Vinpocetine tablets 5mg №10×5

Name:
Vinpocetine tabl. Producer: Borisov ZMP INN: Vinpocetine FTG: Cerebrovasodilating agent Composition 1 tablet contains: active ingredient – vinpocetine 5 mg; excipients – potato starch, lactose monohydrate, microcrystalline cellulose, magnesium stearate, talc, povidone.
Description:
Pills white or white with a yellowish tint, flat-cylindrical, with a bevel. Pharmacotherapeutic group Other psychostimulants and nootropics. ATX code: N06BX18. Pharmacological properties Pharmacodynamics Vinpocetine has an effect on metabolism, cerebral circulation, and rheological properties of blood. Vinpocetine exhibits neuroprotective effects: it reduces the harmful effects of cytotoxic reactions caused by stimulating amino acids. Vinpocetine inhibits voltage-dependent Na + – and Ca2 + channels, as well as NMDA and AMPA receptors, enhances the neuroprotective effect of adenosine. Vinpocetine stimulates cerebral metabolism: it increases the uptake of glucose and O2 and the consumption of these substances by the brain tissue. Vinpocetine increases the resistance of the brain to hypoxia; increases the transport of glucose – an exclusive source of energy for the brain – through the blood-brain barrier; shifts glucose metabolism towards an energetically more favorable aerobic pathway; selectively inhibits Ca2+ calmodulin-dependent enzyme cGMP-phosphodiesterase (PDE); increases the levels of cAMP and cGMP in the brain. Vinpocetine increases the concentration of ATP and the ratio of ATP / AMP; enhances the exchange of norepinephrine and serotonin in the brain; stimulates the ascending noradrenergic system; has antioxidant activity. Vinpocetine improves microcirculation in the brain: inhibits platelet aggregation; reduces pathologically increased blood viscosity; increases the deformability of erythrocytes and inhibits the capture of adenosine; improves O2 transport in tissues by reducing O2 affinity for erythrocytes. Vinpocetine selectively increases blood flow in the brain: increases the cerebral fraction of cardiac output; reduces the resistance of cerebral vessels without affecting the parameters of systemic circulation (blood pressure, cardiac output, pulse rate, total peripheral resistance); the drug does not cause a “steal effect”. Moreover, against the background of vinpocetine, blood flow improves in damaged (but not yet necrotic) ischemic areas with low perfusion (“reverse steal effect”). Pharmacokinetics Absorption: Vinpocetine is rapidly absorbed; Peak plasma concentrations are reached 1 hour after oral administration. The main site of absorption of vinpocetine is the proximal gastrointestinal tract. The compound is not metabolized while passing through the intestinal wall. Distribution: In studies with oral administration of the drug in rats, radiolabeled vinpocetine was found in the highest concentration in the liver and in the gastrointestinal tract. Maximum concentrations in tissues could be detected 2-4 hours after the use of vinpocetine. The concentration of the radioactive label in the brain did not exceed the concentration in the blood. In humans: binding to blood proteins is 66%. The absolute bioavailability of vinpocetine when taken orally is about 7%. The volume of distribution is 246.7 ± 88.5 l, which means a pronounced binding of the substance in the tissues. The clearance value of vinpocetine (66.7 l/h) in plasma exceeds its value in the liver (50 l/h), indicating extrahepatic metabolism of the compound. Withdrawal: with repeated oral administration of the drug at a dose of 5 mg and 10 mg, vinpocetine demonstrates linear kinetics; equilibrium plasma concentrations are 1.2 ± 0.27 ng / ml and 2.1 ± 0.33 ng / ml, respectively. The half-life in humans is 4.83 ± 1.29 hours. In studies conducted using a radioactively labeled compound, it was found that the main route of elimination is through the kidneys and intestines in a ratio of 60:40 (%,%). A greater amount of radioactive label in rats and dogs was found in the bile, but there was no significant enterohepatic circulation. Apovincamic acid is excreted through the kidneys by simple glomerular filtration, the half-life depends on the dose and route of administration of vinpocetine. Metabolism: The main metabolite of vinpocetine is apovincamic acid (AVA), which in humans is formed in 25 – 30%. After oral administration, the area under the curve (“plasma concentration – time”) of VKA is twice that after intravenous administration of the drug, which indicates the formation of VKA during the first pass metabolism of vinpocetine. Other identified metabolites are hydroxyvinpocetine, hydroxy-AVK, dihydroxy-AVK-glycinate and their conjugates with glucuronides and/or sulfates. In any of the studied species, the amount of vinpocetine that was excreted unchanged was only a few percent of the dose of the drug taken. An important and significant property of vinpocetine is the absence of the need for special selection of the dose of the drug in patients with liver or kidney diseases due to the metabolism of the drug and the absence of cumulation (accumulation). Indications for use Neurology: the following forms of cerebral ischemia: conditions after acute cerebrovascular accident, chronic cerebrovascular insufficiency due to cerebral atherosclerosis or arterial hypertension, including vertebrobasilar insufficiency; as well as vascular dementia, post-traumatic encephalopathy. Helps to reduce mental and neurological symptoms in cerebral ischemia. Ophthalmology: for the treatment of chronic vascular pathology of the choroid (the choroid) and the retina. Otorhinolaryngology: for the treatment of sensorineural hearing loss, Meniere’s disease and idiopathic tinnitus. Contraindications Severe cardiac arrhythmias; ischemic heart disease (severe course); acute period of intracerebral hemorrhage; lactase deficiency; increased intracranial pressure; pregnancy; lactation (breastfeeding); hypersensitivity to the active substance or other components of the drug; children under 18 years. Dosage and administration Vinpocetine should be prescribed 5-10 mg 3 times / day for 2 months. Apply after meals. The duration of the course of treatment is determined by the doctor, taking into account the characteristics of the disease, the effect achieved and the tolerability of the drug. Before discontinuation of the drug, the dose should be gradually reduced. Repeated courses are possible 2-3 times a year. Special instructions In connection with the content of lactose, the drug is not recommended for patients with rare congenital galactose intolerance, lactase deficiency or malabsorption of glucose-galactose. Pregnancy and lactation Vinpocetine is contraindicated for use during pregnancy. If necessary, its use during lactation should stop breastfeeding. Pediatric Use The safety and efficacy of vinpocetine in children has not been established. Experience with vinpocetine in patients under 18 years of age is limited. Use in persons with impaired liver and kidney function The drug should not be prescribed to patients with liver disease with severe impaired function. Use in persons with cardiovascular pathology Caution should be exercised when prescribing vinpocetine to patients taking antihypertensive drugs or drugs that prolong the QT interval (loratadine, terfenadine, erythromycin, probucol) or who have a history of QT interval prolongation syndrome. Influence on the ability to drive vehicles and control mechanisms Patients taking vinpocetine should refrain from potentially hazardous activities associated with the need for increased attention and rapid psychomotor reactions. Interaction with other medicinal products Caution should be used when vinpocetine is administered concomitantly with central nervous system drugs, antiarrhythmic and anticoagulant agents. In clinical studies with the simultaneous use of vinpocetine with beta-blockers such as cloranolol and pindolol, as well as with simultaneous use with clopamide, glibenclamide, digoxin, acenocoumarol or hydrochlorothiazide, no interaction between these drugs has been identified. In rare cases, some additional effect was observed with the simultaneous use of alpha-methyldopa and vinpocetine, therefore, against the background of the use of this combination of drugs, it is necessary to regularly monitor blood pressure. Overdose No cases of overdose have been noted. Treatment is symptomatic. Packaging 10 tablets in a blister pack, 5 packs with a leaflet in a pack. Storage conditions In a place protected from light and moisture, at a temperature of 15 ° C to 25 ° C. Keep out of the reach of children. Shelf life 2 years. Do not use after the expiration date. Terms of dispensing from pharmaciesBy prescription. Buy Vinpocetine tablets 5mg No. 10×5 Price for Vinpocetine tablets 5mg No. 10×5