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

Improves the metabolism of the brain, increasing the intake of glucose and oxygen by brain tissue. Increases the resistance of neurons to hypoxia; facilitating the transport of oxygen and substrates of energy supply to tissues (due to a decrease in the affinity for red blood cells,increasing glucose uptake and metabolism, switching it to an energetically more advantageous aerobic direction). Selectively blocks Ca 2+ - dependent phosphodiesterase (PDE); increases the levels of adenosine monophosphate (AMP) and cyclic guanosine monophosphate with (cGMP) of the brain. 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; stimulates the ascending branch of the noradrenergic system, has an antioxidant effect. The vasodilating effect is associated with a direct relaxing effect on the smooth musculature of vessels predominantly of the brain. Vinpocetine does not cause the phenomenon of "stealing", primarily enhances the blood supply of the ischemic region of the brain, while not changing the blood supply of intact areas. Improves microcirculation in the brain due to a decrease in platelet aggregation, decrease in blood viscosity, increase in the deformability of erythrocytes. Increases cerebral blood flow; reduces the resistance of cerebral vessels without a significant effect on the indices of the systemic circulation.

Pharmacokinetics:

Absorption

Vinpocetine is rapidly 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 radioactively labeled vinpocetine, rats were most concentrated in the liver and in the gastrointestinal tract. The maximum concentration in the tissues was noted after 2-4 h

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 apovincamine acid (DNA), which is 25-30% of the starting compound. The area under the "concentration-time" curve of DNA after oral administration is twice as high as that of intravenous administration of vinpocetine. In this way, vinpocetine subject to the pronounced effect of "first passage" through the liver. Other metabolites include: hydroxyvinpocetine, hydroxy-AVK, AVK-dioxiglycinate and their conjugates (sulfates and (or) glucuronides).

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 radio-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 special groups of patients.

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 tinnitus.

Contraindications:

The acute phase of hemorrhagic stroke, severe form of coronary heart disease, severe heart rhythm disturbances.

Hypersensitivity to vinpocetine or other components of the drug.

Lactose intolerance, lactase deficiency.

Glucose-galactose malabsorption, as the drug contains lactose, pregnancy, the period of breastfeeding. Children's age is up to 18 (due to lack of data from clinical studies).

Carefully:Ischemic heart disease (severe course), severe rhythm disturbances (parenteral administration).With hemorrhagic stroke, parenteral administration is possible only after the subsidence of acute events (usually in 5-7 days).

Pregnancy and lactation:

Dosing and Administration:

Dosing and Administration Inside, after meals, the initial dose - 15 mg / day, the standard daily dose - 5-10 mg 3 times a day. The maximum daily dose is 30 mg. The course of treatment - 1-3 months.

Side effects:

In clinical studies, it has been shown that undesirable drug reactions with frequency "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 system-opgany classes (according to the classification of the Medical Dictionary for regular activities):

*System-Organ Class (MedDRA)*	*Infrequently* *(>1/1000,* *<1/100)*	*Rarely* *(>1/10000,* *<1/1000)*	*Rarely* *(>1/10000)***
On the part of the blood and lymphatic system		Leukopenia, thrombocytopenia	Anemia, agglutination of erythrocytes.
Immunologic disorders			Hypersensitivity
Metabolic and nutritional disorders	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 of the conjunctiva.
From the side of the organ of hearing and balance	Vertigo.	Hyperacusia, hypoacusia, tinnitus.
From the heart		Ischemia / myocardial infarction, angina, bradycardia, tachycardia, extrasystole, 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, dry mouth, nausea.	Pain in epigastrium, constipation, diarrhea, indigestion, vomiting.	Dysphagia, stomatitis.
From the skin and skin tissues		Erythema, hyperhidrosis, urticaria, pruritus, rash,	Dermatitis.
General disorders and disorders at the site of administration		Asthenia, malaise, burning sensation.	Discomfort in the chest, hypothermia.
Instrumental and laboratory data	Decrease in blood pressure.	Increased blood pressure, segment depression ST, impaired functional liver tests,	Increased decrease in the number of leukocytes, a decrease in the number of red blood cells, a decrease in prothrombin time, an increase in body weight.

Overdose:

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

Interaction:

It is possible to intensify the hypotensive effect with simultaneous application with methyldopa (blood pressure control is necessary). Despite the lack of data confirming the possibility of interaction, it is advisable to use caution when used simultaneously with central medicine, antiarrhythmics and anticoagulants.

Special instructions:

In the case of the initial extension of the Q-T interval, as well as with the simultaneous application of drugs extending the Q-T interval, periodic ECG control is necessary during the treatment with vinpocetine.

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

Form release / dosage:

Tablets 5 mg.

Packaging:

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

For 5, 10 contour squares with instructions for use are placed in a pack of cardboard.

Contoured cell packs with an equal number of instructions for use are placed in a group package.

Storage conditions:

In a dry, dark place at temperature not higher than 25 ° С.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-003628/10

Date of registration:30.04.2010 / 18.05.2015

Expiration Date:Unlimited

The owner of the registration certificate:UPDATE OF PFC, CJSC UPDATE OF PFC, CJSC Russia

Manufacturer: & nbsp

UPDATE, PFC CJSC Russia

Information update date: & nbsp18.02.2017

Illustrated instructions

Instructions

Vinpocetine (Vinpocetine)