Vinpocetine

General characteristics. Structure:

International and chemical names: vinpocetine; (3a, 16a) - eburnamenin-14-carboxylic acid ethyl ether; main physical and chemical properties: transparent colourless or slightly greenish liquid; structure: 1 ml of a concentrate contains 5 mg of a Vinpocetine; excipients: ascorbic acid, sodium metabisulphite, tartaric acid, benzyl alcohol, sorbitol; water for injections.

Pharmacological properties:

Pharmacodynamics. The Vinpocetine improves cerebral circulation and brain metabolism, increases portability of ischemia of a brain. Selectively and intensively strengthens a brain blood stream, reduces brain vascular resistance, without influencing parameters of general circulation (arterial pressure, minute volume of blood, pulse rate, the general peripheric resistance of vessels). Strengthens first of all blood supply of the struck, ischemic area of a brain, without causing a phenomenon of "burglarizing"; at the same time blood supply of intact area does not change. Improves microcirculation in a brain, slows down aggregation of thrombocytes, reduces the increased viscosity of blood, increases deformability of erythrocytes and blocks absorption of adenosine by them. Increases portability of a hypoxia brain cells, promoting oxygen transport to fabrics. Strengthens absorption and metabolism of glucose which switches to energetically more favorable aerobic way, stimulates as well anaerobic metabolism of glucose by braking of phosphodiesterase and activation of adenylatecyclase that leads to increase in concentration of tsAMF and catecholamines in a brain.

Pharmacokinetics. Therapeutic concentration in plasma at intravenous administration makes 10-20 ng/ml. Easily gets through gistogematichesky barriers, including through a blood-brain barrier. Distribution volume – 5,3 l/kg. It is metabolized in a liver with formation of several metabolites, the apovinkaminovy acid and a hydroxyvinpocetine having pharmacological activity are basic of which. Elimination half-life of 4-5 h. It is excreted with urine and bile, generally in the form of the metabolites conjugated with glucuronic acid.

Indications to use:

Acute insufficiency of cerebral circulation (tranzitorny ischemia, the progressing stroke, a complete stroke, states after a stroke, a craniocereberal injury, multiinfarctive dementia, atherosclerosis of cerebral arteries, posttraumatic and hypertensive encephalopathy).

Route of administration and doses:

Apply only to treatment at adults, intravenously, in the form of slow drop infusion.
Initial daily dose - 20 mg of a Vinpocetine (4 ml) in 500-1000 ml of solution for infusions (0,9% of sodium chloride, 5% glucose, Ringer's solution). If necessary and good tolerance appoint repeated (2-3 times a day) slow drop infusions, gradually raising a dose within 3-4 days to maximum – 1 mg/kg/days.
Course of treatment of 10-14 days. After achievement of clinical improvement the dose is gradually lowered and passed to administration of drug in the form of tablets.

Features of use:

Drug is used parenterally, as a rule, in acute cases before improvement of a clinical picture; then pass to oral administration of drug. It is necessary to be careful at prescription of medicine by the patient with bradycardia at which on an ECG lengthening of an interval of QT is observed.
At a hemorrhagic cerebral stroke introduction is admissible only after subsiding of the acute phenomena (usually, in 5 - 7 days).
Sensitivity of brain vessels to the running-down effect of drug increases in advanced age that is caused by a sensitization when aging system tsAMF adenylatecyclase. It can lead to increase in probability of development of by-effects in this group of people.

Side effects:

Dizziness, feeling of heat, dermahemia of the person, nausea, thrombophlebitis in an injection site, hypotension, tachycardia, premature ventricular contraction, delay of intra ventricular conductivity.

Interaction with other medicines:

Pharmaceutical it is incompatible with heparin therefore they cannot be entered in one syringe; at simultaneous parenteral purpose of these drugs increase in risk of development of bleedings is possible. There are no data on interaction of a Vinpocetine with other medicines so far.

Contraindications:

Hypersensitivity, acute stage of a hemorrhagic stroke, the expressed coronary heart disease, severe forms of arrhythmias, pregnancy and the period of a lactation, children's age.

Overdose:

It is not described.

Storage conditions:

To store in protected from light, the place, unavailable to children, at a temperature not above 25 °C.
Period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

On 2 ml in ampoules, on 10 ampoules in a pack.