Винпотропил®

General characteristics. Structure:

Active agents: Vinpocetine of 10 mg, piracetam of 800 mg;
excipients: hydrophosphate calcium dihydrate of 120 mg, croscarmellose sodium (primelloza) of 33 mg, magnesium stearate of 7 mg, povidone of 21 mg, talc of 7 mg, cellulose of microcrystallic 102 mg;
structure of a film cover: Опадрай II brown 35 mg, including: gipromelloz (gidroksipropilmetiltsellyuloz) of 9,8 mg, macrogoal (polyethyleneglycol) of 3,5 mg, lactoses monohydrate (sugar milk) 12,6 mg, dye ferrous oxide of red 3,08 mg, dye ferrous oxide of black 5,985 mg, titanium dioxide of 0,035 mg.

Description:
Tablets are oval, with risky, film coated light brown color with a grayish shade. On cross section of almost white color.

Pharmacological properties:

Pharmacodynamics. Винпотропил® – the combined drug. Has the properties characteristic of the means improving a brain blood stream (Vinpocetine) and for nootropic means (piracetam).
As the means improving a brain blood stream
Improves metabolism of a brain, increasing consumption of glucose and oxygen brain tissue. Increases resistance of neurons to a hypoxia, strengthens glucose transport to a brain through a blood-brain barrier; transfers process of disintegration of glucose to energetically more economical, aerobic way; selectively blocks Sa2+-zavisimuyu phosphodiesterase; increases levels of adenosinemonophosphate (AMF), a cyclic guanozinmonofosfat (tsGMF) and adenosinetriphosphate (ATP) of a brain. Strengthens exchange of noradrenaline and serotonin of a brain; has antioxidant effect. Reduces aggregation of thrombocytes and the increased viscosity of blood; increases elasticity of erythrocytes and blocks utilization by adenosine erythrocytes; promotes increase in return by oxygen erythrocytes. Increases a cerebral blood stream; reduces resistance of vessels of a brain without essential change of indicators of system blood circulation. Does not render effect of "burglarizing" and strengthens blood supply, first of all, in ischemic sites of a brain. Gets through a placental barrier.
As nootropic means
Improves integrative activity of a brain, promotes memory consolidation, facilitates training process; changes the speed of spread of activation in a brain, improves microcirculation, without having at the same time vasodilating effect, suppresses aggregation of the activated thrombocytes; has protective action at the injuries of a brain caused by a hypoxia, intoxications, an electroshock; strengthens α-and β-activity, reduces δ-activity on the electroencephalogram, reduces expressiveness of a vestibular nystagmus; improves bonds between cerebral hemispheres and synaptic conduction in neocortical structures, increases intellectual activity, strengthens a brain blood stream; has no sedative, psychogogic influence. The effect develops gradually.
Has the expressed effect concerning symptoms of initial manifestations of cognitive disturbances of cerebral and vascular genesis at patients of advanced and senile age. It is recommended in psychogeriatric practice.

Pharmacokinetics. The Vinpocetine is quickly soaked up. Therapeutic concentration in plasma – 10-20 ng/ml. Time of achievement of the maximum concentration in a blood plasma – 1 h. Absorption happens, mainly, in proximal departments of digestive tract. When passing through a wall of intestines is not exposed to metabolism. The maximum concentration in fabrics is noted in 2-4 h after intake. Communication with proteins – 66%, bioavailability at intake – 7%. The clearance of 66,7 l/h exceeds the plasma volume of a liver (50 l/h) that demonstrates extrahepatic metabolism. The main metabolite is apovinkaminovy acid which has some pharmacological activity. Other inactive metabolites – hydroxy Vinpocetine, hydroxy-apovinkaminovaya acid, a hydroxy-Vinpocetine-glitsinat. At repeated receptions the kinetics has linear character. Elimination half-life (T1/2) at the person – 4,83±1,29 h. It is removed by kidneys and through intestines in the ratio 3:2.
Piracetam after intake is well soaked up and gets into various bodies and fabrics. Bioavailability makes about 100%. After a single dose inside in a dose of 3,2 g the maximum concentration – 84 mkg/ml, after repeated (3,2 g 3 times a day) – 115 mkg/ml. Time of achievement of the maximum concentration in plasma of 1 h, cerebrospinal fluid – 5 h. Distribution volume – about 0,6 l/kg. Gets through hematoencephalic and placental barriers, selectively collects in tissues of a cerebral cortex. Practically is not exposed to biotransformation and it is removed by kidneys in not changed look by glomerular filtering. The general clearance of 80-90 ml/min. of T1/2 from a blood plasma – 4-5 h, from cerebrospinal fluid – 8,5 h.

Indications to use:

Insufficiency of cerebral circulation (recovery period of an ischemic and hemorrhagic stroke); chronic insufficiency of cerebral circulation of hypertensive and posttraumatic genesis, parkinsonism of vascular genesis, intoxication; a psychoorganic syndrome with dominance of signs of an adynamy and adynamia; symptomatic treatment of dizzinesses; prevention of migraine and kinetoz.

Route of administration and doses:

The course of treatment and dosage is defined by the attending physician.
For patients of 18 years is also more senior: inside, irrespective of meal on 1 tablet 2 - 3 times a day, washing down with enough water. The last reception – in 4 hours prior to a dream. Duration of a course of treatment makes from 2-3 weeks to 2-6 months. Before drug withdrawal the dose is recommended to be reduced gradually (possibly use of the drug Vinpotropil® in other dosage form: the capsules containing 5 mg of a Vinpocetine and 400 mg of piracetam).

Features of use:

Existence of a syndrome of the prolonged interval of QT and administration of drugs causing lengthenings of an interval of QT demands periodic control of an ECG. Due to the influence of piracetam on aggregation of thrombocytes care at purpose of drug is recommended to patients with disturbance of a hemostasis, during big surgeries or the patient with symptoms of heavy bleeding.
Influence on ability to driving of motor transport and to control of mechanisms
During treatment it is necessary to be careful when driving motor transport and performing work with mechanisms.

Side effects:

From cardiovascular system: change of the electrocardiogram (ECG) (ST segment depression, lengthening of an interval of QT), tachycardia, premature ventricular contraction, deterioration in a course of stenocardia, lability of arterial pressure, feeling of "inflows".
From the central nervous system: sleep disorders, a headache, dizziness, a hyperphrenia, motive disinhibition, irritability, disbalance, decline in the ability to concentration of attention, uneasiness, a depression, an ataxy, extrapyramidal frustration (including a hyperkinesia), spasms, a tremor.
From system of digestion: a gastralgia, nausea, vomiting, diarrhea, dryness in a mouth, heartburn.
From sense bodys: вертиго.
From integuments: reddening, dermatitis, itch, urticaria.
Others: allergic reactions, increase in sexual activity, increase in body weight, an adynamy, the general weakness, the increased sweating.

Interaction with other medicines:

Raises: risk of a hemorrhagic complication against the background of a geparinoterapiya, effects of hormones of a thyroid gland, antipsychotic means (neuroleptics), psychostimulants, indirect anticoagulants, including an atsenokumarola (more expressed decrease in aggregation of thrombocytes, contents of fibrinogen, Villebrand's factor, viscosity of plasma and blood).
Perhaps some strengthening of hypotensive effect at simultaneous use with metildopy (control of arterial pressure is necessary).
Weakens: effect of anticonvulsant drugs (reduces a convulsive threshold).
Despite the absence of the data confirming a possibility of interaction it is recommended to show care at co-administration with drugs of the central, antiarrhythmic action.

Contraindications:

Hypersensitivity, pregnancy, the lactation period, the expressed disturbances of a heart rhythm, coronary heart disease (heavy current), acute stage of a hemorrhagic stroke, renal and/or liver failure, deficit of lactase, lactose intolerance, glyukozo-galaktozny malabsorption, children aged up to 18 years (in connection with insufficiency of data).

With care:
Disturbance of a hemostasis, heavy bleeding, high-quality hyperbilirubinemias (including Gilbert's syndrome), viral hepatitis, alcoholic damage of a liver, alcoholism, deficit glyukozo-6-fosfatdegidrogenazy, epilepsy, advanced age.

Use at pregnancy and in the period of a lactation:
Drug is contraindicated at pregnancy and in the period of a lactation.

Overdose:

Vinpocetine
Symptoms: strengthening of expressiveness of dozozavisimy side effects.
Treatment: gastric lavage, reception of absorbent carbon, symptomatic therapy.
Piracetam
Symptoms: abdominal pain, diarrhea with blood impurity.
Treatment: symptomatic therapy, hemodialysis (efficiency of 50-60%). There is no specific antidote.

Storage conditions:

In the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity: 2 years. Not to apply after a period of validity.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated, 10 mg + 800 mg.
On 10 tablets in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished.
On 3 or 6 blister strip packagings together with the application instruction place in a pack from a cardboard.