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

Excipients: cellulose microcrystalline - 89.00 mg; corn starch pregelatinized starch - 30,00 mg; silicon dioxide colloidal - 0.30 mg; magnesium stearate - 0.70 mg.

1 tablet of 10 mg contains:

Active substance: vinpocetine - 10,00 mg.

Excipients: cellulose microcrystalline - 178.00 mg; starch corn pregelatinized starch - 60,00 mg; silicon dioxide colloidal - 0.60 mg; magnesium stearate - 1.40 mg.

Description:

Tablets 5 mg

The tablets are round, biconvex, from white to white with a yellowish tinge.

Tablets 10 mg

Tablets are round, biconvex, from white to white with a yellowish tint of color, with a risk on one side.

Pharmacotherapeutic group:Psychostimulating and nootropic remedy

ATX: & nbsp

N.06.B.X.18 Vinpocetine

Pharmacodynamics:

The mechanism of action of vinpocetine consists of several elements: it improves cerebral blood flow and metabolism, has a beneficial effect on the rheological properties of the blood.

The neuroprotective effect is realized by reducing the unfavorable cytotoxic effect of excitatory amino acids. Blocks Na⁺- and Ca²⁺channels and NMDA- and AMPA receptors. Selectively inhibits Ca²⁺-culmodulin-dependent-cGMP-phosphodiesterase.

Increases the exchange of serotonin and norepinephrine in the brain, stimulates the noradrenergic neurotransmitter system and has an antioxidant effect.

Improves microcirculation in the brain due to inhibition of platelet aggregation, a decrease in pathologically increased blood viscosity, increased erythrocyte deformability and inhibition of adenosine reuptake; promotes the transition of oxygen into cells by reducing the affinity of erythrocytes for it.

Selectively increases cerebral blood flow by reducing

cerebral vascular resistance without a significant effect on systemic blood circulation parameters (blood pressure (BP), cardiac output, heart rate,total peripheral vascular resistance); does not cause the effect of "stealing".

Pharmacokinetics:

Suction

After oral administration, it is rapidly absorbed from the gastrointestinal tract. Time to reach the maximum concentration (TC_mOh) in blood plasma for 1 hour. Absorption occurs mainly in the proximal parts of the gastrointestinal tract. When passing through the wall of the intestine is not exposed to metabolism.

Distribution

With oral administration of radiolabeled vinpocetine, rats were most concentrated in the liver and in the gastrointestinal tract. The maximum concentration in the tissues was noted 2-4 hours after administration. Radioactivity in the brain did not exceed the values found in the blood.

In humans, the connection with plasma proteins is 66%, the bioavailability with ingestion is 7%. The volume of distribution is 246.7-88.5 liters, which indicates a high binding to tissues. The total clearance (66.7 l / h) exceeds the rate of hepatic blood flow (50 l / h), which indicates an extrahepatic metabolism.

Metabolism

The main metabolite is apovincaminate (ABA), which is 25-30% of the original compound.The area under the "concentration-time" curve of ABA after oral administration is twice as high as that of intravenous administration of vinpocetine. In this way, vinpocetine is prone to the pronounced effect of "primary transmission" through the liver. Other metabolites include: hydroxyvinpocetine, hydroxy-ABA, ABA-dioxiglycinate and their conjugates (sulphates and9 or) glucuronides). If the liver or kidney function is not corrected, dose adjustment is not required because vinpocetine Do not cumulate.

Excretion

Excretion of unchanged vinpocetine is low (several percent). With multiple administration in doses of 5 mg and 10 mg, the kinetics is linear, the equilibrium plasma concentration is 1.2 ± 0.27 and 2.1 ± 0.33 ng / ml, respectively. The half-life in humans is 4.8 ± 1.29 hours. It is excreted by the kidneys and through the intestine in a ratio of 60:40. In rats and dogs, high radioactivity when administered radiolabelled vinpocetine is found in bile, but significant enterohepatic recirculation has been noted.

Special patient groups

Because the vinpocetine is intended primarily for the treatment of the elderly, it is necessary to take into account the reduction in absorption and distribution, as well as elimination in this age group, especially with prolonged use.However, according to the results of clinical studies, it has been established that the kinetics of vinpocetine in the elderly does not differ significantly from the young, cumulation does not occur. With violations of the liver and kidneys cumulation is not noted, which allows for long-term therapy. Vinpocetine penetrates the placenta and is excreted in breast milk.

Indications:

Neurology: symptomatic therapy of the consequences of ischemic stroke, vascular vertebrobasilar insufficiency, vascular dementia, cerebrovascular atherosclerosis, posttraumatic, hypertensive encephalopathy.

Ophthalmology: chronic vascular diseases of the retina and choroid of the eye.

Otology: perceptual hearing loss, Meniere's disease, tinnitus.

To avoid complications, use strictly according to the doctor's prescription.

Contraindications:

Hypersensitivity to vinpocetine or to any of the components of the drug.

Pregnancy, lactation.

Children under 18 years (due to insufficient data).

Pregnancy and lactation:

The use during pregnancy is contraindicated and in the period of breastfeeding is contraindicated.

Pregnancy

Vinpocetine penetrates the placenta, but this concentration of vinpocetine in the placenta and in the fetal blood is lower than in the pregnant woman's blood. Teratogenic and embryotoxic effects were not detected. In animal studies, when large doses were administered, placental bleeding and spontaneous abortion arose, presumably as a result of increased placental blood flow.

Breastfeeding period

According to preclinical studies with radioactively labeled vinpocetine, the concentration in breast milk of newborn animals exceeded that in the mother's blood 10 times. Within an hour 0.25% of the accepted dose of the drug penetrates into the breast milk. When deciding to stop breastfeeding or refuse treatment with vinpocetine, the benefits of breastfeeding for a child should be correlated with the benefit of vinpocetine therapy for a woman. When using the drug, it is necessary to stop breastfeeding.

Dosing and Administration:

Inside, after eating.

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

Usually the daily dose is 15-30 mg (5-10 mg 3 times a day). The initial daily dose is 15 mg. The maximum daily dose is 30 mg.

Dose adjustments for the elderly, with violations of the liver or kidney function is not required.

Side effects:

To determine the incidence of side effects of the drug, the following classification is used:

Very often (≥ 1/10)

Frequently (≥ 1/100 and <1/10)

Not infrequently (≥ 1/1000 and <1/100)

Rarely (≥ 1/10 000 and <1/1000)

Very rarely (≥ 1/10 000).

From the heart: rarely - ischemia / myocardial infarction, bradycardia, angina pectoris, tachycardia, extrasystole, palpitation; very rarely - arrhythmia, atrial fibrillation.

From the side of the vessels: infrequently - a decrease in blood pressure; rarely - increased blood pressure, sensation of hot flashes, thrombophlebitis; very rarely - instability of blood pressure.

From the central nervous system: infrequently - a headache; rarely - dysgeusia, stupor, hemiparesis, drowsiness, amnesia; very rarely - tremor, spasms.

From the side of the organ of vision: rarely - edema of the optic disc; very rarely congestion hyperemia.

From the side of the organ of hearing and balance: infrequently - vertigo; rarely - hyperacusis, hypoacusia, tinnitus.

From the side of the digestive system: infrequently - discomfort in the abdomen, dry mouth, nausea; rarely - dyspepsia, vomiting, constipation, diarrhea, epigastric pain; very rarely - stomatitis, dysphagia.

Mental disorders: rarely - sleep disturbances (insomnia, increased drowsiness), anxiety; very rarely - euphoria, depression.

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

Immunologic disorders: very rarely - hypersensitivity. OnDisruption of metabolism and nutrition: infrequently - hypercholesterolemia; rarely - decreased appetite, anorexia, diabetes mellitus.

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

General disorders and disorders at the site of administration: rarely - asthenia, malaise, burning sensation; very rarely - discomfort in the chest, hypothermia.

Laboratory violations: infrequently - a decrease in blood pressure; rarely - increased blood pressure hypertriglyceridemia, ECG change (depression ST, lengthening the interval QT), eosinopenia, impaired functional liver tests; very rarely - leukopenia, leukocytopenia, erythropenia, a decrease in thrombin time, weight gain.

Overdose:

Cases of overdose are not registered. According to the literature, 60 mg vinpocetine per day is safe.A single oral intake of vinpocetine in a dose of 360 mg does not cause clinically significant cardiovascular and other reactions.

Treatment is symptomatic.

Interaction:

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

Methyldopa can enhance the giponous effect of vinpocetine, so when they are used simultaneously, systematic monitoring of blood pressure is required. Despite the lack of data confirming the possibility of interaction, it is recommended to exercise caution when concurrently administering with the drugs central, antiarrhythmic and anticoagulant action.

Special instructions:

If there is a syndrome of prolonged interval QT or simultaneous reception of drugs that cause lengthening of the interval QT, periodic ECG monitoring is required. With severe heart rhythm disturbances, increased intracranial pressure, the use of antiarrhythmic drugs, the syndrome of elongated QT or simultaneous use of drugs that cause lengthening of the interval QT use with caution.

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 5 mg, 10 mg

Packaging:

For 10 or 15 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

By 3, 5 or 9 contour mesh packages 10 tablets or 2, 4 or 6

contour cell packs of 15 tablets together with instructions for medical use are placed in a pack of cardboard box.

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 the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002441

Date of registration:28.04.2014 / 24.10.2016

Expiration Date:28.04.2019

The owner of the registration certificate:IZVARINO PHARMA, LLC IZVARINO PHARMA, LLC Russia

Manufacturer: & nbsp

IZVARINO PHARMA, LLC Russia

Information update date: & nbsp17.02.2017

Illustrated instructions

Instructions

Vinpocetine (Vinpocetine)