Universal reference book for medicines

Active substance: vinpocetine

Type: A drug that improves blood circulation and brain metabolism

Manufacturer: GEDEON RICHTER (Hungary) produced by GEDEON RICHTER-RUS (Russia)
Composition, form of production and packaging
Tablets are dispersible white or almost white, round, biconcave, with engraved "N83" on one side.
1 tab.
vinpocetine 10 mg
Additives: mannitol - 75.6 mg, corn pregelatinized corn starch - 38 mg, butyl methacrylate copolymer - 9 mg, giprolose low substituted - 8 mg, crospovidone - 8 mg, magnesium stearate - 2.85 mg, sodium stearyl fumarate - 2.8 mg, silicon dioxide colloid - 1.6 mg , aspartame - 1.28 mg, stearic acid - 1.26 mg, sodium lauryl sulfate - 0.9 mg, dimethicone - 0.39 mg, flavoring orange - 0.32 mg.
15 pcs. - blisters (2) - packs of cardboard.
15 pcs. - blisters (6) - packs of cardboard.
Description of the drug approved by the manufacturer for the printed edition of 2017.
The mechanism of action of vinpocetine consists of several elements: it improves cerebral blood flow and metabolism, has a beneficial effect on the rheological properties of the blood.
The neuroprotective effect is realized by reducing the unfavorable cytotoxic effect of excitatory amino acids. It blocks Na + - and Ca + -channels and NMDA- and AMPA-receptors. Vinpocetine stimulates the metabolism in the brain: increases the uptake and consumption of glucose and oxygen. Increases tolerance to hypoxia: increases the transport of glucose, the only source of energy for brain tissue, through the BBB; shifts the metabolism of glucose towards the energetically more advantageous aerobic pathway. Selectively inhibits Ca 2+ -calmodulin-dependent cGMP phosphodiesterase. Increases the exchange of serotonin and norepinephrine in the brain, stimulates the noradrenergic neurotransmitter system and has an antioxidant effect.
Improves microcirculation in the brain due to inhibition of platelet aggregation, a decrease in pathologically increased blood viscosity, increased erythrocyte deformability and inhibition of adenosine reuptake; promotes the transition of oxygen into cells by reducing the affinity of erythrocytes. Selectively increases cerebral blood flow by decreasing cerebral vascular resistance without significantly affecting systemic blood circulation parameters (blood pressure, cardiac output, heart rate, OPSS); does not cause the effect of "stealing".
Vinpocetine is rapidly absorbed after ingestion and reaches C max in 1 h. Absorption occurs mainly in the proximal parts of the intestine. It is not metabolized when passing through the intestinal wall.
In preclinical studies of the introduction of radioactively labeled vinpocetine, he was determined by mouth in the highest concentrations in the liver and gastrointestinal tract. C max in tissues is noted 2-4 hours after ingestion.
The amount of radioactive isotope in the brain did not exceed that in the blood. Binding to proteins in the human body - 66%. V d is 246.7 ± 88.5 L, which indicates a significant binding to tissues. Bioavailability for ingestion - 7%.
When administered multiple times at doses of 5 mg and 10 mg, the kinetics is linear; while C ss in blood plasma were 1.2 ± 0.27 ng / ml and 2.1 ± 0.33 ng / ml, respectively.
Metabolism and excretion
The clearance is 66.7%, which exceeds the total plasma volume of the liver (50 l / h) and indicates extrahepatic metabolism. T 1/2 in humans is 4.83 ± 1.29 hours. In studies with a radiolabeled drug, it was found that the main ways of elimination are kidney and intestinal excretion in a 3: 2 ratio. In pre-clinical studies, the highest radioactivity was determined in bile, but no evidence of significant entero-hepatic circulation was found. 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. The main metabolite of vinpocetine is apovincamine acid (AVK), whose proportion in humans is 25-30%. After taking vinpocetine inside the AUC AVK is 2 times greater than that after IV introduction. This indicates that AVK is formed in the process of metabolism of the first passage of vinpocetine. Other known metabolites are hydroxyvinpocetine, hydroxy-AVK, dihydroxy-AVK-glycinate, as well as their conjugates with glucuronides and / or sulfates. Unchanged vinpocetine is released in small amounts.
An important and useful characteristic of vinpocetine is the absence of the need for dose adjustment in diseases of the liver and kidneys due to the lack of cumulation due to the characteristics of its metabolism.
Pharmacokinetics in specific patient groups
It was found that the pharmacokinetics of vinpocetine in elderly patients does not significantly differ from that in young patients, cumulation of the drug is absent. Therefore, vinpocetine can be administered to patients with impaired liver and kidney function for a long time and in usual doses.
- symptomatic therapy of the consequences of ischemic stroke, vascular vertebrobasilar insufficiency, vascular dementia, cerebrovascular atherosclerosis, posttraumatic, hypertensive encephalopathy.
- chronic vascular diseases of the retina and choroid of the eye.
- Perceptual hearing loss;
- Ménière's disease;
- noise in ears.
The course of treatment and dose are determined by the attending physician.
The drug is prescribed inside, after eating. The daily dose of the drug is 30 mg (1 table 10 mg 3 times / day). The therapeutic effect develops about a week after the start of the drug.
Tablets dispersible Cavinton ® Comfort can be swallowed whole with a small amount of water, with difficulty swallowing the tablet should be placed on the tongue for resorption. If a patient likes the orange taste of tablets of dispersible Cavinton ® Comfort, they can be taken by dissolving.
In diseases of the kidneys and liver, the drug is prescribed in the usual dose.
Side effects are quite rare. The data are presented according to the system-organ classes according to the MedDRA classification and with the following frequency: infrequently (from? 1/1 000 to <1/100); rarely (from? 1/10 000 to <1/1 000); very rarely (<1/10 000).
On the part of the blood and lymphatic system: rarely - leukopenia, thrombocytopenia; very rarely - anemia, agglutination of erythrocytes.
From the immune system: very rarely - hypersensitivity.
From the side of metabolism and nutrition: infrequently - hypercholesterolemia; rarely - decreased appetite, anorexia, diabetes mellitus.
Disorders of the psyche: rarely - insomnia, sleep disturbances, agitation, restlessness; very rarely - euphoria, depression.
From the nervous system: infrequently - a headache; rarely - dizziness, taste disorders, stupor, hemiparesis, drowsiness, amnesia; very rarely - tremor, spasms.
From the side of the organ of vision: rarely - edema of the optic disc; very rarely congestion hyperemia.
From the side of the organ of hearing and the labyrinth: infrequently - vertigo; rarely - hyperacusis, hypoacusia, ringing in the ears.
From the heart: rarely - ischemia / myocardial infarction, angina, bradycardia, tachycardia, extrasystoles, palpitation; very rarely - arrhythmia, atrial fibrillation.
From the side of the vessels: infrequently - arterial hypotension; rarely - arterial hypertension, "hot flashes", thrombophlebitis; very rarely - fluctuations in blood pressure.
From the digestive tract: infrequently - discomfort in the abdomen, dry mouth, nausea; rarely - abdominal pain, constipation, diarrhea, indigestion, vomiting; very rarely - dysphagia, stomatitis.
From the skin and subcutaneous tissues: rarely - erythema, excessive sweating, pruritus, urticaria, rash; very rarely - dermatitis.
General disorders and disorders at the injection site: rarely - asthenia, fatigue, heat; very rarely - discomfort in the chest, hypothermia.
Influence on the results of laboratory and instrumental studies: infrequent - decrease in blood pressure, rarely - increased blood pressure, increased serum triglyceride concentration, ST-segment depression on ECG, decrease / increase in the number of eosinophils, changes in hepatic enzyme activity; very rarely - an increase / decrease in the number of white blood cells, a decrease in the number of red blood cells, a reduction in thrombin time, an increase in body weight.
- acute phase of hemorrhagic stroke;
- severe form of ischemic heart disease;
- severe arrhythmias;
- phenylketonuria;
- Pregnancy;
- lactation period (lactation);
- children and adolescence under 18 (due to insufficient data);
- a known hypersensitivity to vinpocetine and other components of the drug.
Vinpocetine penetrates the placental barrier and is therefore contraindicated in pregnancy. At the same time, its concentration in the placenta and in the fetal blood is lower than in the pregnant woman's blood. At high doses, placental bleeding and spontaneous abortion are possible, probably as a result of increased placental blood supply.
Within one hour, 0.25% of the accepted dose of the drug penetrates into breast milk. When using the drug, it is necessary to stop breastfeeding.
With kidney disease, the drug is prescribed in the usual dose.
With liver diseases, the drug is prescribed in the usual dose.
Contraindicated in children and adolescents under the age of 18 (due to insufficient data).
The presence of the syndrome of the extended QT interval and the use of drugs that cause prolongation of the QT interval require periodic ECG monitoring.
In a tablet dispersible Cavinton ® Comfort 10 mg contains 1.28 mg of aspartame, a source of phenylalanine, so the drug is contraindicated in patients with phenylketonuria.
Influence on ability to drive vehicles and work with mechanisms
Studies on the impact on the ability to drive vehicles were not conducted. When there are undesirable reactions from the nervous system, care should be taken when driving vehicles and working with mechanisms.
Currently, data on the overdose of vinpocetine are limited.
Treatment: gastric lavage, reception of activated charcoal, symptomatic treatment.
Interactions are not observed with simultaneous use with beta-adrenoblockers (chloranolol, pindolol), clopamid, glibenclamide, digoxin, acenocoumarol, hydrochlorothiazide and imipramine.
The simultaneous use of vinpocetine and methyldopa sometimes caused some strengthening of the hypotensive effect, so this treatment requires regular monitoring of blood pressure.
Despite the lack of data confirming the possibility of interaction, it is recommended to exercise caution while simultaneously appointing Cavinton ® Comfort with preparations of central, antiarrhythmic and anticoagulant action.
The drug is released by prescription.
The drug should be stored out of reach of children, protected from light at a temperature of no higher than 30 ° C. Shelf life - 2 years.
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