Vinpocetine - instructions for use, dose, side effects, contraindications

Composition:1 ampoule (2 ml) contains as active ingredient vinpocetine - 10.0 mg; Excipients sorbitol -160.0 mg, propylene glycol 40.0 mg, citric acid monohydrate 8.0 mg, sodium metabisulphite 2.0 mg, disodium edetate 1.0 mg, sodium sulfite 0.2 mg, 1 M hydrochloric acid solution up to pH 3.4, water for injection - up to 2.0 ml.

Description:transparent colorless or with a slightly greenish-yellow liquid tint.

Pharmacotherapeutic group:cerebral blood flow improves.

ATX: & nbsp

N.06.B.X.18 Vinpocetine

Pharmacodynamics:

Vinpocetine improves cerebral circulation. Has vasodilator, neuroprotective, antihypoxic and antiplatelet effect.

Vinpocetine selectively inhibits the potential-dependent Ca2 + channels, causing a dose-dependent decrease in Na + concentration in the endings of the striatum neurons. It is believed that a decrease in the current of Na + has a neuroprotective effect due to a decrease in excitotoxicity and a weakening of neuronal damage caused by cerebral ischemia or reperfusion.

Vinpocetine increases the concentration of 3,4-dihydroxyphenylacetic acid (dopamine metabolite) in the nerve endings of the striatum. This action is similar to the pharmacological action of reserpine (reminiscent of the chemical structure vinpocetine), which depletes the supplies of catecholamines in the nerve endings of the brain, which causes side effects from the cardiovascular and antipsychotic effects.

Inhibits phosphodiesterase and increases the content of cyclic adenosine monophosphate in cells, which in turn leads to a decrease in calcium content in the cytoplasm of smooth muscle cells and relaxation of myofibrils. It combines vascular and metabolic action. It dilates the blood vessels of the brain, increases blood flow, mainly in ischemic areas,improves the supply of oxygen to the brain; promotes the utilization of glucose and increases the level of catecholamines in the central nervous system, stimulates the metabolism of norepinephrine and serotonin in the brain tissues.

Reduces platelet aggregation, blood viscosity, promotes increased erythrocyte deformability and normalization of venous outflow against a background of decreased resistance of cerebral vessels. Systemic blood pressure slightly decreases. Efficacy in the acute period of ischemic stroke: accelerates the regress of cerebral and focal neurological symptoms. Improves memory, attention, intellectual productivity.

In the elderly and senile age, the sensitivity of cerebral vessels to the relaxing action of vinpocetine increases, which is due to

sensitization of the adenylate cyclase system of cyclic adenosine monophosphate upon aging.

Pharmacokinetics:With parenteral administration, it easily penetrates through the histohematological barriers (including through the blood-brain barrier). Penetrates into breast milk (0.25% within the first hour) through the placental barrier. The volume of distribution is 5.3 l / kg body weight.The connection with the proteins-plasma-blood - 66%, - clearance - 66.7 l / h exceeds the plasma volume of the liver (50 l / h), which indicates extrahepatic metabolism. The half-life is 4.75 hours.

Indications:

- neurology: as a symptomatic agent for various forms of inadequacy, cerebral circulation (transient ischemic attack, acute and residual stages of ischemic stroke, recovery stage of hemorrhagic stroke, consequences of stroke, vascular dementia, vertebrobasilar insufficiency, cerebral arteriosclerosis, posttraumatic and hypertensive encephalopathy) mental and neurological disorders associated with cerebrovascular insufficiency (rasstra) Memory-keeping, dizziness, headache, aphasia, apraxia, motor disorders);

- ophthalmology: chronic vascular diseases of the retina and / or choroid; degenerative changes in the macula caused by atherosclerosis or angiospasm; partial occlusion of blood vessels, arterial and venous thrombosis or embolism, secondary glaucoma;

- otolaryngology: senile hearing loss, Meniere's disease, worsening of vascular hearing, toxic (including medication) or age, dizziness of labyrinthine origin, idiopathic tinnitus, vasovegetative manifestations of climacteric syndrome.

Contraindications:

- hypersensitivity to vinpocetine or excipients of the drug;

- severe ischemic heart disease;

- severe forms of heart rhythm disturbances;

- acute phase of hemorrhagic stroke;

- age under 18 years (due to insufficient data on safety and effectiveness);

- pregnancy and lactation.

If you are hypersensitive to the active ingredient or other components of the drug, be sure to consult a doctor before

Dosing and Administration:

Introduced only intravenously drip, slow (maximum infusion rate of 80 drops per minute!).

Intramuscular and jet administration of the drug is not allowed!

The initial daily dose is 20 mg, diluted in 250 - 500 ml infusion solution. With good tolerability, the dose of the drug for 2-3 days is increased to 1 mg / kg of body weight per day.The course of treatment on average continues for 10-14 days, the usual daily dose at the rate of 70 kg of body weight is 50 mg per day. In view of the lack of hepato-and nephrotoxic action in vinpocetine, there is no need to change the dosage in patients with kidney or liver disease. For the preparation of infusion solutions can be used all electrolytes or glucose solution (e.g., Ringer's solution (Ringer), and Salsol (Salsol), Rindeks (Rindex), Reomakrodeks (Rheomacrodex).

After completing the course of parenteral administration, they switch to oral administration of the drug. Before drug cancellation the dose should be gradually reduced.

Side effects:

From the cardiovascular system: ECG changes (depression segment ST, elongation Q-T interval), tachycardia, arrythmia (causal relationship has not been established), there may be a transient decrease in blood pressure, thrombophlebitis at the injection site.

From the central nervous system: sleep disturbances (insomnia, increased drowsiness), dizziness, headache, general weakness (may be a manifestation of the underlying disease).

Other: skin allergic reactions, increased sweating, a feeling of heat, hyperemia of the skin of the face, nausea.

If you develop any of the side effects listed in the instructions, contact your doctor as soon as possible.

If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose:

Currently, data on the overdose of vinpocetine are limited.

Based on the literature data, the long-term use of 60 mg vinpocetine per day was safe.

At a dose of 1 mg / kg body weight, no side effects were found.

Symptoms: decrease in arterial pressure, dizziness, nausea, tachycardia, extrasystole.

Treatment: symptomatic therapy.

Interaction:

Increases the risk of hemorrhagic complications against heparin therapy. The solution of vinpocetine is pharmaceutically incompatible with heparin.

It is possible to intensify the hypotensive effect with simultaneous application with methyldopa, (AD control is necessary). Despite the lack of data confirming interactions,it is advisable to use caution when used simultaneously with central medicine, antiarrhythmics and anticoagulants.

Combined oral contraceptives, macrolide antibiotics (clarithromycin, erythromycin), antifungal agents (ketoconazole) change the severity of the effect of vinpocetine, slow down its metabolism and increase the concentration of the drug in the plasma.

Special instructions:

When parenteral administration of patients with diabetes mellitus should monitor blood glucose, tk. in solution contains sorbitol.

Patients with cardiac pathology (ischemic heart disease (severe course), severe cardiac arrhythmias) can not be administered intravenously because of the risk of arrhythmia (up to ventricular fibrillation).

With hemorrhagic stroke, parenteral administration is possible only after the subsidence of acute events (usually in 5-7 days).

In the case of the initial extension of the Q-T interval, and also with simultaneous use with drugs extending the Q-T interval, periodic ECG monitoring is necessary during the treatment with vinpocetine.

There is not a sufficient number of observations on the use of the drug in children's practice before the age of 18.

Effect on the ability to drive transp. cf. and fur:Does not affect the ability to manage vehicles and other mechanisms.

Form release / dosage:Concentrate for the preparation of solution for infusions 5 mg / ml.

Packaging:

2 ml per ampoule of light-protective glass with a color fracture ring or with a colored dot and a notch. Ampoules are additionally applied one, two or three color rings and / or a two-dimensional bar code, and / or alphanumeric coding or without additional color rings, a two-dimensional barcode, alphanumeric encoding.

5 ampoules per contour cell pack. 2 contour squares with instructions for use in a pack of cardboard.

Storage conditions:3 years. Do not use after the expiration date printed on the package.

Shelf life:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Terms of leave from pharmacies:On prescription

Registration number:LS-000368

Date of registration:05.04.2010

The owner of the registration certificate:FarmSirma Soteks, ZAO FarmSirma Soteks, ZAO Russia

Manufacturer: & nbsp

FarmSirma Soteks, ZAO Russia

Linnea S.A. Switzerland

Representation: & nbspPharm Company Sotex CJSC Pharm Company Sotex CJSC Russia

Information update date: & nbsp06.10.15

Illustrated instructions

Instructions

Vinpocetine (Vinpocetine)