Cavinton dropper indications for use. Cavinton injections - features of the appointment. Driving a car and other mechanisms
Cavinton is a drug that improves cerebral circulation and metabolism in the brain. What is this remedy for? Instructions for use recommend taking tablets 5 mg, Forte 10 mg, injections for the treatment of circulatory failure of the brain, vascular eye diseases, hearing loss.
Release form and composition
Produce:
- Tablets 5 mg.
- Cavinton forte tablets 10 mg.
- Concentrate for solution for infusion (injections in ampoules for injection).
The drug contains in its composition the active substance vinpocetine 5 mg. In addition, additional substances are contained. In tablets: talc, silicon dioxide, magnesium stearate, lactose monohydrate and corn starch. In a concentrate for infusions: tartaric acid, sodium disulfite, injection water, benzyl alcohol, ascorbic acid and sorbitol.
pharmachologic effect
The use of Cavinton helps to increase blood flow, dilate cerebral vessels, improve oxygen supply to the brain, and glucose utilization.
After the drug, a moderate decrease in systemic blood pressure is observed. Vasodilation under the action of the drug is possible due to its relaxing effect on smooth muscles.
Also, the drug enhances the exchange of serotonin, norepinephrine in brain tissues, increases the plasticity of red blood cells, and reduces increased blood viscosity. Vinpocetine is the active ingredient in Cavinton. Instructions for use (price, reviews, analogues of tablets and injections will be discussed in the article below) indicates that the active substance increases cerebral blood flow, reduces the resistance of cerebral vessels without a significant change in systemic circulation indicators (BP, minute volume, heart rate, OPSS).
It does not have a "steal" effect, increases blood supply, primarily in ischemic areas of the brain with low perfusion.
What helps Cavinton?
Indications for the use of the drug include: 
- hearing loss of the perceptual type, Meniere's disease, idiopathic tinnitus;
- chronic vascular diseases of the choroid and retina (for example, thrombosis / occlusion / of the central artery or vein of the retina);
- decrease in the severity of neurological and mental symptoms in various forms of cerebral circulatory insufficiency;
- atherosclerosis of cerebral vessels;
- post-traumatic and hypertensive encephalopathy;
- consequences of a stroke.
Why is Cavinton prescribed yet? The agent is indicated for use if the patient has:
- transient ischemic attack;
- vascular dementia;
- vertebrobasilar insufficiency;
- ischemic stroke;
- recovery stage of hemorrhagic stroke.
Instructions for use
Cavinton tablets should be taken 3 times a day, 1-2 tablets. Maintenance dose - 1 tablet three times a day. Treatment with the drug, as a rule, is a long process (from 2 months). When using the medicine according to the indications and in strict accordance with the instructions, the patient's condition usually improves in 1-2 weeks.
Cavinton's solution is used for neurological diseases and acute ischemic focal disorders of cerebral circulation (in the absence of cerebral hemorrhage). The drug is started to be administered with a dosage of 10-20 mg, after dissolving it in 500-1000 ml of isotonic sodium chloride solution.
If there are appropriate indications, Cavinton is administered drip repeatedly (3 times a day), after which it should be switched to tablets.
The drug is also used to prevent children's convulsive syndrome after brain injury. The agent is administered by drip intravenously at a dosage of 8-10 mg / kg of body weight 1 time per day (the drug must first be dissolved in a 5% glucose solution). After 2-3 weeks of such treatment, they switch to the use of tablets inside - 0.5-1 mg / kg of body weight once a day.
Contraindications
- pregnancy;
- lactation period;
- age up to 18 years (due to insufficient data);
- severe arrhythmias;
- known hypersensitivity to vinpocetine;
- acute phase of hemorrhagic stroke;
- severe form of coronary artery disease.
Side effects
- headache;
- dizziness;
- ECG changes (ST depression, prolongation of the QT interval);
- dry mouth;
- nausea;
- sleep disorders (insomnia, increased drowsiness);
- skin allergic reactions;
- general weakness (these symptoms may be manifestations of the underlying disease);
- heartburn;
- tachycardia;
- skin redness;
- change in blood pressure (more often a decrease);
- increased sweating;
- extrasystole (a causal relationship with the drug has not been proven, since in the natural population these symptoms are observed with the same frequency).
Children, during pregnancy and lactation
The drug Cavinton during pregnancy is contraindicated, because. Vinpocetine crosses the placental barrier. At the same time, its level in the placenta and in the blood of the fetus is lower than in the blood of a pregnant woman. At high doses, placental bleeding and spontaneous abortions are possible.
Within an hour, 0.25% of the accepted dose of the drug penetrates into breast milk. When using Cavinton, breastfeeding should be discontinued.
The drug is not prescribed in children under 18 years of age.
special instructions
Cavinton tablets contain lactose. If the patient has hypersensitivity to lactose, it should be borne in mind that one tablet contains 41.5 mg of lactose monohydrate.
The solution for infusion contains sorbitol, therefore, in case of diabetes, the concentration of sugar in the blood should be periodically monitored.
In case of fructose intolerance or fructose 1,6-diphosphatase deficiency, it is not recommended to use vinpocetine in the form of a concentrate.
drug interaction
With simultaneous use, there is no interaction with beta-blockers (chloranolol, pindolol), clopamide, glibenclamide, digoxin, acenocoumarol or hydrochlorothiazide. In rare cases, simultaneous use with alpha-methyldopa is accompanied by some increase in the hypotensive effect; when using this combination, regular monitoring of blood pressure is necessary.
The concentrate for the preparation of a solution for infusion and heparin are chemically incompatible, however, treatment with anticoagulants and vinpocetine can be carried out simultaneously. The concentrate for the preparation of a solution for infusion is incompatible with infusion solutions containing an amino acid.
Cavinton's analogs
Full analogues for the active substance: 
- Vincetin.
- Vinpoton.
- Bravinton.
- Vinpocetine forte.
- Telektol.
- Vero-Vinpocetine.
- Vinpocetine.
Holiday conditions and price
The average price of Cavinton (tablets, No. 50) in Moscow is 199 rubles. In Kyiv, you can buy medicine (tablets, No. 50) for 154 hryvnia, in Kazakhstan - for 2160 tenge. Pharmacies in Minsk offer Cavinton tablets (No. 50) for 12-13 bel. rubles. It is released from pharmacies by prescription.
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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 indicators of general 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 dose 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.
Cavinton is a drug from the group of correctors of cerebral circulation, which is used mainly in neurological practice, including the treatment of vegetative vascular dystonia (VVD). The main active ingredient of Cavinton is Vinpocetine.
By its action, it is a vasodilator that improves blood circulation and provides increased blood and oxygen flow to the human brain. Cavinton normalizes metabolism in the brain and improves the absorption of glucose. The vasodilating effect of the drug is associated with a direct relaxing effect on smooth muscles.
Thanks to the specific formula of Cavinton, activation of blood circulation in ischemic areas of the brain is ensured, as a result, their functionality is normalized. The drug increases the amount of ATP, activates the circulation of norepinephrine and serotonin in brain cells, additionally stimulates the ascending pathways of the norepinephrine system, which has a therapeutic cerebroprotective effect.
By suppressing phosphodiesterase, Cavinton contributes to the accumulation of cAMP in tissues and reduces platelet adhesion. There is only a slight decrease in systemic arterial pressure.
Cavinton increases the resistance of brain cells to oxygen deficiency, improves blood microcirculation, helps to reduce increased blood viscosity, enhances the plasticity of erythrocytes and has a blocking effect on the absorption of adenosine by erythrocytes.
Indications for use Cavinton
The therapeutic use of Cavinton is indicated in cases where it is necessary to reduce the severity of neurological and mental signs of cerebrovascular insufficiency of various etiologies. These states include:
- Disorders of cerebral circulation - after a stroke (ischemic or hemorrhagic), with atherosclerosis.
- Memory disorders against the background of metabolic disorders in the brain.
- Atherosclerotic changes in cerebral arteries.
- Dizziness and speech disorders in diseases of the brain and central nervous system.
- Hypertension of unknown etiology.
- Vegetative-vascular disorders (VSD).
- Neurological or mental disorders due to cerebrovascular insufficiency.
- Age-related changes affecting the retina and choroid of the eyes. Visual impairment caused by thrombosis or atherosclerosis of the eye vessels.
- Some eye diseases associated with insufficiency of ocular circulation (vasospasm, violation of the structure of tissues in the area of the macula, increased intraocular pressure);
In the course of clinical studies, the therapeutic effect of Cavinton was revealed in the treatment of acquired deafness (for example, toxic) and labyrinthine vertigo.
In the treatment of children, Cavinton is used for encephalopathies due to birth trauma or hypoxic conditions.
The selection of a course of treatment is based on the severity of the disease and other diagnostic data.
Instructions for use Cavinton, dosage
According to the official instructions for use, Cavinton tablets are prescribed in a standard dosage - 1 tablet 3 times a day after meals.
The drug is taken for a long time, the course of treatment reaches 2 months, then you need to take a break.
Patients begin to feel the therapeutic effect after a week from the start of treatment. In the treatment of patients with impaired liver and kidney function, the drug is used in a standard dosage.
Cavinton tablets - instructions:
Tablets are the basis of the treatment regimen, excluding exacerbation conditions.
Accept 1-2 pcs. (depending on indications), 3 times a day. After the active phase of treatment, they switch to a maintenance regimen - 1 Cavinton tablet three times a day.
Cavinton forte (tablets) is prescribed 1 pc. three times a day. It is recommended to take after meals. If it is necessary to cancel the drugs, do not stop taking the pills abruptly. The dose of reception is reduced gradually, in 2-3 days.
Injections (shots) Cavinton
Before the / in the introduction of Cavinton, the ampoules are diluted in 200 - 400 ml of saline, it is permissible to use 5% glucose as the base solution. Do not administer intramuscularly and intravenously without dilution. In / in injections of Cavinton, the instructions for use allow doing only in a specialized hospital.
The usual initial daily dose is 20 mg (2 amps) in 500 ml infusion solution. Depending on tolerance, within 2-3 days the dosage can be increased to no more than 1 mg / kg / day. The average time of treatment with Cavinton injections is up to 10-14 days.
The average daily dose with a body weight of 70 kg is 50 mg (5 amps in 500 ml of infusion solution).
The use of Cavinton in children
Children after brain injuries: Cavinton is administered intravenously slowly at a dose of 8-10 mg/kg per day in a 5% glucose solution. After 2-3 weeks, oral administration of 0.5-1 mg / kg per day.
Peculiarities:
Cavinton tablets are absorbed within an hour. Does not undergo intestinal metabolism. It is excreted with feces and urine in a ratio of 2 to 3.
The concentration of the solution for infusion is therapeutic in plasma in the range of 10-20 ng / ml. It is excreted by the gastrointestinal tract and by the kidneys in a ratio of 2 to 3.
Despite the lack of confirmed data, it is recommended to exercise caution when administered simultaneously with drugs that act on the central nervous system and with antiarrhythmics. Incompatible with heparin.
Cavinton forte
We should also mention Cavinton Forte - the key difference from the usual Cavinton is the dosage of the active substance (vinpocetine) - it has been increased from 5 to 10 mg.
Contraindications Cavinton
Contraindications to the use of Cavinton (tablets and ampoules):
- Acute phase of hemorrhagic stroke, severe ischemic heart disease, severe forms of arrhythmia.
- Pregnancy, lactation period.
- Hypersensitivity to the active substance or to any of the excipients.
- The use of the drug in children is contraindicated (due to the lack of data from relevant clinical studies).
- 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.
Side effects:
Usually the drug is well tolerated. With rapid in / in the introduction, a drop in blood pressure, tachycardia is possible. Some patients, when taking Cavinton, note an increase in appetite and a constant feeling of hunger.
Analogues of the drug Cavinton, list
Structural analogues of Cavinton according to the active substance (list):
- Bravinton;
- Vero-Vinpocetine;
- Vinpoton;
- Vinpocetine;
- Vinpocetine forte;
- Vincetin;
- Cavinton forte;
- Telektol.
This is important - instructions for use Cavinton, prices and reviews do not apply to analogues. And should not be used as a guide or for prescribing dosages. When looking for a Cavinton substitute, a specialist consultation is required!
solution for injections. 10 mg/2 ml: amp. 10 pieces.
Injection
Excipients:
2 ml - dark glass ampoules (5) - plastic trays (2) - cardboard boxes.
solution for injections. 25 mg/5 ml: amp. 10 pieces.Reg. No: 640/95/2000/05/09/11/14/16/19 dated 04/30/2019 - Validity of reg. beats not limited
Injection colorless or slightly greenish, transparent.
Excipients: ascorbic acid, sodium metabisulfite - 1 mg, tartaric acid, benzyl alcohol - 10 mg, sorbitol - 80 mg, water for injection - up to 1 ml.
5 ml - dark glass ampoules (5) - plastic trays (2) - cardboard boxes.
solution for injections. 50 mg/10 ml: amp. 5 pieces.
Reg. No: 640/95/2000/05/09/11/14/16/19 dated 04/30/2019 - Validity of reg. beats not limited
Injection colorless or slightly greenish, transparent.
Excipients: ascorbic acid, sodium metabisulfite - 1 mg, tartaric acid, benzyl alcohol - 10 mg, sorbitol - 80 mg, water for injection - 1 ml.
10 ml - dark glass ampoules (5) - plastic trays (1) - cardboard boxes.
Description of the medicinal product CAVINTON ® based on officially approved instructions for use of the drug and made in 2019. Update date: 07/12/2019
Vinpocetine affects the metabolism and circulation of the brain, as well as the rheological properties of the blood.
The drug has a neuroprotective effect:
- weakens the negative impact of cytotoxic reactions caused by stimulating amino acids. Inhibits voltage-dependent Na + - and Ca 2+ -channels, as well as NMDA and AMPA receptors, enhances the neuroprotective effect of adenosine.
Vinpocetine stimulates brain metabolism:
- increases the uptake and consumption of glucose and oxygen by brain tissue. Increases the resistance of the brain to hypoxia;
- increases the transport of glucose - an exclusive source of energy for the brain - through the BBB;
- 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. Vinpocetine increases the concentration of ATP and the ratio of ATP / AMP;
- enhances the exchange of norepinephrine and serotonin in the brain;
- stimulates the ascending noradrenergic system;
- has antioxidant activity.
Vinpocetine improves microcirculation in the brain:
- inhibits platelet aggregation;
- reduces pathologically increased blood viscosity;
- increases the deformability of erythrocytes and inhibits the capture of adenosine;
- improves oxygen transport in tissues by reducing the affinity of oxygen for red blood cells.
Vinpocetine selectively increases cerebral blood flow:
- increases the cerebral fraction of cardiac output;
- reduces the resistance of cerebral vessels, without affecting the parameters of systemic circulation (BP, cardiac output, heart rate, peripheral vascular resistance);
- the drug does not cause a "steal" effect. Moreover, against the background of treatment with vinpocetine, blood flow to damaged (but not yet necrotic) ischemic areas with low perfusion improves (the reverse effect of "steal").
Distribution
With repeated oral administration at doses of 5 mg and 10 mg, the kinetics is linear, C ss is 1.2 ± 0.27 ng / ml and 2.1 ± 0.33 ng / ml, respectively. Absolute oral bioavailability is about 7%.
Plasma protein binding in humans is 66%. V d is 246.7±88.5 l, which indicates a good distribution in the tissues.
Studies with radioactively labeled vinpocetine have shown that when the drug is administered orally to rats, the highest radioactivity is observed in the liver and gastrointestinal tract. C max in the tissues is observed 2-4 hours after ingestion. The concentration of the radioactive label in the brain tissues did not exceed the concentration in the blood.
Metabolism
The main metabolite of the main metabolite of apovincamic acid (AVK), the amount of which in humans is 25-30%. The clearance is 66.7 l / h and exceeds the hepatic clearance (50 l / h), which indicates extrahepatic metabolism of vinpocetine.
Compared with intravenous administration, the AUC of VKA after taking the drug orally is more than 2 times, which indicates the formation of VKA during the first pass metabolism of vinpocetine. Other Vinpocetine Metabolites:
- hydroxyvinpocetine, hydroxy-AVK, dihydroxy-AVK-glycinate and their conjugates with glucuronides and/or sulfates. The amount of vinpocetine that is excreted unchanged is a few percent of the dose taken.
breeding
T 1/2 in humans is 4.83±1.29 hours.
In studies conducted with radiolabeled vinpocetine, it was found that excretion is carried out mainly by the kidneys (60%) and through the intestines (40%). A greater amount of radioactive label in rats and dogs was found in the bile, while there was no significant intrahepatic circulation.
VKA is excreted mainly by the kidneys by glomerular filtration, T 1/2 depends on the dose and frequency of the drug.
Pharmacokinetics in special clinical situations
Since vinpocetine is indicated for the treatment of predominantly elderly patients who experience changes in the kinetics of drugs - reduced absorption, different distribution and metabolism, decreased excretion - studies of the pharmacokinetics of vinpocetine were carried out in this group, especially with long-term use. The results of such studies have demonstrated that the kinetics of vinpocetine in the elderly does not differ significantly from the kinetics of vinpocetine in young people and, in addition, there is no cumulation.
An important and significant property of vinpocetine is the absence of the need for special selection of the dose of the drug in patients with liver or kidney diseases due to the metabolism of the drug and the absence of cumulation (accumulation).
In neurology
- the following forms of cerebral ischemia: conditions after an acute cerebrovascular accident, chronic cerebrovascular insufficiency due to cerebral atherosclerosis or arterial hypertension, incl. vertebrobasilar insufficiency; as well as vascular dementia, post-traumatic encephalopathy.
- for the treatment of chronic vascular pathology of the choroid (the choroid) and the retina.
- treatment of sensorineural hearing loss;
- Meniere's disease;
- idiopathic tinnitus.
Helps to reduce mental and neurological symptoms in cerebral ischemia.
In ophthalmology
In otorhinolaryngology
The drug is administered only as a slow intravenous drip infusion at a rate of not more than 80 drops / min.
The initial daily dose is usually 20 mg in 500 ml solution for infusion. This dose may be increased to 1 mg/kg of body weight per day for 2-3 days, depending on the tolerability of the drug. For patients weighing 70 kg the average dose is 50 mg / day (50 mg in 500 ml solution for infusion); the average duration of the course of therapy is 10-14 days.
After completing the course of infusion therapy, it is recommended to continue treatment with the drug in the form of Cavinton ® forte tablets (1 tablet 3 times / day) or Cavinton ® (2 tablets 3 times / day).
At patients with kidney or liver disease special dose selection is not required.
The use of the drug in children and adolescents under the age of 18 contraindicated.
The drug should not be administered intramuscularly. The drug should not be administered intravenously without dilution.
To dilute the drug, you can use saline or solutions containing dextrose (Salsol, Ringer's solution, Rindex, Rheomacrodex). The infusion solution should be used within 3 hours after preparation.
The drug is used immediately after opening the ampoule. The drug ampoule is intended for single use only. Residues of the medicinal product must be destroyed. From a microbiological point of view, the solution prepared for intravenous administration should be used immediately.
Cavinton's solution is chemically incompatible with heparin, so their administration in the same syringe is prohibited.
Due to chemical incompatibility, solutions for infusions containing amino acids cannot be used to dilute Cavinton ® solution, and during infusion therapy Cavinton ® cannot be administered together with solutions for infusions containing amino acids.
Adverse reactions are listed below by organ system class and frequency of occurrence according to MedDRA 20.1 terminology.
| Infrequently (≥1/1000-<1/100) |
Rarely (≥1/10 000-<1/1000) |
Very rarely (<1/10 000) |
| From the hematopoietic and lymphatic systems | ||
| Thrombocytopenia RBC agglutination |
Anemia | |
| allergic reactions | ||
| Hives | Hypersensitivity | |
| From the side of metabolism | ||
| Hypercholesterolemia Diabetes Increasing the level of urea in the blood |
Anorexia Increasing LDH levels |
|
| From the side of the nervous system | ||
| Euphoria | Anxiety Headache Dizziness Hemiparesis Drowsiness |
Depression Tremor Loss of consciousness Pre-fainting state |
| From the organ of vision | ||
| Hemorrhage in the anterior chamber of the eye Hypermetropia Decreased visual acuity Myopia |
Conjunctival hyperemia Optic nerve edema Diplopia |
|
| From the organ of hearing | ||
| Hearing loss Hyperacusia Hypoacusia True dizziness |
Noise in ears | |
| From the side of the cardiovascular system | ||
| Arterial hypotension | Ischemia / myocardial infarction angina pectoris Arrhythmia Bradycardia Tachycardia Extrasystole Feeling the heartbeat Arterial hypertension/hypotension tides Prolongation of the QT interval on the ECG ST segment depression on ECG |
Fluctuations in blood pressure Thrombophlebitis Heart failure Atrial fibrillation Prolongation of the PR interval on the ECG |
| From the digestive system | ||
| Discomfort in the epigastric region Dry mouth Nausea |
Hypersecretion of saliva Vomit |
|
| From the skin and subcutaneous tissue | ||
| Erythema Hyperhidrosis |
Dermatitis Itching |
|
| General reactions | ||
| feeling hot | Asthenia Discomfort in the chest |
|
| Local reactions | ||
| Inflammation/thrombosis at the injection site | ||
Reporting Suspected Adverse Reactions
Reporting suspected adverse reactions after drug registration is important. They allow continuous monitoring of the benefit / risk ratio of the use of the medicinal product. Healthcare professionals are requested to report any suspected adverse reaction through the national reporting system.
Use during pregnancy and lactation
The use of the drug during pregnancy and lactation is contraindicated.
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 the mother. Teratogenic or embryotoxic effect of the drug was not detected. AT experimental studies it has been shown that the administration of the drug in high doses in some cases caused bleeding from the placenta and spontaneous abortion, apparently as a result of increased placental blood flow.
Vinpocetine is excreted in breast milk. In studies using radiolabelled vinpocetine, the radioactivity of breast milk was 10 times higher than that of maternal blood. When taking a single dose of vinpocetine for an hour, 0.25% of the dose of the drug is excreted in breast milk. Since there are no data on the effects of vinpocetine on the body of an infant, the use of the drug during breastfeeding is contraindicated.
According to clinical studies, the pharmacokinetics of vinpocetine, incl. with long-term use, in the elderly does not differ significantly from the pharmacokinetics in young people.
If the patient has increased intracranial pressure, arrhythmia or long QT interval syndrome, as well as against the background of the use of antiarrhythmic drugs, the course of therapy with Cavinton ® can be started only after a thorough analysis of the benefits and risks associated with its use.
The drug contains sorbitol (160 mg / 2 ml), therefore, if a patient has diabetes, it is necessary to periodically monitor the blood glucose level.
If the patient has fructose intolerance, treatment with the drug should not be carried out.
Benzyl alcohol can cause toxic and anaphylactoid reactions.
Sodium metabisulphite can rarely cause severe hypersensitivity reactions and bronchospasm.
Influence on the ability to drive vehicles and control mechanisms
There are no data on the effect of the drug on the ability to drive vehicles and control mechanisms. In the event of visual disturbances, dizziness and other disorders of the nervous system, the patient should refrain from performing potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.
There were no cases of overdose. Based on the literature data, the administration of the drug at a dose of 1 mg/kg of body weight can be considered safe. Since there are no data on the use of the drug in doses exceeding 1 mg / kg, the administration of the drug in higher doses is not allowed.
The simultaneous use of vinpocetine with beta-blockers (chloranolol, pindolol), clopamide, glibenclamide, digoxin, acenocoumarol or hydrochlorothiazide in clinical studies was not accompanied by manifestations of any interaction.
With the simultaneous use of vinpocetine and methyldopa, in rare cases, there was some increase in the hypotensive effect (with the combination, regular monitoring of blood pressure is required).
Despite the lack of data from clinical studies confirming the possibility of drug interactions, it is recommended to prescribe vinpocetine with caution simultaneously with centrally acting drugs, antiarrhythmic and anticoagulant drugs.
Pharmaceutical incompatibility
Cavinton's solution is chemically incompatible with heparin, so their administration in the same syringe is prohibited. However, the concomitant use of anticoagulants is allowed (without mixing in the same syringe or solution).