Vinpotropil® (Vinpotropile®)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceVinpocetine + PyracetamVinpocetine + Pyracetam
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  • Vinpotropil®
    concentrate in / in 
    CANONFARMA PRODUCTION, CJSC     Russia
  • Vinpotropil®
    capsules inwards 
    CANONFARMA PRODUCTION, CJSC     Russia
  • Vinpotropil®
    pills inwards 
    CANONFARMA PRODUCTION, CJSC     Russia
    • Dosage form: & nbspfilm coated tablets
    Composition:

    1 tablet, film-coated, contains:

    active substances: vinpocetine 10.0 mg, pyracetam 800.0 mg;

    Excipients: calcium hydrogen phosphate dihydrate 120 mg, croscarmellose sodium (impellosis) 33 mg, magnesium stearate 7 mg, povidone 21 mg, talc 7 mg, cellulose microcrystalline 102 mg;

    composition of film shell: Opadrai II brown 35 mg, including: hypromellose (hydroxypropylmethylcellulose) 9.8 mg, macrogol (polyethylene glycol) 3.5 mg, lactose monohydrate (sugar milk) 12.6 mg, iron oxide red oxide 3.08 mg, iron dye oxide black 5.985 mg, titanium dioxide 0.035 mg.

    Description:

    The tablets are oval, with a risk, covered with a film coat of light brown color with a grayish tinge. The cross section is almost white.

    Pharmacotherapeutic group:Psychostimulating and nootropic remedy
    ATX: & nbsp

    N.06.B.X.18   Vinpocetine

    N.06.B.X.03   Pyracetam

    Pharmacodynamics:

    Vinpotropil® is a combined preparation. Possesses properties characteristic of a means that improves cerebral blood flow (vinpocetine) and for a nootropic agent (piracetam).

    As a psychostimulating agent:

    Improves the metabolism of the brain, increasing the intake of glucose and oxygen by brain tissue. Increases the resistance of neurons to hypoxia, increases the transport of glucose to the brain through the blood-brain barrier; translates the process of the decay of glucose into an energetically more economical, aerobic pathway; selectively blocks Ca2+- dependent phosphate diestease; increases the levels of adenosine monophosphate (AMP), cyclic guanosine monophosphate (cGMP) and adenosine triphosphate (ATP) of the brain. Increases the exchange of norepinephrine and serotonin of the brain; stimulates the ascending branch of the noradrenergic system, has an antioxidant effect. Reduces platelet aggregation and increased blood viscosity; increases the elasticity of erythrocytes and blocks the utilization of adenosine by erythrocytes; helps to increase the return of oxygen in the erythrocytes. Increases cerebral blood flow; reduces the resistance of cerebral vessels without a significant change in the indices of the systemic circulation.Does not have the effect of "stealing" and enhances blood supply, especially in ischemic areas of the brain. Penetrates through the placental barrier.

    As a nootropic agent:

    Has a positive effect on brain metabolic processes, slightly increases the concentration of ATP in the brain, enhances the synthesis of ribonucleic acid and phospholipids, stimulates glycolytic processes, enhances the utilization of glucose; improves the integrative activity of the brain, promotes memory consolidation, facilitates the learning process; changes the propagation speed excitation in the brain, improves microcirculation, without providing a vasodilating action, inhibits the aggregation of activated platelets; has a protective effect in brain damage caused by hypoxia, intoxication, electric shock; enhances alpha and beta activity, reduces deltaactivity on the electroencephalogram, reduces the severity of the vestibular nystagmus; improves the connections between the cerebral hemispheres and synaptic conductivity in neocortical structures, increases mental activity, enhances cerebral blood flow; does not have sedative effect. The effect develops gradually.

    Has a pronounced effect on the symptoms of initial manifestations of cognitive disorders of cerebrovascular origin in elderly and senile patients. It is recommended in psychogeriatric practice.

    Pharmacokinetics:Vinpocetine.

    Absorption.

    After oral administration, it is rapidly absorbed from the gastrointestinal tract. Time to reach the maximum concentration (TCmOh) in blood plasma for 1 hour. Absorption occurs mainly in the proximal parts of the gastrointestinal tract. When passing through the wall of the intestine is not exposed to metabolism.

    Distribution.

    When oral radioactive labeled vinpocetine was administered to rats, the highest concentration was found in the liver and in the gastrointestinal tract. The maximum concentration in the tissues was noted 2-4 hours after administration. The concentration of radioactive labeled vinpocetine in the brain did not exceed the values ​​found in the blood. In humans, the relationship with plasma proteins is 66%, the bioavailability with ingestion is 7%. The volume of distribution is 246.7 - 88.5 liters, which indicates a high binding to tissues. The total clearance (66.7 l / h) exceeds the rate of hepatic blood flow (50 l / h), which indicates extrahepatic metabolism.

    Metabolism.

    The main metabolite is apovincaminate (ABA), which is 25-30% of the original compound. The area under the "concentration-time" curve of ABA after oral administration is twice as high as when intravenously administered vinpocetine. In this way, vinpocetine is prone to the pronounced effect of "primary transmission" through the liver. Other metabolites include: hydroxyvinpocetine, hydroxy-ABA, ABA-dioxiglycinate and their conjugates (sulfates and (or) glucuronides).

    Excretion.

    Excretion of unchanged vinpocetine is low (several percent). With repeated administration in doses of 5 mg and 10 mg, the kinetics is linear, the equilibrium plasma concentration is 1.2 + 0.27 and 2.1 + 0.33 ng / ml, respectively. The elimination period in humans is 4.8 + 1.29 hours. It is excreted by the kidneys and through the intestine in a ratio of 60:40. In rats and dogs, high radioactivity when radioactive labeled vinpocetine is detected in bile, however, significant enterohepatic recirculation is noted.

    Pharmacokinetics in specific patient groups (age, accompanying illnesses)

    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.

    Piracetam.

    Absorption.

    After oral administration piracetam quickly and almost completely absorbed from the gastrointestinal tract. Bioavailability is about 100 %. After a single dose of piracetam in a dose of 2 g maximum concentration (Cmax) is reached within 30 minutes and is 40-60 μg / ml, after 2-8 hours it is found in the cerebrospinal fluid.

    Distribution.

    Volume of distribution (Vd) is about 0.6 l / kg. Does not bind to plasma proteins. Pyracetam penetrates through blood-brain and placental barriers, as well as hemodialysis membranes. In an animal study, it was found that piracetam selectively accumulates in the tissues of the cerebral cortex, mainly in the frontal, parietal and occipital lobes, in the cerebellum and basal nuclei.

    Metabolism.

    It is not metabolized.

    Excretion.

    The elimination period from the blood (T1 / 2) is 4-5 h and 8.5 h - from the cerebrospinal fluid. T1 / 2 is prolonged with renal failure. It is excreted unchanged by the kidneys. Excretion by the kidneys is almost complete (> 95%) for 30 hours. The total clearance of piracetam in healthy volunteers is 86 ml / min.

    Indications:

    Symptomatic treatment: intellectual-mnestic disorders, 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, Meniere's disease, tinnitus.

    Contraindications:

    - Hypersensitivity to vinpocetine, pyracetam or pyrrolidone derivative, as well as other components of the drug;

    - Pregnancy;

    - The period of breastfeeding;

    - Expressed heart rhythm disturbances;

    - Ischemic heart disease (severe course);

    - Acute stage of hemorrhagic stroke;

    - Renal and / or hepatic insufficiency,

    - Huntington's disease;

    - Children under 18 years (due to insufficient data).

    Patients with rare hereditary diseases, such as lactose intolerance, lactase deficiency or glucose-galactose malabsorption, should not take the drug.

    Carefully:

    Violation of hemostasis, severe bleeding, benign hyperbilirubinemia (including Gilbert's syndrome), viral hepatitis, alcoholic liver damage, alcoholism, deficiency of glucose-6-phosphate dehydrogenase, epilepsy, and advanced age.

    Pregnancy and lactation:The use of Vinpotropil® during pregnancy and during breastfeeding is contraindicated. Both components of the drug (vinpocetine and piracetam) penetrate through the placenta and into breast milk. In animal experiments, there was no teratogenic and embryotoxic effect of vinpocetine and piracetam. However, when high doses of vinpocetine were administered to animals, placental bleeding and abortion occurred (presumably as a result of an increase in placental blood flow). When deciding whether to abort breastfeeding or refusing treatment, the benefits of breastfeeding for a child and the benefits of therapy for the mother should be correlated.
    Dosing and Administration:

    The course of treatment and dosage is determined by the attending physician.

    For patients 18 years and older: inside, regardless of food intake, 1 tablet 2-3 times a day, with plenty of water. Last reception - 4 hours before bedtime. Duration of treatment is from 2-3 weeks to 2-6 months. Before cancellation of the drug, the dose should be gradually reduced (it is possible to use Vinpotropil® in another dosage form: capsules containing 5 mg of vinpocetine and 400 mg of piracetam).

    Side effects:

    Side effects are quite rare.The frequency gradient is defined as follows: very often (≥1 / 10); often (≥1 / 100 to <1/10); infrequently (≥1 / 1000 to <1/100); rarely (≥1 / 10000 to <1/1000), very rarely (<1/10000) and the frequency is unknown (it is impossible to evaluate based on available clinical trial data).

    Vinpocetine

    Violations of the blood and lymphatic system

    Rarely: leukopenia, thrombocytopenia;

    Very rarely: anemia, agglutination of erythrocytes.

    Immune system disorders

    Very rarely: hypersensitivity.

    Disorders from the 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.

    Disturbances from the nervous system

    Infrequently: headache;

    Rarely: dizziness, impaired taste, stupor, hemiparesis, drowsiness, amnesia;

    Very rarely: tremor, spasms.

    Disturbances on the part of the organ of sight

    Rarely: edema of the optic disc;

    Very rarely: conjunctival hyperemia.

    Violations from the organ of hearing and labyrinth

    Infrequently: vertigo;

    Rarely: hyperacusis, hypoacusia, tinnitus.

    Heart Disease

    Rarely: ischemia / myocardial infarction, angina, bradycardia, tachycardia, extrasystole, palpitation;

    Very rarely: arrhythmia, atrial fibrillation.

    Vascular disorders

    Infrequent: arterial hypotension;

    Rarely: arterial hypertension, "hot flashes", thrombophlebitis;

    Very rarely: fluctuations in blood pressure.

    Disorders from the gastrointestinal tract

    Infrequently: discomfort in the abdomen, dry mouth, nausea;

    Rarely: abdominal pain, constipation, diarrhea, indigestion, vomiting;

    Very rarely: dysphagia, stomatitis.

    Disturbances from the skin and subcutaneous tissues

    Rarely: erythema, excessive sweating, itching, urticaria, rash;

    Very rarely: dermatitis.

    General disorders and disorders at the site of administration

    Rarely: asthenia, malaise;

    Very rarely: chest discomfort, hypothermia.

    Impact on the results of laboratory and instrumental studies

    Infrequent: lowering blood pressure;

    Rarely: increased blood pressure, increased serum triglyceride concentration, segment depression ST on the electrocardiogram, decrease / increase of eosinophils, disturbance of functional hepatic tests;

    Very rarely: increase / decrease in the number of leukocytes, a decrease in the number of red blood cells, a decrease in thrombin time, an increase in body weight.

    Pyracetam

    Violations of the blood and lymphatic system

    The frequency is unknown: bleeding.

    Immune system disorders

    The frequency is unknown: anaphylactoid reactions, hypersensitivity.

    Disorders from the psyche

    Often: nervousness;

    Infrequently: depression;

    Frequency unknown: agitation, anxiety, confusion, hallucinations.

    Disturbances from the nervous system

    Often: hyperactivity;

    Infrequently: drowsiness;

    The frequency is unknown: ataxia, imbalance, exacerbation of epilepsy, headache, insomnia, tremor.

    Violations from the organ of hearing and labyrinth

    Frequency unknown: vertigo.

    Disorders from the gastrointestinal tract

    The frequency is unknown: abdominal pain (including in the upper divisions), diarrhea, nausea, vomiting.

    Disturbances from the skin and subcutaneous tissues

    The frequency is unknown: angioedema, dermatitis, itching, urticaria.

    Disorders from the reproductive system

    Frequency unknown: increased sexual desire.

    General disorders and disorders at the site of administration

    Infrequently: asthenia.

    Impact on the results of laboratory and instrumental studies

    Often: weight gain.

    Overdose:

    Symptoms: increased severity of side effects.

    Treatment: gastric lavage, reception of activated charcoal, symptomatic therapy.

    Interaction:

    Vinpocetine

    According to the results of clinical studies of drug interaction with beta-adrenoblockers (pinol), clomipramide, glibenclamide, digoxin, hydrochlorothiazide and acenocoumarol was not detected. Methyldopa can enhance the hypotensive effect of vinpocetine, so when they are used simultaneously, systematic monitoring of blood pressure is required. Despite the lack of clinical data, simultaneous use with agents that affect the central nervous system, anticoagulants and antiarrhythmics should be done with caution.

    Pyracetam

    Thyroid hormones

    With simultaneous use of piracetam and thyroid extract (triiodothyronine + thyroxine), confusion, irritability and sleep disturbance were noted.

    Acenocoumarol

    According to a published blind clinical trial in patients with recurrent venous thrombosis piracetam in a dose of 9.6 g / day did not affect the dose of acenocoumarol necessary to achieve an international normalized ratio of 2.5-3.5, but compared with the effects of acenocoumarol alone, the addition of pyracetam at a dose of 9.6 g / day significantly reduces platelet aggregation, beta-thromboglobin release, fibrinogen concentration, and von Willebrand factor (VIII:C; VIII:vW:Ag; VIII:vW:RCo), as well as the viscosity of whole blood and plasma.

    Pharmacokinetic interactions

    The possibility of changing the pharmacokinetics of pyracetam under the influence of other drugs is low, since 90% of piracetam is excreted unchanged in urine.

    In concentrations of 142, 426 and 1422 mg / ml piracetam Does not inhibit cytochrome P450 isoenzymes (CYP 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 and 4A9 / 11) in vitro. At a concentration of 1422 mg / ml, a minimal inhibition of the isoenzyme CYP2A6 (21%) and 3A4 / 5 (11%). However, the values ​​of the inhibition constant (Ki), probably go far beyond the concentration of 1422 mg / ml. Thus, the metabolic interactions of piracetam with other drugs are unlikely.

    Anticonvulsants

    Admission piracetam at a dose of 20 g / day for 4 weeks in patients with epilepsy, taking a constant dose of antiepileptic drugs (carbamazepine, phenytoin, phenobarbital and valproic acid), did not change their maximum and minimum concentrations.

    Alcohol

    Simultaneous reception with alcohol did not affect the concentration of pyracetam in plasma; when taking 1.6 g of pyracetam, the concentration of ethanol in the plasma did not change.

    Special instructions:

    Presence of the syndrome of the prolonged interval QT and taking medications that cause lengthening of the interval QT, requires periodic ECG monitoring. Due to the antiaggregant effect, piracetam should not be prescribed to patients with hemorrhagic stroke and should be administered with caution to patients with other severe hemorrhagic disorders, risk of bleeding (eg, gastric ulcer), hemostasis disorders, in patients with surgical interventions, including dental interventions, in patients taking anticoagulants and antiplatelet agents, in t.ch. low doses of acetylsalicylic acid.

    Effect on the ability to drive transp. cf. and fur:

    During the treatment period, care should be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

    Form release / dosage:

    Tablets, film-coated, 10 mg + 800 mg.

    Packaging:

    For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

    For 3 or 6 contour squares, together with the instruction for use, they are placed in a pack of cardboard.

    Storage conditions:

    In a dry, protected from light place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-001935
    Date of registration:18.12.2012 / 19.12.2017
    Expiration Date:Unlimited
    The owner of the registration certificate:CANONFARMA PRODUCTION, CJSC CANONFARMA PRODUCTION, CJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp19.03.3018
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