Instructions for Vinpocetine-Darnitsa tablets 5 mg No. 30
Composition
active ingredient: vinpocetine;
1 tablet contains vinpocetine 5 mg;
Excipients: lactose monohydrate, potato starch, magnesium stearate.
Dosage form
Pills.
Main physicochemical properties: white tablets, flat-cylindrical in shape, with a bevel.
Pharmacotherapeutic group
Psychostimulants and nootropics. Vinpocetine.
ATX code N06B X18.
Pharmacological properties
Pharmacodynamics.
Vinpocetine is a compound with a complex mechanism of action that favorably affects metabolism in the brain and improves its blood supply, as well as improves the rheological properties of blood.
Vinpocetine exhibits neuroprotective effects: the drug attenuates the harmful effects of cytotoxic reactions caused by stimulating amino acids. The drug inhibits voltage-gated Na+ and Ca2+ channels, as well as NMDA and AMPA receptors. The drug enhances the neuroprotective effect of adenosine.
Vinpocetine stimulates cerebral metabolism: the drug increases the uptake of glucose and O2 and the consumption of these substances by brain tissue. The drug increases the brain's resistance to hypoxia; increases the transport of glucose - the exclusive source of energy for the brain - through the blood-brain barrier; shifts glucose metabolism towards an energetically more favorable aerobic pathway; selectively inhibits the Ca2+-calmodulin-dependent enzyme cGMP-phosphodiesterase (PDE); increases the level of cAMP and cGMP in the brain. The drug increases the concentration of ATP and the ATP/AMP ratio; enhances the metabolism of noradrenaline and serotonin in the brain; stimulates the ascending noradrenergic system; has antioxidant activity, as a result of all the above effects, vinpocetine has a cerebroprotective effect.
Vinpocetine improves microcirculation in the brain: the drug inhibits platelet aggregation, reduces pathologically increased blood viscosity, increases the ability of erythrocytes to deform and inhibits adenosine uptake; improves O2 transport in tissues by reducing the affinity of O2 for erythrocytes.
Vinpocetine selectively increases blood flow in the brain: the drug increases the cerebral fraction of cardiac output; reduces vascular resistance in the brain, without affecting the parameters of systemic circulation (blood pressure, cardiac output, pulse rate, total peripheral resistance); the drug does not cause a "stealing effect". Moreover, against the background of taking the drug, blood flow to damaged (but not yet necrotic) areas of ischemia with low perfusion improves ("reverse steal effect").
Pharmacokinetics.
Absorption: rapidly absorbed, and an hour after oral administration its concentration in the blood reaches a maximum. Absorption occurs mainly in the proximal parts of the digestive tract. It is not metabolized when passing through the intestinal wall.
Distribution: Studies with radiolabeled vinpocetine have shown that, following oral administration, the highest radioactivity is detected in the liver and gastrointestinal tract. The maximum tissue concentration is observed through
2–4 hours after oral administration. The concentration of vinpocetine in brain tissues does not exceed its concentration in the blood. In the human body, 66% of vinpocetine is bound to proteins, bioavailability when administered orally is 7%, volume of distribution is 246.7 ± 88.5 l, which indicates good distribution in tissues. The value of vinpocetine clearance (66.7 l/h) in blood plasma exceeds its value in the liver (50 l/h), which indicates extrahepatic metabolism of the compound.
Metabolism: The main metabolite of vinpocetine, apovincamic acid (AVC), is formed in the human body in an amount of 25–30% during the first passage of vinpocetine through the liver. Compared with intravenous administration, after oral administration of the drug, the area under the concentration-time curve (AUC) of AVC is twice as large. Other metabolites of vinpocetine are: hydroxyvinpocetine, hydroxy-AVC, dihydroxyapovincamic acid glycinate and their sulfate and glucuronide conjugates. Liver and kidney diseases do not affect the metabolism of vinpocetine.
Elimination: with repeated oral administration of the drug at a dose of 5 and 10 mg, the kinetics are linear, plasma concentrations in the saturation stage 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. It is excreted in urine and feces in a ratio of 3:2. AVK is eliminated by glomerular filtration. The half-life depends on the dose of vinpocetine and the dosage regimen.
Elderly patients. According to clinical studies, there are no significant differences in the kinetics of the drug in elderly and young patients, the drug does not cumulate. Patients with liver and/or kidney diseases are prescribed the drug in the usual dose, the absence of cumulation allows for long-term treatment.
Indication
Neurology. For the treatment of various forms of cerebrovascular pathology: conditions after a stroke, vertebrobasilar insufficiency, vascular dementia, cerebral atherosclerosis, post-traumatic and hypertensive encephalopathy. Helps reduce mental and neurological symptoms in cerebrovascular pathology.
Ophthalmology. For the treatment of chronic vascular pathology of the choroid and retina.
Otorhinolaryngology. For the treatment of senile perceptual hearing loss, Meniere's disease, and tinnitus.
Contraindication
Hypersensitivity to the active substance or to any of the excipients.
Interaction with other medicinal products and other types of interactions
The simultaneous use of vinpocetine with β-blockers (cloranolol, pindolol), as well as with clopamide, glibenclamide, digoxin, acenocoumarol or hydrochlorothiazide in clinical studies was not accompanied by any interaction between them.
The simultaneous use of vinpocetine and α-methyldopa sometimes caused some enhancement of the hypotensive effect, therefore, regular monitoring of blood pressure is required during such treatment.
Despite the lack of clinical study data confirming the possibility of interaction, it is recommended to exercise caution when prescribing vinpocetine simultaneously with drugs that act on the central nervous system, antiarrhythmics and anticoagulants.
The simultaneous use of the drug Vinpocetine-Darnitsa and heparin increases the risk of hemorrhagic complications.
Application features
ECG monitoring is recommended in the presence of long QT syndrome or when taking concomitant medications that prolong the QT interval.
If the patient has increased intracranial pressure, arrhythmia or long QT syndrome, as well as against the background of the use of antiarrhythmic drugs, a course of therapy with the drug can be started only after a thorough analysis of the benefits and risks associated with the use of the drug.
Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.
Reproductive: Does not affect fertility.
No teratogenic effects were detected.
Mutagenicity. Vinpocetine does not have a mutagenic effect.
Carcinogenicity. Vinpocetine does not have a carcinogenic effect.
Use during pregnancy or breastfeeding
The use of the drug during pregnancy or breastfeeding is contraindicated.
Ability to influence reaction speed when driving vehicles or other mechanisms
No studies have been conducted on the effects on the ability to drive or operate machinery, but caution should be exercised, given the possibility of drowsiness, dizziness, and vertigo when using the drug.
Method of administration and doses
Take orally after meals.
Vinpocetine-Darnitsa is recommended for adults to take 5–10 mg (1–2 tablets) 3 times a day (15–30 mg per day).
Patients with kidney or liver disease do not require special dose adjustment.
The duration of treatment is determined by the doctor individually.
Children
The drug is not used in children (due to the lack of clinical data).
Overdose
No cases of overdose have been reported. Long-term use of vinpocetine at a daily dose of 60 mg is also safe. Even a single oral dose of 360 mg of vinpocetine did not cause any clinically significant adverse effects on the cardiovascular system or other effects.
Adverse reactions
On the part of the organs of vision: swelling of the optic nerve head, conjunctival hyperemia.
From the side of the organs of hearing and vestibular apparatus: vertigo, hyperacusis, hypoacusis, tinnitus.
Gastrointestinal: abdominal discomfort, dry mouth, nausea, abdominal pain, constipation, diarrhea, dyspepsia, vomiting, dysphagia, stomatitis.
From the side of metabolism: hypercholesterolemia, decreased appetite, anorexia, diabetes mellitus, weight gain.
From the nervous system: headache, dizziness, dysgeusia, stupor, hemiparesis, drowsiness, amnesia, tremor, convulsions.
On the part of the psyche: insomnia, sleep disorders, agitation, anxiety, euphoria, depression.
Cardiovascular system: hypotension, hypertension, hot flashes, thrombophlebitis, blood pressure fluctuations, myocardial ischemia/infarction, angina pectoris, bradycardia, tachycardia, extrasystole, palpitations, arrhythmia, atrial fibrillation.
From the blood and lymphatic system: leukopenia, thrombocytopenia, anemia, erythrocyte agglutination.
Immune system disorders: hypersensitivity reactions, including rash, itching, urticaria.
Skin and subcutaneous tissue disorders: erythema, hyperhidrosis, pruritus, urticaria, rash, dermatitis.
Laboratory indicators: decreased blood pressure, increased blood pressure, increased triglyceride levels in the blood, ST segment depression on the electrocardiogram, increased/decreased eosinophil count, changes in liver enzyme activity, increased/decreased leukocyte count, decreased erythrocyte count, decreased prothrombin time.
Expiration date
3 years.
Storage conditions
Store out of the reach of children in the original packaging at a temperature not exceeding 25 °C.
Packaging
10 tablets in a contour blister pack; 3 or 5 contour blister packs in a pack.
Vacation category
According to the recipe.
Producer
PrJSC "Pharmaceutical Company "Darnitsa".
Location of the manufacturer and its business address
Ukraine, 02093, Kyiv, Boryspilska St., 13.
