Instructions Barviton solution for injection 5 mg/ml ampoule 2 ml blister No. 10
Composition
active ingredient: vinpocetine;
1 ml of solution contains 5 mg of vinpocetine;
Excipients: ascorbic acid, sodium metabisulfite (E 223), tartaric acid, benzyl alcohol, sorbitol (E 420), water for injections.
Dosage form
Solution for injection.
Main physicochemical properties: colorless or with a slightly greenish tint, transparent liquid.
Pharmacotherapeutic group
Psychostimulants and nootropics. ATX code N06B X18.
Pharmacological properties
Pharmacodynamics.
Barviton 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 the rheological properties of blood.
Barviton exhibits neuroprotective effects: the drug attenuates the harmful effects of cytotoxic reactions caused by stimulating amino acids. The drug inhibits voltage-gated Na+ and Ca2+ channels, as well as NMDA and AMPA receptors. The drug enhances the neuroprotective effect of adenosine.
Barviton stimulates cerebral metabolism: the drug increases the uptake of glucose and O2 and the consumption of these substances by brain tissue. The drug increases the brain's resistance to hypoxia; increases the transport of glucose - the exclusive source of energy for the brain - through the blood-brain barrier; shifts glucose metabolism towards the more energetically favorable aerobic pathway; selectively inhibits the Ca2+-calmodulin-dependent enzyme cGMP-phosphodiesterase (PDE); increases the level of cAMP and cGMP in the brain. The drug increases the concentration of ATP and the ATP/AMP ratio; enhances the circulation of noradrenaline 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.
Barviton improves microcirculation in the brain: the drug inhibits platelet aggregation, reduces pathologically increased blood viscosity, increases erythrocyte deformability and inhibits adenosine uptake, improves O2 transport in tissues by reducing the affinity of O2 for erythrocytes.
Barviton selectively increases blood flow in the brain: the drug 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, total peripheral resistance); the drug does not cause a "stealing effect". Moreover, against the background of the drug, blood flow to damaged (but not yet necrotic) areas of ischemia with low perfusion ("reverse steal effect") improves.
Pharmacokinetics.
Distribution. In oral studies in rats, radiolabeled vinpocetine was found in the liver and gastrointestinal tract in the highest concentrations. Maximum tissue concentrations were detected 2-4 hours after administration. The concentration of radioactivity in the brain did not exceed the concentration in the blood.
In humans, the binding to blood proteins is 66%. The absolute oral bioavailability of vinpocetine is 7%. The volume of distribution is 246.7±88.5 l, which indicates a pronounced binding of the substance 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.
Excretion. With repeated oral administration of the drug at a dose of 5 mg and 10 mg, vinpocetine exhibits linear kinetics; equilibrium concentrations in blood plasma are 1.2 ± 0.27 ng / ml and 2.1 ± 0.33 ng / ml, respectively. The half-life in humans is 83 ± 1.29 hours. In studies conducted using a radioactively labeled compound, it was found that the main route of excretion is through urine and feces in a ratio of 60:40. A larger amount of radioactive label in rats and dogs was detected in bile, but significant enterohepatic circulation was not observed. Apovincamic acid is excreted by the kidneys by simple glomerular filtration, the half-life of this substance varies depending on the dose and route of administration of vinpocetine.
Metabolism. The main metabolite of vinpocetine is apovincamic acid (AVC), which is formed in humans in 25-30%. After oral administration, the area under the curve ("concentration-time") of AVC is twice as high as after intravenous administration of the drug, indicating the formation of AVC in the process of presystemic metabolism of vinpocetine. Other metabolites identified are hydroxyvinpocetine, hydroxy-AVC, dihydroxy-AVC-glycinate and their conjugates with glucuronides and/or sulfates. In each of the studied species, the amount of vinpocetine excreted unchanged was only a few percent of the dose taken.
Change in pharmacokinetic properties in special circumstances (for example, at a certain age, in the presence of concomitant diseases). Since Barviton is indicated for the treatment of mainly elderly patients, in whom changes in the kinetics of drugs are observed - reduced absorption, different distribution and metabolism, reduced excretion - it was necessary to conduct a study to assess the kinetics of the drug in this age group, especially with long-term use. The results of such studies have shown that the kinetics of vinpocetine in elderly people do not differ significantly from the kinetics of vinpocetine in young people, and, in addition, there is no accumulation. In case of impaired liver or kidney function, normal doses of the drug can be used, since vinpocetine does not accumulate in the body of such patients, which allows taking the drug for a long time.
Indication
Neurology. For the treatment of various forms of cerebrovascular pathology: conditions after a stroke, vertebrobasilar insufficiency, vascular dementia, cerebral atherosclerosis, post-traumatic and hypertensive encephalopathy. Helps reduce mental and neurological symptoms in cerebrovascular pathology.
Ophthalmology. For the treatment of chronic vascular pathology of the choroid (the vascular membrane of the eye) and retina (e.g. thrombosis, obstruction of the central retinal artery or vein).
Otorhinolaryngology. For the treatment of senile hearing loss in acute vascular pathology, toxic (drug) damage or damage of a different nature (idiopathic, due to noise exposure), Meniere's disease and tinnitus.
Contraindication
Acute phase of hemorrhagic cerebral stroke, severe ischemic heart disease, severe forms of arrhythmia.
Hypersensitivity to the active substance or to any of the excipients.
Interaction with other medicinal products and other types of interactions
During clinical studies, when vinpocetine was used simultaneously with β-blockers (cloranolol, pindolol), clopamide, glibenclamide, digoxin, acenocoumarol or hydrochlorothiazide, no interaction between these drugs was found. In isolated cases, some additive effect was observed with the simultaneous use of vinpocetine and α-methyldopa, therefore, regular blood pressure monitoring is necessary when using this combination of drugs.
Despite the lack of clinical study data confirming the possibility of interaction, it is recommended to exercise caution when prescribing vinpocetine simultaneously with drugs that affect the central nervous system, antiarrhythmic, anticoagulant and fibrinolytic agents.
Application features
Due to the content of benzyl alcohol (20 mg in 2 ml), hypersensitivity reactions may occur.
Due to the content of sodium metabisulfite, the drug can cause serious allergic reactions and bronchospasm.
If the patient has increased intracranial pressure, arrhythmia or long QT syndrome, as well as against the background of the use of antiarrhythmic drugs, a course of therapy with the drug can be started only after a thorough analysis of the benefits and risks associated with the use of the drug.
ECG monitoring is recommended in the presence of long QT syndrome or concomitant use of a drug that prolongs the QT interval.
The drug contains a small amount of sorbitol, so if a patient has diabetes, it is necessary to periodically monitor blood sugar levels during the course of therapy with the drug.
In case of fructose intolerance or fructose 1,6-diphosphatase deficiency, the drug should be avoided.
Use during pregnancy or breastfeeding
The use of the drug is contraindicated during pregnancy or breastfeeding.
Pregnancy. Vinpocetine crosses the placenta, but is found in lower concentrations in the placenta and in the fetal blood than in the maternal blood. No teratogenic or embryotoxic effects were observed. In animal studies, the administration of high doses of vinpocetine was accompanied in some cases by placental bleeding and miscarriage, mainly as a result of increased placental blood flow.
Breastfeeding. Vinpocetine passes into breast milk. In studies using labeled vinpocetine, the radioactivity in breast milk was ten times higher than in maternal blood. The amount entering milk within 1 hour is 0.25% of the administered dose. Since vinpocetine passes into breast milk and there is no data on the effect on the newborn, the use of vinpocetine during breastfeeding is contraindicated.
Ability to influence reaction speed when driving vehicles or other mechanisms
There is no data on the effect of the drug on the ability to drive a car or operate other mechanisms. However, if side effects such as dizziness, weakness, or other central nervous system disorders develop, it is recommended to refrain from such activities.
Method of administration and doses
Administer only intravenously as a slow drip infusion (infusion rate should not exceed 80 drops/minute).
It is forbidden to administer the drug subcutaneously, intramuscularly and intravenously in concentrated form.
The initial daily dose for adults is usually 20 mg in 500 ml of solution for infusion. This dose may be increased to 1 mg/kg body weight per day for 2-3 days, depending on the patient's tolerance.
The average duration of the course of therapy is 10-14 days, the usual daily dose is 50 mg/day (50 mg in 500 ml of infusion solution) - based on a body weight of 70 kg.
After completing the course of infusion therapy, it is recommended to continue the patient's therapy with Vinpocetine in tablet form.
Barviton solution for injection can be diluted with 0.9% sodium chloride solution or infusion solutions containing glucose. The finished Barviton solution must be used within 3 hours after preparation.
Patients with kidney or liver disease do not require dosage adjustment.
Children
Do not use the drug in children.
Overdose
No cases of overdose were noted.
Based on literature data, administration of the drug at a dose of 1 mg/kg body weight can be considered safe. Since there are no data on the use of the drug at doses exceeding this dose, administration of the drug at higher doses is not allowed.
In case of an overdose of the drug, the following are possible: arterial hypotension, lethargy, nausea, vomiting.
Treatment is symptomatic.
Adverse reactions
From the blood and lymphatic system: thrombocytopenia, erythrocyte agglutination; anemia.
Immune system disorders: hypersensitivity.
Metabolism: hypercholesterolemia, diabetes mellitus; anorexia.
Mental disorders: euphoria, anxiety, agitation; depression.
From the nervous system and sensory organs: headache, dizziness, hemiparesis, drowsiness; tremor, loss of consciousness, state before loss of consciousness, weakness, feeling of heat.
From the organs of vision: hyphema, hyperopia, decreased visual acuity, myopia; conjunctival hyperemia, optic nerve head swelling, diplopia.
From the side of the organs of hearing and vestibular apparatus: hearing impairment, hyperacusis, hypoacusis, vertigo; tinnitus.
Cardiac: myocardial ischemia/infarction, angina pectoris, arrhythmia, bradycardia, tachycardia, extrasystole, palpitations; heart failure, atrial fibrillation.
From the vascular system: arterial hypotension, arterial hypertension, hot flashes; blood pressure fluctuations, thrombophlebitis, venous insufficiency.
From the digestive tract: abdominal discomfort, dry mouth, nausea; vomiting, hypersecretion of saliva.
Skin and subcutaneous tissue disorders: erythema, hyperhidrosis, urticaria; itching, dermatitis.
General disorders: feeling hot; asthenia, chest discomfort, inflammation, thrombosis at the injection site.
Investigations: decreased blood pressure; increased blood pressure, ST segment depression and QT prolongation, increased blood urea; increased lactate dehydrogenase, prolonged PR interval on ECG, ECG changes.
Expiration date
3 years.
Storage conditions
Store out of the reach of children in the original packaging at a temperature not exceeding 30 °C.
Incompatibility.
Do not use solvents that are not listed in the section "Method of administration and doses". Vinpocetine solution is chemically incompatible with heparin and its low molecular weight analogues, therefore their administration in the same syringe is prohibited. At the same time, simultaneous use of anticoagulants and vinpocetine is permissible.
Vinpocetine solution is chemically incompatible with infusion solutions containing amino acids, therefore they cannot be used to dilute the drug.
Packaging
5, or 10, or 100 ampoules in a pack; or 5 ampoules in a blister, 1 or 2 blisters in a pack.
Vacation category
According to the recipe.
Producer
Private Joint-Stock Company "Lekhim-Kharkiv".
Location of the manufacturer and address of its place of business.
Ukraine, 61115, Kharkiv region, Kharkiv city, Severyna Pototskoho street, building 36.
