Compound
Depending on the manufacturer, 1 Vinpocetine tablet may contain 5 or 10 mg of the active ingredient Vinpocetine .
Additional substances: potato starch, colloidal silicon dioxide, lactose, magnesium stearate. 1 ml of concentrated solution for infusion contains 5 mg of vinpocetine . Additional substances: hydrochloric acid, propylene glycol, sodium disulfite, sorbitol, disodium edetate, sodium sulfite, citric acid, water.
Pharmacodynamics and pharmacokinetics
Pharmacodynamics
A drug that enhances cerebral blood circulation and metabolism. Suppresses the activity of phosphodiesterase , causing the accumulation of cAMP in tissues. Demonstrates a vasodilating effect mainly on the blood vessels of the brain, which is due to the antispasmodic myotropic effect. Systemic blood pressure decreases slightly.
Stimulates blood supply to brain tissue, weakens platelet aggregation, regulates the rheological properties of blood. Improves the resistance to hypoxia of brain cells, stimulating the transfer of oxygen to tissues by reducing the tropism of red blood cells to it, activating the metabolism and absorption of glucose. Increases the concentration of catecholamines in brain cells.
Pharmacokinetics
When taken orally, it is quickly absorbed from the intestines. The highest concentration in the blood is reached after about 1 hour. The half-life reaches 5 hours.
Vinpocetine
The drug vinpocetine belongs to the group of correctors of cerebral circulatory disorders. The drug has a vasodilating, antiaggregation, antihypoxic effect, and improves cerebral circulation. It is used mainly for insufficient blood supply to areas of the brain, as well as for vascular diseases of the retina and choroid (the morphological similarity of the blood vessels of the brain and eye makes it possible to use vinpocetine in both cases).
Vinpocetine blocks the action of the phosphodiesterase enzyme, as a result of which the concentration of cyclic adenosine monophosphate in the cells increases, which, in turn, entails a decrease in the content of calcium ions in the cytoplasm of smooth muscle cells and relaxation of muscle fibers. Vinpocetine combines both vascular and metabolic effects. The first is supported by the drug’s ability to increase the lumen of blood vessels in the brain, stimulate blood flow primarily in ischemic areas and solve “supply” problems by improving the mechanisms of oxygen delivery to the brain. The role of vinpocetine in metabolic processes is no less important: it promotes the utilization of glucose, increases the concentration of catecholamines in the central nervous system, and “ignites” the metabolism of the neurotransmitters norepinephrine and serotonin in brain tissue. Affects the quality characteristics of blood: reduces platelet aggregation, reduces blood viscosity, increases the degree of deformability of red blood cells, due to a decrease in vascular resistance, normalizes the outflow of venous blood, slightly reduces blood pressure.
Vinpocetine is very good for acute stroke: it promotes the shortest relief of neurological symptoms, sharpens attention, improves memory, and restores intellectual functions. Elderly patients are particularly sensitive to the relaxing effect of the drug. This is due to the increasing role of the adenylate cyclase system, which is a natural consequence of the aging process.
Vinpocetine is quickly and completely absorbed from the digestive tract. Its maximum concentration in the blood is reached 1 hour after administration. Available in two dosage forms: tablets and solution for intravenous administration. There is also a concentrate for preparing a solution for infusion, but the popularity of this formulation does not extend beyond hospitals. Tablets are taken orally after meals, 5-10 mg 3 times a day. After the so-called During the “loading” period, vinpocetine is taken in a maintenance dose: 5 mg 3 times a day. The duration of treatment is 60 days. The injection solution of the drug is administered intravenously, by drip. The therapeutic course is 1.5 - 2 weeks, after which the patient is transferred to the tablet form - 10 mg 3 times a day - with a gradual reduction in dosage before completely discontinuing the drug.
Indications for use of Vinpocetine
Indications for use of Vinpocetine Forte and Vinpocetine are identical.
What are Vinpocetine tablets for?
The use of the drug according to the instructions is justified when:
- cerebral circulatory failure of an acute or chronic nature;
- post-traumatic encephalopathy;
- discirculatory encephalopathy , causing dizziness, memory impairment, headache;
- vascular lesions of the choroid and retina;
- vegetative-vascular dystonia against the background of menopausal syndrome;
- hearing loss of vascular or toxic origin, dizziness of labyrinthine origin, Meniere's disease .
Indications for use of Vinpocetine Acri:
- to reduce the severity and strength of neurological and mental symptoms in various forms of cerebral circulatory failure (consequences of stroke , recovery stage of stroke, temporary ischemic attack , vertebrobasilar circulatory failure, dementia of vascular origin, atherosclerosis of the cerebral arteries, encephalopathy of post-traumatic and hypertensive origin);
- Meniere's disease , perceptual hearing loss, tinnitus of unknown origin;
- chronic vascular lesions of the choroid and retina.
Contraindications
-Acute phase of hemorrhagic stroke, severe form of coronary heart disease, severe cardiac arrhythmias. -Hypersensitivity to vinpocetine or other components of the drug, deficiency of sucrose, isomaltose, lactose, hereditary lactose intolerance, lactase deficiency, glucose-galactose malabsorption.
-Pregnancy, breastfeeding period.
-Children under 18 years of age (due to lack of clinical trial data).
Use during pregnancy and breastfeeding
The drug is contraindicated during pregnancy, since vinpocetine penetrates the placental barrier. Moreover, its concentration in the placenta and in the blood of the fetus is lower than in the blood of a pregnant woman. At high doses, placental bleeding and spontaneous abortions are possible, probably as a result of increased placental blood supply.
Breastfeeding period: within an hour, 0.25% of the taken dose of the drug penetrates into breast milk. When using the drug, you must stop breastfeeding.
Side effects
Side effects are the same for Vinpocetine and other drugs with a similar composition.
- Reactions from the blood circulation: increased heart rate, instability of blood pressure, ECG changes, extrasystole , hot flashes .
- Reactions from nervous activity: dizziness, insomnia , headache .
- Digestive reactions: nausea, dry mouth, heartburn .
- Other reactions: weakness, allergic reactions, increased sweating.
pharmachologic effect
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”.
Instructions for use of Vinpocetine (Method and dosage)
Vinpocetine tablets, instructions for use
For oral administration, tablets with a dosage of 5-10 mg are usually used, which are taken 1 to 3 times a day, depending on the type of pathology and the doctor’s recommendations.
Instructions for use of Vinpocetine Acree
The medicine should be taken after meals, orally, 1 tablet three times a day. The initial daily dosage is 15 mg. The highest daily dosage is 30 mg. The duration of treatment, depending on the doctor’s recommendations, can reach 3 months.
In case of kidney or liver function disorders, the dosage of the medication is not changed.
The dose is reduced gradually until complete withdrawal.
Vinpocetine ampoules, instructions for use
In the form of injections, Vinpocetine IV is used mainly for acute conditions, a single dose is 20 mg. With normal tolerance, the dosage is increased after 3-4 days to 1 mg/kg body weight. The duration of therapy is usually 10-14 days.
The drug is prohibited for use by children under 18 years of age.
Pharmacokinetics
Distribution of radioactively labeled vinpocetine, when administered to rats, the highest concentrations were 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 AVA 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.
Interaction
No interaction was detected when used simultaneously with Clopamide , β-blockers, Hydrochlorothiazide , Glibenclamide , Acenocoumarol , Digoxin , imipramine .
In some cases, combined use with methyldopa , from which the drug sometimes causes a hypotensive effect. This treatment requires regular monitoring of blood pressure.
There is no data confirming drug interactions with centrally acting drugs, antiarrhythmics and anticoagulants, so caution is recommended during such simultaneous use.
The drug increases the risk of hemorrhagic complications during simultaneous heparin therapy.
Directions for use and doses
The course of treatment and dosage is determined by the attending physician.
Inside, after eating.
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.
The therapeutic effect develops approximately a week from the start of taking the drug. The course of treatment is 1-3 months.
For kidney and liver diseases, the drug is prescribed in the usual dose; the absence of accumulation allows for long courses of treatment.
special instructions
The drug should be used orally with caution in cases of angina , arrhythmia , unstable blood pressure and reduced vascular tone.
In acute cases, parenteral medication is used until the patient’s condition improves, then switched to oral administration. For chronic disorders, the drug is also taken orally.
In case of cerebral hemorrhagic stroke, intravenous administration of the drug is permitted only after the acute effects have subsided.
Vinpocetine analogs
Level 4 ATX code matches:
Bravinton
Acefen
Carnicetine
Pyracesin
Nooclerin
Semax
Piracetam
Olatropil
Fezam
Cerebrocurin
Cavinton Forte
Calcium hopantenate
Glutamic acid
Cephabol
Olanzapine
Cerebrolysate
Pramistar
Sidnocarb
Vinpotropil
Glycine Ozone
Analogues of Vinpocetine:
- Cavintazole
- Bravinton
- Vicebrol
- Cavinton
- Neurovin
- Oxopotin
Vinpocetine price, where to buy
The price of Vinpocetine tablets in Russia is 50 - 100 rubles depending on the manufacturer, and the price of Vinpocetine Forte 10 mg No. 30 is about 90 rubles.
The average price of such tablets in Ukraine in the above release form is about 30 hryvnia.
- Online pharmacies in RussiaRussia
- Online pharmacies in UkraineUkraine
- Online pharmacies in KazakhstanKazakhstan
ZdravCity
- Vinpocetine-AKOS tablets 5 mg 50 pcs. JSC Sintez
83 rub. order - Vinpocetine tablets 5 mg 50 pcs. Izvarino Pharma LLC
103 rub. order
- Vinpocetine tablets 5 mg 50 pcs. Gedeon Richter JSC Gedeon Richter
107 RUR order
- Vinpocetine tablets 5 mg 50 pcs. Pharmproekt JSC
53 RUR order
- Vinpocetine tablets 5mg 50 pcs. AO Update PFK
108 RUR order
Pharmacy Dialogue
- Vinpocetine Welfarm (5 mg tablet No. 50) Welfarm LLC
96 RUR order
- Vinpocetine (5 mg tablet No. 50) Pharmproject CJSC
54 RUR order
- Vinpocetine tablets 5mg No. 50Update PFK JSC
112 rub. order
- Vinpocetine Forte (tab. 10 mg No. 30) Ozone LLC
140 rub. order
- Vinpocetine Forte Canon tablets 10 mg No. 30Canonpharma Production
90 rub. order
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Pharmacy24
- Vinpocetine-Darnitsa 0.5% 2 ml No. 10 solution for infusion PrAT" Pharmaceutical company "Darnitsa", Ukraine
26 UAH. order - Vinpocetine 5 mg No. 30 tablets TOV Astrapharm, Ukraine
30 UAH order
- Vinpocetine-Darnitsa N30 tablets PrAT” Pharmaceutical company “Darnitsa”, Ukraine
27 UAH order
- Vinpocetine 0.005 g No. 30 tablets PrAT "Lekhim-Kharkiv", Kharkiv, Ukraine
26 UAH order
PaniPharmacy
- Vinpocetine infusion Vinpocetine solution d/in. 0.5% amp. 2ml No. 10 Ukraine, Darnitsa ChAO
35 UAH order
- VINPOCETINE ampoule Vinpocetine solution d/in. 0.5% amp. 2ml No. 5 Ukraine, OZ GNTsLS LLC
14 UAH order
- Vinpocetine tablets Vinpocetine tablets. 5mg No. 30 Ukraine, Astrapharm LLC
30 UAH order
- Vinpocetine tablets Vinpocetine tablets. 5mg No. 30 Ukraine, OZ GNTsLS LLC
24 UAH order
- VINPOCETINE ampoule Vinpocetine-LH solution d/in. 5mg/ml 2ml No. 10 Ukraine, Lekhim-Kharkov JSC
33 UAH order
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