Винпосан®

General characteristics. Structure:

Active agent - a Vinpocetine of 5.012 mg (in terms of 100% substance of 5.000 mg).

Excipients: cellulose microcrystallic, potato starch, коповидон, sodium of starch glikolit, calcium stearate.

Pharmacological properties:

Pharmacokinetics. It is quickly soaked up from digestive tract. Easily gets through gistogematichesky barriers (including through a blood-brain barrier), it is allocated with breast milk. The maximum concentration in a blood plasma is noted in 1 h after use. Value of therapeutic concentration of a Vinpocetine in a blood plasma makes from 10 to 20 ng/ml, bioavailability is made by 50-70%. Contacts proteins of a blood plasma for 66%.

It Biotransformirutsya in a liver. The main metabolite is apovinkaminovy acid.

The elimination half-life makes 3,54 - 6,12 h. Other part - in the form of metabolites is removed by kidneys and through digestive tract, insignificant quantity in an invariable look.

Pharmacodynamics. Drug improves blood circulation and metabolism in a brain. Effect of drug is implemented at the expense of the complex mechanism of action. Reduces expressiveness of the damaging cytotoxic reactions caused by the stimulating amino acids; inhibits functional activity as cellular transmembrane natrium and calcium channels, and NMDA receptors (N - methyl - D - aspartate) and AMPA (-амино-3-гидрокси-5-метил-4-изоксазол-пропионовая acid). Exponentiates neuroprotective effect of adenosine. Stimulates brain metabolism, strengthens absorption and assimilation by a brain of glucose and oxygen. Stimulates glucose transport through a blood-brain barrier, shifts metabolism of glucose in the aerobic direction. Selectively inhibits Sa +2-calmodulin-dependent tsGMF-phosphodiesterase, increases concentration of tsAMF and tsGMF in brain tissues, and also concentration of ATP and a ratio of ATF/AMF. Activates cerebral metabolism of noradrenaline and serotonin, thereby stimulates activity of the ascending noradrenergichesky system, having antioxidant effect.

Винпосан® improves microcirculation of a brain, reduces aggregation of thrombocytes, reduces the increased viscosity of blood, increases the deforming ability of erythrocytes and blocks absorption of adenosine by them.

Винпосан® improves portability of a hypoxia brain cells, promoting oxygen transport to fabrics owing to reduction of affinity of erythrocytes to it.

Drug selectively and intensively strengthens a brain blood stream and cerebral fraction of minute volume of blood, reduces brain vascular resistance, without influencing parameters of general circulation (the ABP, the minute volume, pulse rate, OPSS). Does not cause a phenomenon of "burglarizing", strengthens blood supply of the struck, ischemic area of a brain, at the same time blood supply of intact area does not change.

Indications to use:

- the insufficiency of cerebral circulation which is followed by neurologic and mental disorders: tranzitorny ischemia, an ischemic stroke, states after a stroke, vascular dementia, atherosclerosis of cerebral arteries, vertebro-bazillyarny insufficiency, posttraumatic and hypertensive encephalopathy;

- vascular diseases of a retina and choroid of an eye, including vasomotor spasm and thrombosis of the central artery or vein of a retina;

- decrease in hearing vascular, toxic (including, medicamentous) or other genesis (idiopathic, caused by a noise overload), Menyer's disease, an idiopathic sonitus;

- vegeto-vascular dystonia at a menopausal syndrome.

Route of administration and doses:

Inside on 5-10 mg (1-2 tablets) 3 times a day. A maintenance dose - 5 mg (1 tablet) 3 times a day. Improvement is observed usually in 1-2 weeks. Treatment duration - 2 months. After consultation with the doctor repeated courses of treatment can be appointed (2-3 times a year).

Features of use:

In the presence of a syndrome of the extended interval of QT or at simultaneous use of the drugs provoking lengthening of an interval of QT control of an ECG is recommended.

There is no sufficient experience of use of the drug Vinposan® in pediatric practice.

Considering side effects of drug it is necessary to be careful when driving or potentially dangerous mechanisms.

Side effects:

- lowering of arterial pressure, tachycardia, premature ventricular contraction, lengthening of an interval of QT;

- sleep disorders (sleeplessness, drowsiness), dizziness, headache, weakness;

- dryness in a mouth, nausea, heartburn;

- hyperemia of integuments;

- allergic reactions in the form of skin rash, a small tortoiseshell.

Interaction with other medicines:

At simultaneous use with warfarin it is reported about small reduction of anticoagulating effect of warfarin.

However, if necessary simultaneous therapy by anticoagulants is admissible.

Anticonvulsants (carbamazepine, dipheninum), barbituric drugs accelerate metabolism of a Vinpocetine and reduce its concentration in a blood plasma.

The combined oral contraceptives, makrolidny antibiotics (кларитромицин, erythromycin), antifungal means (кетоканозол) change expressiveness of effect of a Vinpocetine, slow down his metabolism and increase concentration of drug in a blood plasma.

Contraindications:

- hypersensitivity to a Vinpocetine or any other component of drug;

- acute stage of a hemorrhagic stroke;

- severe forms of coronary heart disease;

- heavy disturbances of a rhythm;

- pregnancy and period of a lactation;

- children's and teenage age up to 18 years.

Overdose:

Symptoms: strengthening of symptoms of side effects.

Treatment: symptomatic.

Storage conditions:

To store in the dry, protected from light place, at a temperature not above 30 °C.

 

To store in the place, unavailable to children!

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in a blister strip packaging from a film of polyvinyl chloride and aluminum foil.

On 5 planimetric packagings together with the approved instruction on a medical use in the state and Russian languages place in a pack from a cardboard or chrome-ersatz.

Packs place in boxes from a cardboard.