Vinpocetine
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Clinical Pharmacology
A means of improving cerebral circulation and brain metabolism. Inhibits phosphodiesterase activity, which contributes to the accumulation of cAMP in tissues. It has a vasodilating effect mainly on the vessels of the brain, which is caused by direct myotropic antispasmodic action. Systemic blood pressure drops slightly. It improves blood flow and microcirculation in the brain tissues, reduces platelet aggregation, and contributes to the normalization of the rheological properties of blood. It improves the portability of hypoxia by brain cells, facilitating the transport of oxygen to tissues due to a decrease in the red blood cell affinity for it, enhancing the absorption and metabolism of glucose. Increases the content of catecholamines in brain tissue.
Indications
Acute and chronic cerebrovascular insufficiency. Dyscirculatory encephalopathy, accompanied by memory impairment, dizziness, headache. Posttraumatic encephalopathy. Vascular diseases of the retina and choroid. Hearing impairment of vascular or toxic origin, Meniere's disease, dizziness of labyrinth origin. Vegetative-vascular dystonia in climacteric syndrome.
Composition
1 tab .:
Vinpocetine 5 mg
Excipients: potato starch - 64.3 mg, lactose monohydrate (milk sugar) - 171.9 mg, colloidal silicon dioxide (aerosil) - 1.7 mg, talc - 4.7 mg, magnesium stearate - 2.4 mg.
Vinpocetine is marketed under different brands and generic names, and comes in different dosage forms:
Brand name | Manufacturer | Country | Dosage form |
---|---|---|---|
Vinpocetine | PFK Obnovlenie | Russia | pills |
Vinpocetine | Obolensky OP | Russia | pills |
Vinpocetine | Izvarino Pharma | Russia | pills |
Vinpocetine-Akos | Synthesis AKOMP | Russia | ampoules |
Cavinton Comforte | Gedeon Richter | Hungary | pills |
Cavinton | Gedeon Richter | Hungary | pills |
Cavinton | Gedeon Richter | Hungary | ampoules |
Vinpocetin-Sar | Biochemist Saransk | Russia | ampoules |
Vinpocetine | Gedeon Richter | Hungary | pills |
Vinpocetine | Canonpharma | Russia | pills |
Cavinton Forte | Gedeon Richter | Hungary | pills |
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Dosage and Administration
Inside, after eating.
The course of treatment and the dose is determined by the attending physician.
Typically, the daily dose is 15-30 mg (5-10 mg 3 times a day).
The initial daily dose is 15 mg. Maximum Daily Dose
30 mg.
Dose adjustment for the elderly, for violations of the liver or kidneys is not required.
Adverse reactions
To determine the incidence of side effects of the drug used the following classification:
Very often (≥ 1/10)
Often (≥ 1/100 and <1/10)
Infrequently (≥ 1/1000 and <1/100)
Rarely (≥ 1/10 000 and <1/1000)
Very rarely (≥ 1/10 000).
From the side of the heart: rarely - ischemia / myocardial infarction, bradycardia, angina pectoris, tachycardia, extrasystole, palpitations; very rarely - arrhythmia, atrial fibrillation.
From the side of vessels: infrequently - decrease in blood pressure; rarely - increased blood pressure, tidal sensation, thrombophlebitis; very rarely - the instability of blood pressure.
From the side of the central nervous system: infrequently - headache; rarely - dysgeusia, stupor, hemiparesis, drowsiness, amnesia; very rarely - tremor, spasms.
On the part of the organ of vision: rarely - swelling of the optic nerve head; very rarely - conjunctival hyperemia.
From the organ of hearing and balance: infrequently - vertigo; rarely - hyperacusia, hypoacusia, tinnitus.
On the part of the digestive system: infrequently - abdominal discomfort, dry mouth, nausea; rarely - dyspepsia, vomiting, constipation, diarrhea, epigastric pain; very rarely - stomatitis, dysphagia.
Mental disorders: rarely - sleep disorders (insomnia, increased drowsiness), anxiety; very rarely - euphoria, depression.
From the side of blood and lymphatic system: rarely - leukopenia, thrombocytopenia; very rarely - anemia, erythrocyte agglutination.
Immunological disorders: very rarely - hypersensitivity.
Metabolism and nutrition disorders: infrequently - hypercholesterolemia; rarely, decreased appetite, anorexia, diabetes.
On the part of the skin and subcutaneous tissue: rarely - hyperemia of the skin, hyperhidrosis, pruritus, urticaria, skin rash; very rarely - dermatitis.
General disorders and disorders at the injection site: rarely - asthenia, malaise, burning sensation; very rarely - chest discomfort, hypothermia.
Laboratory disorders: infrequently - decrease blood pressure; rarely - increased blood pressure, hypertriglyceridemia, ECG changes (ST depression, prolongation of the QT interval), eosinopenia, impaired liver function tests; very rarely - leukopenia, leukocytopenia, erythropenia, a decrease in thrombin time, an increase in body weight.
Contraindications
Hypersensitivity to vinpocetine or to any of the components of the drug.
Pregnancy, lactation.
Children under 18 years (due to lack of data).
Drug interactions
No interaction was observed when used simultaneously with beta-blockers (pindolol), clopamide, glibenclamide, digoxin, acenocoumarol and hydrochlorothiazide.
Methyldopa can enhance the hyponenzic effect of Vinpocetine, so with their simultaneous use requires systematic monitoring of blood pressure.
Despite the lack of data confirming the possibility of interaction, it is recommended to be cautious with the simultaneous appointment with drugs of central, antiarrhythmic and anticoagulant action.
Pregnancy and Lactation
Use during pregnancy is contraindicated and during breastfeeding is contraindicated.
Pregnancy
Vinpocetine crosses the placenta, but the concentration of vinpocetine in the placenta and fetal blood is lower than in the blood of the pregnant woman. No teratogenic and embryotoxic effect was detected. In animal studies with large doses, placental bleeding and spontaneous abortions occurred, presumably as a result of increased placental blood flow.
Breastfeeding period
According to preclinical studies with radioactively labeled Vinpocetine, the concentration in breast milk of newborn animals was 10 times higher than that in the mother’s blood.Within an hour, 0.25% of the received dose of the drug penetrates into breast milk. When deciding whether to breastfeed or refuse treatment with Vinpocetine, the benefit of breastfeeding for the child should be correlated with the benefit of Vinpocetine for the woman. When using the drug must stop breastfeeding.
Special instructions
In the presence of prolonged QT interval syndrome or simultaneous administration of drugs that cause prolongation of the QT interval, periodic ECG monitoring is required. In severe cardiac arrhythmias, increased intracranial pressure, taking antiarrhythmic drugs, prolonged QT syndrome, or the simultaneous use of drugs that cause the QT interval to lengthen, use the drug with caution.
Effect on the ability to concentrate: during the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and psychomotor reactions.
Overdosage
Cases of overdose are not registered. According to the literature, the use of 60 mg of vinpocetine per day is safe. A single oral dose of 360 mg of vinpocetine does not cause clinically significant cardiovascular and other reactions.
Symptomatic treatment.
- Active ingredient: Vinpocetine
- Capillary electrophoresis separation of vinpocetine and related compounds: Prediction of electrophoretic mobilities in partly aqueous media
- Effects of vinpocetine in scopolamine-induced learning and memory impairments
- General neuropharmacology of vinpocetine: A putative cerebral activator
- Possible memory-enhancing properties of vinpocetine
- Correlation between cerebral circulation and intellectual impairment in patients with “aging brain,” and the effect of vinpocetine on cerebral circulation
- Restoration of microsieve filterability of human red cells after exposure to hyperosmolarity and lactacidosis: Effect of vinpocetine
- Computed tomography study of cerebral infarctions treated with vinpocetine
- Placebo-controlled, double-blind, crossover study to investigate the hypoxia-protective effect of vinpocetine by psychophysiological methodology in healthy volunteers
- On the possible role of central monoaminergic systems in the central nervous system actions of vinpocetine
- Effect of vinpocetine on monoamine receptor binding and synaptosomal uptake in the rat brain
- Vinpocetine facilitates noradrenaline release in rat brain cortex slices
- Calcium antagonist activity of vinpocetine and vincamine in several models of cerebral ischaemia
- Electrophysiologic effects of vinpocetine and vincamine on isolated rabbit papillary muscle in normal- and low-potassium medium
- Effect of vinpocetine on age-related differences in brain function of aged fischer rats
- Effect of vinpocetine on the sleep-wake cycle of rats
- Comparison of the effects of vinpocetine, vincamine, and nicergoline on the normal and hypoxia-damaged learning process in spontaneously hypertensive rats
- Cognitive effects of a Ginkgo biloba/vinpocetine compound in normal adults: systematic assessment of perception, attention and memory
- Clinical evidence of the effectiveness of vinpocetine in the treatment of organic psychosyndrome
- Cyclodextrin multicomponent complexation and controlled release delivery strategies to optimize the oral bioavailability of vinpocetine
- Multidisciplinary approach on characterizing a mechanochemically activated composite of vinpocetine and crospovidone
- Kinetics and mechanisms of vinpocetine degradation in aqueous solutions
- Quantitative determination of vinpocetine in human plasma by capillary gas chromatography—mass spectrometry
- Vinpocetine inhibits the epileptic cortical activity and auditory alterations induced by pentylenetetrazole in the guinea pig in vivo
- Pharmacokinetics of vinpocetine and its metabolite, apovincaminic acid, in plasma and cerebrospinal fluid after intravenous infusion