Винпосан®

General characteristics. Structure:

Active agent – a Vinpocetine (in terms of 100% substance) 10.0 mg.

Excipients: ascorbic acid, benzyl alcohol, sodium metabisulphite, sorbitol, tartaric acid, water for injections.

Pharmacological properties:

Pharmacokinetics. At parenteral administration volume distribution - 5,3 l/kg. 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 is made by from 10 to 20 ng/ml. bioavailability makes 57 - 70%. Contacts proteins of a blood plasma for 66%.

Metabolism and removal. The period semi-removal is equal to 4,75 h to Biotransformiruyetsya in a liver. The main metabolite is apovinkaminovy acid. It is removed with urine: insignificant quantity - in not changed look, other part - in the form of metabolites.

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, slows down aggregation of thrombocytes, reduces the increased viscosity of blood, increases deformability 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.

Винпосан® 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 disturbances of cerebral circulation which are followed by neurologic and mental disorders: tranzitorny ischemia, an ischemic stroke, states after a stroke, vascular dementia, atherosclerosis of cerebral arteries, vertebro-basilar 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:

Винпосан® enter only intravenously kapelno, slowly with the maximum speed of infusion of 80 кап. / min.

Contents of 2 ampoules (20 mg) dissolve in 500 ml of solution for infusions (0,9% solution of sodium of chloride, 5% glucose solution, Ringer's solution).

At good tolerance the drug dose within 2-3 days can be raised to 1 mg/kg of body weight. The average daily dose makes 50 mg (5 ampoules in 500 ml of infusion solution) at the rate on 70 kg of body weight.

Duration of a course of treatment - 10 – 14 days.

Then pass to a maintenance therapy (administration of drug inside in the form of tablets).

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 it is recommended to control an ECG.

Patients with pathology from cardiovascular system cannot enter intravenously because of danger of development of arrhythmia (up to fibrillation of ventricles). At a hemorrhagic stroke parenteral administration is possible only after reduction of the acute phenomena (usually in 5-7 days).

At patients with a diabetes mellitus during treatment of Vinposanom® control of level of glucose in blood as solution contains sorbitol is recommended (120,0 g in 2 ml of solution).

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;

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

- dryness in a mouth, nausea, heartburn;

- hyperemia of integuments, skin rash, small tortoiseshell;

- thrombophlebitis in an injection site.

Interaction with other medicines:

Винпосан® in the form of solution for injections it is incompatible with heparin.

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 kontsenration 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 other components of drug;

- acute stage of a hemorrhagic stroke;

- severe forms of coronary heart disease;

- severe forms of arrhythmia;

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

- pregnancy, lactation period.

Overdose:

There are no data on overdose.

Symptoms: strengthening 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 2 ml of drug in ampoules from light-protective glass of the CHC-1 brand or import.

On 5 ampoules pack into a blister strip packaging from a film of polyvinyl chloride and aluminum foil.

2 planimetric packagings together with the approved instruction on a medical use in the state and Russian languages place in a pack from a cardboard bandbox. Put the scarificator in each pack ampoule.

When packaging ampoules with notches, rings and points scarificators do not invest.