Vinpotropile® Instruction
International Non-Proprietary Name (INN): vinpocetine + piracetam
Dosage form: tablets
Structure
In 1 tablet:
Active ingredients: vinpocetine 10 mg, piracetam 800 mg;
Excipients: dicalcium phosphate dehydrate, croscarmellose sodium, magnesium stearate, povidone, talc, microcrystalline cellulose.
Description
Oval tablets with a film coating of light brown color with a grayish tint and a separating break line. The color of the transection is almost white.
Pharmacological classification: psycho-stimulating and nootropic medication.
ATC code: N06BX
Pharmacological action: vasodilatory, antiaggregational, nootropic, antihypoxic, improving cerebral circulation
Pharmacodynamics
Vinpotropile® is a combination drug. It has properties of medication improving the cerebral blood flow (vinpocetine) and of a nootropic medication (piracetam).
As a medication for improving cerebral blood flow, it improves the metabolism of the brain increasing the glucose and oxygen consumption by the brain tissue. It increases the resistance of neurons to hypoxia; enhances the glucose transport to the brain, through the blood-brain barrier; makes the process of the glucose breakdown more energy efficient and aerobic; selectively blocks Ca2+-dependent phosphodiesterase; increases the levels of adenosine monophosphate (AMP), of 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 the 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 by erythrocytes. Increases the cerebral blood flow; reduces the resistance of cerebral vessels without a significant change in indicators of the systemic blood circulation. Does not have the “steal” effect and enhances the blood supply, especially in ischemic areas of the brain. Penetrates through the placental barrier.
As a nootropic medication, it has a positive effect on the brain’s metabolic processes. It slightly increases the ATP concentration 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, enhances memory consolidation, facilitates the learning process; changes the speed of the brain excitation spreading, improves microcirculation without having a vasodilatory action, inhibits the aggregation of activated platelets; has a protective effect in case of brain injury caused by hypoxia, intoxications, electric shock; strengthens alpha- and beta-activity, reduces delta-activity 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, psycho-stimulating effect. The effect develops gradually.
Vinpotropile® has a pronounced effect on symptoms of initial manifestations of cognitive disorders of cerebrovascular origin in elderly and senile patients. It is recommended in psychogeriatric practice.
Pharmacokinetics
Vinpocetine
Absorption & distribution: Vinpocetine is quickly absorbed. The therapeutic concentration in plasma is 10–20 ng/ml. The time to reach the maximum concentration in blood plasma is 1 hour. Absorption occurs mainly in the proximal areas of the gastrointestinal tract.
Metabolism: It does not metabolize when it penetrates through the intestinal wall. The maximum concentration in tissues is reached 2–4 hours after the intake. Protein binding – 66%, bioavailability at the intake – 7%. The clearance of 66.7 l/h exceeds the plasma volume of the liver (50 l/h), which indicates extrahepatic metabolism. The main metabolite is apovincamine acid, which has some pharmacological activity. Other inactive metabolites are hydroxyvinpocetine, hydroxyapovinkaminic acid, hydroxyvinpocetine glycinate. At reingestion the kinetics is linear.
Excretion: The half-life in humans – (4.83 ± 1.29) hours. Excreted by the kidneys and through the intestine in the ratio of 3:2.
Piracetam
Absorption: After the intake, Piracetam is well absorbed and it penetrates into various organs and tissues. Bioavailability is about 100%. After a single intake of 3.2 g, the maximum concentration is 84 mcg/ml, after multiple intakes (3.2 g 3 times a day) – 115 mcg/ml. The time to reach the maximum concentration in plasma is 1 hour, in cerebrospinal fluid – 5 hours.
Distribution: The distribution volume is about 0.6 l/kg. It penetrates through the blood-brain and placental barriers, accumulates selectively in the tissues of the cerebral cortex.
Excretion: Almost does not undergo biotransformation and is excreted in the unchanged form by the kidneys through the glomerular filtration. The total clearance is 80–90 ml/min. The half-life from the blood plasma – 4-5 hours, from the cerebrospinal fluid – 8.5 hours.
Intended uses
Cerebrovascular insufficiency (the recovery period after an ischemic and hemorrhagic stroke), Parkinsonism of the vascular genesis, intoxications, psycho-organic syndrome with prevailing symptoms of asthenia and adynamia, symptomatic treatment of dizziness, prevention of migraine and kinetosis.
Encephalopathy of various genesis, including alcoholism; brain trauma and other diseases of the central nervous system accompanied by the decrease of intellectual and mnestic functions; asthenic syndrome; labyrinthopathy, Meniere’s syndrome.
Contraindications
- hypersensitivity;
- severe cardiac rhythm disorders;
- cardiac ischemia (severe state);
- acute stage of hemorrhagic stroke;
- renal and/or hepatic impairment;
- intolerance to galactose, lactase deficiency or glucose-galactose malabsorption;
- children under 18 years old (due to insufficient data);
- pregnancy and lactation.
With caution: In case of disturbed hemostasis, severe bleeding; benign hyperbilirubinemia (including Gilbert’s syndrome); viral hepatitis; alcoholic liver damage; alcoholism; deficiency of glucose-6-phosphate dehydrogenase; epilepsy; elderly age.
Dosage and administration
Ingest without regard to timing of food.
For patients over 18 years old: 1 tablet 2-3 times a day with water. The last intake should be no later than 4 hours before sleep. The duration of treatment is from 2-3 weeks to 2–6 months. Before cancellation, the dose should be gradually reduced (transfer to taking Vinpotropile® in the form of capsules with 5 mg of vinpocetine and 400 mg of piracetam is possible).
Dosage and duration of the treatment are determined by the doctor.
Side effects
The cardiovascular system
Rare: Changes in the ECG (depression of the ST segment, prolongation of the QT interval), tachycardia, extrasystole, lability of arterial pressure (AP) (mainly a decrease).
The central nervous system (CNS)
Rare: Motor disinhibition, irritability, depression, asthenia, dizziness, headache, sleep disturbances (insomnia, increased drowsiness), mental agitation, balance disorder, exacerbation of epilepsy, anxiety, hallucinations, confusion, extrapyramidal disorders, decreased ability to concentrate.
The digestive system
Rare: Nausea, vomiting, epigastric burning, diarrhea, abdominal pain, decreased appetite, gastralgia, constipation.
Metabolism
Rare: Weight gain, increased sweating.
Hearing disorders
Rare: Vertigo.
Dermatological reactions
Rare: Dermatitis, itching, urticaria, skin hyperemia.
Allergic reactions
Rare: Hypersensitivity, anaphylactic reactions, angioedema.
Special precautions
If the patient has the long QT syndrome (the length of the ventricular complex reflecting the length of the electrical systole of the ventricles) or takes medications that cause prolongation of the QT interval, periodic ECG (electrocardiogram, electrocardiography) monitoring is required.
In case of lactose intolerance, it should be taken into account that one capsule contains about 225 mg of lactose.
Overdose
Symptoms
Increased severity of side effects.
Treatment
Stomach lavage, activated carbon intake, symptomatic therapy.
Interaction with other drugs
Increases the risk of hemorrhagic complications against heparin therapy, effects of thyroid hormones, antipsychotics (neuroleptics), indirect anticoagulants, psychostimulants.
Reduces the effect of anticonvulsants (reduces the convulsive threshold). Despite the lack of data confirming the possibility of interaction, it is recommended to exercise caution when co-prescribing drugs with the central and antiarrhythmic mode of action.
Pregnancy and lactation
The drug is contraindicated during pregnancy and lactation.
Influence on the ability to drive vehicles and operate mechanisms
Taking into account possible undesirable effects, caution needs to be taken when operating mechanisms and driving vehicles.
Terms of release from pharmacy
On prescription.
Storage conditions
Store in a dry, dark place at a temperature no higher than 25°C. Keep out of reach of children.
Shelf life
2 years. Do not use beyond the expiration date.
Manufacturer
Canonpharma Production, Russia. https://canonpharma.ru/en/