Cavinton 5mg 50 tablets — Made in Hungary — Free Delivery

Pharmacological properties

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

Vinpocetine exhibits a neuroprotective effect: the preparation weakens the harmful effect of cytotoxic reactions caused by stimulating amino acids. The preparation inhibits voltage-gated Na + and Ca2 + channels, as well as NMDA and AMPA receptors. The preparation enhances the neuroprotective effect of adenosine.

Vinpocetine stimulates cerebral metabolism: the preparation increases the uptake of glucose and O2 and the consumption of these substances by the brain tissue. Increases the brain's resistance 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 the Ca2 + -calmodulin-dependent enzyme cGMP-PDE, increases the level of cAMP and cGMP in the brain. The preparation 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; as a result of the action of all of the above effects, vinpocetine has a cerebroprotective effect.

Vinpocetine improves microcirculation in the brain: the preparation inhibits platelet aggregation, reduces pathologically increased blood viscosity, increases erythrocyte deformability and inhibits adenosine uptake, improves O2 transport in tissues by reducing the O2 affinity for erythrocytes.

Vinpocetine selectively increases blood flow in the brain: the preparation increases the cerebral fraction of cardiac output; reduces vascular resistance in the brain, without affecting the parameters of systemic circulation (blood pressure, cardiac output, pulse rate, OPSS), the preparation does not cause a steal effect. Moreover, against the background of the use of the preparation, the blood flow to the damaged (but not yet necrotic) areas of ischemia with low perfusion improves (the opposite effect of stealing).

Pharmacokinetics. Absorption: Vinpocetine is rapidly absorbed, Cmax in blood plasma is achieved 1 hour after oral administration. The main site of vinpocetine absorption is the proximal gastrointestinal tract. The compound is not metabolized when passing through the intestinal wall.

Distribution: in studies with oral administration of the preparation in rats, radioactively labeled vinpocetine in the highest concentration was detected in the liver and gastrointestinal tract. Cmax in tissues could be observed 2–4 hours after taking the preparation. The concentration of radioactivity in the brain did not exceed the concentration in the blood.

In humans, plasma protein binding is 66%. The oral bioavailability of vinpocetine is 7%. The volume of distribution is 246.7 ± 88.5 liters, which means a pronounced binding of the substance in the tissues. The value of the clearance of vinpocetine (66.7 l / h) in blood plasma exceeds its value in the liver (50 l / h), which indicates the extrahepatic metabolism of the compound.

Excretion: with repeated oral administration of the preparation at a dose of 5 and 10 mg, vinpocetine demonstrates linear kinetics; equilibrium plasma concentrations are 1.2 ± 0.27 and 2.1 ± 0.33 ng / ml, respectively. T½ in humans is 4.83 ± 1.29 hours. In studies carried out using a radioactively labeled compound, it was found that the main route of excretion is through the kidneys and intestines in a ratio of 60: 40%. A large amount of radioactive label in rats and dogs was manifested in bile, but no significant hepatic circulation was noted. Apovincaminic acid (AVA) is excreted by the kidneys by simple glomerular filtration, T½ of this substance varies depending on the dose and route of administration of vinpocetine.

Metabolism: the main metabolite of vinpocetine is VKA, which is formed in humans in 25-30%. After oral administration, the AUC of AVK is 2 times higher than that after intravenous administration of the preparation, which indicates the formation of AVK during the presystemic metabolism of vinpocetine. Other identified metabolites are hydroxyvinpocetin, hydroxy-AVK, dihydroxy-AVK-glycinate and their conjugates with glucuronides and / or sulfates. In each of the studied species, the amount of vinpocetine that was excreted unchanged was only a few percent of the taken dose of the preparation.

An important and significant property of vinpocetine is the absence of the need for a special selection of the dose of the preparation in patients with liver or kidney disease, taking into account the metabolism of the preparation and the absence of accumulation (accumulation).

Changes in pharmacokinetic properties in special circumstances (for example, at a certain age, in the presence of concomitant diseases). Since vinpocetine is indicated for therapy mainly in elderly patients, in whom there is a change in the kinetics of preparations- a decrease in absorption, a different distribution and metabolism, a decrease in excretion, it was necessary to conduct studies to assess the kinetics of the preparation in this age group, especially with prolonged use. The results of such studies showed that the kinetics of vinpocetine in elderly people does not differ significantly from the kinetics of vinpocetine in young patients, and, in addition, there is no cumulation. In case of impaired liver or kidney function, the usual doses of the preparation can be used, since vinpocetine does not accumulate in the body of such patients, which allows taking the preparation for a long time.

Indications

Neurology. for the treatment of various forms of cerebrovascular pathology: conditions after suffering a cerebrovascular accident (stroke), vertebrobasilar insufficiency, vascular dementia, cerebral atherosclerosis, post-traumatic and hypertensive encephalopathy. helps to reduce the severity of mental and neurological symptoms in cerebrovascular pathology.

Ophthalmology. For the treatment of chronic vascular pathology of the choroid (choroid) and retina.

Otorhinolaryngology. For the treatment of senile hearing loss of the perceptual type, Meniere's disease and tinnitus.

Application

Take orally after meals. the daily dose for adults is 15-30 mg (3 times a day, 5-10 mg). the duration of treatment is determined by the doctor individually.

No dose adjustment is required in patients with kidney or liver disease.

Contraindications

Hypersensitivity to the active substance or any of the excipients. During pregnancy and breastfeeding. the use of the preparation in children is contraindicated (due to the lack of data from relevant clinical studies).

Side effects

Cavinton is a safe preparation, as evidenced by safety studies involving tens of thousands of patients and demonstrating that even the most common adverse effects did not fall under the category “often 1/100” as defined by meddra, that is, side effects with the highest probability of occurrence was recorded with a frequency of 1%. for this reason, the "frequently" category is missing from the list below.

The adverse reactions listed below are categorized by organ system class and frequency of occurrence according to MedDRA terminology.

From the blood and lymphatic system: leukopenia, thrombocytopenia (rare), anemia, erythrocyte agglutination (very rare).

From the immune system: hypersensitivity (very rare).

Metabolic and nutritional disorders: hypercholesterolemia (rare), decreased appetite, anorexia, diabetes mellitus (rare).

Mental disorders: insomnia, sleep disturbances, anxiety, agitation (rare), euphoria, depression (very rare).

From the nervous system: headache (rare), dizziness, dysgeusia, stupor, hemiparesis, drowsiness, amnesia (rare), tremor, convulsions (very rare).

From the side of the organ of vision: edema of the nipple of the optic nerve (rare), hyperemia of the conjunctiva (very rare).

On the part of the organ of hearing and the labyrinth: vertigo (infrequently), hyperacusis, hypoacusia, tinnitus (rarely).

From the heart: ischemia / myocardial infarction, angina pectoris, bradycardia, tachycardia, extrasystole, palpitations (rare), arrhythmia, atrial fibrillation (very rare).

From the side of the vessels: arterial hypotension, hypertension, hot flashes, thrombophlebitis (rare), fluctuations in blood pressure (very rare).

From the digestive system: abdominal discomfort, dry mouth, nausea (rare), abdominal pain, constipation, diarrhea, dyspepsia, vomiting (rare), dysphagia, stomatitis (very rare).

Skin and subcutaneous tissue disorders: erythema, hyperhidrosis, pruritus, urticaria, rash (rare), dermatitis (very rare).

General disorders: asthenia, weakness, fever (rare), chest discomfort, hypothermia (very rare).

Results of laboratory and instrumental studies: decrease in blood pressure (rarely), increase in blood pressure, increase in the level of TG in the blood, depression of the ST segment on the ECG, increase / decrease in the number of eosinophils, change in the activity of liver enzymes (rare), increase / decrease in the number of leukocytes, decrease in the number of erythrocytes , decrease in prothrombin time, increase in body weight (very rare).

Special instructions

The presence of a syndrome of prolonged q-t interval and taking preparations that cause lengthening of q-t require periodic monitoring of the ecg.

If the patient has increased intracranial pressure, arrhythmias or prolonged Q – T interval syndrome, as well as against the background of the use of antiarrhythmic preparations, the course of preparation therapy can be started only after a thorough analysis of the benefits and risks associated with the use of the preparation.

The preparation contains lactose. Patients with rare hereditary diseases such as galactose intolerance, Lapp lactase deficiency or impaired glucose-galactose malabsorption should not take this preparation (1 Cavinton tablet contains 140 mg of lactose, 1 Cavinton forte tablet (10 mg) contains 83 mg of lactose).

During pregnancy and breastfeeding. The use of the preparation during pregnancy and lactation is contraindicated.

Pregnancy. Vinpocetine crosses the placental barrier, while the concentration of the preparation in the placenta and in the blood of the fetus is lower than in the blood of a pregnant woman. No teratogenic effect of the preparation has been identified. In preclinical studies of the use of the preparation in high doses, in some cases, placental bleeding and spontaneous termination of pregnancy were noted, possibly as a result of increased placental blood supply.

Lactation. 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 in breast milk and the lack of sufficient clinical observations regarding the safety of the preparation in infants. After a single dose of vinpocetine for an hour, 0.25% of the taken dose of the preparation penetrates into breast milk.

Children. In children, the preparation is not used (due to the lack of clinical data).

The ability to influence the reaction rate when driving and working with other mechanisms. There is no data on the effect of vinpocetine on the ability to drive vehicles or work with mechanisms, but caution should be exercised, given the likelihood of drowsiness, dizziness when using the preparation.

Interactions

The simultaneous use of vinpocetine with β-adrenergic receptor blockers (cloranolol, pindolol), clopamide, glibenclamide, digoxin, acenocoumarol or hydrochlorothiazide in clinical trials was not accompanied by any interaction between them. the simultaneous use of vinpocetine and α-methyldopa sometimes caused some increase in the hypotensive effect, therefore, against the background of the use of this combination of preparations, regular monitoring of blood pressure is necessary. despite the lack of data from clinical studies confirming the possibility of interaction, it is recommended to be careful while prescribing vinpocetine with preparations that affect the central nervous system, as well as in the case of concomitant antiarrhythmic and anticoagulant therapy.

Overdose

Overdose symptoms are unknown. according to studies, the dose of 60 mg / day is safe. a single dose of 360 mg of vinpocetine was not accompanied by the development of either cardiovascular or other side effects.

Storage conditions

In the original packaging to protect from light at a temperature not exceeding 30 ° C.