Vinpocetin forte - instructions for use, dose, side effects, contraindications

Excipients: lactose monohydrate (sugar milk) - 157.0 mg; microcrystalline cellulose - 20.0 mg; povidone (polyvinylpyrrolidone) 6.0 mg; magnesium stearate - 3.0 mg; sodium carboxymethyl starch 4.0 mg.

Description:Tablets are white or white with a yellowish tint of color, round flat, with a risk on one side and chamfers on both sides.

Pharmacotherapeutic group:Cerebral blood flow improver

ATX: & nbsp

N.06.B.X.18 Vinpocetine

Pharmacodynamics:

Improves the metabolism of the brain, increasing the intake of glucose and oxygen by brain tissue.Increases the resistance of neurons to hypoxia; enhancing glucose transport to the brain, through the blood-brain barrier; translates the process of decay of glucose into an energetically more economical, aerobic pathway. Increases the concentration of ATP and the ratio of ATP / AMP in the brain tissues; enhances the metabolism of noradrenaline and serotonin of the brain; has an antioxidant effect.

Vinpocetine selectively inhibits the potential-dependent sodium channels, causing a dose-dependent decrease in the concentration of calcium ions in the endings of neurons of the striatum.

It is believed that a decrease in the current of sodium ions has a neuroprotective effect due to a decrease in excitotoxicity and a weakening of neuronal damage caused by cerebral ischemia and reperfusion. Vinpocetine increases the concentration of 3,4-dihydroxyphenylacetic acid (dopamine metabolite) in the nerve endings of the striatum. It also inhibits phosphodiesterase-1, which leads to an increase in the concentration of intracellular cyclic guanosine monophosphate. Reduces platelet aggregation and increased blood viscosity; increases the deforming ability of erythrocytes and blocks the utilization of erythrocytesadenosine; helps to increase the oxygen release of red blood cells. Strengthens the neuroprotective effect of adenosine.

Increases cerebral blood flow; reduces the resistance of cerebral vessels without significant changes in the systemic blood circulation (blood pressure, minute volume, heart rate, total peripheral resistance). Not only does it not have the effect of "stealing," but it also increases blood supply, especially in ischemic areas of the brain with low perfusion.

Pharmacokinetics:

Suction: when ingested quickly and completely absorbed in the gastrointestinal tract (mainly in the proximal parts of the small intestine). Bioavailability when taken on an empty stomach - about 7%. The maximum concentration in blood plasma is reached after 1 hour, in tissues - in 2-4 hours. When passing through the wall of the intestine is not exposed to metabolism. When introducing repeated doses, the kinetics is linear.

Distribution: communication with plasma proteins - 66%. The volume of distribution is 246.7 ± 88.5 liters, which indicates a good distribution in tissues. When re-ingested at doses of 5 mg and 10 mg, the kinetics is linear, the equilibrium concentrations are 1.2 ± 0.27 ng / ml and 2.1 ± 0.33 ng / ml, respectively.Easily penetrates through gistogematicheskie barriers (including through the blood-brain barrier). Penetrates into breast milk (0.25% within 1 hour), through the placental barrier. The concentration in the brain tissues does not exceed that in the blood. Vinpocetine does not cumulate in the body.

Metabolism: vinpocetine is subjected to the effect of "primary passage" through the liver to form the main metabolite of apovincaminic acid (AVA), the amount of which is 25-30%. The ground clearance is 66.7 l / h. and exceeds the hepatic clearance (50 g / l), which indicates extrahepatic metabolism of vinpocetine.

Compared with intravenous administration, the AUC (area under the concentration-time curve) of apovincamine acid after oral administration is more than 2-fold. Other metabolites of vinpocetine: hydroxyvinpocetine, hydroxy-apovicamic acid, dihydroxy-apovincamine acid-glycinate and their conjugates with glucuronides and / or sulfates.

Excretion:

The half-life is 4.83 ± 1.29 hours, excreted by the kidneys and intestines in a ratio of 3: 2.

Excretion of apovinamic acid is carried out by glomerular filtration.The half-life period depends on the dose and frequency of the drug.

Pharmacokinetics in special clinical cases

Diseases of the liver and kidneys do not affect the metabolism of vinpocetine (dose adjustment is not required).

Pharmacokinetics in the elderly does not differ from the pharmacokinetic parameters of vinpocetine in young, dose adjustment for the elderly is not required.

Indications:

Neurology (as part of complex therapy): as a symptomatic agent for various forms of cerebral circulatory insufficiency (ischemic stroke, restorative stage of hemorrhagic stroke, consequences of a stroke, transient ischemic attack, vascular dementia, vertebrobasilar insufficiency, cerebrovascular atherosclerosis, posttraumatic and hypertensive encephalopathy).

Ophthalmology: chronic vascular diseases of the choroid and retina (including occlusion of the central artery or retinal vein).

Otology: a decrease in the severity of perceptual hearing, Meniere's disease, idiopathic tinnitus.

Contraindications:

Hypersensitivity to vinpocetine and other components of the drug.The acute phase of hemorrhagic stroke, severe ischemic heart disease, severe heart rhythm disturbances.

Pregnancy and lactation.

Children under 18 years (due to insufficient data).

Lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

Pregnancy and lactation:

The drug is contraindicated during pregnancy, tk. vinpocetine penetrates the placental barrier. At the same time, its concentration in the placenta and in the fetal blood is lower than in the pregnant woman's blood. In animal studies, teratogenic and embryotoxic effects were not detected. At high doses, placental bleeding and spontaneous abortion are possible, probably as a result of increased placental blood supply.

Lactation period: within one hour, 0.25% of the accepted dose of the drug penetrates into breast milk. When using the drug, it is necessary to stop breastfeeding.

Dosing and Administration:

The course of treatment and dosage is determined by the attending physician.

Inside, after eating.

The standard daily dose of 5-10 mg 3 times a day.

The maximum daily dose is 30 mg.

The therapeutic effect develops about a week after the start of the drug. The course of treatment is 1-3 months.

In diseases of the kidneys and liver, the drug is prescribed in the usual dose, the absence of cumulation allows for long-term treatment.

Precautionary measures

Precautions should be taken in patients with QT prolonged interval syndrome or with simultaneous use with drugs that cause prolongation of the QT interval (periodic ECG monitoring is necessary).

Side effects:

The frequency of adverse reactions is given in the form of the following gradation: very often (≥1 / 10); often (≥1 / 100 - <1/10); infrequently (≥1 / 1000 - <1/100); rarely (≥1 / 10000 - <1/1000); very rarely (<1/10000), including individual messages; frequency (frequency can not be calculated from available data).

From the hemopoietic system and lymphatic system: rarely - leukopenia, thrombocytopenia; very rarely - anemia, agglutination of erythrocytes, leukopenia.

Allergic reactions: rarely - hives; very rarely - hypersensitivity reactions.

From the side of metabolism: infrequently - hypercholesterolemia; rarely - decreased appetite, anorexia, diabetes, increased triglyceride levels in the blood; very rarely - weight gain.

Mental disorders: rarely - insomnia, sleep disturbance, anxiety; very rarely - euphoria, depression, anxiety.

From the nervous system: infrequently - a headache; rarely - dysgeusia, stupor, hemiparesis, drowsiness, loss of consciousness; very rarely - a tremor, cramps.

From the side of the organ of vision: rarely - edema of the nipple of the optic nerve; very rarely - hyperemia of the conjunctiva, blurred vision, diplopia.

From the organ of hearing: infrequently - dizziness; rarely - hyperacusis, hypoacusia, tinnitus.

From the cardiovascular system: infrequently - arterial hypotension; rarely - ischemia / myocardial infarction, stress angina, bradycardia, tachycardia, extrasystole, palpitations, arterial hypertension, sensation of hot flashes, ECG change (ST segment depression, QT interval prolongation); very rarely - arrhythmia, lability of blood pressure (mainly in the direction of decline), atrial fibrillation.

From the digestive system: infrequently - discomfort in the abdomen, dry mouth, nausea; rarely - abdominal pain, constipation, diarrhea, indigestion, drooling, vomiting; very rarely - dysphagia, stomatitis.

From the skin and subcutaneous tissue: rarely - erythema, hyperhidrosis, itching, rash; very rarely - dermatitis.

Common violations: rarely - asthenia, weakness, sensation of fever; very rarely - discomfort in the chest.

Other: rarely - decrease / increase in the number of eosinophils; very rarely - a decrease in prothrombin time, an increase in urea, an increase in lactate dehydrogenase.

Overdose:

Increased severity of dose-dependent side effects.

Treatment for overdose: gastric lavage, taking activated charcoal, symptomatic therapy.

Interaction:

Interactions are not observed with simultaneous use with beta-blockers (chloranolol, pindolol), clopamid, glibenclamide, digoxin, acenocoumarol and hydrochlorothiazide, imipramine.

Simultaneous application of Vinpocetine and methyldopa sometimes caused some strengthening of the hypotensive effect, so this treatment requires regular monitoring of blood pressure.

Despite the lack of data confirming the possibility of interaction, it is recommended to exercise caution when concurrently administering with the drugs the central action, antiarrhythmic drugs and anticoagulants.

Special instructions:In the case of the initial extension of the QT interval, as well as simultaneous use with drugs extending the QT interval, periodic electrocardiographic monitoring is necessary during the treatment with vinpocetine.

Effect on the ability to drive transp. cf. and fur:During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:Tablets 10 mg.

Packaging:

For 10, 20, 30, 50 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

By 10, 20, 30, 40, 50 or 100 tablets in cans of polymeric for medicines.

One jar or 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10 contour mesh packages together with the instruction for use are placed in a cardboard package.

Storage conditions:

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

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002190

Date of registration:20.08.2013

Expiration Date:20.08.2018

The owner of the registration certificate:ATOLL, LLC ATOLL, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Representation: & nbspOZONE LLC OZONE LLC Russia

Information update date: & nbsp19.02.2017

Illustrated instructions

Instructions

Vinpocetin forte (Vinpocetine forte)