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

Excipients: lactose monohydrate - 135 mg, potato starch - 100 mg, aerosil (silicon dioxide colloid) - 5 mg, talc - 2.5 mg, magnesium stearate - 2.5 mg.

Description:Round, flat-cylindrical tablet form, white or white with a yellowish color of the color, with a risk and chamfer.

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. It blocks Na + - and Ca2 + -channels and NMDA- and AMPA-receptors. Selectively inhibits Ca2 + -calmodulin-dependent-cGMP-phosphodiesterase. Increases the exchange of serotonin and norepinephrine in the brain, stimulates the pradrenergic 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 quickly absorbed, after oral administration, the maximum concentration in the plasma is reached within 1 hour. 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 radiolabeled vinpocetine to rats, the highest concentration 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 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 apovincaminic acid (AVK), 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 function of the liver or nights, 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 enterogenic recirculation is 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 slowing of distribution and metabolism, 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, sensation of noise in the ears.

Contraindications:

-hypersensitivity to vinpocetine or other components of the drug;

- acute phase of hemorrhagic stroke, severe form of coronary heart disease, severe heart rhythm disturbances;

- pregnancy and the period of breastfeeding;

- lactose intolerance, lactase deficiency, glucose-galactose malabsorption;

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

Pregnancy and lactation:

Application during pregnancy and during breastfeeding is contraindicated. Vinpocetine 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 animal studies, high doses were associated with placental bleeding and spontaneous abortion, presumably as a result of increased placental blood flow.

Vinpocetine penetrates into breast milk. According to preclinical studies with radioactively labeled vinpocetine, its concentration in breast milk of newborn animals exceeded that in the mother's blood 10 times. Within one hour, 0.25% of the dose is absorbed into breast milk. Do not use during breastfeeding or stop breastfeeding with 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 the function of the nights or the liver is not required.

Side effects:

If any of the undesirable effects specified in the instruction are aggravated, or if you notice any other undesirable phenomena not listed in the manual, inform the doctor about it.

The frequency of unwanted reactions is given in accordance with the following scale: very often (> 10%); often (> 1% and <10%); infrequently (> 0.1% and <1%); rarely (> 0.01% and <0.1%); very rarely (<0.01%).

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 - hyperacusis, 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 - stomatitis, dysphagia.

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.

Instrumental and laboratory data: infrequently - reduction of blood pressure: rarely - increased blood pressure, ginertriglyceridemia, depression of the ST segment. 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. 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.

Symptoms: increased severity of side effects.

Treatment: gastric lavage, reception of activated charcoal, symptomatic treatment.

Interaction:

According to the results of clinical studies of drug interaction with β-adrenergic 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 done with caution.

Special instructions:With extended QT interval syndrome or simultaneous use of QT prolonging agents. ECG monitoring should be performed.

Effect on the ability to drive transp. cf. and fur:During the treatment period, care must be taken when driving vehicles, mechanisms and when engaging in potentially hazardous activities requiring increased concentration of attention and speed of psychomotor reactions. Studies on the impact on the ability to drive vehicles were not conducted.

Form release / dosage:

Tablets 5 mg.

Packaging:

10 tablets per contour cell pack. 2, 3, 5 or 6 contour squares with instructions for use in a pack of cardboard.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not apply but the expiration date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-000207

Date of registration:05.03.2010 / 15.06.2016

Expiration Date:Unlimited

The owner of the registration certificate:FARMPROJECT, CJSC FARMPROJECT, CJSC Russia

Manufacturer: & nbsp

FARMPROJECT, CJSC Russia

Information update date: & nbsp18.02.2017

Illustrated instructions

Instructions

Vinpocetine (Vinpocetine)