Vinpocetine

General characteristics. Structure:

Active ingredient: 5 mg of a Vinpocetine in 1 ml of solution.

Excipients: ascorbic acid, sodium disulphite (sodium metabisulphite), alcohol petrol, tartaric acid, sorbitol (D-sorbite), sodium tartrate, water for injections.

Pharmacological properties:

Pharmacodynamics. Improves metabolism of a brain, increasing consumption of glucose and oxygen brain tissue. Increases resistance of neurons 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).

Selectively blocks Sa2+-zavisimuyu phosphodiesterase (FDE); increases the level of adenosinemonophosphate (AMF) and a cyclic guanozinmonofosfat (tsGMF) of a brain. Increases concentration of ATP and a ratio of ATF/AMF in brain tissues; strengthens exchange of noradrenaline and serotonin of a brain; stimulates the ascending branch of noradrenergichesky system, has antioxidant effect. Vazodilatiruyushchy action is connected with the direct running-down impact on smooth muscles of vessels preferential of a brain.

The Vinpocetine does not cause a phenomenon of "burglarizing", 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 plasticity of erythrocytes. Raises a cerebral blood stream; reduces resistance of vessels of a brain without significant effect on indicators of system blood circulation.

Pharmacokinetics. Therapeutic concentration at parenteral administration in plasma - 10-20 ng/ml, distribution volume - 5,3 l/kg. Easily gets through gistogematichesky barriers (including hematoencephalic and hemato-ophthalmic barriers). Gets into breast milk (0,25% within the first hour), through a placental barrier. T1/2 - 4,74-5 h. It is removed by kidneys and intestines in the ratio 3:2.

Indications to use:

Neurology: as symptomatic - means at various forms of insufficiency of cerebral circulation (an ischemic stroke, a recovery stage of a hemorrhagic stroke, an effect of the had stroke; tranzitorny ischemic attack; vascular dementia; vertebrobazilyarny insufficiency; atherosclerosis of vessels of a brain; posttraumatic and hypertensive encephalopathy).

Ophthalmology: chronic vascular diseases of a choroid and retina of an eye (including occlusion of the central artery or vein of a retina).

Decrease in auditory acuity of perceptual type, Menyer's disease, idipatichesky sonitus.

Route of administration and doses:

Intravenously kapelno (speed of infusion should not exceed 80 caps/min.). An initial daily dose - 20 mg (in 0,5-1 l of 0,9% of solution of sodium of chloride or the solutions containing a dextrose). An average daily dose at the body weight of 70 kg - 50 mg. At good. portability within 2-3 days the dose of drug is raised to maximum - 1 mg/kg/days.

Course of treatment of-10-14 days. After achievement of improvement pass to administration of drug inside.

Features of use:

At administration of the solutions of a Vinpocetine containing sorbitol at patients with a diabetes mellitus it is necessary to control the content of glucose in blood.

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

Influence on ability to manage vehicles and mechanisms. At intravenous administration the Vinpocetine can cause dizziness in this connection at the first introductions the increased care in driving and working mechanisms is recommended.

Side effects:

From cardiovascular system: changes on an ECG (ST segment depression, lengthening of Q-T of an interval), tachycardia, premature ventricular contraction / lability of arterial pressure (decrease is more often).

From the central nervous system: a sleep disorder (sleeplessness, the increased drowsiness); dizziness, headache, general weakness.

From the alimentary system: dryness in a mouth, nausea, heartburn.

Others: skin allergic reactions, the increased sweating, a dermahemia, phlebitis in an injection site, heavy allergic reactions, a bronchospasm.

Interaction with other medicines:

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

Strengthening of hypotensive action at simultaneous use with metildopy is possible (control of arterial pressure is necessary).

Despite the absence of the data confirming a possibility of interaction it is recommended to be careful at simultaneous use with the drugs influencing the central nervous system, antiaritmikam and anticoagulants.

Contraindications:

Hypersensitivity, acute phase of a hemorrhagic stroke, severe form of coronary heart disease, heavy disturbances of a heart rhythm, pregnancy, the lactation period, age up to 18 years, intolerance of fructose, deficit 1,6 diphosphatases.

Overdose:

Now data on overdose are limited to a Vinpocetine.

Treatment at overdose: symptomatic therapy.

Storage conditions:

To store in the place protected from light at a temperature from 10 to 30 °C. To store in the place, unavailable to children. A period of validity - 2 years. Not to use after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

On 2 ml in ampoules from light-protective glass. On 5 ampoules in a blister strip packaging from a film of polyvinyl chloride and aluminum foil (or without foil). 1 or 2 blister strip packagings with the scarificator ampoule ceramic or a knife for opening of ampoules and the application instruction place in a pack from a cardboard. When using ampoules with a ring of a break or a point of a break the knife or the scarificator do not put.