Vinpocetine pills 5mg 50pcs

Composition

Active ingredient:

vinpocetine – 5.00 mg.

Auxiliary substances:

microcrystalline cellulose – 89.00 mg;

pregelatinized corn starch-30.00 mg;

colloidal silicon dioxide-0.30 mg;

magnesium stearate-0.70 mg

Pharmacological action

The mechanism of action of vinpocetine consists of several elements: it improves cerebral blood flow and metabolism, and has a beneficial effect on the rheological properties of blood.

Neuroprotective effect is realized by reducing the adverse cytotoxic effect of excitatory amino acids. Blocks Na+ and Ca2+channels and NMDA and AMPA receptors. Selectively inhibits Ca2+ – calmodulin-dependent-cGMP-phosphodiesterase. Increases the metabolism of serotonin and norepinephrine in the brain, stimulates the noradrenergic neurotransmitter system and has an antioxidant effect.

Improves microcirculation in the brain by inhibiting platelet aggregation, reducing pathologically increased blood viscosity, increasing red blood cell deformability and inhibiting adenosine reuptake; promotes oxygen transfer to cells by reducing the affinity of red blood cells for it.

Selectively increases cerebral blood flow by reducing cerebral vascular resistance without significantly affecting systemic circulatory parameters (blood pressure (BP), cardiac output, heart rate, total peripheral vascular resistance); does not cause the effect of “stealing”.

Indications

Neurology: symptomatic treatment of the consequences of ischemic stroke, vascular vertebrobasilar insufficiency, vascular dementia, cerebral vascular atherosclerosis, post-traumatic, hypertensive encephalopathy.

Ophthalmology: chronic vascular diseases of the retina and choroid of the eye.

Otology: perceptual hearing loss, Meniere’s disease, tinnitus.

To avoid complications, use strictly as prescribed by your doctor.

Contraindications

Hypersensitivity to vinpocetine or to any of the components of the drug.

Pregnancy and lactation.

Children under 18 years of age (due to insufficient data).

Side effects

To determine the frequency of side effects of the drug, the following classification is used: :

Very often (≥ 1/10)

Often (≥ 1/100 and < 1/10)

Infrequently (≥ 1/1000 and

Rarely (≥ 1/10,000 and

Very rare (≥ 1/10,000).

From the heart: rarely-ischemia/myocardial infarction, bradycardia, angina, tachycardia, extrasystole, palpitation sensation; very rarely-arrhythmia, atrial fibrillation.

Vascular disorders: infrequently-decreased blood pressure; rarely-increased blood pressure, hot flashes, thrombophlebitis; very rarely-unstable blood pressure.

From the central nervous system: infrequently-headache; rarely-dysgeusia, stupor, hemiparesis, drowsiness, amnesia; very rarely-tremor, spasms.

From the side of the organ of vision: rarely-edema of the optic nerve disc; very rarely-conjunctival hyperemia.

From the side of the organ of hearing and balance: infrequently-vertigo; rarely-hyperacusis, hypoacusia, tinnitus.

From 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.

Blood and lymphatic system disorders:  rarely-leukopenia, thrombocytopenia; very rarely-anemia, agglutination of red blood cells.

Immunological disorders: very rarely – hypersensitivity.

Metabolic and nutritional disorders: infrequently-hypercholesterolemia; rarely-decreased appetite, anorexia, diabetes mellitus.

From 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 violations:   infrequently-decreased blood pressure; rarely-increased blood pressure hypertriglyceridemia, ECG changes (ST depression, QT interval prolongation), eosinopenia, impaired liver function tests; very rarely-leukopenia, leukocytopenia, erythropenia, decreased thrombin time, increased body weight.

Interaction

Interactions are not observed when used concomitantly with beta-blockers (pindolol), clopamide, glibenclamide, digoxin, acenocoumarol and hydrochlorothiazide.

Methyldopa may increase the hypontensive effect of vinpocetine, so when they are used simultaneously, systematic blood pressure monitoring is required.

Despite the lack of data confirming the possibility of interaction, it is recommended to exercise caution when prescribing concomitantly with drugs of central, antiarrhythmic and anticoagulant action.

How to take, course of use and dosage

Inside, after eating.

The course of treatment and dose is determined by the attending physician.

Usually, the daily dose is 15-30 mg (5-10 mg 3 times a day).

The initial daily dose is 15 mg. The maximum daily dose is 30 mg.

No dose adjustment is required for the elderly, with impaired liver or kidney function.

Overdose

No overdose cases have been reported. According to the literature, the use of 60 mg of vinpocetine per day is safe. A single oral dose of vinpocetine 360 mg does not cause clinically significant cardiovascular and other reactions.

Treatment is symptomatic.

Description

Tablets are round, biconvex in shape, from white to white with a yellowish tinge of color.

Functional features

Suction

After oral use, it is rapidly absorbed from the gastrointestinal tract. Time to reach the maximum concentration (TMAX) in blood plasma is 1 h. Absorption occurs mainly in the proximal parts of the gastrointestinal tract. When passing through the intestinal wall, it is not metabolized.

Distribution

When radiolabeled vinpocetine was administered orally to rats, the highest concentrations were found in the liver and gastrointestinal tract. The maximum concentration in the tissues was observed 2-4 hours after use. Radioactivity in the brain did not exceed the values found in the blood.

In humans, plasma protein binding is 66%, and oral bioavailability is 7%. The volume of distribution is 246.7-88.5 liters, which indicates a high binding to tissues. Total clearance (66.7 l/h) exceeds the rate of hepatic blood flow (50 l / h), which indicates extrahepatic metabolism.

Metabolism

The main metabolite is apovincaminate (ABA), which makes up 25-30% of the initial compound. The area under the concentration – time curve of ABA after oral use is twice that of intravenous vinpocetine. Thus, vinpocetine is subject to a pronounced effect of “primary passage” through the liver. Other metabolites include: hydroxyvinpocetine, hydroxy-ABA, ABA-dioxyglycinate and their conjugates (sulfates and (or) glucuronides). If liver or kidney function is impaired, no dose adjustment is required because vinpocetine does not accumulate.

Deduction

The elimination of unchanged vinpocetine is low (several percent). When administered multiple times in doses of 5 mg and 10 mg, the kinetics is linear, the equilibrium plasma concentration is 1.2±0.27 and 2.1±0.33 ng / ml, respectively. The human half-life is 4.8±1.29 hours. It is excreted by the kidneys and through the intestines in a ratio of 60: 40. In rats and dogs, high radioactivity is detected in the bile when radiolabeled vinpocetine is administered, but significant enterohepatic recirculation is noted.

Special patient groups

Since vinpocetine is primarily intended for the treatment of the elderly, it is necessary to take into account the decrease in absorption and distribution, as well as elimination in this age group, especially with prolonged use. However, based on the results of clinical studies, it was found that the kinetics of vinpocetine in the elderly does not significantly differ from the young, and accumulation does not occur. In cases of impaired liver and kidney function, accumulation is not noted, which allows for long-term therapy. Vinpocetine passes through the placenta and is released into breast milk.

Special instructions

In the presence of prolonged QT syndrome or concomitant use of drugs that cause prolongation of the QT interval, periodic ECG monitoring is required. In case of severe cardiac arrhythmias, increased intracranial pressure, taking antiarrhythmic drugs, prolonged QT syndrome, or concomitant use of drugs that cause prolongation of the QT interval, the drug should be used with caution.

Influence on the ability to concentrate attention:  during the treatment period, care should be taken when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Storage conditions

Keep out of the reach of children in a dark place, at a temperature not exceeding 25 °C.

Shelf

life is 3 years.

Active ingredient

Vinpocetine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults

Indications

Vegetative-vascular disorders, Cerebral circulation disorders, Meniere’s disease, Atherosclerosis, Stroke consequences