CAVINTON COMFORT PILLS DISPERSIBLE 10MG

pharmachologic effect

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. Vinpocetine stimulates metabolism in the brain: it increases the absorption 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 the metabolism of glucose towards an energetically more favorable aerobic pathway. 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.

It improves microcirculation in the brain by inhibiting platelet aggregation, reducing pathologically increased blood viscosity, increasing red blood cell deformability and inhibiting adenosine reuptake; promotes the transition of oxygen into the cells by reducing the affinity of red blood cells.Selectively increases cerebral blood flow by reducing cerebral vascular resistance without significantly affecting systemic blood circulation parameters (BP, cardiac output, heart rate, OPSS); does not cause the "steal".

Pharmacokinetics

Suction

Vinpocetine is rapidly absorbed after ingestion and after 1 h reaches Cmax. Absorption occurs mainly in the proximal intestine. Not metabolized when passing through the intestinal wall.

Distribution

In preclinical studies of the administration of radioactively labeled Vinpocetine inside it was determined in the highest concentrations in the liver and gastrointestinal tract. Cmax in tissues observed 2-4 hours after ingestion.

The amount of radioactive isotope in the brain did not exceed that in the blood. Binding to proteins in the human body - 66%. Vd is 246.7 ± 88.5 l, which indicates a significant binding to the tissues. Bioavailability by ingestion - 7%.

With repeated ingestion in doses of 5 mg and 10 mg, the kinetics is linear; with Css plasma levels were 1.2 ± 0.27 ng / ml and 2.1 ± 0.33 ng / ml, respectively.

Metabolism and excretion

The clearance is 66.7%, which exceeds the total plasma volume of the liver (50 l / h) and indicates extrahepatic metabolism. T1/2 in humans it is 4.83 ± 1.29 hours. In studies with a radioactively labeled drug, it was found that the main ways of elimination are kidney and through the intestines in a ratio of 3: 2.In preclinical studies, the highest radioactivity was determined in bile, however, no evidence of significant enterohepatic circulation was found. Apovinkamic acid is excreted by the kidneys by simple glomerular filtration, T1/2 depends on the dose taken and the route of administration of vinpocetine. The main metabolite of vinpocetine is apovincaminic acid (AVK), whose share in humans is 25-30%. After taking Vinpocetine inside the AUC AVK is 2 times greater than that after iv administration. This suggests that AVK is formed in the process of metabolism of the first passage of Vinpocetine. Other known metabolites are hydroxyquinpocetin, hydroxy-AVK, dihydroxy-AVK-glycinate, as well as their conjugates with glucuronides and / or sulfates. In unchanged form, vinpocetine is released in a small amount.

An important and useful characteristic of Vinpocetine is the lack of the need for dose adjustment in diseases of the liver and kidneys due to the lack of cumulation due to the nature of its metabolism.

Pharmacokinetics in Special Patient Groups

Revealed that the pharmacokinetics of vinpocetine in elderly patients is not significantly different from that in young patients, the drug does not accumulate. Therefore, Vinpocetine can be prescribed to patients with impaired liver and kidney function for a long time and in usual doses.

Indications

Neurology:

- symptomatic therapy of the consequences 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 perceptual type;

- Meniere's disease;

- noise in ears.

Dosing regimen

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

The drug is prescribed inside, after eating. The daily dose of the drug is 30 mg (1 tab. 10 mg 3 times / day). The therapeutic effect develops approximately in a week from the beginning of the drug intake.

Cavinton Dispersible Tablets® Comfort can be swallowed whole with a small amount of water, in case of difficulty swallowing, the pill should be placed on the tongue for resorption. If the patient likes the orange flavor of dispersible Cavinton tablets® Comfort, they can be taken by sucking.

Atkidney and liver diseases the drug is prescribed in the usual dose.

Side effect

Side effects are rare. Data are presented by system-organ classes in accordance with the MedDRA classification and with the following frequency: infrequently (from ≥1 / 1000 to <1/100); rarely (from ≥1 / 10,000 to <1/1000); very rarely (<1/10 000).

From the blood and lymphatic system:rarely - leukopenia, thrombocytopenia; very rarely - anemia, erythrocyte agglutination.

Immune system:very rarely - hypersensitivity.

Metabolism and nutrition:infrequently, hypercholesterolemia; rarely - loss of appetite, anorexia, diabetes.

Psychological:rarely - insomnia, sleep disorders, agitation, restlessness; very rarely - euphoria, depression.

Nervous system:infrequently - headache; rarely - dizziness, taste disturbances, stupor, hemiparesis, drowsiness, amnesia; very rarely - tremor, spasms.

Special senses: rarely - swelling of the optic nerve head; very rarely - conjunctival hyperemia.

From the organ of hearing and the labyrinth:infrequently - vertigo; rarely - hyperacusia, hypoacusia, tinnitus.

From the side of the heart:rarely, ischemia / myocardial infarction, angina pectoris, bradycardia, tachycardia, extrasystoles, palpitations; very rarely - arrhythmia, atrial fibrillation.

From the side of the vessels:infrequently - arterial hypotension; rarely - arterial hypertension, "hot flashes", thrombophlebitis; very rarely - fluctuations in blood pressure.

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

Dermatological:rarely - erythema, increased sweating, itching, urticaria, rash; very rarely - dermatitis.

Other:rarely - asthenia, fatigue, feeling hot; very rarely - chest discomfort, hypothermia.

Impact on the results of laboratory and instrumental studies:infrequently - decrease in blood pressure, rarely - increase in blood pressure, increase in serum triglyceride concentration, depression of ST segment on ECG, decrease / increase in the number of eosinophils, changes in liver enzyme activity; very rarely - an increase / decrease in the number of leukocytes, a decrease in the number of red blood cells, a reduction in thrombin time, an increase in body weight.

Contraindications

- hypersensitivity to vinpocetine and other components of the drug;

- acute phase of hemorrhagic stroke;

- severe form of coronary artery disease;

- severe arrhythmias;

- phenylketonuria;

- pregnancy;

- lactation period (breastfeeding);

- children and adolescents up to 18 years (due to insufficient data).

Use during pregnancy and lactation

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 the pregnant woman. At high doses, placental bleeding and spontaneous abortions are possible, probably as a result of increased placental blood supply.

Within an hour, 0.25% of the received dose of the drug penetrates into breast milk. When using the drug must stop breastfeeding.

Application for violations of the liver

In case of liver diseases, the drug is prescribed in the usual dose.

Application for violations of kidney function

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

Use in children

Contraindicated in children and adolescents under the age of 18 years (due to lack of data).

special instructions

The presence of a syndrome of prolonged QT interval and taking drugs that cause lengthening of the QT interval, require periodic monitoring of the ECG.

In the dispersible pill Cavinton® Comfort 10 mg contains 1.28 mg of aspartame, a source of phenylalanine, so the drug is contraindicated in patients with phenylketonuria.

Influence on ability to drive vehicles and mechanisms

Studies on the effect on the ability to drive vehicles were not conducted. At occurrence of undesirable reactions from the nervous system, care should be taken when driving and working with mechanisms.

Overdose

Currently, data on overdose of vinpocetine is limited.

Treatment: gastric lavage, reception of Activated carbon, symptomatic treatment.

Drug interaction

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

The simultaneous use of vinpocetine and methyldopa sometimes caused some enhancement of the hypotensive effect, therefore, such treatment requires regular blood pressure control.

Despite the lack of data confirming the possibility of interaction, it is recommended that caution be exercised while appointing Cavinton®Comfort with drugs central, antiarrhythmic and anticoagulant action.

Terms and conditions of storage

The drug should be stored out of the reach of children, protected from light at a temperature not higher than 30 ° C. Shelf life - 2 years.

Pharmacy sales terms

The drug is available on prescription.