Vinpocetine

General characteristics. Structure:

Active ingredient: 5 mg of a Vinpocetine in each tablet.

Excipients: potato starch, lactose monohydrate, cellulose microcrystallic, magnesium stearate, talc, povidone.

Pharmacological properties:

Pharmacodynamics. The medicine improving cerebral circulation. Has vasodilating, anti-hypoxemic and antiagregantny effect. The mechanism of action is connected with phosphodiesterase inhibition, it leads to increase in content of cyclic adeninemonophosphate (tsAMF) in cells that, in turn, causes decrease in content of calcium in cytoplasm of smooth muscle cells and relaxation of myofibrils.

Expands brain vessels, strengthens a blood stream, it is preferential in ischemic areas, improves supply of a brain with oxygen. Promotes utilization of glucose and increases the level of catecholamines in the central nervous system, stimulates metabolism of noradrenaline and serotonin in brain tissues. Reduces aggregation of thrombocytes, viscosity of blood, promotes increase in deformability of erythrocytes and normalization of venous outflow against the background of decrease in resistance of brain vessels. System arterial pressure goes down slightly.

Sensitivity of brain vessels to the running-down action of a Vinpocetine increases in advanced and senile age that is caused by a sensitization of system of adenylatecyclase-tsAMF when aging.

Pharmacokinetics. Absorption. After intake the Vinpocetine is well and quickly absorbed from digestive tract. Bioavailability makes about 60%. Cmax is reached in 1 h. Easily gets through gistogematichesky barriers (including through a blood-brain barrier) and gets into fabrics.

Removal of T1/2 makes about 5 h.

Indications to use:

– the early and late recovery periods of a stroke, a stroke effect, a state after the postponed tranzitorny ischemic attack, distsirkulyatorny and posttraumatic encephalopathy;

– vascular diseases of a retina and/or a choroid of an eye (owing to atherosclerosis, a vasomotor spasm, thrombosis); the degenerative changes of a macula lutea caused by atherosclerosis or a vasomotor spasm; secondary glaucoma (owing to obturation of vessels);

– age vascular or toxic (medicamentous) hearing disorder, Menyer's disease, dizzinesses of a labyrinth origin.

Route of administration and doses:

It is necessary to appoint a Vinpocetine on 5 – 10 mg of 3 times/days within 2 months. To apply after meal.

Before cancellation of medicine it is necessary to reduce a dose gradually. Repeated courses 2 – 3 times a year are possible.

Features of use:

Pregnancy and lactation. The Vinpocetine is contraindicated to use at pregnancy. In need of its use in the period of a lactation it is necessary to stop breastfeeding.

Use in pediatrics. Safety and efficiency of use of a Vinpocetine for children is not established. Experience of use of a Vinpocetine for patients aged up to 18 years is limited.

Use for persons with an abnormal liver function and kidneys. Patients should not appoint medicine with liver diseases with the expressed dysfunction.

Use for persons with cardiovascular pathology. It is necessary to be careful at purpose of a Vinpocetine to the patients accepting the antihypertensives or medicines extending QT interval (лоратадин, терфенадин, erythromycin, probucol) or QT having a syndrome of prolongation of an interval in the anamnesis.

Influence on ability to driving of motor transport and control of mechanisms. The patients accepting a Vinpocetine have to abstain from potentially dangerous types of activity connected with need of special attention and bystry psychomotor reactions.

Side effects:

From cardiovascular system: lowering of arterial pressure, tachycardia, premature ventricular contraction, delay of intra ventricular conductivity.

From the central nervous system: a sleep disorder (sleeplessness, the increased drowsiness), dizziness, a headache, the general weakness (symptoms can be manifestations of a basic disease).

From digestive tract: nausea, heartburn, dryness in a mouth.

Others: allergic reactions, erubescences.

Interaction with other medicines:

The combined oral contraceptives, makrolidny antibiotics (кларитромицин, erythromycin), antimicrobic medicines (кетоконазол) increase expressiveness of effect of a Vinpocetine and its side effects. Anticonvulsants (carbamazepine, dipheninum), barbituric drugs reduce expressiveness of effect of a Vinpocetine.

With care it is necessary to appoint a Vinpocetine along with drugs of the central nervous action, antiarrhythmic and anticoagulating means.

Contraindications:

– the expressed disturbances of a cordial rhythm;

– coronary heart disease (heavy current);

– acute period of intracerebral bleeding;

– lactose intolerance;

– the increased intracranial pressure;

– pregnancy;

– lactation (breastfeeding);

– hypersensitivity to medicine.

Overdose:

Intoxication symptoms nonspecific. In the beginning nausea, dizziness, tachycardia, a lowering of arterial pressure are possible; further – arrhythmias in the form of ventricular ekstrasistoliya, blockade, in hard cases – arrhythmias like "pirouette".

Treatment: the medicine cancellation, a gastric lavage with absorbent carbon supporting and the symptomatic therapy directed to elimination of the arisen disturbances.

Storage conditions:

In the place protected from light and moisture, at a temperature from 15 to 25 ºС. To store in the place, unavailable to children. A period of validity - 2 years. Not to apply after the termination of a period of validity.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in a blister strip packaging, on 5 packagings with a leaf insert in a pack (packaging No. 10 × 5).