Cavinton forte in ampoules instructions for use. Cavinton tablets - instructions for use, indications. In what cases does cavinton help?

Name:

Cavinton

Pharmacological
action:

Cavinton - drug, improving cerebral circulation, brain metabolism and rheological properties of blood.
Has a cerebroprotective effect. Reduces the severity of damaging cytotoxic reactions caused by stimulating amino acids; inhibits the functional activity of both cellular transmembrane sodium and calcium channels, and NMDA and AMPA receptors. Potentiates the neuroprotective effect of adenosine. Stimulates brain metabolism, enhances the absorption and assimilation of glucose and oxygen by the brain. Stimulates the transport of glucose through the BBB, shifts glucose metabolism in an energetically more favorable aerobic direction. Selectively inhibits Ca2 +-calmodulin-dependent cGMP-phosphodiesterase, increases the concentration of cAMP and cGMP in brain tissues, as well as the concentration of ATP and the ratio of ATP / AMP. Stimulates the cerebral metabolism of norepinephrine and serotonin, stimulates the ascending noradrenergic system, and has an antioxidant effect.
A drug selectively enhances cerebral blood flow: increases brain fraction of minute volume; reduces the resistance of cerebral vessels without affecting the parameters of general circulation (BP, minute volume, heart rate, OPSS).
Does not cause the "steal" phenomenon; on the contrary, its application primarily increases the blood supply to the ischemic, but still viable area with low perfusion - the phenomenon of "reverse steal".
Improves tolerance to hypoxia brain cells, facilitating the transport of oxygen to the tissues due to a decrease in the affinity of red blood cells for it.
The drug improves brain microcirculation, inhibits platelet aggregation, reduces pathologically increased blood viscosity, increases the deformability of erythrocytes and blocks their absorption of adenosine.

Indications for
application:

In neurology- acute and chronic cerebrovascular insufficiency (transient ischemia, progressive stroke, post-stroke conditions, vascular dementia, cerebral atherosclerosis, post-traumatic and hypertensive encephalopathy, vertebrobasilar insufficiency); mental and neurological disorders in patients with cerebrovascular insufficiency (including memory impairment, dizziness, headache, aphasia, apraxia, movement disorders).
In ophthalmology- vascular eye diseases (atherosclerosis, angiospasm of the choroid and retina, degenerative diseases of the choroid, retina or macula, arterial and venous thrombosis or embolism, secondary glaucoma).
In ENT practice- hearing loss (vascular, toxic or age-related), Meniere's disease, cochleovestibular neuritis, tinnitus, dizziness (labyrinthine origin); vasovegetative manifestations of climacteric syndrome.

Mode of application:

Taken orally in the form of tablets (5 mg) 1-2 tablets 3 times a day. Maintenance dose - 1 tablet 3 times a day. Apply for a long time. Improvement is usually observed after 1-2 weeks; course of treatment for about 2 months. and more.
Intravenously(only drip) is used in neurological practice for acute focal ischemic disorders of cerebral circulation (discrepancy between the need for oxygen in the brain tissue and its delivery with blood), in the absence of hemorrhage (bleeding into the brain). Enter first 10-20 mg (1-2 ampoules) in 500-1000 ml of isotonic sodium chloride solution (drip infusion). If necessary, repeat (3 times a day) slow drip infusions are prescribed, then they switch to taking the drug inside.
There is evidence of the use of Cavinton for the prevention of convulsive syndrome in children who have had a brain injury. The drug is administered intravenously at a rate of 8-10 mg/kg per day in a 5% glucose solution with a transition in 2-3 weeks. for oral administration at 0.5-1 mg / kg per day.

Side effects:

From the side of the cardiovascular system: with a frequency of 0.1% - depression of the ST segment and prolongation of the QT interval, tachycardia, extrasystole (the relationship of these disorders with the use of the drug is doubtful due to their spontaneous appearance), with a frequency of 0.8% - slight fluctuations in blood pressure (mainly in downward direction), skin hyperemia, phlebitis.
From the side of the central nervous system (with a frequency of 0.9%): sleep disturbance (insomnia, drowsiness), dizziness, headache, weakness, increased sweating (may be symptoms of the underlying disease).
From the digestive tract(with a frequency of 0.6%): dry mouth, nausea, heartburn.
Allergic reactions: in some cases - skin manifestations of allergies.

Contraindications:

Severe ischemic heart disease, severe arrhythmias (heart rhythm disturbances); do not use during pregnancy. It is not recommended to prescribe the drug for labile (unstable) blood pressure and low vascular tone.

Contraindications:
- known hypersensitivity to vinpocetine;
- acute phase of hemorrhagic stroke;
- severe form of coronary heart disease;
- severe forms of arrhythmia;
- pregnancy;
- lactation period;
- children under 18 (due to insufficient data).
Extras for tablets: lactose intolerance.

Injectable solution is incompatible with heparin. Do not inject the solution under the skin.

special instructions

Cavinton does not have a hepato- and nephrotoxic effect, therefore, when prescribing the drug to patients with liver and kidney diseases, correction of the dosing regimen is not required.
In case of lactose intolerance, please note that each tablet contains 83 mg of lactose.
Pediatric use
It is not recommended to prescribe the drug to children under the age of 18 due to the lack of experience with Cavinton in this category of patients.

Interaction
other medicinal
by other means:

Combined therapy with Cavinton and anticoagulants, if necessary, is acceptable.

Not seen with concomitant use with pindolol, clopamide, glibenclamide, digoxin, acenocoumarol and hydrochlorothiazide; imipramine.

In rare cases, concomitant use with α-methyldopa accompanied by some increase in the hypotensive effect, when using this combination, regular monitoring of blood pressure is necessary.

Despite the lack of data confirming the possibility of interaction, it is recommended to exercise caution when administered simultaneously with drugs of central, antiarrhythmic and anticoagulant action.

Cavinton® concentrate for solution for infusion and heparin are chemically incompatible, therefore their administration in one infusion mixture is prohibited, however, treatment with anticoagulants and vinpocetine can be carried out simultaneously.

Cavinton® concentrate for solution for infusion is incompatible with infusion solutions containing amino acids, therefore they cannot be used to dilute the drug.

Pregnancy:

Vinpocetine crosses the placental barrier, while the concentration of the drug in the placenta and in the blood of the fetus is lower than in the blood of a pregnant woman. The teratogenic effect of the drug has not been identified. In preclinical studies of the use of the drug in high doses, in some cases, placental bleeding and spontaneous abortion were noted, possibly as a result of increased placental blood supply.
Vinpocetine passes into breast milk. In preclinical studies using a radioactive isotope, the radioactivity of breast milk was 10 times higher than that in the blood of an adult animal.
The use of vinpocetine during lactation is contraindicated due to the excretion of vinpocetine with breast milk and the lack of a sufficient number of clinical observations regarding the safety of the drug in infants. After a single dose of vinpocetine within an hour, 0.25% of the accepted dose of the drug penetrates into breast milk.

Cavinton is a representative of a group of drugs, the main therapeutic effect of which is the effect on the nervous system. The main active ingredient of the drug is vinpocetine.

According to the ATC code, Cavinton refers to psychostimulants that have an effect on the cognitive functions of the brain. In addition, the drug is considered a nootropic drug, as a result of which it is widely used for disorders in the mental sphere, decreased attention and memory, as well as in the presence of hyperactivity.

Due to the specific structure of the drug, blood circulation is activated in the ischemic areas of the brain, as a result of which their functionality is normalized. In addition, sufficient blood supply is restored, which contributes to the improvement of the general condition and stimulation of cognitive functions.

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ATX code

N06BX18 Vinpocetine

Active ingredients

Vinpocetine

Pharmacological group

Correctors of cerebrovascular disorders

pharmachologic effect

Drugs that improve cerebral circulation

analeptic preparations

Indications for use Cavinton

The drug has proven its effectiveness in various pathological conditions in ophthalmology, neurology, neurosurgery and many other medical fields. Cerebrovascular pathology is considered the main indication for treatment in neurology.

Cavinton is used to restore blood supply to all areas of the brain that do not receive enough oxygen and nutrients as a result of a stroke.

Indications for the use of Cavinton include dementia of vascular origin, vertebrobasilar insufficiency, damage to atherosclerotic plaques of cerebral vessels and encephalopathy, the development of which is based on a persistent increase in pressure or injury.

With the help of Cavinton, there is a decrease in the intensity of neurological and mental symptoms, the cause of which is the vascular pathology of the brain.

Disturbances in the blood supply of vascular origin in the retina and choroid - indications for the use of Cavinton in ophthalmology.

In ENT practice, the drug is used with therapeutic need for hearing loss of the perceptual form of age-related genesis to restore local blood circulation. In addition, Cavinton successfully eliminates the clinical manifestations of Meniere's disease, as well as tinnitus.

Release form

The dosage form of Cavinton is a tablet form and a solution for infusion. The main physical and chemical characteristics of the drug are white (almost white) color and flat round shape of the tablet. Its diameter is about 9 mm. On the surface on one side the inscription "CAVINTON" is applied.

Cavinton contains 5 mg of vinpocetine, which is considered the main active ingredient of the drug. Tablets are packaged in blisters, 25 pieces each. One package of the drug contains 2 blisters.

The next form of release is a solution for intravenous use. 1 ml of Cavinton concentrate contains 5 mg of vinpocetine. Important physical and chemical characteristics of the drug is a colorless liquid, sometimes with a greenish tint, and the absence of suspension, which ensures the transparency of the concentrate.

This form of release of the drug is stored in 2 ml ampoules. Each carton contains 10 ampoules. Cavinton in the form of a solution is used in the acute period of the pathological condition, as it has a quick access to the bloodstream of the body.

Pharmacodynamics

Due to the main characteristics of vinpocetine, Cavinton has a complex mechanism of action. It consists in influencing the metabolic processes in the brain and activating local blood circulation, improving the rheological parameters of the blood.

Pharmacodynamics Cavinton performs a protective function for nerve tissues, reducing the negative impact of cytotoxic processes caused by stimulation with amino acids.

The drug blocks receptors and voltage-gated channels for calcium and sodium. In addition, the drug stimulates the protective effect on adenosine neurons.

Vinpocetine stimulates the metabolic processes in brain cells with the help of activated uptake and delivery of glucose and oxygen. The drug increases the resistance of tissues to insufficient oxygen supply, accelerates the transport of glucose, which is one of the important energy processes.

Cavinton increases the amount of ATP, activates the circulation of norepinephrine and serotonin in brain cells, and also stimulates the ascending pathways of the norepinephrine system, which provides a cerebroprotective effect.

Pharmacodynamics Cavinton provides activation of the microvasculature by blocking the "gluing" of platelets, reducing blood viscosity, increasing the ability of red blood cells to change shape and inhibition of adenosine uptake. In addition, there is an accelerated circulation of oxygen in the brain cells.

The drug selectively stimulates blood circulation in the tissues, increasing the cerebral systolic volume of the heart and reducing peripheral vascular resistance, while not affecting the overall blood circulation.

Vinpocetine provides activation of cerebral circulation without "robbing" other tissues and organs. On the contrary, which is typical, the drug increases the blood supply in those areas where there is an insufficient supply of oxygen and nutrients.

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Pharmacokinetics

The drug is rapidly absorbed through the mucosa of the digestive tract after oral use. Already after 1 hour, the maximum level of concentration of the main active component - vinpocetine in the blood is noted. The same time for accumulation in the blood is required for the drug when administered intravenously Cavinton. As the drug passes through the intestinal wall, there are no metabolic processes with its participation.

Pharmacokinetics Cavinton within 2-4 hours causes the greatest accumulation of the drug in the liver. However, it should be noted that the volume of vinpocetine in the brain tissues is much lower than its concentration in the blood.

Only 66% of the drug circulates in the blood in a protein-bound state. Due to the pronounced tissue affinity, vinpocetine provides the maximum therapeutic effect in those areas where it is most important.

The elimination half-life ranges from 3.5 hours to 6 hours, based on the dosage taken. Excretion of vinpocetine is carried out by the intestines (40%) and kidneys (60%), and only 3-5% is excreted unchanged, the remaining 97% are metabolized.

Pharmacokinetics Cavinton ensures the production of apovincamic acid from vinpocetine, which is its main metabolite. An important feature of the drug is the lack of requirements for the selection of individual dosages for people with kidney and liver pathology.

The pharmacodynamic and pharmacokinetic properties of the drug do not differ when used in the elderly or in the presence of concomitant diseases.

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Use Cavinton during pregnancy

Before using any drug, you need to make sure that the person has no contraindications for taking it.

Such a contraindication is the use of Cavinton during pregnancy. At a time when the fetus is intensively growing and developing, not a single negative factor from the pregnant woman or the external environment should act. It can become decisive in the formation of pathology in the fetus, which later manifests itself as insufficient functionality of any organ or system.

The ban on the use of vinpocetine is due to its ability to penetrate into the bloodstream of the fetus, bypassing the placental barrier. The volume of the drug that enters the blood of the fetus is much less than in the circulatory system of a pregnant woman, however, even a small concentration can provoke the development of adverse reactions from the fetus.

The teratogenic and toxic effects of vinpocetine have not been proven, but despite this, the use of Cavinton during pregnancy is prohibited. Thanks to animal studies, it was found that when using high doses of the drug, it provoked the development of placental bleeding, followed by abortion. The reason for the occurrence of adverse reactions is an excessive increase in local blood circulation.

In addition, it is necessary to abandon the use of Cavinton during breastfeeding the baby. Vinpocetine has a high ability to penetrate into breast milk, exceeding the concentration in the blood of a woman by more than 10 times.

With breast milk, up to a quarter of the entire dose of the drug taken can be excreted within an hour. As a result, the baby can receive a large dose of vinpocetine, which threatens his health and possibly even life.

Contraindications

In order to avoid the negative effect of the drug on the body, it is necessary to familiarize yourself with possible contraindications to its use in advance. This will allow you to get the desired therapeutic effect without adverse reactions.

Contraindications to the use of Cavinton include the acute phase of hemorrhagic stroke, severe heart damage due to insufficient supply of oxygen and nutrients to the myocardium (ischemia), as well as severe cardiac arrhythmias.

In addition, it should be remembered that the drug is prohibited for use by pregnant women and those women whose child is breastfed. During pregnancy, when taking the drug, there is a high risk of bleeding and abortion.

Contraindications to the use of Cavinton also prohibit its use under the age of 18, since there is no reliable information about the absence of side effects at this age.

The drug is not recommended to be taken if a person has an individual intolerance to the main active ingredient or auxiliary components. In addition, vinpocetine should be used with caution in the presence of allergic reactions to drugs from the group to which Cavinton belongs.

Particular attention should be paid to taking vinpocetine together with drugs that can lengthen the QT segment on the ECG, which can disrupt the heart. Also among the contraindications is lactose intolerance, since in the presence of this syndrome, the use of Cavinton is limited due to the fact that the drug has 83 mg of lactose monohydrate.

Side effects of Cavinton

Most often, the drug is quite well tolerated by humans, but despite this, it is still recommended to be aware of the possible negative effects that may develop after using vinpocetine.

Their appearance is due to the individual characteristics of the body and its reaction to certain components of the drug.

Side effects of Cavinton can be manifested by any system of the body. So, due to long-term use of the drug, changes in the circulatory system are possible. The blood picture in this case may display an insufficient number of leukocytes, platelets, erythrocytes with their possible gluing.

The immune response to the use of vinpocetine is manifested by a hypersensitivity reaction, and metabolic disorders are manifested by an increase in cholesterol, the development of diabetes mellitus and a decrease in appetite.

Side effects of Cavinton from the side of the central nervous system are represented by insomnia, tremor, headaches, convulsions, dizziness, changes in skin sensitivity, amnesia, depressive or euphoric state.

In addition, in rare cases, swelling of the papilla of the optic nerve, hyperemia of the conjunctiva of the eyes, an increase in the hearing threshold and an increase in tinnitus are possible. The use of the drug may cause fluctuations in blood pressure. In addition, due to myocardial ischemia, the risk of developing a heart attack increases.

On the part of the gastrointestinal tract after using Cavinton, an uncomfortable sensation in the abdomen, dryness in the oral cavity, intestinal dysfunction, nausea, vomiting and ulcerative lesions of the oral mucosa may appear.

It happens that the skin can become covered with a rash, itching, erythema, dermatitis and hyperhidrosis appear. The general condition of a person worsens due to weakness, a feeling of heat and discomfort in the chest area.

Laboratory and instrumental examination may reveal some deviations. Among them, it is worth paying attention to an increase in the amount of triglycerides, an increase / decrease in eosinophils, activation of liver enzymes, and ST depression on the ECG.

Dosage and administration

Based on the severity of the pathology, the patient's age and comorbidity, the method of application and dose of Cavinton is selected.

It is forbidden to administer vinpocetine intramuscularly, as well as intravenously without preliminary dilution of the concentrate. The initial dosage is most often 20 mg of the drug, diluted in 500 ml of solution. This dose can be increased up to 1 mg/kg/day for 2-3 days, taking into account the tolerability of the drug.

On average, the therapeutic course is up to 2 weeks. With a weight of 70 kg, the usual dose is 50 mg / day, diluted in 500 ml of solution.

To dilute the vinpocetine concentrate, saline or a solution with glucose is used. It is worth highlighting that when diluting the drug, it should be used within 3 hours.

The method of administration and doses after the end of the acute period of the pathological condition are selected individually, but in most cases Cavinton is used in tablet form.

Cavinton with a dosage of 5 mg can be taken 1 tablet three times a day for several weeks to months. In old age, as well as in the presence of liver and kidney dysfunction, vinpocetine does not require correction.

The drug can be used for monotherapy or for complex treatment in order to restore cerebral circulation and normalize cognitive functions.

Overdose

When using the tablet form of Cavinton, an overdose is observed much less frequently than when using vinpocetine concentrate.

A feature of the solution is the obligatory slow introduction and observance of a certain speed. If the dose exceeds 1 mg / kg / day, the likelihood of an overdose increases.

As for Cavinton tablets, they have a certain dosage, which, if the frequency of administration is observed, excludes the development of an overdose.

The maximum dose per day for tablets is 60 mg, which should not be exceeded. Usually prescribed 1-2 tablets with a dosage of 5 mg three times a day.

In addition, when taking 360 mg Cavinton, no side effects from the heart, vascular or digestive systems were observed.

In case of exceeding the dosage, it is necessary to carry out a gastric lavage in a hospital to prevent further absorption of the drug into the bloodstream. If vinpocetine was administered intravenously, then it is recommended to use solutions for detoxification and stimulate urination with diuretics.

Throughout the decrease in concentration due to an overdose, the work of the heart and respiratory system should be monitored.

Excipients: colloidal silicon dioxide, magnesium stearate, talc, corn starch, lactose monohydrate.

25 pcs. - blisters (2) - packs of cardboard.

pharmachologic effect

The mechanism of action of vinpocetine consists of several elements: it improves cerebral blood flow and brain metabolism, and has a beneficial effect on the rheological properties of blood.

The neuroprotective effect is realized by reducing the adverse cytotoxic effect of excitatory amino acids. It blocks voltage-dependent Na + and Ca 2+ channels and NMDA and AMPA receptors. Increases the neuroprotective effect of adenosine. Vinpocetine stimulates the metabolism of the brain: it increases the uptake and consumption of oxygen. Increases tolerance to hypoxia; increases the transport of glucose, the only source of energy for brain tissue, through the BBB; shifts glucose metabolism towards the energetically more favorable aerobic pathway. Selectively inhibits Ca 2+ -calmodulin-dependent cGMP-phosphodiesterase; increases the content of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) of the brain, the concentration of ATP and the ratio of ATP / AMP in the brain tissues; enhances metabolism and norepinephrine in the brain, stimulates the noradrenergic neurotransmitter system, and also has an antioxidant effect; as a result of all these effects, vinpocetine has a cerebroprotective effect.

Improves microcirculation in the brain by inhibiting platelet aggregation, reducing pathologically increased blood viscosity, increasing the ability of red blood cells to deform and inhibiting the capture of adenosine; promotes the passage of oxygen into cells by reducing the affinity of red blood cells for it. Selectively increases cerebral blood flow due to an increase in cerebral ejection fraction, a decrease in cerebral vascular resistance without a significant effect on systemic circulatory parameters (BP, cardiac output, heart rate, OPSS); does not have a "steal" effect. Against the background of the use of vinpocetine, the blood supply to damaged (but not yet necrotic) ischemic areas with low perfusion improves ("reverse steal effect").

Pharmacokinetics

Suction

Vinpocetine is rapidly absorbed after oral administration and reaches Cmax in the blood after 1 hour. Absorption occurs mainly in the proximal intestine. It is not metabolized when passing through the intestinal wall. Bioavailability when taken orally - 7%.

Distribution

In preclinical studies of oral administration of radioactively labeled vinpocetine, it was determined in the highest concentrations in the liver and gastrointestinal tract. C max in the tissues is observed 2-4 hours after ingestion. The amount of radioactive isotope in the brain did not exceed that in the blood. Protein binding in the human body - 66%. V d is 246.7 ± 88.5 l, which indicates a significant distribution in tissues. Clearance is 66.7%, which exceeds the plasma volume of the liver (50 l / h), metabolism is predominantly extrahepatic.

With repeated administration at a dose of 5 and 10 mg, the kinetics of vinpocetine is linear. C ss were 1.2±0.27 ng/ml and 2.1±0.33 ng/ml, respectively.

Metabolism

The main metabolite of vinpocetine is apovincamic acid (AVA), whose share in humans is 25-30%. After taking vinpocetine orally, AUC of AVK is 2 times higher than that after intravenous administration. This indicates that VKA is formed during the first pass metabolism of vinpocetine. Other known metabolites are hydroxyvinpocetine, hydroxy-AVK, dihydroxy-AVK-glycinate, as well as their conjugates with glucuronides and/or sulfates.

breeding

T 1/2 in humans is 4.83 ± 1.29 hours. In studies with a radioactive label, the drug was excreted by the kidneys and through the intestines in a ratio of 60:40. In preclinical studies, a significant part of the radioactivity was detected in bile, but no significant enterohepatic circulation was found. In preclinical studies, it was found that unchanged vinpocetine is excreted in a small amount. Apovincaminic acid is excreted by the kidneys by simple glomerular filtration, T 1/2 depends on the dose taken and the route of administration of vinpocetine.

Pharmacokinetics in selected groups of patients

It was found that the pharmacokinetics of vinpocetine in elderly patients does not differ significantly from that in young patients, there is no cumulation of the drug. Therefore, vinpocetine can be prescribed to patients with impaired liver and kidney function for a long time and in normal doses.

Indications

Neurology:

- reduction in the severity of neurological and mental disorders in various forms of cerebral circulatory insufficiency (symptomatic therapy for the consequences of ischemic stroke, vertebrobasilar insufficiency, vascular dementia, cerebral atherosclerosis, post-traumatic and hypertensive encephalopathy);

Ophthalmology:

- chronic vascular diseases of the retina and choroid;

Otorhinolaryngology:

- for the treatment of hearing loss of the perceptual type, Meniere's disease, sensation of tinnitus.

Contraindications

- galactose intolerance, lactase deficiency, glucose-galactose malabsorption;

- pregnancy;

- the period of breastfeeding;

- age up to 18 years (due to insufficient data);

- hypersensitivity to vinpocetine or other components of the drug.

Carefully: long QT interval syndrome, taking drugs that cause a prolongation of the QT interval.

Dosage

Accept inside, after food.

Usually the daily dose is 15-30 mg (5-10 mg 3 times / day).

The initial daily dose is 15 mg. The maximum daily dose is 30 mg.

At kidney and liver diseases the drug is prescribed in the usual dose, the absence of cumulation allows for long courses of treatment.

Side effects

In clinical studies, the most common adverse reactions occurred in the following system organ classes (according to MedDRA classification), which are listed according to the frequency of occurrence: infrequently (from ≥1 / 1000 to<1/100), редко (от ≥1/10 000 до <1/1000); очень редко (<1/10 000).

From the hematopoietic system: rarely - leukopenia, thrombocytopenia; very rarely - anemia, erythrocyte agglutination.

From the immune system: very rarely - hypersensitivity reactions.

From the side of metabolism and nutrition: infrequently - hypercholesterolemia; rarely - loss of appetite, anorexia, diabetes mellitus.

Mental disorders: rarely - insomnia, sleep disturbance, anxiety; very rarely - euphoria, depression.

From the nervous system: infrequently - ; rarely - dizziness, taste disorder, stupor, unilateral paresis, drowsiness, amnesia; very rarely - tremor, spasms.

From the side of the organ of vision: rarely - swelling of the nipple of the optic nerve; very rarely - conjunctival hyperemia.

On the part of the organ of hearing and labyrinth disorders: infrequently - vertigo; rarely - hyperacusis, hypoacusis, tinnitus.

From the side of the cardiovascular system: infrequently - a decrease in blood pressure; rarely - myocardial ischemia / infarction, angina pectoris, bradycardia, tachycardia, extrasystole, palpitations, increased blood pressure, hot flashes, thrombophlebitis; very rarely - blood pressure lability, arrhythmia, atrial fibrillation.

From the digestive system: infrequently - abdominal discomfort, dry mouth, nausea; rarely - epigastric pain, constipation, diarrhea, dyspepsia, vomiting; very rarely - dysphagia, stomatitis.

From the skin and subcutaneous tissues: rarely - erythema, hyperhidrosis, itching, urticaria, rash; very rarely - dermatitis.

General disorders and disorders at the injection site: rarely - asthenia, malaise, feeling of heat; very rarely - a feeling of discomfort in the chest, hypothermia.

Laboratory and instrumental data: rarely - hypertriglyceridemia, ST segment depression on the ECG, decrease / increase in the number of eosinophils, increased activity of liver enzymes; very rarely - a decrease / increase in the number of leukocytes, erythropenia, a decrease in thrombin time, an increase in body weight.

Overdose

There are no data on overdose with vinpocetine. A single dose of 360 mg of vinpocetine did not cause clinically significant reactions, incl. from the cardiovascular system.

Treatment: gastric lavage, activated charcoal, symptomatic therapy.

drug interaction

Interaction is not observed with simultaneous use with (chloranolol, pindolol), clopamide, glibenclamide, digoxin, acenocoumarol, hydrochlorothiazide and imipramine.

The simultaneous use of vinpocetine and alpha-methyldopa sometimes caused some increase in the hypotensive effect, therefore, with this treatment, regular monitoring of blood pressure is required.

Despite the lack of data confirming the possibility of interaction, it is recommended to exercise caution when administered simultaneously with drugs that act on the central nervous system, and with antiarrhythmic and anticoagulant drugs.

special instructions

The presence of the syndrome of prolonged QT interval and the use of drugs that cause prolongation of the QT interval requires periodic monitoring of the ECG.

1 tablet of the drug contains 140 mg of lactose monohydrate. Patients with rare hereditary problems of galactose intolerance, lactase deficiency or glucose-galactose malabsorption should not take this medicine.

Influence on the ability to drive vehicles and mechanisms

Data on the effect of vinpocetine on the ability to drive vehicles and work with mechanisms are not available.

Pregnancy and lactation

Pregnancy

Vinpocetine crosses the placental barrier and is therefore contraindicated in pregnancy. At the same time, its concentration in the placenta and in the blood of the fetus is lower than in the blood of a pregnant woman. Teratogenic and embryotoxic effects have not been identified. In animal studies, placental bleeding and spontaneous abortions occurred with the introduction of large doses, probably as a result of increased placental blood flow.

breastfeeding period

Vinpocetine passes into breast milk. In studies using labeled vinpocetine, the radioactivity of breast milk was ten times higher than that of maternal blood. Within 1 hour, 0.25% of the accepted dose of the drug penetrates into breast milk. Since vinpocetine passes into breast milk, and there are no data on the effect of vinpocetine on infants, the use of the drug during breastfeeding is contraindicated.

Application in childhood

Use is contraindicated under the age of 18 years (due to insufficient data).

For impaired renal function

At kidney disease

For impaired liver function

At liver diseases the drug is prescribed in the usual dose.

Terms of dispensing from pharmacies

The drug is dispensed by prescription.

Terms and conditions of storage

The drug should be stored in its original packaging to protect from light, out of reach of children at a temperature not exceeding 30°C. Shelf life - 5 years. Do not use after the expiry date stated on the packaging.

Instructions for medical use

medicinal product

Cavinton®

Tradename

Cavinton®

International non-proprietary name

Vinpocetine

Dosage form

Solution for injection 10 mg/2 ml

Compound

2 ml of solution contains

active substance- vinpocetine 10 mg,

Excipients: ascorbic acid, sodium metabisulphite, tartaric acid, benzyl alcohol, sorbitol, water for injection.

Description

Colorless or slightly greenish clear solution

Pharmacotherapeutic group

Psychoanaleptics. Psychostimulants and nootropics. Psychostimulants and nootropics others. Vinpocetine

ATX code N06BX18

Pharmacological properties

Pharmacokinetics

When administered intravenously in the process of metabolism of the primary passage through the liver, 25-30% of vinpocetine is converted into apo-vincamic acid (AVA). Diseases of the liver and kidneys do not affect the metabolism of vinpocetine. Binding to blood proteins is 66%. The volume of distribution is 246.7 ± 88.5 l, which indicates a good distribution in the tissues. The clearance value of vinpocetine (66.7 l / h) exceeds the values ​​​​in plasma and in the liver (50 l / h), which indicates extrahepatic metabolism of the compound.

It penetrates well into various tissues and body fluids, including cerebrospinal fluid. The half-life is 4.83 ± 1.29 hours. It is excreted by the kidneys and through the gastrointestinal tract. Removal of apovincamic acid is carried out by glomerular filtration. The half-life depends on the dose of vinpocetine and the dosing regimen.

Elderly age: there are no significant differences in the kinetics of the drug in elderly and young patients, the drug does not accumulate. For patients with chronic diseases of the liver and kidneys, the drug is prescribed in the usual dose, the absence of cumulation allows for long courses of treatment.

Pharmacodynamics

Vinpocetine is a compound with a complex mechanism of action that has a beneficial effect on brain metabolism and improves its blood supply, as well as improves blood rheology.

The neuroprotective effect of vinpocetine is associated with the blockade of voltage-dependent Na + and Ca 2+ tubules and the protection of neurons from inadequate Na + influx under hypoxic conditions and the excess Ca 2+ influx into the cell caused by it. The interaction of vinpocetine with glutamate receptors protects nerve cells from the cytotoxic effects of glutamate and N-methyl-D-aspartate, as well as alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid.

Vinpocetine enhances the neuroprotective effect of adenosine by blocking its utilization. It has a direct antioxidant effect, preventing the formation of reactive substances.

Vinpocetine stimulates cerebral metabolism: the drug increases the uptake of glucose and oxygen, increasing the consumption of these substances by the brain tissue. The drug increases the resistance of the brain to hypoxia; increases the transport of glucose - an exclusive source of energy for the brain - through the blood-brain barrier; shifts glucose metabolism towards an energetically more favorable aerobic pathway; selectively inhibits Ca 2+ -calmodulin-dependent enzyme cGMP-phosphodiesterase (PDE); increases the levels of cAMP and cGMP in the brain. The drug increases the concentration of ATP and the ratio of ATP / AMP; enhances the turnover of norepinephrine and serotonin in the brain; stimulates the ascending noradrenergic system; has antioxidant activity; as a result of all the above effects, vinpocetine has a cerebroprotective effect.

Vinpocetine improves microcirculation in the brain: the drug inhibits platelet aggregation; reduces pathologically increased blood viscosity; increases the deformability of erythrocytes and inhibits the capture of adenosine; improves the transport of O 2 in tissues by reducing the affinity of O 2 to erythrocytes.

Vinpocetine selectively increases blood flow in the brain: the drug increases the cerebral fraction of cardiac output; reduces vascular resistance in the brain without affecting systemic circulation parameters (blood pressure, cardiac output, pulse rate, total peripheral resistance); the drug does not cause a “steal effect”. Moreover, the drug improves blood flow to damaged (but not yet necrotic) ischemic areas with low perfusion (“reverse steal effect”).

As a result of such a complex mechanism of action, Vinpocetine accelerates the regression of cerebral and focal symptoms, improves memory, attention, and intellectual productivity.

Indications for use

transient cerebral ischemia

Cerebral ischemic stroke

Conditions after cerebral stroke

Dementia due to multiple brain lesions

Atherosclerosis of cerebral vessels

Post-traumatic and hypertensive encephalopathy

Vertebrobasilar insufficiency

Mental and neurological disorders caused by cerebrovascular insufficiency

Ophthalmic diseases of the retina and choroid (caused by atherosclerosis, arterial or venous thrombosis and embolism, angiospasm)

Diseases of the inner ear (hearing loss due to vascular disease or toxic effects (including iatrogenic), Meniere's disease, tinnitus

Dosage and administration

Intended for intravenous infusion, administered slowly (infusion rate should not exceed 80 drops/min!).

It is forbidden to administer intramuscularly and in a concentrated form intravenously!

To prepare the infusion, you can use saline or infusion solutions containing glucose (Salsol, Ringer, Rindex, Rheomacrodex). The infusion solution with Cavinton® should be used within the first 3 hours after preparation.

Initial daily dose: 20 mg (2 amps) in 500 ml infusion solution for intravenous administration. Depending on the tolerance of the patient, the dose can be increased within 2-3 days, but not more than 1 mg/kg of body weight. The average course of treatment is 10-14 days, the average daily dose is 50 mg with a body weight of 70 kg (5 amps in 500 ml of infusion solution).

Patients with diseases of the liver and kidneys can be prescribed in the same doses.

Side effects

Infrequently ( > 1/1000 <1/100)

feeling hot

Lowering blood pressure

Euphoria

Rarely ( > 1/10000 <1/1000)

Headache, dizziness, drowsiness, restlessness, hemiparesis

Hearing loss, hyperacusis, hypoacusis

Myocardial ischemia/infarction, exertional angina, arrhythmia, bradycardia, tachycardia, extrasystoles, palpitations

Hemorrhage in the anterior chamber of the eye, hypermetropia, decreased visual acuity, myopia

Increased blood pressure, prolongation of the QT interval, depression of the ST segment on the ECG

Hot flashes, asthenia, chest discomfort, injection site thrombosis

Nausea, dry mouth, abdominal discomfort

Erythema, hyperhidrosis, urticaria

Thrombocytopenia, erythrocyte agglutination

Hypercholesterolemia, diabetes mellitus

Increasing the concentration of urea in the blood

Very rarely (<1/10000)

Depression, tremor, loss of consciousness, presyncope

Anorexia, vomiting, hypersecretion of saliva

Heart failure, atrial fibrillation, prolongation of the PR interval on the ECG

Thrombophlebitis

Conjunctival hyperemia, papilledema, diplopia

Noise in ears

Skin itching, dermatitis

Increased activity of lactate dehydrogenase

Contraindications

Hypersensitivity to any component of the drug

Acute cerebral hemorrhage

Severe ischemic heart disease

Severe cardiac arrhythmias

Pregnancy and lactation

Children and adolescents up to 18 years of age

Individuals with hereditary fructose intolerance

Drug Interactions

Cavinton® solution is chemically incompatible with heparin, so their administration in the same syringe is prohibited.

Cavinton® solution is chemically incompatible with infusion solutions containing amino acids, therefore they cannot be used to dilute the Cavinton® injection form.

The simultaneous use of vinpocetine and alpha-methyldopa can cause an increase in the hypotensive effect, therefore, when they are used together, regular monitoring of blood pressure is required.

Despite the lack of data from clinical studies confirming the possibility of interaction, it is recommended to exercise caution when prescribing vinpocetine with drugs that act on the central nervous system, antiarrhythmic drugs and anticoagulants. However, if necessary, the simultaneous use of anticoagulants and Cavinton® is permissible.

special instructions

In the case of increased intracranial pressure, taking antiarrhythmic drugs, cardiac arrhythmias or prolongation of the QT interval, Cavinton® is prescribed after a thorough assessment of the intended benefit and potential risk to the patient.

The presence of the syndrome of prolonged QT interval and the simultaneous use of drugs that cause QT prolongation require periodic monitoring of the electrocardiogram.

Cavinton® injection solution contains sorbitol (160 mg / 2 ml), therefore, if a patient has diabetes, it is necessary to control blood sugar levels.

In case of fructose intolerance or fructose 1,6-diphosphatase deficiency, the drug should be avoided.

Features of the influence of the drug on the ability to drive a vehicle or potentially dangerous mechanisms

There are no data confirming the adverse effect of vinpocetine on the ability to drive a car and potentially dangerous mechanisms, but given the possibility of developing side effects such as dizziness, drowsiness, care should be taken.

Overdose

Cavinton is a drug whose action is aimed at regulating blood circulation in the brain and improving brain metabolism. The drug is used in neurological practice for the treatment of patients of different age categories. It is well tolerated and has a minimum of side effects. The main active ingredient of the drug is vinpocetine, which improves oxygen metabolism and has an antithrombotic and vasodilating effect, thereby improving cerebral circulation.

Numerous medical studies have proven the high therapeutic efficacy of the drug. After the course of therapy, patients noted the restoration of the ability to concentrate, assimilate and remember information. The use of Cavinton helps to improve memory, prevent degenerative changes in atherosclerosis of the eye vessels and hearing loss, as well as disorders of nervous activity caused by menopause. The drug is widely used for the prevention of strokes, in the treatment of vegetovascular dystonia and ischemic disorders.

Cavinton - the effect of the drug

Cavinton is a drug belonging to a large pharmacological group of nootropics. It improves blood circulation and metabolic processes in the brain. The active substance - vinpocetine has a direct effect on the smooth muscles of the walls of blood vessels. In the affected area, spasmodic vessels relax and expand, blood circulation normalizes, carrying oxygen and nutrients to those parts of the brain where tissues experience hypoxia. Due to this, metabolic processes in the brain cells are normalized, the consumption of glucose and oxygen increases, the exchange of serotonin and norepinephrine increases. The drug has a number of therapeutic effects:

• It has a neuroprotective effect, that is, it increases the resistance of the brain to various toxic and harmful influences and helps to restore the functions of nerve cells.
• Helps brain cells to absorb glucose and increases the amount of specific substances (ATP) that provide energy to nerve cells.
• Stimulates and accelerates metabolism (metabolism) in brain tissues.
• It has an antioxidant effect, reducing the adverse effects of free radicals.
• Normalizes blood circulation in the brain due to the expansion of blood vessels. A pronounced positive result is first observed precisely in those parts of the brain that suffer most from a lack of oxygen. This is the main feature of the drug, making it indispensable in the treatment of strokes.
• Increases the ability of red blood cells to penetrate the walls of capillaries and deliver oxygen to those tissues that lack it.
• Reduces the increased viscosity of the blood, due to which the blood flow in the brain is significantly accelerated.

In addition to the fact that Cavinton protects brain cells from any adverse effects (, toxic substances), it also has an antithrombotic effect. That is, the drug prevents platelets from sticking together and prevents the formation of blood clots that can cause a stroke and other serious disorders.

At the same time, the ability expanding blood vessels can be dangerous, as this can cause a sharp decrease in blood pressure and problems with the cardiovascular system. But in practice, such conditions are rare.

Cavinton is able to selectively increase cerebral blood flow, that is, the blood first of all flows to the ischemic area of ​​the brain, which suffers most from hypoxia (lack of oxygen). Only after this, the effect of the drug extends to other viable areas with poor blood flow.

The use of Cavinton allows you to restore the functions of brain cells, improve memory, speech, coordination of movements, and prevent the manifestations of senile dementia. The drug improves the condition of patients with migraine, increased meteosensitivity, vegetative-vascular dystonia, including in women during menopause. By increasing the ability to endure physical and mental stress, removing vascular symptoms, Cavinton significantly improves the quality of life of patients.

The drug is rapidly absorbed after ingestion (in 1-2 hours). The maximum concentration in the brain tissues is reached within 4 hours. The active substance easily passes through the barrier between blood and tissues. It is excreted by the kidneys and organs of the gastrointestinal tract.

The composition of the drug and the form of release

Cavinton is produced in several varieties:

• Cavinton 5mg. Round, flat tablets, odorless, white. The surface is chamfered and the name "CAVINTON" is engraved on one side. One tablet contains 5 mg of vinpocetine. The package contains 50 tablets (two blisters of 25 pieces).
• Cavinton Forte 10 mg. Tablets with slightly bevelled edges, white or with a yellowish tinge, on one side are engraved "10 mg". One tablet contains twice the amount of vinpocetine - 10 mg. The package contains 30 or 90 tablets.

Of the excipients, the tablets include: magnesium stearate, talc, starch, lactose, colloidal silica.

• A concentrated solution for injections (infusions) is produced in ampoules of 2 ml. One ampoule with a clear, colorless or greenish solution contains 10 mg of vinpocetine. The package contains 10 ampoules with Cavinton's solution.

As additional components in the composition of the concentrated solution, there are benzene alcohol, sorbitol, tartaric and ascorbic acids, sodium metabisulfate.

Indications for use

Cavinton is used for various diseases and, in addition to neurological practice, is used to treat pathological conditions in other areas of medicine.

In neurology the drug is used to treat the following conditions:

• Insufficiency of cerebral circulation in acute or chronic form (cerebral ischemia, progressive stroke or post-stroke conditions)
• Atherosclerotic changes in cerebral arteries
• Encephalopathies
• Vascular Disorders
• Vertebrobasilar insufficiency
• Neurological or mental disorders that develop as a result of cerebrovascular insufficiency (impaired memory, speech, coordination of movements, apraxia, headaches, dizziness)
• Manifestations of vegetative - vascular dystonia

In ophthalmology the drug is used for the following disorders:

• Visual disturbances caused by embolism, thrombosis, angiospasm, atherosclerosis of the eye vessels
• Secondary glaucoma
• Age-related changes affecting the retina and choroid of the eyes

The drug is used in the following cases:

• Senile hearing loss
• Hearing loss caused by vascular disorders, toxic effects from taking certain drugs
• Idiopathic tinnitus
• Meniere's disease
• Vertigo of labyrinthine origin
• Neuritis cochleovestibular

Cavinton is effective in the treatment of ophthalmic diseases of a vascular nature, when, against the background of a spasm of cerebral vessels, the blood supply to the optic nerve and retina suffers.

Taking the drug in these cases helps to improve blood circulation and restore vision. With hearing impairment and diseases of the auditory nerve, the drug helps to eliminate vascular and toxic disorders and cope with pathological changes.

(Meet also the highly effective drug Mexidol, which improves cerebral circulation -)

Instructions for use

Instructions for the use of Cavinton as a standard treatment regimen prescribes taking tablets after meals, three times a day. The initial dose in the acute period is 15-30 mg. When carrying out maintenance therapy, it is enough to take 1 tablet of the drug 3 times a day. Cavinton Forte 10 mg is taken three times a day, one tablet.

The maximum dose that can be taken during the day should not exceed 30 mg. Upon completion of the course of therapy, the dose of the drug should be gradually reduced over 3 days, it is not recommended to abruptly cancel the drug.

Patients begin to feel the therapeutic effect after a week from the start of treatment. The course of treatment with Cavinton is long and takes from 1 to 3 months. In the treatment of patients with pathology of the liver and kidneys, the drug is used in a standard dose.

Cavinton's solution is used for acute ischemic disorders of cerebral circulation and neurological diseases. The concentrated solution for injection is intended for intravenous administration. The concentrate should be diluted before the procedure. For these purposes, saline or dextrose solutions are used. Intravenously, the medicine is poured using a dropper, do it slowly, at a speed of no more than 80 drops per minute. It is forbidden to inject the drug into a vein by jet. The prepared solution must be used within three hours after dilution.

As an initial daily dose, 20 mg of the drug diluted in 500-1000 ml of saline is used. Depending on how the drug is tolerated by the patient, the daily dose can be increased over the next 3 days. The required dosage will be determined by the doctor. The duration of therapy is from 10 to 14 days, after which it is recommended to switch to taking the drug in tablets.

Cavinton for children

Cavinton is prescribed for children strictly according to the doctor's indications for perinatal injuries of the nervous system or for the prevention of convulsive syndrome after brain injuries. For infusions, the drug is used at a dose of 8-10 mg per 1 kg of body weight. Intravenous administration of the solution using a dropper is carried out once a day. After two weeks of treatment, they switch to taking Cavinton tablets, the dose of the drug for children is calculated by the attending physician.

In pediatric practice, Cavinton is used for encephalopathies that appear as a result of birth trauma or hypoxic conditions. If such children are not prescribed adequate treatment in time, then severe pathologies may develop. For children with lactose intolerance, the drug in tablets should be prescribed with extreme caution, since this substance is present in their composition.

Contraindications

Cavinton is contraindicated in the following conditions:

• Hemorrhagic stroke in the acute phase
• Arrhythmia in severe form
• Severe coronary heart disease
• Pregnancy, lactation
• Hypersensitivity to vinpocetine

Side effects

When using the drug, adverse reactions are rare, but in some cases the following conditions may develop:

1. From the CNS: weakness, headache, dizziness, sleep disturbances, expressed in excessive drowsiness or insomnia.
2. From the side of the cardiovascular system: pressure jumps (more often there is a decrease in blood pressure), a feeling of hot flashes, accompanied by reddening of the skin, symptoms of tachycardia, extrasystole.
3. From the gastrointestinal tract: dry mouth, nausea, heartburn.
4. allergic reactions: rash, urticaria, hyperemia of the skin, increased sweating.

Some patients, when taking the drug, note an increase in appetite and a constant feeling of hunger.

drug interaction

Cavinton is incompatible with heparin, these drugs cannot be administered simultaneously and combined in one infusion mixture. The solution of the drug intended for intravenous injection should not be used with infusion solutions containing amino acids. With extreme caution, Cavinton is prescribed with simultaneous treatment with antiarrhythmic drugs. You can prescribe the combined use of vinpocetine and anticoagulants.

Cavinton infusion solution contains sorbitol, therefore, when treating patients with diabetes, it is necessary to control the level of glucose in the blood. With fructose intolerance, vinpocetine should be avoided. It should be remembered that this drug should not be administered subcutaneously. During treatment with the drug, you should not take alcoholic beverages. Patients taking drugs to lower blood pressure, the drug should be administered with caution.

With special attention, it is necessary to select the dosage of the drug for persons driving vehicles or, by the nature of their professional activities, employed in industries that require increased attention and speed of reaction.

In no case should you self-medicate and use the drug without consulting a doctor, this can lead to unwanted complications. The specialist will select the treatment regimen and dosage individually, taking into account possible contraindications, the severity of the disease and the general condition of the patient.

In general, patients are satisfied with the effectiveness of this drug. Its advantages include a quick therapeutic result, which is noticeable after a week of use and the absence of pronounced side effects. The drug is quite well tolerated and has a minimum of contraindications. Among the shortcomings, a long course of treatment and a high cost of the drug are noted.

Analogues

Cavinton has a number of structural analogues. These are drugs such as:

• Vinpocetine
• Bravinton
• Vero-Vinpocetine
• Nootropil
• Actovegin (More about the drug -)

How much does Cavinton cost and can it be bought without pills? In pharmacies, the drug is dispensed without a prescription. The price of Cavinton tablets is on average:

1. Cavinton 5 mg(50 pieces) - 230-250 rubles
2. Cavinton Forte(30 pieces) - 240 - 280 rubles
3. Concentrated Cavinton solution(10 ampoules) - 250-300 rubles.