Cavinton tablets 5mg, no. 50

Neurology:

• a decrease in the severity of neurological and mental disorders in various forms of cerebral circulatory insufficiency (symptomatic therapy of the consequences of ischemic stroke, vertebrobasilar insufficiency, vascular dementia, cerebral atherosclerosis, post-traumatic and hypertensive encephalopathy);

Ophthalmology:

• chronic vascular diseases of the retina and choroid;

Otorhinolaryngology:

• for the treatment of hearing loss of the perceptual type, Meniere's disease, tinnitus.

It is taken orally, after meals.

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

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

In diseases of the kidneys and liver, the drug is prescribed in the usual dose, the absence of cumulation allows for long courses of treatment.

Vinpocetine - 5 mg

• galactose intolerance, lactase deficiency, glucose-galactose malabsorption;

• pregnancy;

• breastfeeding period;

• age under 18 (due to insufficient data);

• hypersensitivity to vinpocetine or other components of the drug.

With caution: long QT interval syndrome, taking drugs that cause QT interval lengthening.

Clinical and pharmacological group: A drug that improves blood circulation and brain metabolism

Pharmaco-therapeutic group: Psychostimulating and nootropic agent

pharmachologic effect

The mechanism of action of vinpocetine consists of several elements: it improves cerebral blood flow and brain 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 voltage-gated Na + and Ca2 + channels and NMDA- and AMPA-receptors. Increases the neuroprotective effect of adenosine. Vinpocetine stimulates brain metabolism: increases the uptake and consumption of glucose and oxygen. Increases tolerance to hypoxia; increases the transport of glucose, the only source of energy for brain tissue, through the BBB; shifts glucose metabolism towards an energetically more beneficial aerobic pathway. Selectively inhibits Ca2 + -calmodulin-dependent cGMP-phosphodiesterase; increases the content of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) of the brain, the concentration of ATP and the ratio of ATP / AMP in the tissues of the brain;enhances the exchange of serotonin and norepinephrine in the brain, stimulates the noradrenergic neurotransmitter system, and also has an antioxidant effect; as a result of all these effects, vinpocetine has a cerebroprotective effect.

Improves microcirculation in the brain by inhibiting platelet aggregation, reducing pathologically increased blood viscosity, increasing the ability of erythrocytes to deform and inhibiting the capture of adenosine; promotes the transfer of oxygen into cells by reducing the affinity of erythrocytes to it. Selectively increases cerebral blood flow by increasing the cerebral fraction of cardiac output, reducing cerebral vascular resistance without significantly affecting the systemic indicators of blood circulation (blood pressure, cardiac output, heart rate, systemic vascular resistance); has no 'steal' effect. Against the background of the use of vinpocetine, the blood supply to the damaged (but not yet necrotic) areas of ischemia with low perfusion improves ('the opposite stealing effect').

Pharmacokinetics

Suction

Vinpocetine is rapidly absorbed after oral administration and after 1 hour reaches Cmax in the blood. Absorption occurs mainly in the proximal intestine. Does not undergo metabolism when passing through the intestinal wall. Oral bioavailability is 7%.

Distribution

In preclinical studies of the introduction of radioactively labeled vinpocetine inside, it was determined in the highest concentrations in the liver and gastrointestinal tract. Cmax in tissues is noted 2-4 hours after ingestion. The amount of the radioactive isotope in the brain did not exceed that in the blood. Protein binding in the human body - 66%. Vd is 246.7 ± 88.5 L, which indicates a significant tissue distribution. The clearance is 66.7%, which exceeds the plasma volume of the liver (50 l / h), the metabolism is predominantly extrahepatic.

With multiple doses of 5 and 10 mg, the kinetics of vinpocetine is linear. Css were 1.2 ± 0.27 ng / ml and 2.1 ± 0.33 ng / ml, respectively.

Metabolism

The main metabolite of vinpocetine is apovincaminic acid (AVA), the proportion of which in humans is 25-30%. After taking vinpocetine inside, the AUC of AVK is 2 times higher than that after intravenous administration. This indicates that VKA is formed during the metabolism during the 'first pass' of vinpocetine. Other known metabolites are hydroxyvinpocetin, hydroxy-AVK, dihydroxy-AVK-glycinate, and their conjugates with glucuronides and / or sulfates.

Withdrawal

T1 / 2 in humans - 4.83 ± 1.29 hours. In studies with a radioactive label, the drug was excreted by the kidneys and through the intestines in a ratio of 60:40. In preclinical studies, a significant part of the radioactivity was detected in bile, but no significant intestinal-hepatic circulation was found. In preclinical studies, it was revealed that unchanged vinpocetine is excreted in a small amount. Apovincaminic acid is excreted by the kidneys by simple glomerular filtration, T1 / 2 depends on the dose taken and the route of administration of vinpocetine.

Pharmacokinetics in selected patient groups

It was revealed that the pharmacokinetics of vinpocetine in elderly patients does not differ significantly from that in young patients, there is no accumulation of the drug. Therefore, vinpocetine can be prescribed to patients with impaired liver and kidney function for a long time and in normal doses.

Indications

Neurology:

• a decrease in the severity of neurological and mental disorders in various forms of cerebral circulatory insufficiency (symptomatic therapy of the consequences of ischemic stroke, vertebrobasilar insufficiency, vascular dementia, cerebral atherosclerosis, post-traumatic and hypertensive encephalopathy);

Ophthalmology:

• chronic vascular diseases of the retina and choroid;

Otorhinolaryngology:

• for the treatment of hearing loss of the perceptual type, Meniere's disease, tinnitus.

Dosage regimen

It is taken orally, after meals.

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

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

In diseases of the kidneys and liver, the drug is prescribed in the usual dose, the absence of cumulation allows for long courses of treatment.

Side effect

In clinical studies, the most common adverse reactions occurred in the following system-organ classes (according to the MedDRA classification), which are given in accordance with the frequency of occurrence: infrequently (from? 1/1000 to <1/100), rarely (from? 1/10 000 to <1/1000); very rare (<1/10 000).

From the hematopoietic system: rarely - leukopenia, thrombocytopenia; very rarely - anemia, erythrocyte agglutination.

From the immune system: very rarely - hypersensitivity reactions.

From the side of metabolism and nutrition: infrequently - hypercholesterolemia; rarely - decreased appetite, anorexia, diabetes mellitus.

Mental disorders: rarely - insomnia, sleep disturbances, anxiety; very rarely - euphoria, depression.

From the nervous system: infrequently - headache; rarely - dizziness, taste disorder, stupor, unilateral paresis, drowsiness, amnesia; very rarely - tremor, spasms.

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

On the part of the organ of hearing and labyrinth disorders: infrequently - vertigo; rarely - hyperacusis, hypoacusia, tinnitus.

From the side of the cardiovascular system: infrequently - lowering blood pressure; rarely - ischemia / myocardial infarction, angina pectoris, bradycardia, tachycardia, extrasystole, palpitations, increased blood pressure, hot flashes, thrombophlebitis; very rarely - blood pressure lability, arrhythmia, atrial fibrillation.

From the digestive system: infrequently - abdominal discomfort, dry mouth, nausea; rarely - epigastric pain, constipation, diarrhea, dyspepsia, vomiting; very rarely - dysphagia, stomatitis.

Skin and subcutaneous tissue disorders: rarely - erythema, hyperhidrosis, pruritus, urticaria, rash; very rarely - dermatitis.

General disorders and disorders at the injection site: rarely - asthenia, malaise, fever; very rarely - a feeling of discomfort in the chest, hypothermia.

Laboratory and instrumental data: rarely - hypertriglyceridemia, depression of the ST segment on the ECG, a decrease / increase in the number of eosinophils, an increase in the activity of hepatic enzymes; very rarely - a decrease / increase in the number of leukocytes, erythropenia, a decrease in thrombin time, an increase in body weight.

Contraindications for use

• galactose intolerance, lactase deficiency, glucose-galactose malabsorption;

• pregnancy;

• breastfeeding period;

• age under 18 (due to insufficient data);

• hypersensitivity to vinpocetine or other components of the drug.

With caution: long QT interval syndrome, taking drugs that cause QT interval lengthening.

Application during pregnancy and lactation

Pregnancy

Vinpocetine crosses the placental barrier and is therefore contraindicated in pregnancy. Moreover, its concentration in the placenta and in the blood of the fetus is lower than in the blood of a pregnant woman. Teratogenic and embryotoxic effects have not been identified. In animal studies, when high doses were administered, placental bleeding and spontaneous abortions occurred, probably as a result of increased placental blood flow.

Breastfeeding period

Vinpocetine passes into breast milk. In studies using labeled vinpocetine, the radioactivity in breast milk was ten times higher than in the mother's blood. Within 1 hour, 0.25% of the taken dose of the drug penetrates into breast milk. Since vinpocetine passes into breast milk, and there is no data on the effect of vinpocetine on infants, the use of the drug during breastfeeding is contraindicated.

Application for violations of liver function

For liver diseases, the drug is prescribed in the usual dose.

Application for impaired renal function

For kidney disease, the drug is prescribed in the usual dose.

Application in children

The use is contraindicated under the age of 18 years (due to insufficient data).

special instructions

The presence of prolonged QT interval syndrome and the use of drugs that cause prolongation of the QT interval require periodic monitoring of the ECG.

1 tablet of CavintonЃ contains 140 mg of lactose monohydrate. Patients with rare hereditary diseases such as galactose intolerance, lactase deficiency or glucose-galactose malabsorption should not take this drug.

Influence on the ability to drive vehicles and mechanisms

There are no data on the effect of vinpocetine on the ability to drive vehicles and work with mechanisms.

Overdose

There are no data on overdose with vinpocetine. A single dose of 360 mg of vinpocetine did not cause clinically significant reactions, incl. on the part of the cardiovascular system.

Treatment: gastric lavage, intake of activated charcoal, symptomatic therapy.

Drug interactions

Interaction is not observed with simultaneous use with beta-blockers (chloranolol, pindolol), clopamide, glibenclamide, digoxin, acenocoumarol, hydrochlorothiazide and imipramine.

The simultaneous use of vinpocetine and alpha-methyldopa sometimes caused some increase in the hypotensive effect, therefore, with such treatment, regular monitoring of blood pressure is required.

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

Storage conditions

The drug should be stored in its original packaging to protect from light, out of the reach of children at a temperature not exceeding 30 ? C.

Shelf life

The shelf life is 5 years. Do not use after the expiration date printed on the package.

Terms of sale

The drug is available with a prescription.