Cavinton Comforte, 10 mg, dispersible tablets, 90 pcs.

Cavinton Comforte, 90 pcs., 10 mg, dispersible tablets

Vinpocetine is rapidly absorbed after oral administration and reaches its maximum blood concentration (Cmax) within 1 hour. Absorption occurs mainly in the proximal intestine. It is not metabolized when passing through the intestinal wall.

In preclinical studies of oral administration of radiolabeled vinpocetine, it was detected in the highest concentrations in the liver and gastrointestinal tract. The maximum concentration in tissues is observed 2–4 hours after oral administration.

The amount of radioactive isotope in the brain did not exceed that in the blood. Connection with proteins in the human body - 66%. The volume of distribution is 246.7 ± 88.5 l, indicating significant tissue binding. Bioavailability when taken orally - 7%. Clearance is 66.7%, which exceeds the total plasma volume of the liver (50 l/h) and indicates extrahepatic metabolism.

With repeated oral doses of 5 mg and 10 mg, the kinetics are linear; while the equilibrium concentrations in 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 radioactively labeled drug, it was found that the main routes of elimination are excretion through the kidneys and through the intestines in a ratio of 3:2. In preclinical studies, the greatest radioactivity was detected in bile, but no evidence of significant enterohepatic circulation was found. Apovinamic acid is excreted by the kidneys by simple glomerular filtration; the half-life depends on the dose taken and the route of administration of vinpocetine.

The main metabolite of vinpocetine is apovincamic acid (AVA), the proportion of which in humans is 25–30%. After oral administration of vinpocetine, the area under the concentration-time curve of VKA is 2 times greater than that after intravenous administration. This indicates that VKA is formed during the first pass metabolism of vinpocetine. Other known metabolites are hydroxyvinpocetine, hydroxy-AVA, dihydroxy-AVA-glycinate, and their conjugates with glucuronides and/or sulfates. Vinpocetine is excreted unchanged 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 peculiarities of its metabolism.

Pharmacokinetics in special groups of patients (age, concomitant diseases):

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.

Pharmacological features

According to the instructions for use for Cavinton Comforte, the features of the active substance are as follows: it improves cerebral blood flow and improves material metabolism, and also has a positive effect on the rheological characteristics of the blood. Its neuroprotective effect is realized by reducing the cytotoxic adverse effects of excitatory amino acids. Selectively inhibits Ca2+-calmodulin-dependent cGMP phosphodiesterase. Thanks to vinpocetine, Ca+ and Na+ channels, AMPA and NMDA receptors are blocked.

The main characteristics of the substance:

• increased metabolism of serotonin and norepinephrine in the brain of the head, which stimulates the neurotransmitter noradrenergic system and has an antioxidant effect;
• stimulation of metabolic processes in the brain, which is reflected in the form of increased consumption and uptake of glucose and oxygen;
• increased tolerance to hypoxia: increased glucose transport (the only energy source for brain tissue) across the blood-brain barrier;
• glucose metabolism shifts towards the more energetically beneficial aerobic pathway;
• improvement of microcirculation in the brain of the head by reducing pathologically high blood viscosity, increasing erythrocyte deformability, inhibition of adenosine reuptake, inhibition of platelet aggregation;
• a positive effect on the oxygen transition into cells, which is created by reducing the affinity of red blood cells for it; Vinpocetine does not provoke the effect of stealing;
• selective enhancement of cerebral blood flow due to a decrease in cerebral vascular resistance, while the drug does not have a significant effect on systemic blood circulation values ​​(cardiac output, blood pressure, heart rate, total peripheral vascular resistance).

Cavinton Comfort - what is the difference?

The difference between Cavinton Comforte and its analogues lies in the dispersible structure of the tablet. This dosage form will be convenient for patients who have difficulty swallowing pills due to disorders of various origins, such as:

• dysphagia as a result of organic damage to the central nervous system (after severe cerebral strokes or traumatic brain injuries),
• individual characteristics,
• neurological diseases characterized by swallowing disorders (myasthenia gravis, myasthenic syndromes, etc.).

Cavinton Comforte dispersible tablet can be swallowed whole with plenty of water, or dissolved in the mouth until completely dissolved. The tablets have a pleasant orange flavor, which makes taking the medicine even more comfortable.

Analogs of Cavinton Comforte

Vinpocetine in the medicine is not just the main active ingredient, but also the international non-proprietary name. Among other analogues with this substance, this drug is known for its high level of purification during production, and because of this its cost is higher than the cost of many other similar drugs. There are other options for “Cavinton”, besides “Comforte”, namely: injection solution; Cavinton Forte. The difference between them lies only in the amount of the main active ingredient and the method of use. But, unlike Cavinton Forte in tablet form, the Comforte version can dissolve in the mouth, and this is very useful if the patient has problems swallowing the medicine.

Analogues have a similar effect, however, they have minor differences in the mechanism of influence and their composition. You have to look for them if there is no result or an allergic reaction occurs. One of the following analogues is usually purchased:

• "Vinpocetine." The drug serves to improve the nutrition of brain tissue and metabolism. You can understand the difference between medications if you look at the cost, which is half that of Cavinton; usually this amount is up to one hundred rubles.
• "Bravinton". The drug is used to stimulate blood flow to the brain, eliminate spasms and improve memory. Among the advantages, its price is 60 rubles.
• "Korsavin". The drug is intended for vascular expansion, as a result of which blood flow is improved. Mainly prescribed for the prevention of strokes and ischemia. “Korsavin” costs from 100 to 200 rubles.
• "Cinnarizine." The drug can relieve labyrinthine disorders, including nausea, dizziness, and tinnitus. The cost varies from 20 to 30 rubles.
• "Actovegin". The product has the ability to stimulate regeneration and metabolic processes. Tablets cost a maximum of 120 rubles.
• "Mexidol". It is usually prescribed simultaneously with Cavinton to enhance effectiveness. It serves to eliminate problems with blood circulation in the brain, and its cost is 300-400 rubles.
• "Betaserk." The drug is intended to improve brain activity and relieve tinnitus, dizziness and other symptoms of labyrinthine defect. Its cost is approximately 400 rubles.

When drawing up a therapeutic course, you need to discuss the issue of cost with your attending physician if you do not have a lot of financial resources to purchase the drug. A number of analogues are much cheaper. They are not inferior in quality, however, they have their own nuances of use, which the doctor will tell you about.

Pregnancy and breastfeeding

Vinpocetine can cross the placental barrier and is therefore contraindicated during pregnancy. Its concentration in the blood of the fetus and placenta is lower than in the blood of the woman herself. At high dosages, spontaneous abortions and placental bleeding may occur, possibly as a result of increased placental blood supply.

0.25 percent of the administered dosage of the drug enters breast milk within an hour. While using the drug, you should not breastfeed your baby.

Contraindications

Cavinton Comforte, according to the instructions for use, is contraindicated in the following cases:

• severe type of ischemic heart disease;
• acute stage of hemorrhagic stroke;
• severe forms of arrhythmia;
• pregnancy;
• phenylketonuria;
• breastfeeding period;
• revealed high sensitivity to the active and excipients in the composition;
• the patient's age is up to eighteen years, since the data has not been sufficiently studied.

Purpose

Cavinton Comfort is prescribed in neurology:

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

In ophthalmology:

• for chronic diseases of the retinal vessels, as well as the choroid.

In otology:

• with perceptual hearing impairment;
• with tinnitus;
• with Meniere's disease.

Instructions for use

The treatment course and dosage are determined by the attending physician. The medicine is prescribed after ingestion. The daily dosage of the drug is 30 mg (three times a day, one 10 mg tablet). Instructions for use for Cavinton Comfort must be strictly followed. The therapeutic effect is observed approximately a week after the start of use.

Dispersible tablets can be swallowed whole with a small amount of water; if this is difficult, they must be dissolved. This will be especially suitable for those patients who like the orange flavor of their pills.

For pathologies of the liver and kidneys, the drug is prescribed in the usual dosage.

Reviews of Cavinton Comfort

This medicine has gained wide popularity among specialists because it shows itself only from its best side. But doctors prepare patients for the fact that they do not need to expect an immediate effect from the drug Cavinton Comforte 10 mg. At least a week should pass, and only after that improvements in well-being are noted.

Patients who took the pills saw significant improvements in their health. Pain in the head appears less and less often, mental processes, memory, concentration and attention improve. Side effects are rare. Sometimes there are digestive problems and fatigue, but this usually goes away after a week. The drug copes with its purpose perfectly, which is why it is often prescribed to patients.

We reviewed the instructions for use and reviews of Cavinton Comforte. Before starting treatment, consult your doctor.

Side effects

According to the instructions and reviews of Cavinton Comfort, side effects are observed quite rarely. Information is presented according to systemic organ classes that correspond to the MedDRA classification:

• from the lymphatic system and blood: rarely – thrombocytopenia, leukopenia; very rarely - erythrocyte agglutination, anemia;
• from the immune system: in rare cases – high sensitivity;
• mental disorders: rarely - restlessness, agitation, sleep disturbances, insomnia; very rarely - depression, euphoria;
• from the side of nutrition and material metabolism: hypercholesterolemia - infrequently, rarely - diabetes mellitus, anorexia, loss of appetite;
• from the nervous system: rarely - amnesia, dizziness, drowsiness, taste disturbances, hemiparesis, stupor; infrequently – headaches; very rarely - spasms, tremors;
• from the visual organs: in rare cases – conjunctival hyperemia, papilledema;
• from the labyrinth and organ of hearing: rarely - tinnitus, hypoacusis, hyperacusis, vertigo;
• from the heart: in rare cases - myocardial infarction/ischemia, palpitations, extrasystoles, tachycardia, bradycardia, angina pectoris; very rarely - atrial fibrillation, arrhythmia;
• from the blood vessels: in rare cases – arterial hypertension, pressure fluctuations, thrombophlebitis, “hot flashes”, arterial hypertension;
• from the stomach and intestines: rarely - dry mouth, abdominal discomfort, nausea, vomiting, dyspepsia, diarrhea, constipation, abdominal pain, stomatitis, dysphagia;
• from the subcutaneous tissues and skin: in rare cases - dermatitis, rash, urticaria, itching, excessive sweating, erythema;
• general disorders and disorders at the injection site: in rare cases - feeling of heat, fatigue, asthenia, hypothermia, discomfort in the sternum.

Impact on the results of instrumental and laboratory tests: infrequently - decreased blood pressure, rarely - high blood pressure, increased triglycerides in the blood serum, increased/decreased eosinophil levels, depression of the ST segment on the cardiogram, changes in the activity of liver enzymes, decreased/increased concentration of leukocytes, decreased number red blood cells, weight gain, decreased thrombin time.