, as well as the long period of elimination of the drug Caberlon from the body, women planning pregnancy are advised to stop taking it one month before the desired conception. This will prevent possible effects of the drug on the fetus. If pregnancy occurs during the period of taking the drug, it must be immediately discontinued in order to prevent any effects on the fetus.

The ability of cabergoline and its metabolites to penetrate into milk in rats has been proven. According to some assumptions, lactation may be delayed or suppressed when taking Caberlon due to the fact that the drug has dopamine agonist properties.

Due to the lack of any data on the effect of cabergoline on lactation, women are advised to discontinue breastfeeding if any symptoms of the drug's influence appear, in particular, delayed or suppressed lactation.

Contraindications

Caberlon is not recommended for use simultaneously with antibiotics and antipsychotics due to increased bioavailability of cabergoline and the severity of its side effects. It should be noted that symptomatic hypotension may occur after taking Caberlon.

Contraindications for the use of Caberlon:

• serious heart diseases and problems with the cardiovascular system;
• liver and kidney dysfunction;
• the patient has gastric ulcer (including peptic ulcer) and duodenal ulcer;
• occurrence of gastrointestinal bleeding;
• Raynaud's syndrome;
• history of serious mental disorders;
• history of lung diseases (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 for patients with severe liver dysfunction. Caberlon is given with caution when taken simultaneously with drugs that are aimed at reducing blood pressure.

Patients taking dopamine agonists showed signs of hypersexuality, increased libido, and risk-taking.

There is currently no information regarding the effect of alcohol on the tolerability of the drug.

Side effects Caberlon

Caberlon, like any other drug with a similar effect, has a number of side effects.

The side effects of Caberlon are short-term and moderate. Withdrawal syndrome is observed only in very rare cases.

Basically, when taking the drug, side effects occur from the nervous system and gastrointestinal tract and manifest themselves in the form of:

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

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

It should be noted that patients taking Caberlon often experienced heart valve pathology, including regurgitation, as well as associated disorders in the form of pericarditis and pericardial effusion. Other adverse reactions arose due to the vasoconstrictive properties of this drug and concerned the development of angina, peripheral edema, and erythromelalgia. However, no changes in ECG or heart rate were observed during treatment with Caberlon.

Gastric dysfunction was more often observed in women than in men, and CNS side effects were more common in elderly patients.

Taking the drug may also be accompanied by drowsiness, and less commonly, cases of sudden falling asleep.

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

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

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Overdose

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

• decrease in blood pressure,
• skin rash,
• disturbance of consciousness,
• drowsiness,
• psychomotor agitation,
• hallucinations.

Overdose occurs for a number of reasons, most often including a person's tendency to self-medicate, which leads to dangerous consequences, uncontrolled treatment with disregard for doctor's recommendations, as well as over-the-counter dispensing of the drug. Unfortunately, overdose can also be intentional (in the case of a suicide attempt).

In any case, at the first symptoms of overdose of Caberlon, the patient needs urgent medical care. The severity of the condition depends on the age, gender, the presence of concomitant diseases in the patient and the general condition of the body.

Treatment for overdose is symptomatic, with reverse-action drugs administered and measures taken primarily to support the liver.

Interactions with other drugs

Caberlon 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, butyrophenone, phenothiazine, thioxanthene).

Interactions Caberlon with other drugs can cause a number of undesirable effects. For example, when Caberlon is used together with macrolide antibiotics (in particular, erythromycin), the patient may experience an increase in the level of bromocriptine in the blood plasma. This drug should be taken with particular caution in combination with other drugs that are aimed at reducing blood pressure.

Taking into account the currently available information on the metabolism of cabergoline, the pharmacokinetic interaction of the drug Caberlon with other drugs cannot be foreseen in advance. In medical studies of patients with Parkinsonism, the pharmacokinetic interaction of this drug with L-dopa and selegiline was not noted.

As for the effect of alcohol on the tolerability of the drug, there is currently no reliable information on this issue. However, given the negative impact of alcohol on drugs in general, it can be assumed that the simultaneous use of Caberlon with alcohol will have pronounced negative consequences.

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Storage conditions

It is recommended to store Caberlon in its original packaging at an air temperature not exceeding 30 °C. The storage location should be well protected from sunlight and moisture, and inaccessible to small children. It is recommended not to remove the silica gel capsule from the bottle containing the preparation, which is designed to absorb moisture.

Storage conditions of Caberlon also depend on the general requirements for storing medicines. Following them, this drug should be kept away from light, preferably in a dark place. To avoid moisture getting into the tablets, they should be stored in a dry place. Therefore, a bathroom or other room with an unstable humidity level is not suitable for this purpose.

The medicine must not be stored in an open state, as this may lead to the absorption of volatile substances and cause a reaction with oxygen. Therefore, after taking the next dose of the medicine, the bottle must be tightly closed. It is advisable to store the tablets in a sealed factory package, and not pour them into any other container.

It should be remembered that it is best to keep medicines for internal and external use separately. It is advisable in this case to put them on different shelves of the cabinet, or store them in separate bags.

Shelf life

Caberlon is a medicine with clearly defined storage periods. The shelf life of this medicine is 2 years.

The "shelf life" means the period of time during which the medicinal products meet all the conditions and requirements of the relevant documentation, referring to which they were manufactured. The initial shelf life of the product is determined directly by the manufacturer. Then, after the registration of the medicinal product and the start of its industrial production, the manufacturer undertakes to continue research work aimed at studying the stability level of the given medicinal product. Thus, the specified shelf life is confirmed or clarified.

The shelf life of a medicinal product cannot exceed 5 years, even though the final results of its stability studies allow this to be done.

The date of manufacture of the drug Caberlon is the starting date for calculating its shelf life. During storage of the drug, it is necessary to comply with all conditions specified in the instructions and on the packaging label.

After the expiration date, it is strictly forbidden to use any medicine, as this is fraught with irreversible health consequences. Tablets should be stored in their original packaging, in a dry place protected from moisture and sun.