Vinpocetine

General characteristics. Structure:

Active ingredient: 10 mg of a Vinpocetine in 2 ml of solution.

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

Pharmacological properties:

Pharmacodynamics. The Vinpocetine possesses the complex mechanism of medical action, favorably influencing cerebral circulation and cerebral metabolism, and also rheological properties of blood. Causes small decrease in system arterial pressure, brain vasodilatation, strengthening of a blood-groove and improvement of supply of a brain with oxygen and glucose. Increases resistance of cells of a brain to a hypoxia, facilitating transport of oxygen and substrates of power providing to fabrics (owing to reduction of affinity to it of erythrocytes, strengthening of absorption and metabolism of glucose, its switching to energetically more favorable aerobic direction).

Promotes accumulation in fabrics of cyclic adenosinemonophosphoric acid and adenosinetriphosphate (braking of phosphodiesterase and stimulation of adenylatecyclase), increase in maintenance of catecholamines in brain tissues. Vazodilatiruyushchy action is connected with the direct running-down action on smooth muscles of vessels preferential of a brain, does not cause a phenomenon of "burglarizing", and first of all strengthens blood supply of ischemic area of a brain, without changing at the same time blood supply of intact areas. Improves microcirculation in a brain due to reduction of aggregation of thrombocytes, decrease in viscosity of blood, increase in deformability of erythrocytes.

Pharmacokinetics. At intake it is quickly and completely absorbed in a GIT. Bioavailability - 50-70%. There is 1 h TCmax. Therapeutic concentration in plasma - 10-20 ng/ml. At parenteral administration distribution volume – 5,3 l/kg. T1/2 is 4,74-5 h. Easily gets through gistogematichesky barriers (including GEB).

Indications to use:

Acute and chronic disorder of cerebral circulation (tranzitorny ischemia, the progressing stroke, a complete stroke, a state after a stroke). Neurologic and mental disturbances at patients with cerebrovascular insufficiency (memory disturbance; dizziness; aphasia, apraxia, motive frustration, headache). Encephalopathy (hypertensive, posttraumatic). Vazovegetativny symptomatology in a climacteric. Vascular diseases of eyes (degenerative diseases of a choroid, retina or macula lutea; partial occlusions of arteries, secondary glaucoma). Decrease in auditory acuity of vascular or toxic genesis, senile relative deafness, Menyer's disease, kokhleovestibulyarny neuritis, sonitus, dizziness of a labyrinth origin.

Route of administration and doses:

In an acute phase of a disease if necessary - in/in kapelno. An initial daily dose - 20 mg (to dissolve in 500-1000 ml of infusion solution). An average daily dose at the body weight of 70 kg - 50 mg. At good tolerance within 3-4 days the dose is raised to maximum - 1 mg/kg/days. A course of treatment - 10-14 days.

After achievement of clinical improvement pass to medicine reception inside, 5-10 mg 3 times a day. A maintenance dose - 5 mg 3 times a day for a long time. Before cancellation the dose should be reduced gradually.

Features of use:

At parenteral administration by a sick diabetes mellitus it is necessary to control the content of glucose in blood since solution contains sorbitol, patients with cardial pathology cannot enter in/in because of danger of development of arrhythmia (up to fibrillation of ventricles).

In case of initial lengthening of Q-T of an interval, and also at simultaneous use with the HP extending Q-T an interval during treatment by a Vinpocetine periodic ECG control is necessary.

Side effects:

From CCC: changes on an ECG (ST segment depression, lengthening of Q-T of an interval); tachycardia, premature ventricular contraction (relationship of cause and effect is not established), lability of the ABP (decrease is more often).

From TsNS: a sleep disorder (sleeplessness, the increased drowsiness); dizziness, a headache, the general weakness (can be manifestation of a basic disease).

From the alimentary system: dryness of a mucous membrane of an oral cavity, nausea, heartburn.

Others: skin allergic reactions, the increased sweating, feeling of heat, a dermahemia, thrombophlebitis in an injection site.

Interaction with other medicines:

Vinpocetine solution pharmaceutical is incompatible with the heparin, solutions containing amino acids.

Strengthens action of antihypertensives. Strengthening of hypotensive action at simultaneous use with metildopy is possible (control of the ABP is necessary).

Contraindications:

Hypersensitivity, pregnancy, the lactation period, age up to 18 years. With care – coronary heart disease (a heavy current), heavy disturbances of a rhythm (parenteral administration). At a hemorrhagic stroke parenteral administration is possible only after subsiding of the acute phenomena (usually in 5-7 days).

Overdose:

Symptoms: metal smack in a mouth; thirst, the expressed tremor, a dysarthtia, an ataxy.

Treatment: gastric lavage, reception of absorbent carbon, symptomatic treatment.

Storage conditions:

In the place protected from light, at a temperature not over 25 ºС. To store in the place, unavailable to children. A period of validity - 2 years. Not to use medicine after the termination of a period of validity.

Issue conditions:

According to the recipe

Packaging:

On 2 ml in ampoules in packaging No. 10, No. 10 x 1.