Nosological classification (ICD-10)
- F01.9 Vascular dementia, unspecified
- F07.2 Post-concussion syndrome
- G45 Transient transient cerebral ischemic attacks [attacks] and related syndromes
- G46 Vascular cerebrovascular syndromes in cerebrovascular diseases
- G93.4 Encephalopathy, unspecified
- H31.1 Uveal degeneration
- H34.0 Transient retinal arterial occlusion
- H34.8 Other retinal vascular occlusions
- H35.3 Macular and posterior pole degeneration
- H40.5 Glaucoma secondary to other eye diseases
- H81.0 Meniere's disease
- H81.8 Other vestibular function disorders
- H81.9 Vestibular function disorder, unspecified
- H83.3 Noise effects of the inner ear
- H91 Other hearing loss
- H91.0 Ototoxic hearing loss
- H93.0 Degenerative and vascular diseases of the ear
- I61 Intracerebral hemorrhage
- I63 Cerebral infarction
- I67 Other cerebrovascular diseases
- I67.2 Cerebral atherosclerosis
- I67.9 Cerebrovascular disease, unspecified
- I69 Consequences of cerebrovascular diseases
- I69.4 Consequences of stroke, not specified as cerebral hemorrhage or infarction
- N95.1 Menopausal and menopausal conditions in women
- T90 Consequences of head injuries
Vinpocetine tablets 5 mg No. 50
Compound
Active substance: vinpocetine 5 mg.
Excipients: magnesium stearate, colloidal silicon dioxide, talc, lactose monohydrate, corn starch.
Pharmacokinetics
Suction
Vinpocetine is rapidly absorbed after oral administration and reaches Cmax in the blood within 1 hour. Absorption occurs mainly in the proximal intestine. It is not metabolized when passing through the intestinal wall. Bioavailability when taken orally - 7%.
Distribution
In preclinical studies of oral administration of radioactively labeled vinpocetine, it was detected in the highest concentrations in the liver and gastrointestinal tract. Cmax in tissues is observed 2-4 hours after oral administration. The amount of radioactive isotope in the brain did not exceed that in the blood.
Protein binding in the human body is 66%. Vd is 246.7±88.5 l, which indicates significant distribution in tissues.
With repeated doses of 5 and 10 mg, the kinetics of vinpocetine is linear. Css were 1.2±0.27 ng/ml and 2.1±0.33 ng/ml, respectively.
Metabolism
Metabolism is predominantly extrahepatic. The main metabolite of vinpocetine is apovincamic acid (AVA), the proportion of which in humans is 25-30%. After taking vinpocetine orally, the AUC of VKA is 2 times greater than that after intravenous administration. This indicates that VKA is formed during the “first pass” process of vinpocetine. Other known metabolites are hydroxyvinpocetine, hydroxy-AVA, dihydroxy-AVA-glycinate, and their conjugates with glucuronides and/or sulfates. Preclinical studies revealed that vinpocetine is excreted unchanged in small quantities.
Removal
Clearance is 66.7 l/h, which exceeds the plasma volume of the liver (50 l/h). T1/2 in humans is 4.83±1.29 hours. In studies with a radioactive label, the drug was excreted by the kidneys and through the intestines in a ratio of 60:40. In preclinical studies, a significant portion of the radioactivity was detected in bile, but significant enterohepatic circulation was not found. Apovinamic acid is excreted by the kidneys by simple glomerular filtration, T1/2 depends on the dose taken and the route of administration of vinpocetine.
Pharmacokinetics in selected patient groups
It was found that the pharmacokinetics of vinpocetine in elderly patients does not differ significantly from that in young patients.
There is no accumulation of the drug. Therefore, vinpocetine can be prescribed to patients with impaired liver and kidney function for a long time and in normal doses.
Indications for use
Neurology
- symptomatic treatment of the consequences of ischemic stroke, vertebrobasilar insufficiency, vascular dementia, cerebral atherosclerosis, post-traumatic and hypertensive encephalopathy (to reduce the severity of neurological and mental disorders associated with impaired blood supply to the brain).
Ophthalmology
- chronic vascular diseases of the retina and choroid.
Otology
- perceptual hearing loss;
- Meniere's disease;
- sensation of tinnitus.
Contraindications
- Hypersensitivity to vinpocetine or other components of the drug;
- rare hereditary diseases: galactose intolerance, lactase deficiency, glucose-galactose malabsorption;
- pregnancy;
- breastfeeding period;
- use in women with preserved reproductive function who do not use a reliable method of contraception;
- age under 18 years (due to lack of clinical trial data);
With caution: long QT syndrome, taking drugs that cause prolongation of the QT interval.
Directions for use and doses
The drug is taken orally after meals.
Typically the daily dose is 15-30 mg (5-10 mg 3 times a day).
The initial daily dose is 15 mg. The maximum daily dose is 30 mg.
For kidney and liver diseases, the drug is prescribed in the usual dose; the absence of accumulation allows for long courses of treatment.
Storage conditions
The drug should be stored in its original packaging (blister in a pack), out of the reach of children, protected from light at a temperature not exceeding 30°C.
Best before date
5 years. Do not use after the expiration date.
special instructions
The presence of long QT interval syndrome and the use of drugs that cause prolongation of the QT interval require periodic ECG monitoring.
Patients with rare hereditary diseases such as galactose intolerance, lactase deficiency or glucose-galactose malabsorption should not take this drug.
Description
Psychostimulant and nootropic agent.
Use in children
The use of the drug is contraindicated in people under 18 years of age.
Pharmacodynamics
The mechanism of action of the drug consists of several elements: vinpocetine improves cerebral blood flow and brain 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 voltage-gated Na+ and Ca2+ channels and NMDA and AMPA receptors. Increases the neuroprotective effect of adenosine. Vinpocetine stimulates brain metabolism: increases the uptake and consumption of glucose and oxygen. Increases tolerance to hypoxia; increases the transport of glucose, the only source of energy for brain tissue, across the BBB; shifts glucose metabolism towards the energetically more favorable aerobic pathway. Selectively inhibits Ca2+-calmodulin-dependent cGMP phosphodiesterase; increases the content of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) in the brain, the concentration of ATP and the ATP/AMP ratio in brain tissue; enhances the exchange of serotonin and norepinephrine in the brain, stimulates the noradrenergic neurotransmitter system, and also has an antioxidant effect; As a result of all these effects, vinpocetine has a cerebroprotective effect.
Improves microcirculation in the brain by inhibiting platelet aggregation, reducing pathologically increased blood viscosity, increasing the ability of red blood cells to deform and inhibiting adenosine uptake; promotes the transition of oxygen into cells by reducing the affinity of red blood cells for it.
Selectively increases cerebral blood flow by increasing the cerebral fraction of cardiac output, reducing cerebral vascular resistance without significantly affecting systemic circulatory parameters (BP, cardiac output, heart rate, OPSS), and does not cause a “steal” effect. The use of vinpocetine improves blood supply to damaged (but not yet necrotic) ischemic areas with low perfusion (“reverse steal effect”).
Side effects
During clinical trials, the most common adverse reactions occurred in the following systemic organ classes (according to the MedDRA classification), which are listed according to the frequency of occurrence: uncommon (from ≥1/1000 to <1/100), rare (from ≥1/10000 up to <1/1000); very rare (<1/10000).
From the hematopoietic system: rarely - leukopenia, thrombocytopenia; very rarely - anemia, red blood cell agglutination.
From the immune system: very rarely - hypersensitivity reactions.
From the side of metabolism: infrequently - hypercholesterolemia; rarely - loss of appetite, anorexia, diabetes mellitus.
Mental disorders: rarely - insomnia, sleep disturbance, anxiety; very rarely - euphoria, depression.
From the nervous system: infrequently - headache; rarely - dizziness, dysgeusia, stupor, hemiparesis, drowsiness, amnesia; very rarely - tremors, spasms.
From the organ of vision: rarely - swelling of the optic nerve nipple; very rarely - conjunctival hyperemia.
From the organ of hearing and labyrinthine disorders: infrequently - vertigo; rarely - hyperacusis, hypoacusia, tinnitus.
From the cardiovascular system: infrequently - decreased blood pressure; rarely - myocardial ischemia/infarction, angina pectoris, bradycardia, tachycardia, extrasystole, palpitations, increased blood pressure, hot flashes, thrombophlebitis; very rarely - arrhythmia, atrial fibrillation, blood pressure lability.
From the gastrointestinal tract: infrequently - abdominal discomfort, dry mouth, nausea; rarely - epigastric pain, constipation, diarrhea, dyspepsia, vomiting; very rarely - dysphagia, stomatitis.
From the skin and subcutaneous tissues: rarely - erythema, hyperhidrosis, itching, urticaria, rash; very rarely - dermatitis.
Other: rarely - asthenia, malaise, feeling hot; very rarely - chest discomfort, hypothermia.
Laboratory and instrumental data: rarely - hypertriglyceridemia, depression of the ST segment on the ECG, decrease/increase in the number of eosinophils, increased activity of liver enzymes; very rarely - decrease/increase in the number of leukocytes, erythropenia, decrease in thrombin time,
Use during pregnancy and breastfeeding
During pregnancy and breastfeeding, as well as in women with preserved reproductive function who do not use a reliable method of contraception, the use of vinpocetine is contraindicated.
Pregnancy
Vinpocetine penetrates the placental barrier, but its concentration in the placenta and fetal blood is lower than in the blood of a pregnant woman. Animal studies have shown reproductive toxicity, including malformations in rats. In animal studies, placental hemorrhage and spontaneous abortion occurred when large doses were administered, probably as a result of increased placental blood flow.
Breastfeeding period
Vinpocetine passes into breast milk. In studies using labeled vinpocetine, the radioactivity of breast milk was 10 times higher than that in the mother's blood. Within 1 hour, 0.25% of the administered dose of the drug passes into breast milk. Since vinpocetine passes into breast milk, and there is no data on the effect of vinpocetine on infants, the use of the drug during breastfeeding is contraindicated.
Interaction
Interaction is not observed when used simultaneously with beta-blockers (chloranolol, pindolol), clopamide, glibenclamide, digoxin, acenocoumarol, hydrochlorothiazide, imipramine.
The simultaneous use of vinpocetine and α-methyldopa sometimes caused a slight increase in the hypotensive effect, so this treatment requires regular monitoring of blood pressure.
Despite the lack of data confirming the possibility of interaction, caution is recommended when co-prescribing with drugs acting on the central nervous system, antiarrhythmic and anticoagulant effects.
Overdose
There are no data on overdose of vinpocetine. A single dose of 360 mg of vinpocetine did not cause clinically significant reactions, incl. from the cardiovascular system.
Treatment: gastric lavage, taking activated carbon, symptomatic therapy.
Impact on the ability to drive vehicles and operate machinery
There are no data on the effect of vinpocetine on the ability to drive vehicles and machines.
