Cavinton tablets 5mg №25×2

Name:
Cavinton tab 5mg in a blister in pack No. 25×2
Description:
Cavinton tablets: white or almost white, flat, round tablets with a bevel, about 9 mm in diameter, odorless, engraved with “CAVINTON” on one side. Cavinton Forte tablets: white or almost white flat, round, beveled tablets, about 8.0 mm in diameter, with the inscription “10 mg” on one side and a line on the other. The main active ingredient Vinpocetine Release form Tablets Dosage 5 mg Pharmacological properties Pharmacodynamics Vinpocetine has an effect on metabolism, cerebral circulation, blood rheology. Vinpocetine exhibits neuroprotective effects, 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 excretion 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 is formed in humans 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). Change in pharmacokinetic properties in special circumstances (eg, at a certain age, in the presence of concomitant diseases). Since vinpocetine is indicated for the treatment of predominantly elderly patients who experience changes in the kinetics of drugs – reduced absorption, different distribution and metabolism, reduced excretion – it was necessary to conduct studies to evaluate the kinetics of vinpocetine in this age group, especially with long-term use. The results of such studies have demonstrated that the kinetics of vinpocetine in the elderly does not differ significantly from the kinetics of vinpocetine in young people, and, in addition, there is no cumulation. In case of impaired liver or kidney function, the usual doses of the drug can be used, since vinpocetine does not accumulate in the body of such patients, which allows for long-term use. Indications for use Neurology: The following forms of cerebral ischemia: conditions after an 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. Dosing and Administration Usual doses of the drug are 5-10 mg 3 times a day (15-30 mg per day). Tablets must be taken after meals. For patients with kidney or liver disease, special dose selection is not required. The use of the drug Cavinton or Cavinton Forte in children under 18 years of age is contraindicated. Use during pregnancy and lactation During pregnancy and lactation, the use of vinpocetine is contraindicated. Pregnancy: Vinpocetine crosses the placenta, but in the placenta and in the blood of the fetus is found in lower concentrations than in the blood of the mother. No teratogenic or embryotoxic effect was noted. In preclinical studies, the administration of the drug at high doses in some cases caused placental bleeding and spontaneous abortion, mainly as a result of increased placental blood flow. Lactation: Vinpocetine is excreted in breast milk. In studies using the radioactive isotope vinpocetine, the radioactivity of breast milk was ten times higher than that in the mother’s blood. The amount excreted in milk within 1 hour is 0.25 percent of the administered dose of the drug. Since vinpocetine is excreted in mother’s milk, and there are no data on the effects on the body of the newborn, the use of vinpocetine during breastfeeding is contraindicated. PrecautionsECG monitoring is recommended in the presence of long QT interval syndrome or while taking a drug that helps prolong the QT interval. In case of lactose intolerance, it must be taken into account that the drug contains lactose: each Cavinton 5 mg tablet contains 140 mg of lactose, each Cavinton Forte tablet (10 mg) contains 83 mg of lactose. Interaction with other drugs 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. Although data from clinical studies have not confirmed interactions, caution is advised in the case of simultaneous use of vinpocetine with drugs that affect the central nervous system, as well as in the case of concomitant antiarrhythmic and anticoagulant therapy. Contraindications Pregnancy, lactation. Hypersensitivity to the active substance or to any of the excipients. Acute phase of hemorrhagic cerebral stroke, severe ischemic heart disease, severe forms of arrhythmia. Children under 18 years of age (due to lack of clinical data). Use during pregnancy and lactation During pregnancy and lactation, the use of vinpocetine is contraindicated. Pregnancy: Vinpocetine crosses the placenta, but in the placenta and in the blood of the fetus is found in lower concentrations than in the blood of the mother. No teratogenic or embryotoxic effect was noted. In preclinical studies, the administration of the drug at high doses in some cases caused placental bleeding and spontaneous abortion, mainly as a result of increased placental blood flow. Lactation: Vinpocetine is excreted in breast milk. In studies using the radioactive isotope vinpocetine, the radioactivity of breast milk was ten times higher than that in the mother’s blood. The amount excreted in milk within 1 hour is 0.25 percent of the administered dose of the drug. Since vinpocetine is excreted in mother’s milk, and there are no data on the effects on the body of the newborn, the use of vinpocetine during breastfeeding is contraindicated. Composition Each tablet contains: Cavinton tablets Active ingredient: 5 mg vinpocetine Excipients: magnesium stearate; silicon dioxide colloidal anhydrous; talc; corn starch; lactose monohydrate. Cavinton Forte tablets: Active ingredient: 10 mg of vinpocetine Excipients: magnesium stearate; silicon dioxide colloidal anhydrous; talc; corn starch; lactose monohydrate. Overdose No cases of overdose have been noted. Based on literature data, long-term use of vinpocetine at a daily dose of 60 mg is safe. A single oral intake of 360 mg of vinpocetine was not accompanied by the development of either cardiovascular or other side effects. Adverse reactions Adverse reactions are listed below, classified by organ system class and frequency of occurrence according to MedDRA terminology: Organ system class (MedDRA 12.1) Uncommon (? 1/1000 – < 1/100) Rare (? 1/10,000 - < 1/1000) Very rare (< 1/10,000) Blood and lymphatic disorders Leukopenia Thrombocytopenia AnemiaErythrocyte agglutination Immune system disorders Hypersensitivity Metabolic and nutritional disorders Hypercholesterolemia Decreased appetiteAnorexiaDiabetes mellitus Psychiatric disorders Insomnia Sleep disturbance Anxiety Euphoria Depression Nervous disorders system Headache Dizziness Dysgeusia Stupor Hemiparesis Drowsiness Amnesia TremorConvulsions Eye disorders Optic disc edema Conjunctival hyperemia Hearing and labyrinth disorders Dizziness Hyperacusia Hypoacusia Tinnitus Cardiac disorders Ischemia/s Myocardial infarction Angina pectoris BradycardiaTachycardia Extrasystole Palpitations Arrhythmia Atrial fibrillation Vascular disorders Hypotension Hypertension Hot flushesThrombophlebitis Arterial pressure fluctuations Gastrointestinal tract disorders Abdominal discomfort Dry mouth Nausea Abdominal pain ConstipationDiarrhea DyspepsiaVomiting Dysphagia Stomatitis Urticaria Urticaria Rash Dermatitis General disorders and reactions at the injection site Asthenia Weakness Feeling of heat Discomfort in the chest Hypothermia Results of laboratory and instrumental studies Decrease in blood pressure Increase in blood pressure Increase in blood triglycerides ST segment depression on the electrocardiogram Decrease/increase in the number of eosinophils Change in the activity of "liver" enzymes Increase / decrease in the number of leukocytes Decrease in the number of erythrocytes Shortening of the prothrombin time Increase body weight Storage conditionsStore at a temperature of +15 °C to +30 °C, protected from light. Keep out of the reach of children. Buy Cavinton tablets 5mg No. 25x2 Price for Cavinton tablets 5mg No. 25x2