Vinpocetine, concentrate 5 mg/ml 5 ml 10 pcs

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Indications

Neurology: transient ischemic attack, symptomatic treatment of the consequences of ischemic stroke, vascular vertebrobasilar insufficiency, vascular dementia, cerebral atherosclerosis, post-traumatic, hypertensive encephalopathy.

Ophthalmology: chronic vascular diseases of the retina and choroid.

Otology: perceptual hearing loss, Meniere’s disease, tinnitus, hearing impairment of vascular or toxic (including drug) origin.

Pharmacological effect

Psychostimulant and nootropic agent

ATC: N.06.B.X.18 Vinpocetine

Pharmacodynamics:

The mechanism of action of vinpocetine consists of several elements: it improves cerebral blood flow and metabolism, and has a beneficial effect on the rheological properties of blood.

The neuroprotective effect is realized by reducing the adverse cytotoxic effect of excitatory amino acids. 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 noradrenergic neurotransmitter system and has an antioxidant effect.

Improves microcirculation in the brain by inhibiting platelet aggregation, reducing pathologically increased blood viscosity, increasing the deformability of erythrocytes and inhibiting the reuptake of adenosine; promotes the transition of oxygen into cells by reducing the affinity of red blood cells for it.

Selectively increases cerebral blood flow by reducing cerebral vascular resistance without significantly affecting systemic circulatory parameters (blood pressure (BP), cardiac output, heart rate, total peripheral vascular resistance); does not cause the effect of “stealing”.

Pharmacokinetics:

Distribution

Distribution of radioactively labeled vinpocetine, when administered to rats, the greatest radioactivity was found in the liver and gastrointestinal tract. The maximum concentration in tissues was observed 2-4 hours after administration. The concentration in the brain did not exceed the values ​​found in the blood.

In humans, the binding to plasma proteins is 66%. Bioavailability is about 7%. The volume of distribution is 246.7±88.5 l, indicating high tissue binding. The total clearance (66.7 l/h) exceeds the hepatic blood flow rate (50 l/h), indicating extrahepatic metabolism.

Metabolism

The main metabolite is apovincamic acid (AVA), accounting for 25-30% of the parent compound. The area under the concentration-time curve of VKA after oral administration is twice that of intravenous vinpocetine. Thus, vinpocetine is subject to a pronounced first-pass effect through the liver.

Other metabolites include: hydroxyvinpocetine, hydroxy-AVK, ABC-dioxyglycinate and their conjugates (sulfates and (or) glucuronides). The excretion of unchanged vinpocetine is low (several percent).

If liver or kidney function is impaired, no dose adjustment is required, since vinpocetine does not accumulate.

Removal

With repeated administration in doses of 5 and 10 mg, vinpocetine exhibits 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 was found that excretion by the kidneys and intestines occurs in a ratio of 60:40%.

In rats and dogs, high concentrations are found in bile, but significant enterohepatic recirculation is noted.

Pharmacokinetics in special groups of patients

Since vinpocetine is intended primarily for the treatment of the elderly, slower distribution, metabolism, and elimination in this age group must be considered, especially with long-term use. Based on the results of clinical studies, it was established that the kinetics of vinpocetine in the elderly does not differ significantly from that in the young, and accumulation does not occur.

In cases of liver and kidney dysfunction, cumulation is not observed, which allows for long-term therapy.

Special instructions

The drug should be used with caution in cases of intracranial hypertension, when used concomitantly with antiarrhythmic drugs, as well as in long QT syndrome or concomitant use with drugs that prolong the QT interval. In case of long QT syndrome or concomitant use of drugs that prolong the QT interval, ECG monitoring should be performed.

Impact on the ability to drive vehicles. Wed and fur.:

No studies have been conducted on the effect on the ability to drive vehicles. If undesirable reactions from the nervous system occur, care should be taken when driving vehicles and working with moving mechanisms.

Active ingredient

Vinpocetine

Composition

One ampoule contains:

active ingredient:

vinpocetine – 5 mg;

excipients:

ascorbic acid – 0.5 mg,

benzyl alcohol – 10 mg,

sodium disulfite (sodium metabisulfite) – 1 mg,

sorbitol (sorbitol) – 75 mg,

tartaric acid – 3 mg,

water for injection – up to 1 ml.

Pregnancy

Use during pregnancy and breastfeeding is contraindicated.

Pregnancy

Vinpocetine crosses the placenta, but plasma concentrations in the placenta and fetus are lower than in the mother. Teratogenic and embryotoxic effects were not detected. In animal studies, placental hemorrhage and abortion have occurred with high doses (presumably due to increased placental blood flow).

Breastfeeding

Vinpocetine passes into breast milk. According to preclinical studies with radioactively labeled vinpocetine, its concentration in animal breast milk was 10 times higher than that in the mother’s blood. In 1 hour, 0.25% of the dose taken penetrates into milk.

Since vinpocetine passes into breast milk and there is no experience with its use in children, use during breastfeeding is contraindicated.

Contraindications

Acute phase of hemorrhagic stroke, severe form of coronary heart disease, severe cardiac arrhythmias.

Hypersensitivity to vinpocetine or other components of the drug.

Pregnancy, breastfeeding period.

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

Side Effects

Adverse reactions are classified depending on the frequency of their occurrence: very often (≥1/10), often (≥1/100, <1/10), infrequently (≥1/1000, <1/100), rarely (≥1/10000, <1/1000), very rarely (<1/10000), frequency unknown (due to insufficient data).

Disorders of the blood and lymphatic system: rarely – thrombocytopenia, erythrocyte agglutination; very rarely – anemia.

Immune system disorders: very rarely – hypersensitivity.

Metabolic and nutritional disorders: rarely – hypercholesterolemia, diabetes mellitus, loss of appetite; very rarely – anorexia.

Mental disorders: infrequently – euphoria; rarely – anxiety; very rarely – depression, sleep disturbance.

Nervous system disorders: rarely – headache, dizziness, hemiparesis, drowsiness; very rarely – tremor, loss of consciousness, hypotension, presyncope.

Violations of the organ of vision: rarely – hemorrhage in the anterior chamber of the eye, hypermetropia, decreased visual acuity, myopia; very rarely – conjunctival hyperemia, papilledema, diplopia.

Disorders of the organ of hearing and labyrinth: rarely – hearing impairment, hyperacusis, hypoacusia, true dizziness; very rarely – tinnitus.

Cardiac disorders: rarely – myocardial ischemia/infarction, angina pectoris, bradycardia, tachycardia, extrasystole, palpitations; very rarely – heart failure, atrial fibrillation, arrhythmia.

Vascular disorders: rarely – hypotension, hypertension, hot flashes; very rarely – fluctuations in blood pressure, thrombophlebitis.

Gastrointestinal disorders: rarely – abdominal discomfort, epigastric pain, dry mouth, nausea; very rarely – hypersecretion of saliva, vomiting, dysphagia, stomatitis.

Pathology of the skin and subcutaneous tissue: rarely – erythema, hyperhidrosis, urticaria; very rarely – dermatitis, itching.

General disorders and reactions at the injection site: rarely – asthenia, malaise, burning sensation and inflammation at the injection site, thrombosis, chest discomfort.

Laboratory abnormalities: infrequently – decreased blood pressure; rarely – increased blood pressure; hypertriglyceridemia, ST segment depression, eosinopenia, abnormal liver function tests, QT segment prolongation; very rarely – increased LDH, abnormal EEG, PR prolongation.

Interaction

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

Methyldopa may enhance the hypotensive effect of vinpocetine, therefore, when used simultaneously, systematic monitoring of blood pressure is required.

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

Vinpocetine solution is pharmaceutically incompatible with heparin and solutions containing amino acids.

Storage conditions

In a place protected from light, at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life

2 years.

Do not use after expiration date.

Manufacturer

Ozon, Russia