Vinpotsetin-Pharmak

General characteristics. Structure:

Active ingredient: vinpocetine;

1 ml of solution contains 5 mg of a Vinpocetine in terms of 100% substance;

excipients: glycine, a betaine a hydrochloride, dinatrium эдетат, propylene glycol, water for injections.

Pharmacological properties:

Pharmacodynamics. Vinpotsetin-Pharmak improves cerebral circulation and brain metabolism. The effect is implemented at the expense of the complex mechanism of action. 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 (arterial pressure, minute volume of blood, pulse rate, the general peripheric resistance of vessels). First of all, strengthens 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 owing to reduction of affinity of erythrocytes with it. Strengthens absorption and metabolism of glucose which passes to energetically 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 in brain fabric. Increases the maintenance of catecholamines in brain tissue.

Pharmacokinetics. Therapeutic concentration in plasma at intravenous administration – 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. An elimination half-life – 4-5 h. It is excreted with urine and bile, generally in the form of the metabolites conjugated with glucuronic acid.

Pharmaceutical characteristics.

Main physical and chemical properties: transparent colourless or slightly greenish liquid.
Incompatibility.

Solution of a Vinpocetine is chemically incompatible with heparin and its low-molecular analogs therefore their introduction in one syringe is forbidden. At the same time simultaneous use of anticoagulants and Vinpotsetin-Pharmak is admissible.

Solution of a Vinpocetine is chemically incompatible with the infusion solutions containing amino acids therefore they cannot be used for cultivation of a concentrate of Vinpotsetin-Pharmak.

Indications to use:

Neurology: acute and chronic insufficiency of cerebral circulation (tranzitorny ischemia, an ischemic stroke, states after a stroke and a craniocereberal injury, multiinfarctive dementia, atherosclerosis of cerebral arteries, posttraumatic and hypertensive encephalopathy, vertebrobazilyarny insufficiency, neurologic and mental symptoms of disturbance of cerebral circulation).

Ophthalmology: the vascular diseases of eyes first of all caused by a vasomotor spasm of a choroid and a retina (including degenerative diseases of a choroid, a retina or a macula lutea; arterial and venous fibrinferments or embolisms; secondary glaucoma).

Otology: deterioration in hearing of vascular or toxic genesis (including medicamentous), senile relative deafness, Menyer's disease, kokhleovestibulyarny neuritis, dizziness of a labyrinth origin, idiopathic sonitus.

Route of administration and doses:

Apply only intravenously in the form of slow drop infusion (speed of infusion should not exceed 80 drops in 1 min.).

It is forbidden to administer the drug subcutaneously, intramusculary and in the concentrated look intravenously.

Initial daily dose for adults - 20 mg of a Vinpocetine (2 ampoules) divorced in 500-1000 ml of infusion solution for intravenous administration. 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/body weight a day. The average duration of treatment makes 10-14 days, an average daily dose of-50 mg at the body weight of 70 kg (the maintenance of 5 ampoules in 500 ml of infusion solution). Patients with diseases of a liver and kidneys can appoint drug in the same doses. On the termination of a course of intravenous therapy it is recommended to continue treatment by Vinpocetine drugs in the form of tablets.

For preparation of infusion solution it is possible to use 0,9% the solution of sodium of chloride or solutions containing glucose (Salsol, Ringer's solution, Rindexum, Reomakrodeks). Ready solution of Vinpotsetin-Pharmak needs to be used within 3 hours after preparation.

Features of use:

Use during pregnancy or feeding by a breast

During pregnancy use of drug is contraindicated. For the period of treatment it is necessary to stop breastfeeding.
Children.

There is no sufficient experience of use of drug for children therefore it is not applied in pediatric practice.

In case of increase in intracranial pressure, use of antiarrhythmic means, disturbance of a heart rhythm or lengthening of an interval of QT, before Vinpotsetin-Pharmak's use it is necessary to weigh carefully a ratio advantage/risk.

Existence of a syndrome of the prolonged interval of QT and use of the drugs provoking lengthening of an interval of QT demands carrying out periodic control of an ECG. In case of intolerance of fructose or deficit 1,6 diphosphatases of fructose it is necessary to avoid drug use.

Precautionary measures: it is not recommended to appoint with a labile arterial pressure and a low vascular tone.

With care appoint to the patients accepting hypotensive drugs and also patients with bad portability of alkaloids of a periwinkle of small (Vinca minor) and to patients with a liver failure.

Ability to influence speed of response at control of motor transport or work with other mechanisms. There are no data on influence of a Vinpocetine on ability to drive the car and to work with difficult mechanisms.

Side effects:

From a nervous system and sense bodys: sleep disorders (sleeplessness, the increased drowsiness), dizziness, a headache, weakness, feeling of heat, the increased perspiration (symptoms can be manifestations of a basic disease).

From heart (0,9%): the depression of a segment of ST and lengthening of an interval of QT, tachycardia, premature ventricular contraction, but existence of a causal relationship between such side effect and treatment by a Vinpocetine is not proved as in natural population these symptoms are observed with the same frequency.

From vascular system (2,5%): changes of arterial pressure (is more often - arterial hypotension, but also arterial hypertension is possible), erubescence, phlebitis, an agranulocytosis.

From system of digestion (0,6%): dryness in a mouth, nausea, heartburn.

From integuments: the increased perspiration.

From immune system: skin hypersensitivity reactions are possible.

Interaction with other medicines:

Simultaneous use of a Vinpocetine with β-blockers ((((((((((hloranololy, Pindololum), Clopamidum, glibenclamide, digoxin, atsenokumaroly or Hydrochlorthiazidum in clinical trials was not followed by any interaction between them.

Simultaneous use of a Vinpocetine and α-Methyldopums sometimes caused strengthening of hypotensive effect. Therefore at such treatment regular control of arterial pressure is necessary. Despite the lack of these clinical trials confirming a possibility of interaction it is recommended to show care at co-administration of a Vinpocetine with the drugs influencing the central nervous system, antiarrhythmic, anticoagulating and fibrinolitic means.

Contraindications:

Hypersensitivity to any component of drug, an acute stage and the first days after a hemorrhagic stroke, heavy coronary heart disease, severe forms of arrhythmias, the increased intraocular and intracranial pressure, pregnancy and the period of feeding by a breast, children's age (due to the lack of clinical data).

Overdose:

At overdose of drug are possible: arterial hypotension, block, nausea, vomiting. Symptomatic treatment.

Storage conditions:

Period of validity. 2 years. Not to use drug after the termination of the period of validity specified on packaging. To store in the unavailable to children, protected from light place at a temperature from 15 °C to 25 °C.

Issue conditions:

According to the recipe

Packaging:

On 2 ml in an ampoule. On 10 ampoules in a pack.