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

auxiliary substances - a sufficient amount to obtain a tablet weighing 0.16 g: milk sugar (lactose), microcrystalline cellulose, potato starch, polyvinylpyrrolidone (povidone), talc, calcium stearate.

Description:

Tablets are white with a yellowish hue of color, flat-cylindrical shape.

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 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, 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. The concentration of radioactively labeled vinpocetine 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 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 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 is prone to the pronounced effect of "primary transmission" 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 or 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 of radioactively labeled vinpocetine is found in the bile, but significant enterohepatic recirculation has been noted.

Pharmacokinetics in specific patient groups

Because the vinpocetine is primarily for the treatment of the elderly, it is necessary to take into account the decrease in absorption and distribution, as well as elimination in this age group, especially with prolonged use.According to the results of clinical studies, it is 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.

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.

Contraindications:

Hypersensitivity to vinpocetine or other components of the drug.

Pregnancy, the period of breastfeeding.

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

Rarely occurring hereditary intolerance of galactose (galactosemia), lactose deficiency, glucose-galactose malabsorption - due to the presence of lactose in the formulation.

Carefully:

There is no information.

Pregnancy and lactation:

Application during pregnancy and during breastfeeding 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).

Breastfeeding period

Vinpocetine penetrates into breast milk. 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. For 1 hour in the milk penetrates 0.25% of the dose.

Do not use during breastfeeding or stop breastfeeding while treating vinpocetine. When deciding to stop breastfeeding or refuse treatment with vinpocetine, the benefits of breastfeeding for a child and the benefits of therapy for a woman should be correlated. Because the vinpocetine penetrates into breast milk and the experience of its use in children is absent, the use during breastfeeding is contraindicated.

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:

Clinical studies have shown that undesirable drug reactions with a frequency of "often" (> 1/100) did not occur, so this frequency category was excluded from the table below.

In clinical trials, the most common adverse reactions occurred in the following systemic and organ classes (according to the classification of the Medical Dictionary for regulatory activity):

System-Organ Class (MedDRA)	Infrequently (>1/1000, <1/100)	Rarely (>1/10000, <1/1000)	Very rarely (<1/1000)
From the side of blood and lymphatic systems		Leukopenia, thrombocytopenia	Anemia, agglutination of erythrocytes
Immunological violations			Hypersensitivity
Disorders of metabolism and nutrition	Hypercholesterolemia	Decreased appetite, anorexia, diabetes mellitus
Mental disorders		Insomnia, sleep disturbance, anxiety	Euphoria, depression
From the nervous system	Headache	Dysgeusia, stupor, unilateral paresis, drowsiness, amnesia	Tremor, spasms
From the side of the organ of vision		Edema of the nipple of the optic nerve	Hyperemia conjunctiva
From the side of the organ of hearing and balance	Vertigo	Hyperacusia, hypoacusia, tinnitus
From the heart		Ischemia / infarction myocardium, angina pectoris, bradycardia, tachycardia, extrasystole, sensation palpitation	Arrhythmia, atrial fibrillation
From the side of the vessels	Arterial hypotension	Arterial hypertension, hot flashes, thrombophlebitis	Lability of blood pressure
From the gastrointestinal tract	Discomfort in the abdomen, dryness of the oral mucosa, nausea	Pain in epigastrium, constipation, diarrhea, indigestion, vomiting	Dysphagia, stomatitis
From the skin and subcutaneous tissues		Erythema, hyperhidrosis, pruritus, urticaria, rash	Dermatitis
General disorders and disorders at the site of administration		Asthenia, malaise, burning sensation	Discomfort in the chest, hypothermia
Laboratory violations	Decreased blood pressure	Increased blood pressure, hypertriglyceridemia, segment depression ST, decrease / increase quantities eosinophils, violation of functional liver tests	Reduction / increase in the number of leukocytes, a decrease in the number of red blood cells, a decrease 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.

In intoxication, gastric lavage, activated charcoal and symptomatic treatment are recommended.

Interaction:

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

Methyldopa can enhance the hypotensive effect of vipocetine, 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 done 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.

Form release / dosage:

Tablets, 5 mg.

Packaging:

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

For 50 tablets in a jar of lightproof glass.

Each jar or 5 contour mesh packages together with the instruction for use is placed in a pack of cardboard.

Storage conditions:

In a dry, 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:P N000327 / 01

Date of registration:03.04.2012 / 05.10.2015

Expiration Date:Unlimited

The owner of the registration certificate:VEROPHARM SA VEROPHARM SA Russia

Manufacturer: & nbsp

VEROPHARM SA Russia

Representation: & nbspVEROPHARM, AO VEROPHARM, AO Russia

Information update date: & nbsp03.02.2017

Illustrated instructions

Instructions

Vero-Vinpocetine (Vero-Vinpocetin)