Vinpocetine
Vinpocetine: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Drug interactions
- 11. Analogs
- 12. Terms and conditions of storage
- 13. Terms of dispensing from pharmacies
- 14. Reviews
- 15. Price in pharmacies
Latin name: Vinpocetinum
ATX code: N06BX18
Active ingredient: vinpocetine (vinpocetine)
Producer: Sotex PharmFirma, Severnaya Zvezda, DEKO Company, Valenta Pharmaceuticals, Binnopharm CJSC, MAKIZ-PHARMA, Novosibkhimpharm, ALSI Pharma, Ellara LLC, Moskhimfarmpreparaty them. N. A. Semashko ", JSC" Biosynthesis "(Russia), MJ Biopharm, Pvt. Ltd. (India), Alchem International Limited (India), Borisov Medicines Plant (Belarus), Covex (Spain), Gedeon Richter (Hungary), Chedom Pharmaceutical Co., Ltd. (China), Linnea (Switzerland)
Description and photo update: 2019-16-08
Prices in pharmacies: from 21 rubles.
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Vinpocetine is a drug that improves cerebral circulation, and also has antiaggregatory, antihypoxic and vasodilating effects.
Release form and composition
Dosage forms:
- Concentrate for the preparation of a solution for infusion 5 mg / ml, 2 ml in ampoules made of dark glass (5 ampoules in blisters, 1-2 packs, complete with an ampoule knife in a cardboard box);
- Solution for injection 5 mg / ml, 2 ml in ampoules made of dark glass (5 ampoules in blisters, 1 or 2 packs each with an ampoule knife in a cardboard box);
- Tablets 5 mg, flat-cylindrical, with a chamfer, white or white with a yellowish tinge, (10 pieces in blisters, 2 or 5 packs in a cardboard box; 30 pieces in a blister, 1 or 3 packages in a cardboard box) …
The active substance of the drug is vinpocetine.
Pharmacological properties
Pharmacodynamics
The mechanism of action of vinpocetine is to improve metabolism and cerebral blood flow, as well as a beneficial effect on the rheological parameters of blood. The neuroprotective effect is due to a decrease in the adverse cytotoxic effect of excitatory amino acids. The substance blocks sodium and calcium channels, as well as AMPA and NMDA receptors. It is characterized by selective inhibition of Ca 2+ -calmodulin-dependent-cGMP-phosphodiesterase. Vinpocetine improves the metabolism of norepinephrine and serotonin in the brain, has an antioxidant effect and activates the noradrenergic neurotransmitter system.
The drug normalizes microcirculation in the brain by inhibiting platelet aggregation, increasing the deformability of erythrocytes, inhibiting the reuptake of adenosine and reducing pathologically increased blood viscosity. It ensures the saturation of cells with oxygen by reducing the affinity of red blood cells for it. Vinpocetine selectively stimulates cerebral blood flow due to a decrease in cerebral vascular resistance, and the systemic parameters of blood circulation (total peripheral vascular resistance, blood pressure, heart rate, cardiac output) do not change significantly. There is no “steal” effect during treatment.
Pharmacokinetics
Vinpocetine is subject to rapid absorption. After oral administration, its maximum plasma level is reached in about 1 hour. The compound is absorbed mainly in the proximal intestine. When passing through the intestinal wall, it is not metabolized.
After oral administration of vinpocetine, labeled with radioactive isotopes, to rats, the highest level of radioactivity was observed in the gastrointestinal tract and liver. The maximum concentration in tissues was recorded 2–4 hours after administration. The concentration of the drug in the brain did not exceed that in the blood.
When the drug is administered in the form of a solution for infusion or a solution for intravenous administration, its therapeutic concentration in blood plasma is 10–20 mg / ml. With parenteral administration, the volume of distribution is 5.3 l / kg, and the half-life in this case is 4.74-5 hours. Vinpocetine easily crosses the histohematogenous barriers (including the blood-brain barrier) and the placental barrier, and is also determined in breast milk (0.25% of the administered dose during the first hour).
When used in humans, vinpocetine binds to plasma proteins by about 66%. Its bioavailability is 7%. The volume of distribution is 246.7 ± 88.5 L, which confirms the high degree of tissue binding. The total clearance, reaching 66.7 l / h, is higher than the hepatic blood flow rate (50 l / h), which indicates extrahepatic metabolism.
In the process of metabolism of vinpocetine, apovincamic acid (AVA) is formed, the amount of which is 25–30% of the dose taken. The area under the concentration-time curve for VKA after oral administration is 2 times higher than that for intravenous administration of vinpocetine. Consequently, the drug is characterized by a pronounced "first pass" effect through the liver. AVK-dioxyglycinate, hydroxy-AVK, hydroxy-vinpocetine and their conjugates (glucuronides and / or sulfates) are also formed as metabolites. In unchanged form, vinpocetine is excreted in a small amount (no more than a few percent).
With dysfunction of the kidneys or liver, there is no need for dose adjustment, since vinpocetine practically does not accumulate in the body.
With repeated administration at a dose of 5 and 10 mg, the pharmacokinetic parameters of vinpocetine demonstrate a linear relationship, and 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. Studies with radioactively labeled vinpocetine have confirmed that excretion in urine and faeces occurs in a percentage ratio of about 60:40.
In dogs and rats, vinpocetine is determined in bile in significant concentrations, but there is a significant enterohepatic recirculation.
In elderly patients, especially those undergoing a long course of treatment, one should take into account the slowdown in the distribution of vinpocetine and its reduced metabolism. However, the results of clinical studies indicate that the pharmacokinetics of vinpocetine in elderly patients does not differ significantly from that in young patients, and there is no accumulation of the substance in the body, as in the case of renal and liver dysfunctions (in the latter case, a long course of treatment is permissible).
Indications for use
- Chronic and acute cerebrovascular accident;
- Dyscirculatory encephalopathy, accompanied by headache, dizziness, memory impairment;
- Vascular diseases of the choroid and retina;
- Post-traumatic encephalopathy;
- Vegetovascular dystonia with climacteric syndrome;
- Meniere's disease, hearing impairment of toxic or vascular origin, dizziness of a labyrinthine origin.
Contraindications
- Pregnancy;
- Hypersensitivity to drug components.
For parenteral administration of Vinpocetine, additional contraindications are:
- Severe arrhythmias;
- Severe ischemic heart disease.
There are no data on the safety of the drug in lactating women.
Instructions for the use of Vinpocetine: method and dosage
Inside Vinpocetine is taken 3 times a day, 5-10 mg. The initial daily dose is 15 mg, the maximum is 30 mg.
The drug in the form of injections is most often used in acute conditions in a single dose of 20 mg. With good tolerance, the dose is increased to 1 mg / kg within 3-4 days.
The duration of therapy is 10-14 days. During the withdrawal process, the dosage of the drug should be reduced gradually. No more than 2-3 courses of taking the drug are allowed per year.
Side effects
- Cardiovascular system and blood (hemostasis, hematopoiesis): slowing down of intraventricular conduction; depression of the ST segment and lengthening of the QT interval, tachycardia, hypotension, extrasystole, skin redness, thrombophlebitis at the injection site;
- Nervous system and sensory organs: headache, dizziness, weakness, drowsiness, insomnia;
- Organs of the gastrointestinal tract (GIT): heartburn, nausea, dry mouth;
- Skin: sweating;
- Other: allergic reactions.
Overdose
At the moment, no cases of overdose have been reported. If necessary, symptomatic therapy is prescribed.
special instructions
According to the instructions, Vinpocetine inside should be taken with caution in case of angina pectoris, arrhythmias, decreased vascular tone and unstable blood pressure.
As a rule, the drug is used parenterally in acute cases, and, after the improvement of the clinical picture, they switch to taking it in the form of tablets.
When treating chronic diseases, the drug should be taken orally.
Parenteral administration for hemorrhagic cerebral stroke is allowed only after a decrease in acute events (as a rule, after 5-7 days).
Influence on the ability to drive vehicles and complex mechanisms
Studies of the effect of Vinpocetine on the ability to drive vehicles have not been conducted. In case of diagnosed adverse reactions from the central nervous system during treatment with the drug, it is recommended to be careful when driving and working with complex moving mechanisms.
Application during pregnancy and lactation
The appointment of Vinpocetine during pregnancy and lactation is contraindicated. It crosses the placenta, but the drug content in the placenta and the fetus is lower than that of the mother. The presence of teratogenic and embryotoxic effects has not been confirmed. Animal studies have shown that when high doses were administered, placental bleeding and spontaneous abortions were observed in pregnant females, probably due to the activation of placental blood flow.
Vinpocetine is determined in breast milk. In accordance with the results of preclinical studies using radioactively labeled vinpocetine, its content in the breast milk of lactating females was 10 times higher than that in the mother's blood.
Drug interactions
With the simultaneous use of Vinpocetine with warfarin, there were reports of a slight decrease in the anticoagulant effect of the latter.
With joint parenteral use with heparin, an increase in the risk of bleeding is possible.
Analogs
Vinpocetine analogues are: Vinpocetine Acri, Vinpocetine-Akos, Vinpocetin Forte, Vinpocetin-Sar, Vicebrol, Cavinton, Cavinton Forte, Cavinton Comfort, Telektol, Neurovin, Piracetam, Oxopotin.
Terms and conditions of storage
Store in a dark, dry place out of reach of children.
Shelf life:
- Concentrate for preparation of solution for infusion - 2 years at temperatures up to 25 ° C;
- Solution for injection - 2 years at a temperature of 10-30 ° C;
- Tablets - 3 years at a temperature of 15-25 ° C.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Vinpocetine
According to reviews, Vinpocetine and its therapeutic properties were highly appreciated in patients. Most often, the drug is used to improve the blood supply to the brain. Experts confirm that adverse reactions during treatment rarely develop and advise taking Vinpocetine only as directed by a doctor. It is not recommended to assign it to children.
Price for Vinpocetine in pharmacies
The approximate price of Vinpocetine in tablets is 59-130 rubles (5 mg each, 50 pieces are included in the package) or 96-149 rubles (10 mg each, 30 pieces are included in the package), depending on the manufacturer. You can purchase a concentrate for the preparation of a solution for infusion for 45-76 rubles (the package includes 10 ampoules). The cost of a solution for injection 5 mg / ml varies in the range from 77 to 141 rubles (the package contains 10 ampoules).
Vinpocetine: prices in online pharmacies
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Drug name Price Pharmacy |
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Vinpocetine 5 mg tablets 20 pcs. RUB 21 Buy |
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Vinpocetine 5 mg tablets 50 pcs. 34 rbl. Buy |
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Vinpocetine 5 mg tablets 30 pcs. RUB 38 Buy |
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Vinpocetine 5 mg tablets 50 pcs. RUB 44 Buy |
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Vinpocetine 5 mg tablets 60 pcs. RUB 47 Buy |
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Vinpocetine 5 mg / ml concentrate for preparation of solution for infusion 2 ml 10 pcs. RUB 48 Buy |
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Vinpocetine tablets 5mg 50 pcs. 52 RUB Buy |
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Vinpocetine 5 mg tablets 50 pcs. 52 RUB Buy |
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Vinpocetine 5 mg / ml solution for injection 2 ml 10 pcs. RUB 59 Buy |
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Vinpocetine 5 mg tablets 50 pcs. RUB 60 Buy |
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Vinpocetine tablets 5mg 50 pcs. RUB 67 Buy |
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Vinpocetine 5 mg / ml concentrate for preparation of solution for infusion 2 ml 10 pcs. RUB 68 Buy |
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Vinpocetine 5 mg tablets 50 pcs. RUB 70 Buy |
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Vinpocetine 5 mg tablets 50 pcs. RUB 70 Buy |
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Vinpocetine conc. for prig solution for inf. 0.5% 2ml 10 pcs. 73 rbl. Buy |
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Vinpocetine 5 mg tablets 50 pcs. RUB 75 Buy |
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Vinpocetine 5 mg tablets 50 pcs. 79 RUB Buy |
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Vinpocetine 5 mg tablets 50 pcs. 79 RUB Buy |
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Vinpocetine forte 10 mg tablets 30 pcs. 79 RUB Buy |
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Vinpocetine forte 10 mg tablets 30 pcs. RUB 80 Buy |
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Vinpocetine forte 10 mg tablets 30 pcs. RUB 88 Buy |
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Vinpocetine forte tablets 10mg 30 pcs. 93 rbl. Buy |
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Vinpocetine forte 10mg tablets 30 pcs. RUB 105 Buy |
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Vinpocetine tablets 5mg 50 pcs. Gedeon Richter 107 RUB Buy |
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Vinpocetine 5 mg tablets 50 pcs. 107 RUB Buy |
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Vinpocetine forte Canon 10mg tablets 30 pcs. 109 RUB Buy |
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Vinpocetine tablets 5mg 50 pcs. 115 RUB Buy |
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Vinpocetine 10 mg tablets 30 pcs. 122 RUB Buy |
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Vinpocetine tablets 5mg 50 pcs. 162 RUB Buy |
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Vinpocetine conc-t d / prigot. solution for inf 5mg / ml amp. 2ml No. 10 179 r Buy |
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Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
