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

Excipients: lactose monohydrate (sugar milk) - 91.0 mg, microcrystalline cellulose - 90.0 mg, calcium stearate 2.0 mg, talc 6.0 mg, silicon dioxide colloid (aerosil) 1.0 mg.

Description:Round tablets of flat-cylindrical form, white or white with a yellowish tinge, with a facet and a risk. Presence of "marble" is admissible.

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 decreasing 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:

Suction

After ingestion, it is rapidly absorbed in the gastrointestinal tract (mainly in the proximal parts of the small intestine). Time to reach the maximum concentration (TC_m_Oh) in blood plasma 1 hour. 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 tissues did not exceed the values found in the blood.

In humans, the relationship with plasma proteins is 66%. Bioavailability is 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.

Easily penetrates through gistogematicheskie barriers (including through the blood-brain barrier). Penetrates into breast milk (0.25% within the first hour), through the placental barrier.

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 of vinpocetine include: hydroxyviniocetine, hydroxy-AVK, AVK-dihydroxy glycinate and their conjugates (sulfates and / or glucuronides).

If there is a violation of the liver or kidney function, dose adjustment is not required, since vinpocetine does not accumulate in the body.

Excretion

With repeated admission in a dose of 10 mg vinpocetine exhibits a linear pharmacokinetics, the equilibrium plasma concentration is 2.1 ± 0.33 ng / ml.

Excretion of unchanged vinpocetine is low (several percent). The half-life in humans (T_1/2) is 4.83 ± 1.29 hours.

In studies with radioactively labeled vinpocetine, it was established that excretion by the kidneys and intestines occurs in a ratio of 60:40%. Excretion of apovinamic acid is carried out by glomerular filtration.

In rats and dogs, high radioactivity when administered radioactively labeled vinpocetine is found in 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 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 has been established that the pharmacokinetics 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.

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

Contraindications:

- Hypersensitivity to vinpocetine or other components of the drug;

- acute phase of hemorrhagic stroke;

- severe form of ischemic heart disease;

- severe heart rhythm disturbances;

- pregnancy, the period of breastfeeding;

- Children under 18 years of age (due to the lack of data from clinical trials);

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

Carefully:Precautions should be taken in patients with prolonged interval syndrome QT or with simultaneous use with drugs that cause lengthening of this interval (ECG monitoring should be performed periodically).

Pregnancy and lactation:

Application during pregnancy and during breastfeeding is contraindicated.

Pregnancy

Vinpocetine penetrates the placenta, but its concentration in the placenta and fetal blood is lower than in the pregnant woman's blood. Teratogenic and embryotoxic effects were not detected. In studies on animals with the administration of large doses, placental bleeding and spontaneous abortion arose, probably 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 are determined by the attending physician.

The standard daily dose is 15-30 mg (5-10 mg, corresponding to ½ - 1 tablet of the drug, 3 times a day).

The maximum daily dose is 30 mg (3 tablets Vinpocetine Forte 10 mg). The therapeutic effect develops approximately 1 week after the start of the drug.

The course of treatment is 1-3 months.

In diseases of the kidneys and liver, the drug is prescribed in the usual dose, the absence of cumulation allows for long-term treatment.

Side effects:

Clinical studies have shown that undesirable drug reactions with a frequency of "often" (> 1/100, <1/10) did not occur.

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 (<1/10000)
On the part of the blood and lymphatic system		Leukopenia, thrombocytopenia	Anemia, agglutination of erythrocytes
From the immune system			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 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 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 and instrumental data	Reduction of blood pressure	Increased blood pressure, hypertriglyceridemia, ST-segment depression, decrease / increase number of eosinophils, impaired functional liver tests	Increase / decrease the number of white blood cells, a decrease in the number of red blood cells, reduction of thrombin time, increase in body weight

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: gastric lavage, taking activated charcoal, symptomatic therapy.

Interaction:

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

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

Despite the lack of data confirming the possibility of interaction, it is recommended to exercise caution when concurrently administering with the drugs the central action, antiarrhythmic drugs and anticoagulants.

Special instructions:

In the case of the original interval extension QT, as well as with simultaneous use with drugs that extend the interval QT, During the treatment with vinpocetine, periodic electrocardiographic monitoring (ECG monitoring) is necessary.

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 potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:Tablets 10 mg.

Packaging:

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

10, 20, 30, 40, 50, 60, 80, 100 tablets in cans of polymer made of polypropylene, low-density polyethylene, sealed with lids tightened with the control of the first opening or caps screwed on.

One jar or 1, 2, 3, 4, 5 contour squares with instructions for use are placed in a pack of cardboard.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

5 years.

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

Terms of leave from pharmacies:On prescription

Registration number:LP-004090

Date of registration:23.01.2017

Expiration Date:23.01.2022

The owner of the registration certificate:SYNTHESIS, OJSC SYNTHESIS, OJSC Russia

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Information update date: & nbsp06.02.2017

Illustrated instructions

Instructions

Vinpocetine FORTE (Vinpocetine forte)