Vinpocetine pills 10mg №30

Dosage Form

Pills

Composition:

1 pill 10 mg contains:

Active substance: Vinpocetine - 10.00 mg.

Excipients: microcrystalline cellulose - 178.00 mg; pregelatinized corn starch - 60.00 mg; colloidal silicon dioxide - 0.60 mg; Magnesium stearate - 1.40 mg.

Description

10 mg tablets

Tablets are round, biconvex in shape, from white to white with a yellowish tinge, with a risk on one side.

Pharmacotherapeutic group

Psychogogic and nootropic agent.

Pharmacological properties

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

The neuroprotective effect is realized by reducing the adverse cytotoxic effect of excitatory amino acids. Blocks Na⁺- and Sa²⁺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 due to inhibition of platelet aggregation, reduction of pathologically increased blood viscosity,increased red blood cell deformability and inhibition of adenosine reuptake; promotes the transition of oxygen into the cells by reducing the affinity for it of red blood cells.

Selectively increases cerebral blood flow by reducing cerebral vascular resistance without significantly affecting systemic blood circulation parameters (arterial pressure (BP), cardiac output, heart rate, total peripheral vascular resistance); does not cause the "steal".

Suction

After ingestion is rapidly absorbed from the gastrointestinal tract. The time to reach the maximum concentration (TC_max) in the blood plasma for 1 hour. Absorption occurs mainly in the proximal gastrointestinal tract. When passing through the intestinal wall is not metabolized.

Distribution

Upon oral administration of radioactively labeled Vinpocetine to rats, the highest concentration was found in the liver and the gastrointestinal tract. The maximum tissue concentration was observed 2-4 hours after administration. Radioactivity in the brain did not exceed the values ​​found in the blood.

In humans, the relationship with plasma proteins is 66%, bioavailability when taken orally - 7%. The volume of distribution is 246.7-88.5 l, which indicates a high binding to the tissues. The 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 apovinkinat (ABA), constituting
25-30% of the original compound. The area under the curve “concentration - time” of ABA after oral administration is twice as high as intravenous administration of vinpocetine. Thus, Vinpocetine is subject to a pronounced effect of “primary passage” through the liver. Other metabolites include: hydroxyquinpocetin, hydroxy-ABA, ABA-dioxyglycinate and their conjugates (sulfates and 9 or) glucuronides). In case of impaired liver or kidney function, dose adjustment is not required since Vinpocetine does not accumulate.

Removal

Removal of unchanged vinpocetine is low (a few percent). With multiple administrations 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. Half-life in humans
4.8 ± 1.29 h. It is excreted by the kidneys and through the intestines in the ratio 60:40. In rats and dogs, high radioactivity with the introduction of radioactively labeled Vinpocetine is found in the bile, however, significant enterohepatic recycling has been noted.

Special patient groups

Since Vinpocetine is primarily intended for the treatment of the elderly, it is necessary to take into account a decrease in absorption and distribution, as well as elimination in this age group, especially with prolonged use. However, according to the results of clinical studies, it was established that the kinetics of vinpocetine in the elderly is not significantly different from the young, cumulation does not occur.In case of impaired liver function and kidney accumulation is not observed, which allows for long-term therapy. Vinpocetine crosses the placenta and is secreted into breast milk.

Indications for use

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

Ophthalmology: chronic vascular diseases of the retina and choroid.

Otology: hearing loss of the perceptual type, Meniere's disease, tinnitus.

To avoid complications, apply strictly as prescribed by a doctor.

Contraindications

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

Pregnancy, lactation.

Children under 18 years (due to lack of data).

Use during 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. Teratogenic and embryotoxic action was not 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 benefits of breastfeeding for the child should be correlated with the benefit of Vinpocetine for the woman. When using the drug must stop breastfeeding.

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.

Side effect

The following classification is used to determine the incidence of side effects of the drug:

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 the 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.

On the part of 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 disturbance (insomnia, increased sleepiness), anxiety; very rarely - euphoria, depression.

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.

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 site of administration: rarely - asthenia, malaise, burning sensation; very rarely - chest discomfort, hypothermia.

Laboratory disorders: infrequently - decrease in 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.

Overdose

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.

Interaction with other drugs

No interaction was observed with simultaneous use with beta-blockers (pindolol), clopamide, glibenclamide, Digoxin, acenocoumarol and hydrochlorothiazide.

Methyldopa can enhance the hyponenzic effect of Vinpocetine, therefore, with their simultaneous use, systematic control of blood pressure is required.

Despite the lack of data confirming the possibility of interaction, it is recommended to be cautious with the simultaneous appointment with drugs of central, anti-arrhythmic and anticoagulant action.

special instructions

In the presence of prolonged QT 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.

Effects on attention span: 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.

Storage conditions

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.