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

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 significantly affecting systemic blood circulation parameters (blood pressure (BP), cardiac output, heart rate, total peripheral vascular resistance); does not cause the effect of "stealing".

Pharmacokinetics:

Absorption

Vinpocetine is rapidly absorbed, after oral administration, the maximum concentration in the plasma is reached within 1 h. It is absorbed mainly in the proximal part of the intestine. When passing through the wall of the intestine is not exposed to metabolism.

Distribution

With oral administration of radioactively labeled vinpocetine to rats, the highest radioactivity was found in the liver and gastrointestinal tract. The maximum concentration in the tissues was noted 2-4 hours after administration. The concentration in the brain did not exceed the values found in the blood.

In humans, the relationship with plasma proteins is 66%. Bioavailability of about 7%. The volume 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 extrahepatic metabolism.

Metabolism

The main metabolite is apovincamine acid (ABC), which is 25-30% of the original compound. The area under the concentration-time curve AVK after oral administration is twice as high as when intravenously administered vinpocetine. In this way, vinpocetine subject to the pronounced effect of "first passage" through the liver. Other metabolites include: hydroxyvinpocetine, hydroxy-AVK, AVK-dihydroxy glycinate and their conjugates (sulfates and / or glucuronides). Excretion of unchanged vinpocetine is low (several percent).

If there is a violation of the liver or kidney function, dose adjustment is not required, since vinpocetine Do not cumulate.

Excretion.

With repeated administration in a dose of 5 and 10 mg vinpocetine shows a linear pharmacokinetics, the equilibrium plasma concentration is 1.2 + 0.27 and 2.1 ± 0.33 ng / ml, respectively. The half-life in humans is 4.83 + 1.29 hours. In studies with radioactively labeled vinpocetine, it has been established that excretion by the kidneys and intestines occurs in a ratio of 60:40%.

In rats and dogs, a high concentration is found in bile, but significant enterohepatic recirculation has been noted.

Pharmacokinetics in specific patient groups

It is necessary to take into account the slowing of distribution and metabolism, as well as the elimination in elderly patients, especially with prolonged use. However, according to the results of clinical studies, it was found 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.

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

Contraindications:

Hypersensitivity to vinpocetine or other components of the drug.

Pregnancy and lactation.

Children under 18 years of age (due to lack of clinical research data).

Lactase deficiency, lactose intolerance, glucose-galactose malabsorption (due to the presence of lactose in the formulation).

Pregnancy and lactation:

Application during pregnancy and during lactation is contraindicated.

Pregnancy

Vinpocetin penetrates the placenta, but the plasma concentration in the placenta and in the fetus is lower than that of the mother. Teratogenic and embryotoxic effects were not detected.In studies on animals with the introduction of high doses, placental bleeding and abortion arose (presumably as a result of an increase in placental blood flow).

Lactation

Vinpocetine penetrates into breast milk. According to preclinical studies with radioactively labeled vinpocetine, its concentration in the breast milk of animals exceeded that in the mother's blood 10 times. For 1 hour in the milk penetrates 0.25% of the dose.

Dosing and Administration:

Inside, after eating.

The standard dose is 5-10 mg 3 times a day (15-30 mg / day).

Correction of the dose for violations of kidney or liver function is not required.

Side effects:

In clinical trials, the most common adverse reactions occurred in the following systemic and organ classes (according to the Medical Dictionary classification for regulatory activity). The frequency of side effects is presented in 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 isolated cases; frequency is not known (can not be calculated based on available data).

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

Immunological disorders: very rarely - hypersensitivity.

Metabolic and nutritional disorders: infrequently - hypercholesterolemia; rarely - decreased appetite, anorexia, diabetes mellitus.

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

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

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

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

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

From the side of the vessels: infrequently - arterial hypotension; rarely - arterial hypertension, hot flashes, thrombophlebitis; very rarely - the lability of blood pressure.

From the gastrointestinal tract: infrequently - discomfort in the abdomen, dry mouth, nausea; rarely - epigastric pain, constipation, diarrhea, indigestion, vomiting; very rarely - dysphagia, stomatitis.

From the skin and subcutaneous tissues: rarely erythema, hyperhidrosis, pruritus, urticaria, 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 and instrumental disorders: infrequently - a decrease in blood pressure; rarely - increased blood pressure, hypertriglyceridemia, segment depression ST, decrease / increase in the number of eosinophils, impaired functional liver tests; very rarely - increase / decrease in the number of leukocytes, a decrease in the number of red blood cells, a decrease in thrombin time, weight gain.

Overdose:

Cases of overdose are not registered. Treatment is symptomatic.

Interaction:

Based on the results of clinical studies of drug interaction with β-blockers (pindolol), clomipramide, glibenclamide, digoxin, hydrochlorothiazide and acenocoumarol were not detected.

Methyldopa can enhance the hypotensive effect of vinpocetine, so when they are used simultaneously, systematic monitoring of blood pressure is required.

Despite the lack of clinical data, simultaneous use with agents that affect the central nervous system,anticoagulants and antiarrhythmics should be conducted with caution.

Special instructions:

In the syndrome of an elongated interval QT or simultaneous application of means, extending the interval QT, ECG monitoring should be performed.

Effect on the ability to drive transp. cf. and fur:

Studies on the impact on the ability to drive vehicles were not conducted. When there are undesirable reactions from the nervous system, care should be taken when driving vehicles and working with mechanisms.

Form release / dosage:

Tablets 5 mg.

Packaging:

For 10, 20, 25, 30, 40, 50 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 10, 20, 25, 30, 40, 50 or 100 tablets in cans of polyethylene terephthalate or in polymer cans 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-002784

Date of registration:24.12.2014

Expiration Date:24.12.2019

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: & nbsp17.02.2017

Illustrated instructions

Instructions

Vinpocetine (Vinpocetine)