Vinpocetine

General characteristics. Structure:

Active ingredient - a Vinpocetine of 5,0 mg.

Excipients - ascorbic acid of 0.5 mg, D-sorbitol of 80 mg, tartaric acid to pH 3.0-4.0, benzyl alcohol of 10 mg, sodium disulphite of 1 mg, water for and to 1 ml.

Pharmacological properties:

Pharmacodynamics. The Vinpocetine selectively inhibits potentsialzavisimy natrium channels, causing dozozavisimy decrease in concentration of calcium in the terminations of neurons of a striate body. It is considered that decrease in current of sodium renders the neuroprotective effect caused by decrease in an eksaytotoksichnost and weakening of the neyronalny damage caused by ischemia of a brain or reperfusion.

The Vinpocetine increases concentration of 3,4-dihydroxyphenylacetic acid (a dopamine metabolite) in nerve terminations of a striate body. Such action is similar to pharmacological action of Reserpinum (reminding a Vinpocetine on chemical structure) which exhausts stocks of catecholamines in nerve terminations of a brain that causes side effects from cardiovascular system and antipsychotic effect.

It also inhibits phosphodiesterase 1 that leads to increase in concentration of an intracellular cyclic guanozinmonofosfat. It leads to relaxation of unstriated muscles of vessels of a brain.

Pharmacokinetics: Therapeutic concentration at parenteral administration in plasma - 10-20 ng/ml, distribution volume - 5.3 l/kg. Communication with proteins - 66%, clearance - 66.7 l/h, exceeds the plasma volume of a liver (50 l/h) that demonstrates extrahepatic metabolism.

Gets into breast milk (0.25% within 1 hour), through a placental barrier. It is removed by kidneys and intestines in the ratio 3:2.

Indications to use:

- Neurology (with structure of complex therapy): 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; a circulatory unefficiency in the vertebrobazilyarny pool; atherosclerosis of vessels of a brain; posttraumatic and hypertensive encephalopathy).

- Ophthalmology: chronic diseases of a choroid and vessels of a 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, idiopathic sonitus.

Route of administration and doses:

Intravenously kapelno (speed of infusion should not exceed 80 caps/min.).

Initial daily dose - 20 mg (in 0.5-1 l of 0.9% of NaCl solution or the solutions containing a dextrose). An average daily dose at the body weight of 70 kg - 50 mg. At good tolerance within 2-3 days the dose is raised to maximum - 1 mg/kg/days. A course of treatment - 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 HP extending Q-T an interval during treatment by a Vinpocetine periodic ECG control is necessary.

Side effects:

From cardiovascular system: 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 arterial pressure (decrease is more often).

From the central nervous system: 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, a dermahemia, phlebitis at intravenous administration.

Interaction with other medicines:

Vinpocetine solution 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).

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 (in connection with insufficiency of data).

Overdose:

At overdose - a symptomatic treatment.

Storage conditions:

To store in the place protected from light at a temperature from 15 °C to 25 °C.

To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Concentrate for preparation of solution for infusions 5mg/l on 2 ml or 5 ml in ampoules of light-protective glass.

5 ampoules of light-protective glass in a planimetric strip packaging from a film polyvinyl chloride.

2 blister strip packagings from a film polyvinyl chloride together with the application instruction and the scarificator ampoule or a knife ampoule in a pack cardboard.

When using ampoules with a point or a ring of a break the scarificator or a knife ampoule do not put.