Cavinton concentrate 5mg / ml, 10 ml No. 5
Expiration Date: 05/2027
Russian Pharmacy name:
Кавинтон концентрат 5мг/мл, 10 мл №5
Neurology
to reduce the severity of neurological and mental disorders associated with disorders of the blood supply to the brain (transient ischemic attack, ischemic stroke, symptomatic therapy of the consequences of stroke, vascular dementia, cerebral atherosclerosis, post-traumatic and hypertensive encephalopathy, vertebrobasilar insufficiency).
Ophthalmology
chronic vascular diseases of the retina and choroid (for example, thrombosis or occlusion of the central artery or retinal vein).
Otology
hearing loss in acute vascular disease, toxic (drug) damage or other origin (idiopathic, due to noise exposure), Meniere's disease and tinnitus.
The drug is intended for intravenous drip infusion. Enter slowly, the infusion rate should not exceed 80 drops / min.
It is forbidden to enter the / m!
It is forbidden to enter / in without dilution!
To prepare the infusion, you can use saline or solutions containing dextrose (Salsol, Ringer, Rindex, Reomakrodex). Infusion solution with CavintonЃ should be used within the first 3 hours after preparation.
The usual starting daily dose is 20 mg (2 amp. 2 ml) in 500 ml of infusion solution. Depending on tolerance, within 2-3 days the dose can be increased to no more than 1 mg / kg / day. The average duration of treatment is 10-14 days.
The average daily dose with a body weight of 70 kg is 50 mg in 500 ml of infusion solution.
In case of liver and kidney diseases, dose adjustment is not required.
The use of the drug CavintonЃ concentrate for the preparation of a solution for infusion in children and adolescents under the age of 18 is contraindicated.
At the end of the course of infusion therapy, it is recommended to continue therapy with oral forms according to the scheme: 1 tab. drug CavintonЃ forte or 1 tab. the drug CavintonЃ Comfort 3 times / day (30 mg / day).
1 ml
Active substance: vinpocetine - 5 mg
Excipients: ascorbic acid - 0.5 mg; sodium disulfite - 1 mg; tartaric acid - 10 mg; benzyl alcohol - 10 mg; sorbitol - 80 mg; water for injection - up to 1 ml
acute phase of hemorrhagic stroke;
severe ischemic heart disease;
severe heart rhythm disturbances;
pregnancy;
lactation period;
intolerance to fructose or deficiency of the enzyme fructose-1,6-diphosphatase;
age up to 18 years (due to lack of data from clinical trials);
hypersensitivity to vinpocetine or other components of the drug.
With care: increased intracranial pressure, taking antiarrhythmic drugs, heart rhythm disturbances, long QT interval syndrome.
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 potential dependent 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
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%. Oral bioavailability is 7%. Vd is 246.7 ± 88.5 L, which indicates a significant tissue distribution. Vinpocetine clearance (66.7 l / h) exceeds the hepatic blood flow rate (50 l / h), which indicates extrahepatic metabolism.
After repeated oral administration at a dose of 5 or 10 mg, the kinetics of vinpocetine is linear. Css is 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 is 4.83 ± 1.29 hours. In studies with a radioactively labeled drug, it was found that the excretion is carried out by the kidneys and through the intestines in a ratio of 60:40. In preclinical studies, the greatest radioactivity was determined in bile, however, no confirmation of significant enterohepatic circulation was found. In preclinical studies, it has been shown that unchanged vinpocetine is excreted in small amounts. 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 special 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
to reduce the severity of neurological and mental disorders associated with disorders of the blood supply to the brain (transient ischemic attack, ischemic stroke, symptomatic therapy of the consequences of stroke, vascular dementia, cerebral atherosclerosis, post-traumatic and hypertensive encephalopathy, vertebrobasilar insufficiency).
Ophthalmology
chronic vascular diseases of the retina and choroid (for example, thrombosis or occlusion of the central artery or retinal vein).
Otology
hearing loss in acute vascular disease, toxic (drug) damage or other origin (idiopathic, due to noise exposure), Meniere's disease and tinnitus.
Dosage regimen
The drug is intended for intravenous drip infusion. Enter slowly, the infusion rate should not exceed 80 drops / min.
It is forbidden to enter the / m!
It is forbidden to enter / in without dilution!
To prepare the infusion, you can use saline or solutions containing dextrose (Salsol, Ringer, Rindex, Reomakrodex). Infusion solution with CavintonЃ should be used within the first 3 hours after preparation.
The usual starting daily dose is 20 mg (2 amp. 2 ml) in 500 ml of infusion solution. Depending on tolerance, within 2-3 days the dose can be increased to no more than 1 mg / kg / day. The average duration of treatment is 10-14 days.
The average daily dose with a body weight of 70 kg is 50 mg in 500 ml of infusion solution.
In case of liver and kidney diseases, dose adjustment is not required.
The use of the drug CavintonЃ concentrate for the preparation of a solution for infusion in children and adolescents under the age of 18 is contraindicated.
At the end of the course of infusion therapy, it is recommended to continue therapy with oral forms according to the scheme: 1 tab. drug CavintonЃ forte or 1 tab. the drug CavintonЃ Comfort 3 times / day (30 mg / day).
Side effect
Adverse drug reactions (ADRs) / adverse events (AEs) are presented by systemic organ classes in accordance with the MedDRA classification and with a frequency of occurrence: infrequently (from? 1/1000 to <1/100), rarely (from? 1/10 000 up to <1/1000); very rare (<1/10 000).
From the hematopoietic system: rarely - thrombocytopenia, agglutination of erythrocytes; very rarely - anemia.
From the immune system: very rarely - hypersensitivity reactions.
From the side of metabolism and nutrition: rarely - hypercholesterolemia, diabetes mellitus; very rarely - anorexia.
Mental disorders: infrequently - euphoria; rarely - anxiety; very rarely - depression.
From the nervous system: rarely - headache, dizziness, unilateral paresis, drowsiness; very rarely - tremor, loss of consciousness, hypotension, light-headedness.
From the side of the organ of vision: rarely - hyphema, hyperopia, myopia, blurred vision; very rarely - conjunctival hyperemia, edema of the optic nipple, diplopia.
On the part of the organ of hearing and labyrinth disorders: rarely - hearing impairment, hyperacusis, hypoacusia, vertigo; very rarely - tinnitus.
From the side of the cardiovascular system: rarely - ischemia / myocardial infarction, angina pectoris, arrhythmia, bradycardia, tachycardia, extrasystole, palpitations, decreased blood pressure, increased blood pressure, 'hot flashes'; very rarely - heart failure, atrial fibrillation, blood pressure lability, venous insufficiency.
From the digestive system: rarely - epigastric discomfort, dry mouth, nausea; very rarely - increased salivation, vomiting.
Skin and subcutaneous tissue disorders: rarely - erythema, hyperhidrosis, urticaria; very rarely - dermatitis, itching.
General disorders and disorders at the injection site: infrequently - a feeling of heat; rarely - asthenia, chest discomfort, inflammation and thrombosis at the injection site.
Laboratory and instrumental data: rarely - prolongation of the QT interval on the ECG, depression of the ST segment on the ECG, increased serum urea concentration; very rarely - an increase in LDH activity, lengthening of the PR interval on the ECG, changes on the ECG.
Contraindications for use
acute phase of hemorrhagic stroke;
severe ischemic heart disease;
severe heart rhythm disturbances;
pregnancy;
lactation period;
intolerance to fructose or deficiency of the enzyme fructose-1,6-diphosphatase;
age up to 18 years (due to lack of data from clinical trials);
hypersensitivity to vinpocetine or other components of the drug.
With care: increased intracranial pressure, taking antiarrhythmic drugs, heart rhythm disturbances, long QT interval syndrome.
Application during pregnancy and lactation
Pregnancy
Vinpocetine crosses the placental barrier, but its concentration in the placenta and in the blood of the fetus is lower than in the blood of a pregnant woman. Vinpocetine is contraindicated in pregnancy. Teratogenic and embryotoxic effects have not been identified. In animal studies, when administered in high doses, 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 an 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 its effect on the newborn's body, the use of the drug during breastfeeding is contraindicated.
Application for violations of liver function
For liver disease, dose adjustment is not required.
Application for impaired renal function
In case of kidney disease, dose adjustment is not required.
Application in children
Use under the age of 18 is contraindicated (due to the lack of data from clinical studies).
special instructions
If the patient has increased intracranial pressure, arrhythmia or prolonged QT interval syndrome, as well as against the background of the use of antiarrhythmic drugs CavintonЃ, a concentrate for the preparation of a solution for infusion can be prescribed only after a thorough analysis of the benefits and risks associated with its use.
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.
Due to the fact that the preparation contains a small amount of sorbitol (80 mg / 1 ml), it is necessary to control the blood glucose level in patients during treatment.
CavintonЃ, a concentrate for the preparation of a solution for infusion, is contraindicated in patients with hereditary fructose intolerance.
The gasoline alcohol contained in the drug (10 mg in 1 ml) can cause toxic and anaphylactic reactions.
The sodium disulfite contained in the drug (1 mg in 1 ml) can in rare cases cause serious hypersensitivity reactions and bronchospasm.
Influence on the ability to drive vehicles and use 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 an overdose of vinpocetine. It is known that the use of vinpocetine at a dose of 1 mg / kg of body weight can be considered safe. Due to the lack of data, the use of vinpocetine in higher doses should be avoided.
Drug interactions
With simultaneous use, there is no interaction with beta-blockers (chloranolol, pindolol), clopamide, glibenclamide, digoxin, acenocoumarol, hydrochlorothiazide, imipramine.
In rare cases, simultaneous use with alpha-methyldopa is accompanied by a slight increase in the hypotensive effect; when using this combination, regular monitoring of blood pressure is required.
Despite the lack of data confirming the possibility of interaction, it is recommended to exercise caution while prescribing with centrally acting drugs, antiarrhythmic and anticoagulant agents.
The drug is chemically incompatible with heparin, therefore, these two drugs cannot be mixed in the same syringe or intravenous drip system, but simultaneous anticoagulant therapy can be performed.
Vinpocetine is also incompatible with solutions for infusion containing amino acids, therefore, CavintonЃ concentrate for preparation of solution for infusion during infusion therapy should not be administered together with solutions containing amino acids.
Storage conditions
The drug should be stored in its original packaging (cardboard box) to protect it from exposure to light, out of the reach of children at a temperature not exceeding 25 ? 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.