Vinpocetine

General characteristics. Structure:

Deysvuyushchy substance: 5 mg of a Vinpocetine in 1 ml of solution.

The drug rendering the vasodilating, anti-aggregation, improving cerebral circulation, anti-hypoxemic.

Pharmacological properties:

Pharmacodynamics. Relaxes smooth muscles of vessels of a brain, strengthens blood supply of ischemic sites. Inhibits Sa2+-kalmodulinzavisimuyu tsGMF-phosphodiesterase, increases the maintenance of catecholamines (dopamine and noradrenaline), activity of adenylatecyclase and the maintenance of tsGMF and tsAMF in brain tissues. Reduces functional activity of cellular transmembrane natrium and calcium channels, receptors of NMDA and AMPA. Facilitates transport of oxygen and power substrates to fabrics. Strengthens absorption and exchange of glucose, switches metabolism to the aerobic direction, improves portability of a hypoxia brain cells.

Has antioxidant effect, increases deformability of erythrocytes and slows down aggregation of thrombocytes, reduction of viscosity of blood is a consequence of what. Has neurotyre-tread activity. Slightly lowers system the ABP.

Pharmacokinetics. It is quickly and completely absorbed from a GIT. Bioavailability — 50–70%. Contacts proteins of plasma for 66%. Cmax is reached in 1 h. Therapeutic concentration in plasma — 10–20 ng/ml. At parenteral administration the volume of distribution reaches 5,3 l/kg. Passes through a placenta and gets into breast milk.

The dihydroxy-Vinpocetine-glitsinata is exposed to biotransformation in a liver to apovinkaminovy acid, hydroxy Vinpocetine, gidroksiapovinkaminovy acid. The main metabolite — apovinkaminovy acid — has some pharmacological activity. The Vinpocetine is removed with urine in not changed look (slightly) and in the form of metabolites. T1/2 is 4,8–5 h.

Indications to use:

Disturbance of cerebral circulation (including a stroke, vertebro-basilar insufficiency, a brain injury, atherosclerotic changes of vessels of a brain, vascular dementia, hypertensive and posttraumatic encephalopathy), the alternating insufficiency and a vasospasm of a brain; partial occlusion of arteries, a headache, dizziness (including a labyrinth origin), memory disturbance, motive frustration, including apraxia, aphasia, arteriolosklerotichesky and angiospastic changes of a retina and a choroid of an eye, arterial and venous fibrinferments of vessels of an eye, degenerative changes of a macula lutea, secondary glaucoma owing to obturation of vessels; age, vascular or toxic (medicamentous) hearing disorder, Menyer's disease, kokhleovestibulyarny neuritis, sonitus; vazovegetativny manifestations of a menopausal syndrome (in combination with hormonal therapy).

Route of administration and doses:

Inside, after food, on 5–10 mg 3 times a day. A maintenance dose — on 5 mg 3 times a day. A course of treatment within 2 months.

In/in kapelno, slowly (the maximum speed of infusion — 80 thaws/min.), on 10–20 mg in 500–1000 ml of isotonic solution of sodium of chloride. In need of a current of 3-4 days the dose is increased to maximum — 1 mg/kg/days. A course of treatment — 10–14 days. Then pass to administration of drug inside (10 mg 3 times a day) with gradual reduction of a dose before cancellation.

Features of use:

Contraindicated at pregnancy. The category of action on a fruit — is not determined by FDA. For the period of treatment it is necessary to stop breastfeeding.

It is not recommended to appoint at the labile ABP and a low vascular tone.

With care appoint to the patients accepting the hypotensive drugs or drugs increasing QT interval, and also patients with bad portability of alkaloids of the Periwinkle of small (Vinca minor) and having a liver failure.

It is not allowed п / to, in oil and jet in/in introduction.

It is not necessary to apply in operating time to drivers of vehicles and people whose profession is connected with the increased concentration of attention.

At parenteral administration by a sick diabetes mellitus control of content of glucose in blood is necessary (solution contains sorbite). In the presence of a syndrome of the extended interval of QT or at simultaneous use of the drugs provoking lengthening of an interval of QT control of an ECG is necessary.

At a hemorrhagic stroke parenteral use of drug is admissible only after disappearance of the acute phenomena (in 5–7 days).

There is no sufficient number of observations on use of drug in children's practice.

Side effects:

From a nervous system and sense bodys: dizziness, headache, sleeplessness, drowsiness, weakness.

From cardiovascular system and blood (a hemopoiesis, a hemostasis): delay of intra ventricular conductivity; a depression of a segment of ST and lengthening of an interval of QT, hypotension, tachycardia, premature ventricular contraction, erubescence, thrombophlebitis in an injection site.

From bodies of a GIT: dryness in a mouth, nausea, heartburn.

From integuments: perspiration.

Others: allergic reactions.

Interaction with other medicines:

Increases risk of hemorrhagic complications against the background of a geparinoterapiya. Strengthens action of antihypertensives.

Contraindications:

Hypersensitivity, severe forms of an ischemic heart disease and arrhythmias, the first days after a cerebral hemorrhagic stroke, the increased intracranial pressure; pregnancy, feeding by a breast.

Overdose:

Treatment: gastric lavage, purpose of absorbent carbon, symptomatic therapy.

Storage conditions:

To store at a temperature of 15-25 °C, in dry, protected from light and the place, unavailable to children. Period of validity 3 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Solution for injections of 5 mg/ml, on 2 ml in each ampoule. On 5 or on 10 ampoules, together with the application instruction in cardboard packaging.