Cavinton Comfort - instructions for use, dose, side effects, contraindications

Excipients: mainitol 75.60 mg, corn starch, pregelatinized starch 38.00 mg, butyl methacrylate copolymer 9.00 mg, low-substituted giprolose 8.00 mg, crospovidone 8.00 mg, magnesium stearate 2.85 mg, sodium stearyl fumarate 2.80 mg, silicon dioxide colloid 1 , 60 mg, aspartame 1.28 mg, stearic acid 1.26 mg, sodium lauryl sulfate 0.90 mg, dimethicone 0.39 mg, orange flavoring 0.32 mg.

Description:

White or almost white, round, biconvex tablets, engraved with "N83" on one side.

Pharmacotherapeutic group:Psychostimulating and nootropic remedy

ATX: & nbsp

N.06.B.X.18 Vinpocetine

Pharmacodynamics:

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 the blood.

The neuroprotective effect is realized by reducing the unfavorable cytotoxic effect of excitatory amino acids. Blocks Na⁺ and Ca²⁺ channels and NMDA- and AMPA receptors. Vinpocetine stimulates the metabolism in the brain: it increases the uptake and consumption of glucose and oxygen. Increases tolerance to hypoxia; increases the transport of glucose, the only energy source for brain tissue, through the blood-brain barrier; shifts the metabolism of glucose towards the energetically more advantageous aerobic pathway. Selectively inhibits Ca²⁺- calmodulin-dependent cGMP phosphodiesterase. Increases the metabolism of serotenin and norepinephrine in the brain, stimulates the noradrenergic neuromednagornaya system and has an antioxidant effect.

Improves microcirculation in the brain due to inhibition of platelet aggregation, a decrease in the pathologically increased viscosity of the blood,increased erythrocyte deformability and inhibition of adenosine reuptake; promotes the transition of oxygen into cells by reducing the affinity of erythrocytes. Selectively increases cerebral blood flow by decreasing cerebral vascular resistance without significantly affecting systemic blood circulation parameters (blood pressure (BP), cardiac output, heart rate, total peripheral vascular resistance); does not cause the effect of "stealing".

Pharmacokinetics:

Vinpocetine is rapidly absorbed after ingestion and after 1 hour reaches the maximum concentration in the blood (Cmax). Absorption occurs mainly in the proximal parts of the intestine. It is not metabolized when passing through the intestinal steak.

In preclinical studies of the introduction of radioactively labeled vinpocetine, he was determined by mouth in the highest concentrations in the liver and gastrointestinal tract. The maximum concentration in the tissues is noted 2-4 hours after ingestion.

The amount of radioactive isotope in the brain did not exceed that in the blood. The connection with proteins in the human body is 66%.The volume of distribution is 246.7 ± 88.5 l, which indicates a significant binding to tissues. Bioavailability with ingestion - 7%. The clearance is 66.7%, which exceeds the total plasma volume of the liver (50 l / h) and indicates extrahepatic metabolism.

With multiple doses of 5 mg and 10 mg taken internally, the kinetics is linear; while the equilibrium concentrations in the blood plasma were 1.2 ± 0.27 ng / ml and 2.1 ± 0.33 ng / ml, respectively. The half-life in humans is 4.83 ± 1.29 hours. In studies with a radiolabeled drug, it was found that the main ways of elimination are kidney and intestinal excretion in a 3: 2 ratio. In pre-clinical studies, the highest radioactivity was determined in bile, but no evidence of significant enteric-hepatic circulation was found. Apovincaminic acid is excreted by the kidneys by simple glomerular filtration, the half-life period depends on the dose taken and the route of administration of vinpocetine.

The main metabolite of vinpocetine is apovincamine acid (AVK), whose proportion in humans is 25-30%. After taking vinpocetine, the area under the concentration-time curve of AVK is 2 times greater than that after intravenous administration.This indicates that AVK is formed in the process of metabolism of the first passage of vinpocetine. Other known metabolites are hydroxyvinpocetine, hydroxy-AVK, dihydroxy-AVK-glycinate, as well as their conjugates with glucuronides and / or sulfates. Unchanged vinpocetine is released in small quantities.

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

Pharmacokinetics in special groups of patients (age, concomitant diseases): It was found that the pharmacokinetics of vinpocetine in elderly patients does not significantly differ from that in young patients, cumulation of the drug is absent. therefore vinpocetine can be prescribed to patients with impaired liver and kidney function for a long time and at regular doses.

Indications:

Neurology: symptomatic therapy of the consequences of ischemic stroke, vascular vertebrobasillar insufficiency, vascular dementia, atherosclerosis of cerebral vessels, posttraumatic, hypertensive encephalopathy.

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

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

Contraindications:

Known hypersensitivity to vinpocetine and other components of the drug. Acute phase of hemorrhagic stroke, severe form of coronary heart disease, or severe arrhythmias. Phenylketonuria. Pregnancy and lactation. Children and adolescents under 18 years (due to insufficient data).

Pregnancy and lactation:

Vinpocetine penetrates the placental barrier and is therefore contraindicated in pregnancy. At the same time, its concentration in the placenta and in the fetal blood is lower than in the pregnant woman's blood. At high doses, placental bleeding and spontaneous abortion are possible, probably as a result of increased placental blood supply.

Breastfeeding period: within one hour, 0.25% of the accepted dose of the drug penetrates into breast milk. When using the drug, it is necessary to stop breastfeeding.

Dosing and Administration:

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

The drug is administered orally after eating.The daily dose of the drug is 30 mg (one tablet 10 mg 3 times a day). The therapeutic effect develops about a week after the start of the drug.

Cavinton Comfort, dispersible tablets, 10 mg can be swallowed whole with a small amount of water, with difficulty swallowing the tablet should be placed on the tongue for resorption. If the patient is satisfied with the orange flavor of Cavinton ® Comfort tablets are dispersible, then they can be taken by dissolving.

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

Side effects:

Side effects are quite rare. The data are presented according to the system-organ classes according to the MedDRA classification and with the following frequency: infrequently (from ≥ 1/1 000 to <1/100); rarely (from ≥1 / 10,000 to <1/1 000); very rarely (<1/10 000).

Violations of the blood and lymphatic system

Rarely: leukopenia, thrombocytopenia.

Very rarely: anemia, agglutination of erythrocytes.

Immune system disorders

Very rarely: hypersensitivity.

Disorders from the metabolism and nutrition

Infrequently: hypercholesterolemia.

Rarely: decreased appetite, anorexia, diabetes mellitus.

Disorders of the psyche

Rarely: insomnia, sleep disturbances. excitement, restlessness.

Very rarely: euphoria, depression.

Impaired nervous system:

Infrequently: a headache.

Rarely: dizziness, taste disorders, stupor, hemiparesis, drowsiness, amnesia.

Very rarely: tremor, spasms.

Disturbances on the part of the organ of sight

Rarely: edema of the optic disc.

Very rarely: conjunctival hyperemia.

Violations from the organ of hearing and labyrinth

Infrequently: vertigo.

Rarely: hyperacusis, hypoacusia, ringing in the ears.

Heart Disease

Rarely: ischemia / myocardial infarction, angina, bradycardia, tachycardia, extrasystoles, palpitation.

Very rarely: arrhythmia, atrial fibrillation.

Vascular disorders

Infrequent: arterial hypotension.

Rarely: arterial hypertension, "hot flashes", thrombophlebitis.

Very rarely: fluctuations in blood pressure.

Disorders from the gastrointestinal tract:

Uncommon: discomfort in the abdomen, dry mouth, nausea.

Rarely: abdominal pain, constipation, diarrhea, indigestion, vomiting.

Very rarely: dysphagia, stomatitis.

Disturbances from the skin and subcutaneous tissues:

Rarely: erythema, excessive sweating, pruritus, urticaria, rash.

Very rarely: dermatitis.

General disorders and disorders at the site of administration

Rarely: asthenia, fatigue, a feeling of heat.

Very rarely: chest discomfort, hypothermia.

Impact on the results of laboratory and instrumental studies

Infrequent: lowering blood pressure.

Rarely: increased blood pressure, increased concentration of triglycerides in the blood serum, depression of the ST segment on the electrocardiogram, decrease / increase in the number of eosinophils, changes in the activity of "hepatic" enzymes.

Rarely: increase / decrease in the number of white blood cells, a decrease in the number of red blood cells, a reduction in thrombin time, an increase in body weight.

Overdose:

Currently, data on the overdose of vinpocetine are limited.

Treatment: gastric lavage, reception of activated charcoal, symptomatic treatment.

Interaction:

Interactions are not observed with simultaneous use with beta-blockers (chloranolol, pindolol), clopamid, glibenclamide, digoxin, acenocoumarol, hydrochlorothiazide and imipramine.

The simultaneous use of vinpocetine and methyldopa sometimes caused some strengthening of the hypotensive effect, so this treatment requires regular monitoring of blood pressure.

Despite the lack of data confirming the possibility of interaction, it is advisable to be cautious in the simultaneous administration of Cavinton® Comfort, tablets dispersible, 10 mg with preparations of central antiarrhythmic and anticoagulant action.

Special instructions:

The presence of the syndrome of the lengthened interval QT and taking medications that elongate the interval QT, require periodic ECG monitoring.

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

Effect on the ability to drive transp. cf. and fur:

Studies on the impact on the ability to drive vehicles were not conducted. If there are undesirable reactions from the nervous system, care should be taken when driving vehicles and working with mechanisms.

Form release / dosage:

Tablets are dispersible 10 mg.

Packaging:

For 15 tablets in a blister of PVC - aluminum foil.

For 2 or 6 blisters are placed in a cardboard box together with instructions for use.

Storage conditions:

In the dark place at a temperature of no higher than 30 ° C.Inaccessible to children!

Shelf life:

2 years.

Do not use the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002864

Date of registration:19.02.2015 / 01.12.2015

Expiration Date:19.02.2020

The owner of the registration certificate:GEDEON RICHTER, OJSC GEDEON RICHTER, OJSC Hungary

Manufacturer: & nbsp

GEDEON RICHTER OJSC Hungary

GEDEON RICHTER-RUS, CJSC Russia

Representation: & nbspGEDEON RICHTER OJSC GEDEON RICHTER OJSC Hungary

Information update date: & nbsp27.11.2017

Illustrated instructions

Instructions

Cavinton Comfort (CAVINTON® COMFORTE)