Винпотропил® solution

General characteristics. Structure:

Active agents: Vinpocetine of 1,0 mg, piracetam of 80,0 mg;
excipients: ascorbic acid of 5,00 mg, succinic acid of 13,40 mg, sodium disulphite (sodium metabisulphite) 3,00 mg, water for injections to 1 ml.

Description:
The transparent colourless or slightly painted liquid.

Pharmacological properties:

Pharmacodynamics. ВИНПОТРОПИЛ® - the combined drug. Has the properties characteristic for tserebrovazodilatiruyushchy (Vinpocetine) and for nootropic (piracetam) of means.
The Vinpocetine improves cerebral circulation, causes brain vasodilatation, strengthening of a blood-groove and improvement of supply of a brain with oxygen and glucose. Increases resistance of cells of a brain 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, switching it to energetically more favorable aerobic direction). Promotes accumulation in fabrics of cyclic adenosinemonophosphate and adenosinetriphosphate (inhibition of phosphodiesterase and stimulation of adenylatecyclase), increase in maintenance of catecholamines in brain tissues. Vazodilatiruyushchy action is connected with the direct weakening action on smooth muscles of vessels preferential of a brain, does not cause a phenomenon of "burglarizing" and 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 elasticity of erythrocytes.
Piracetam - cyclic derivative piperidic acid, influences directly a brain, improving cognitive (cognitive) processes, such as ability to training, memory, attention, and also intellectual working capacity. Exerts impact on the central nervous system in various ways: changes the speed of spread of activation in a brain, improves metabolic processes in nervous cells, improves microcirculation, influences rheological characteristics of blood, without having at the same time vazodilatiruyushchy effect.
Improves communication between cerebral hemispheres and synaptic conduction in neocortical structures, improves a brain blood stream.
Inhibits aggregation of thrombocytes and recovers configuration properties of an outer membrane of rigid erythrocytes, and also ability of the last to a passage through vessels of a microcirculator bed. In a dose of 9,6 g reduces concentration of fibrinogen and Villebrand's factor by 30-40% and extends a bleeding time.
Has the tire-tread and recovering effect at dysfunction of a brain owing to a hypoxia and intoxication. Reduces expressiveness and duration of a vestibular nystagmus.

Pharmacokinetics. For a Vinpocetine. Therapeutic concentration in plasma - 10-20 ng/ml. At parenteral administration 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. Easily gets through gistogematichesky barriers (including a blood-brain barrier (GEB)). An elimination half-life of T1/2 - 3,54-6,12 h. It is removed by kidneys and intestines in the ratio 3:2. Out of medullispinal liquid it is brought much more slowly, than out of other fabrics.
For piracetam. An elimination half-life of T1/2 from a blood plasma - 4,5 h, from a brain - 7,7 h, from cerebrospinal fluid - 8,5 h. Practically is not exposed to biotransformation and on 2/3 it is allocated with kidneys in an invariable look during 30 h. The general clearance - 80-90 ml/min. The elimination half-life of T1/2 is extended at the chronic renal failure (CRF) (at terminal HPN - to 59 h). The liver failure does not influence piracetam pharmacokinetics. The specific volume of distribution of Vd - about 0,6 l/kg. Gets through GEB and a placental barrier; is removed at a hemodialysis. In experiments on animals selectively collects in tissues of a cerebral cortex, it is preferential in frontal, parietal and occipital lobes, in a cerebellum and basal kernels. Does not contact proteins of plasma.

Indications to use:

Insufficiency of cerebral circulation (the recovery period of an ischemic and hemorrhagic stroke), encephalopathies of various genesis, including at alcoholism; parkinsonism of vascular genesis, intoxication, a brain injury and other diseases of the central nervous system which are followed by decrease intellectual мнестических functions; a psychoorganic syndrome with dominance of signs of an adynamy and adynamia, an asthenic syndrome; labyrinthopathies, Menyer's syndrome.

Route of administration and doses:

In/in kapelno on 50-100 ml (2-3 ampoules of the drug which is previously divorced in 500 ml of infusion solution (0,9% of solution of sodium of chloride or the solutions containing a dextrose)), 1 time a day (speed of infusion should not exceed 80 caps/min.). A course of treatment - 10-14 days.
In need of it it is possible to repeat in 6-8 weeks.
After achievement of improvement pass to administration of drug inside.

Features of use:

Constant control behind indicators of function of kidneys (especially at patients with HPN) - the content of nitrogen and concentration of creatinine is recommended, and patients with diseases of a liver have a functional condition of a liver.
At long therapy at patients of advanced age regular control of function of kidneys is recommended, if necessary carry out correlation of a dose depending on concentration of creatinine.
Gets through the filtering membranes of devices for a hemodialysis.
In case of initial lengthening of Q-T of an interval, and also at simultaneous use with the medicines extending Q-T an interval during treatment periodic ECG control is necessary.
During treatment it is necessary to be careful during the driving of motor transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

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 the arterial pressure (AP) (decrease is more often).
From the central nervous system (CNS): motive disinhibition, irritability, a depression, an adynamy, dizziness, a headache, a sleep disorder (sleeplessness, the increased drowsiness), a hyperphrenia, balance disturbance, an aggravation of a course of epilepsy, alarm, hallucinations, confusion of consciousness, extrapyramidal disturbances, decline in the ability to concentration of attention.
From the alimentary system: nausea, vomiting, heartburn, diarrhea, abdominal pain, loss of appetite, gastralgias, lock.
From a metabolism: increase in body weight, the increased sweating.
From sense bodys: вертиго.
From integuments: dermatitis, itch, urticaria, dermahemia.
Allergic reactions: hypersensitivity, anaphylactic reactions, Quincke's disease.
Local reactions: pain in an injection site, thrombophlebitis.
Others: fever, the general weakness (can be manifestation of a basic disease), increase in sexual activity.

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 the ABP is necessary).
Piracetam solution pharmaceutical is compatible to dextrose solutions (5%, 10%, 20%), fructose (5%, 10%, 20%), 0,9% chloride sodium solution, Ringer's solution, 20% Mannitolum solution, hydroxyethylstarch (6%, 10%).
Increases risk of a hemorrhagic complication against the background of a geparinoterapiya, efficiency of hormones of a thyroid gland, antipsychotic medicines (neuroleptics), indirect anticoagulants (against the background of high doses of piracetam).
At simultaneous use with the medicines stimulating TsNS excessive stimulation of TsNS is possible.
Weakens effect of anticonvulsant drugs (reduces a convulsive threshold).
At appointment with neuroleptics reduces danger of emergence of extrapyramidal disturbances.
Use during pregnancy and breastfeeding.
Drug is not recommended to be used during pregnancy and a lactation.

Contraindications:

Hypersensitivity to drug components, pregnancy, the lactation period, the expressed disturbances of a heart rhythm, coronary heart disease (a heavy current), a hemorrhagic stroke, heavy HPN (the clearance of creatinine (CC) less than 20 ml/min.), a liver failure, age of the patient up to 18 years.

With care:
Disturbance of a hemostasis, extensive surgical interventions, heavy bleeding, HPN (KK of 20-80 ml/min.).

Overdose:

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 3 years. Not to apply after a period of validity.

Issue conditions:

According to the recipe

Packaging:

Concentrate for preparation of solution for infusions of 1 mg + 80 mg/ml.
On 5 ml in the ampoules from glass of the 1st hydrolytic class of brown color having a break point.
On 5 or 10 ampoules place in a blister strip packaging from a film polyvinyl chloride.
On 1 or 2 blister strip packagings together with the application instruction place in a pack from a cardboard.
It is allowed to put the scarificator in a pack.