Vinpotsetin-Darnitsa konts. for solution for inf. 5mg/ml amp. 2 ml No. 10

Pharmacological properties

Pharmakodinamichesky parameters. the Vinpocetine is to semi-synthetic derivatives of Vincaminum — the alkaloid emitted from leaves of a periwinkle of small (vinca minor).

Main effects of a Vinpocetine:

• selective strengthening of a brain blood-groove and utilization of oxygen without significant change of parameters of system blood circulation;
• increase in tolerance of tissues of brain to a hypoxia and ischemia;
• inhibition of activity of FDE;
• improvement of rheological properties of blood and inhibition of aggregation of thrombocytes.

Vinpocetine selectively inhibits Ca ²⁺ - kalmodulinzavisimy tsGMF-FDE, thereby increasing the intracellular maintenance of tsGMF in unstriated muscles of a vascular wall. It leads to decrease in resistance of cerebral vessels and increase in a brain blood-groove (including in ischemic sites at patients with cerebrovascular diseases).

Vinpocetine strengthens cerebral metabolism by increase in oxygen absorption and glucose and stimulation of products of ATP in brain neurons (including undergone hypoxia/ischemia).

tire-tread effect at ischemic damage of fabrics, including a brain, a liver and an endothelium of vessels. So, the Vinpocetine reduces metabolic requirements of a retina in the conditions of hypoxia/ischemia; reduces death of cells and improves functions of a retina after ischemia reperfusion.

with decrease of the activity of potentsialzavisimy neuronalny Na ⁺ - channels, indirect inhibition of some molecular cascades caused by increase in the intracellular Ca ^{2+ levels} , and, to a lesser extent, an obstacle to the return capture of adenosine.

In implementation of neuroprotection such properties of a Vinpocetine as strengthening of cerebral circulation and cerebral metabolism, decrease in viscosity of blood and also easing of an oxidizing stress, removal of hydroxyl radicals, modulation of immune responses make a contribution.

Inhibiting activity of a kinase of IκB, the Vinpocetine works as the powerful anti-inflammatory agent. Besides, the Vinpocetine suppresses accumulation of lipids in macrophages, prevents proliferation of cells of unstriated muscles of vessels and remodeling of vessels.

Vinpocetine improves cognitive functions: both short-term, and long-term memory; increases alertness and attentiveness; reduces severity of senile cerebral dysfunction.

Vinpocetine increases spatial memory thanks to the antioxidant mechanism, modulation of cholinergic functions and prevention of injury of neurons; increases the level of the neurotransmitters participating in memory functions (noradrenaline, dopamine, acetylcholine and serotonin).

Pharmacokinetic parameters. After reception the Vinpocetine is quickly absorbed from a small intestine, the C _max medicament in blood reached in 1 h. Thanks to high lipophilicity the Vinpocetine easily gets through GEB.

Vinpocetine is exposed to extensive metabolism during which about 75% of a Vinpocetine are hydrolyzed in its main active metabolite — apovinkaminovy acid. The t _½ a Vinpocetine after oral administration makes 1–2 h 60% of a dose is allocated with kidneys, 40% — are removed with a stake.

Indication

State after the postponed disturbance of cerebral circulation / stroke, disturbance of a blood-groove in arteries of a vertebrobazilyarny system, dementia (vascular genesis), atherosclerosis of cerebral vessels, encephalopathy (posttraumatic, hypertensive); chronic pathology of a uveal path and retina of an eye. presbyacusis (perceptual type), disease of a menyer, tinnitus.

Use

Solution: in/in by drop infusion (speed of ≤80 thaws/min.). starting dose: 20 mg in 500 ml of solution for infusions which contains glucose (possibly cultivation of 0.9% nacl solution). divorced solution is stored 3ch. the maximum daily dose — 1 mg/kg of body weight (increase from starting within 2–3 days). a course — 10–14 days.

Tablet: adult per os (after meal) on 5–10 mg 3 times a day.

Contraindication

Gipechuvstvitelnost to active ingredient of medicament or other its components;

at patients with such pathology:

• hemorrhagic stroke (sharp phase);
• an ischemic heart disease (severe form);
• significant disturbances of a warm rhythm.

Parenteral and oral administration of a Vinpocetine is well transferred by

and has a favorable profile of safety. it was not reported about any considerable side effects connected with treatment. there is information on such side effects:

• decrease in maintenance of thrombocytes (150∙10 ⁹ / l), agglutination of erythrocytes, anemia, it is rare — an agranulocytosis;
• increase in level of cholesterol in blood, diabetes, lack of appetite (at objective food requirement);
• depression, euphoria, irritability, excitement, concern;
• headache, dizziness, drowsiness, faint, preunconscious state, hemiparesis, tremor, block, sleep disorder;
• hemorrhage in an anterior chamber of an eye, decrease in visual acuity, far-sightedness, short-sightedness, a diplopia, conjunctiva hyperaemia, a papilledema;
• a hearing disorder, hyper - a gipoakuziya, vertigo, tinnitus;
• ischemia/necrosis of a cardiac muscle, stenocardia, disturbances of a warm rhythm, decrease (40 ud. / mines) or increase (90 ud. / mines) ChSS, premature ventricular contraction, heart consciousness, heart failure, atrial fibrillation;
• venous insufficiency, thrombophlebitis, rushes of blood;
• hypersalivation, dryness in a mouth, heartburn nausea, vomiting, abdominal discomfort, dyspepsia;
• reaction of hypersensitivity (include hyperaemia, rash, an itching, urticaria), dermatitis, excess sweating;
• feeling of heat, discomfort in a thorax, weakness;
• inflammatory process, thrombosis in the place of injection introduction.
• decrease (or increase, fluctuations of level) ABP; disturbances of the ECG: lengthening of an interval P–R, Q–T, ST segment depression; in blood plasma: increase in level of urea, activity of LDG.

Special instructions

Should observe discretion at use for patients with stenocardia and with the significant disturbances of a warm rhythm.

during therapy by a Vinpocetine should not take alcohol.

is not applied during pregnancy and feeding by a breast.

information on influence of medicament on speed of response at control of vehicles and other mechanisms.

Expressed inhibition of p-gp indicates

Interaction

Vinpocetine can not influence the metabolism of medicines mediated by CYP.

As the Vinpocetine reduces aggregation of thrombocytes, it is necessary to avoid its combined use with anticoagulants.

Combined use from α-metildopy strengthens antihypertensive action.

does not have influence of a Vinpocetine on pharmacokinetic parameters of Imipraminum and oxazepam.

Combined use of a Vinpocetine and glibenclamide is safe.

Overdose

Data are absent.

Storage conditions

At a temperature of ≤25 °C in original packing. not to subject solution to freezing.

Translation of the instruction Mose