Pharmacological properties
Pharmacodynamics.
Vinpocetine is a compound with a complex mechanism of action that has a beneficial effect on metabolism in the brain and improves its blood supply, as well as improves the rheological properties of the blood. Vinpocetine exhibits a neuroprotective effect: the drug weakens the harmful effects of cytotoxic reactions caused by stimulating amino acids. The drug inhibits voltage-gated Na+ and Ca2+ channels, as well as NMDA and AMPA receptors. The drug enhances the neuroprotective effect of adenosine.
Vinpocetine stimulates cerebral metabolism: the drug increases the uptake of glucose and O2 and the consumption of these substances by brain tissue. Increases the brain's resistance to hypoxia; increases the transport of glucose - an exclusive source of energy for the brain - across the BBB; shifts glucose metabolism towards the energetically more favorable aerobic pathway; selectively inhibits the Ca2+-calmodulin-dependent enzyme cGMP-PDE, increases the level of cAMP and cGMP in the brain. The drug increases the concentration of ATP and the ATP/AMP ratio; enhances the exchange of norepinephrine and serotonin in the brain; stimulates the ascending noradrenergic system; has antioxidant activity; As a result of all of the above effects, vinpocetine has a cerebroprotective effect.
Vinpocetine improves microcirculation in the brain: the drug inhibits platelet aggregation, reduces pathologically increased blood viscosity, increases the deformability of erythrocytes and inhibits the uptake of adenosine, improves O2 transport in tissues by reducing the affinity of O2 for erythrocytes.
Vinpocetine selectively increases blood flow in the brain: the drug increases cerebral cardiac output fraction; reduces vascular resistance in the brain without affecting the parameters of systemic circulation (blood pressure, cardiac output, pulse rate, peripheral vascular resistance); the drug does not cause a steal effect. Moreover, the use of the drug improves blood flow to damaged (but not yet necrotic) ischemic areas with low perfusion (reverse steal effect).
Pharmacokinetics. Absorption: Vinpocetine is rapidly absorbed, Cmax in blood plasma is achieved 1 hour after oral administration. The main site of absorption of vinpocetine is the proximal gastrointestinal tract. The compound is not metabolized as it passes through the intestinal wall.
Distribution: In studies with oral administration of the drug in rats, radioactively labeled vinpocetine was detected in the highest concentrations in the liver and gastrointestinal tract. Cmax in tissues could be observed 2–4 hours after taking the drug. The concentration of radioactivity in the brain did not exceed the concentration in the blood.
In humans, plasma protein binding is 66%. The bioavailability of vinpocetine when taken orally is 7%. The volume of distribution is 246.7 ± 88.5 l, which means pronounced binding of the substance in tissues. The clearance value of vinpocetine (66.7 l/h) in the blood plasma exceeds its value in the liver (50 l/h), which indicates extrahepatic metabolism of the compound.
Elimination: with repeated oral administration of the drug at a dose of 5 and 10 mg, vinpocetine demonstrates linear kinetics; equilibrium concentrations in blood plasma are 1.2±0.27 and 2.1±0.33 ng/ml, respectively. T½ in humans is 4.83 ± 1.29 hours. In studies conducted using a radioactively labeled compound, it was found that the main route of elimination is through the kidneys and intestines in a ratio of 60:40%. Large amounts of radioactive tracer were detected in bile in rats and dogs, but no significant hepatic circulation was observed. Apovinamic acid (AVA) is excreted by the kidneys by simple glomerular filtration; the T½ of this substance varies depending on the dose and route of administration of vinpocetine.
Metabolism: The main metabolite of vinpocetine is VKA, which is formed in 25–30% of people. After oral administration, the AUC of VKA is 2 times higher than that after intravenous administration of the drug, which indicates the formation of VKA in the process of first-pass metabolism of vinpocetine. Other metabolites identified are hydroxyvinpocetine, hydroxy-AVA, dihydroxy-AVA-glycinate and their conjugates with glucuronides and/or sulfates. In each of the species studied, the amount of vinpocetine that was released unchanged was only a few percent of the dose taken.
An important and significant property of vinpocetine is that there is no need for special selection of the drug dose in patients with liver or kidney diseases, taking into account the metabolism of the drug and the absence of cumulation (accumulation).
Changes in pharmacokinetic properties in special circumstances (for example, at a certain age, in the presence of concomitant diseases). Since vinpocetine is indicated for therapy mainly in elderly patients who experience changes in drug kinetics - decreased absorption, different distribution and metabolism, decreased excretion - it was necessary to conduct studies to evaluate the kinetics of the drug in this age group, especially with long-term use. The results of such studies showed that the kinetics of vinpocetine in elderly patients does not differ significantly from the kinetics of vinpocetine in young patients, and, in addition, there is no accumulation. If liver or kidney function is impaired, normal doses of the drug can be used, since vinpocetine does not accumulate in the body of such patients, which allows the drug to be taken for a long time.
Cavinton Forte tablet 10 mg x30 (D)
Cavinton Forte tablet 10 mg x30 (D)
ATX code: N06BX18 (Vinpocetine) Active substance: vinpocetine (vinpocetine) Rec.INN registered by WHO
Dosage form
Cavinton® forte
Tab. 10 mg: 30 or 90 pcs.reg. No.: P N014556/01 dated 08/15/07 - Indefinitely Re-registration date: 03/12/19
Release form, packaging and composition of the drug Cavinton® forte
Tablets are white or almost white, round, flat, bevelled, with the inscription “10 mg” on one side and scored on the other.
1 tab.
vinpocetine 10 mg
Excipients: magnesium stearate - 2 mg, colloidal silicon dioxide - 2.5 mg, talc - 5 mg, lactose monohydrate - 83 mg, corn starch - 97.5 mg.
Clinical-pharmacological group: A drug that improves blood circulation and brain metabolism Pharmaco-therapeutic group: Psychostimulant and nootropic drug
pharmachologic effect
Improves brain metabolism by increasing the consumption of glucose and oxygen by brain tissue. Increases the resistance of neurons to hypoxia, enhancing the transport of glucose to the brain through the BBB, transfers the process of glucose breakdown to an energy-efficient aerobic pathway, selectively blocks Ca2+-dependent phosphodiesterase, increases the levels of AMP and cGMP in the brain. Increases the concentration of ATP and the ATP/AMP ratio in brain tissue, enhances the exchange of norepinephrine and serotonin in the brain, stimulates the ascending branch of the noradrenergic system, and has an antioxidant effect.
Reduces platelet aggregation and increased blood viscosity, increases the deforming ability of erythrocytes and blocks the utilization of adenosine by erythrocytes, helps to increase the release of oxygen by erythrocytes. Strengthens the neuroprotective effect of adenosine.
Increases cerebral blood flow, reduces cerebral vascular resistance without significantly changing systemic circulatory parameters (BP, minute volume, heart rate, OPSS). Not only does it not have a “stealing” effect, but it also increases blood supply, primarily in ischemic areas of the brain with low perfusion.
Pharmacokinetics
Suction
After oral administration, it is quickly absorbed. Cmax in blood plasma is achieved 1 hour after administration. Absorption occurs mainly in the proximal gastrointestinal tract. When passing through the intestinal wall it is not metabolized. Cmax in tissues is observed 2-4 hours after oral administration. Bioavailability is 7%.
Distribution
With repeated oral doses of 5 mg and 10 mg, the kinetics are linear.
Binds to plasma proteins by 66%. Penetrates through the placental barrier.
Metabolism and excretion
Clearance of 66.7 l/h exceeds the plasma volume of the liver (50 l/h), indicating extrahepatic metabolism.
T1/2 is 4.83±1.29h. Excreted in urine and feces in a ratio of 3:2.
Indications for Cavinton® forte
Neurology:
to reduce the severity of neurological and mental symptoms in various forms of cerebral circulatory failure (including conditions after an ischemic stroke, the recovery stage of hemorrhagic stroke, the consequences of a stroke, transient ischemic attack, vascular dementia, vertebrobasilar insufficiency, cerebral atherosclerosis, post-traumatic and hypertensive encephalopathy).
Ophthalmology:
chronic vascular diseases of the choroid and retina.
Otorhinolaryngology:
for the treatment of perceptual hearing loss, Meniere's disease, idiopathic tinnitus.
To avoid complications, use strictly as prescribed by your doctor.
ICD-10 codes
Dosage regimen
The duration of treatment and dose are determined by the doctor.
Inside, after eating.
Typically the daily dose is 15-30 mg (5-10 mg 3 times a day). The initial daily dose is 15 mg. The maximum daily dose is 30 mg.
The therapeutic effect develops approximately a week from the start of taking the drug. It takes 3 months to achieve the full therapeutic effect.
For diseases of the kidneys and liver, no adjustment of the dosage regimen is required; the absence of accumulation allows for long courses of treatment.
Side effect
Side effects associated with the use of the drug were rarely detected.
From the cardiovascular system: ECG changes (ST depression, prolongation of the QT interval), tachycardia, extrasystole (however, a causal relationship has not been proven, since in the natural population these symptoms are observed with the same frequency), blood pressure lability, hot flashes .
From the central nervous system: sleep disturbances (insomnia, increased drowsiness), dizziness, headache, general weakness (these symptoms may be manifestations of the underlying disease).
From the digestive system: dry mouth, nausea, heartburn.
Other: allergic skin reactions, increased sweating.
Contraindications for use
acute phase of hemorrhagic stroke, severe ischemic heart disease, severe arrhythmias, pregnancy, lactation (breastfeeding), childhood and adolescence under 18 years of age, hypersensitivity to vinpocetine or other components of the drug.
Use during pregnancy and breastfeeding
Cavinton® Forte is contraindicated for use during pregnancy, because Vinpocetine penetrates the placental barrier. Moreover, its concentration in the placenta and in the blood of the fetus is lower than in the blood of a pregnant woman. When taken in high doses, placental bleeding and spontaneous abortion may develop, probably as a result of increased placental blood supply.
Within 1 hour, 0.25% of the administered dose of the drug is excreted in breast milk. If it is necessary to use the drug during lactation, breastfeeding should be stopped.
Use for liver dysfunction If liver function is impaired, no dosage adjustment is required.
Use for impaired renal function In case of impaired renal function, no adjustment of the dosage regimen is required; the absence of accumulation allows for long courses of treatment.
special instructions
The presence of long QT interval syndrome and simultaneous use of drugs that cause prolongation of the QT interval require periodic ECG monitoring. In case of lactose intolerance, please note that one tablet of Cavinton® Forte contains 83 mg of lactose monohydrate.
Use in pediatrics
The drug Cavinton® Forte should not be prescribed to children and adolescents under the age of 18 years due to insufficient data on its use in this category of patients.
Impact on the ability to drive vehicles and operate machinery
There is no data on the effect of taking Cavinton® Forte on the ability to drive a car or operate machinery.
Overdose
Currently, data on overdose of vinpocetine are limited.
Treatment: gastric lavage, taking activated carbon, symptomatic therapy.
Drug interactions
No interaction is observed when used simultaneously with beta-blockers (chloranolol, pindolol), clopamide, glibenclamide, digoxin, acenocoumarol and hydrochlorothiazide, imipramine.
The simultaneous use of Cavinton® Forte and methyldopa sometimes caused a slight increase in the hypotensive effect, therefore, when using this combination, regular blood pressure monitoring is required.
Despite the lack of data confirming the possibility of interaction, it is recommended to exercise caution when prescribing Cavinton Forte simultaneously with centrally acting drugs, antiarrhythmics and anticoagulants.
Storage conditions for the drug Cavinton® forte
The drug should be stored out of the reach of children, protected from light at a temperature of 15° to 30°C.
Shelf life of the drug Cavinton® forte Shelf life - 5 years.
Terms of sale The drug is available with a prescription.
Indications
Neurology. for the treatment of various forms of cerebrovascular pathology: conditions after a cerebrovascular accident (stroke), vertebrobasilar insufficiency, vascular dementia, cerebral atherosclerosis, post-traumatic and hypertensive encephalopathy. helps reduce the severity of mental and neurological symptoms in cerebrovascular pathology.
Ophthalmology. For the treatment of chronic vascular pathology of the choroid (choroid) and retina.
Otorhinolaryngology. For the treatment of senile perceptual hearing loss, Meniere's disease and tinnitus.
Side effects
Cavinton is a safe drug, as demonstrated by safety studies that included data on tens of thousands of patients and demonstrated that even the most frequently occurring adverse events did not fall into the “common 1/100” category as defined by meddra, i.e., side effects with the highest probability of occurrence was recorded with a frequency of 1%. For this reason, the list below does not include the “often” category.
The adverse reactions listed below are classified by organ system class and frequency of occurrence according to MedDRA terminology.
From the blood and lymphatic system: leukopenia, thrombocytopenia (rare), anemia, erythrocyte agglutination (very rare).
From the immune system: hypersensitivity (very rare).
Metabolic and nutritional disorders: hypercholesterolemia (rare), loss of appetite, anorexia, diabetes mellitus (rare).
Mental disorders: insomnia, sleep disorders, anxiety, agitation (rare), euphoria, depression (very rare).
From the nervous system: headache (rare), dizziness, dysgeusia, stupor, hemiparesis, drowsiness, amnesia (rare), tremor, convulsions (very rare).
From the side of the organ of vision: swelling of the optic nerve nipple (rarely), hyperemia of the conjunctiva (very rarely).
From the organ of hearing and labyrinth: vertigo (uncommon), hyperacusis, hypoacusia, tinnitus (rare).
From the heart: myocardial ischemia/infarction, angina pectoris, bradycardia, tachycardia, extrasystole, palpitations (rare), arrhythmia, atrial fibrillation (very rare).
Vascular disorders: arterial hypotension, hypertension, hot flashes, thrombophlebitis (rare), blood pressure fluctuations (very rare).
From the digestive system: abdominal discomfort, dry mouth, nausea (rare), abdominal pain, constipation, diarrhea, dyspepsia, vomiting (rare), dysphagia, stomatitis (very rare).
From the skin and subcutaneous tissue: erythema, hyperhidrosis, itching, urticaria, rash (rare), dermatitis (very rare).
General disorders: asthenia, weakness, feeling of heat (rarely), chest discomfort, hypothermia (very rarely).
Results of laboratory and instrumental studies: decreased blood pressure (rarely), increased blood pressure, increased TG levels in the blood, depression of the ST segment on the ECG, increase/decrease in the number of eosinophils, changes in the activity of liver enzymes (rarely), increase/decrease in the number of leukocytes, decrease in the number of erythrocytes , decreased prothrombin time, increased body weight (very rare).
CAVINGTON FORTE TAB 10MG N30
Suction
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.
Distribution
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 plasma volume of the liver (50 l/h), metabolism is predominantly extrahepatic.
Metabolism
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. Preclinical studies revealed that vinpocetine is excreted unchanged in small quantities.
For liver and kidney diseases, no dose adjustment is required due to the peculiarity of the metabolism of vinpocetine - the absence of cumulation.
Removal
With repeated doses of 5 and 10 mg, the kinetics of vinpocetine is linear. Steady-state concentrations 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 radioactive label, the drug was excreted by the kidneys and through the intestines in a ratio of 60:40. In preclinical studies, a significant portion of the radioactivity was detected in bile, but significant enterohepatic circulation was not 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.
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.
special instructions
The presence of prolonged qt interval syndrome and the use of drugs that cause prolongation of qt interval require periodic ECG monitoring.
If the patient has increased intracranial pressure, arrhythmia or long QT interval syndrome, as well as while using antiarrhythmic drugs, a course of drug therapy can be started only after a thorough analysis of the benefits and risks associated with the use of the drug.
The drug contains lactose. Patients with rare hereditary diseases such as galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption disorder should not take this drug (1 Cavinton tablet contains 140 mg of lactose, 1 Cavinton forte tablet (10 mg) contains 83 mg of lactose).
During pregnancy and breastfeeding. The use of the drug during pregnancy and breastfeeding is contraindicated.
Pregnancy. Vinpocetine penetrates the placental barrier, and the concentration of the drug in the placenta and in the blood of the fetus is lower than in the blood of a pregnant woman. The teratogenic effect of the drug has not been detected. In preclinical studies of the drug in high doses, placental bleeding and spontaneous abortion were observed in some cases, possibly as a result of increased placental blood supply.
Lactation. Vinpocetine passes into breast milk. In preclinical studies using a radioactive isotope, the radioactivity of breast milk was 10 times higher than that in the blood of an adult animal. The use of vinpocetine during breastfeeding is contraindicated due to the excretion of vinpocetine in breast milk and the lack of sufficient clinical observations regarding the safety of the drug in infants. After a single dose of vinpocetine within an hour, 0.25% of the taken dose of the drug passes into breast milk.
Children. The drug is not used in children (due to the lack of clinical data).
The ability to influence reaction speed when driving vehicles and working with other mechanisms. There is no data on the effect of vinpocetine on the ability to drive vehicles or operate machinery, but caution should be exercised given the likelihood of drowsiness and dizziness when using the drug.
Cavinton Forte
Cavinton Forte tablet 10 mg x30 (D)
ATX code: N06BX18 (Vinpocetine) Active substance: vinpocetine (vinpocetine) Rec.INN registered by WHO
Dosage form
Cavinton® forte
Tab. 10 mg: 30 or 90 pcs.reg. No.: P N014556/01 dated 08/15/07 - Indefinitely Re-registration date: 03/12/19
Release form, packaging and composition of the drug Cavinton® forte
Tablets are white or almost white, round, flat, bevelled, with the inscription “10 mg” on one side and scored on the other.
1 tab.
vinpocetine 10 mg
Excipients: magnesium stearate - 2 mg, colloidal silicon dioxide - 2.5 mg, talc - 5 mg, lactose monohydrate - 83 mg, corn starch - 97.5 mg.
Clinical-pharmacological group: A drug that improves blood circulation and brain metabolism Pharmaco-therapeutic group: Psychostimulant and nootropic drug
pharmachologic effect
Improves brain metabolism by increasing the consumption of glucose and oxygen by brain tissue. Increases the resistance of neurons to hypoxia, enhancing the transport of glucose to the brain through the BBB, transfers the process of glucose breakdown to an energy-efficient aerobic pathway, selectively blocks Ca2+-dependent phosphodiesterase, increases the levels of AMP and cGMP in the brain. Increases the concentration of ATP and the ATP/AMP ratio in brain tissue, enhances the exchange of norepinephrine and serotonin in the brain, stimulates the ascending branch of the noradrenergic system, and has an antioxidant effect.
Reduces platelet aggregation and increased blood viscosity, increases the deforming ability of erythrocytes and blocks the utilization of adenosine by erythrocytes, helps to increase the release of oxygen by erythrocytes. Strengthens the neuroprotective effect of adenosine.
Increases cerebral blood flow, reduces cerebral vascular resistance without significantly changing systemic circulatory parameters (BP, minute volume, heart rate, OPSS). Not only does it not have a “stealing” effect, but it also increases blood supply, primarily in ischemic areas of the brain with low perfusion.
Pharmacokinetics
Suction
After oral administration, it is quickly absorbed. Cmax in blood plasma is achieved 1 hour after administration. Absorption occurs mainly in the proximal gastrointestinal tract. When passing through the intestinal wall it is not metabolized. Cmax in tissues is observed 2-4 hours after oral administration. Bioavailability is 7%.
Distribution
With repeated oral doses of 5 mg and 10 mg, the kinetics are linear.
Binds to plasma proteins by 66%. Penetrates through the placental barrier.
Metabolism and excretion
Clearance of 66.7 l/h exceeds the plasma volume of the liver (50 l/h), indicating extrahepatic metabolism.
T1/2 is 4.83±1.29h. Excreted in urine and feces in a ratio of 3:2.
Indications for Cavinton® forte
Neurology:
to reduce the severity of neurological and mental symptoms in various forms of cerebral circulatory failure (including conditions after an ischemic stroke, the recovery stage of hemorrhagic stroke, the consequences of a stroke, transient ischemic attack, vascular dementia, vertebrobasilar insufficiency, cerebral atherosclerosis, post-traumatic and hypertensive encephalopathy).
Ophthalmology:
chronic vascular diseases of the choroid and retina.
Otorhinolaryngology:
for the treatment of perceptual hearing loss, Meniere's disease, idiopathic tinnitus.
To avoid complications, use strictly as prescribed by your doctor.
ICD-10 codes
Dosage regimen
The duration of treatment and dose are determined by the doctor.
Inside, after eating.
Typically the daily dose is 15-30 mg (5-10 mg 3 times a day). The initial daily dose is 15 mg. The maximum daily dose is 30 mg.
The therapeutic effect develops approximately a week from the start of taking the drug. It takes 3 months to achieve the full therapeutic effect.
For diseases of the kidneys and liver, no adjustment of the dosage regimen is required; the absence of accumulation allows for long courses of treatment.
Side effect
Side effects associated with the use of the drug were rarely detected.
From the cardiovascular system: ECG changes (ST depression, prolongation of the QT interval), tachycardia, extrasystole (however, a causal relationship has not been proven, since in the natural population these symptoms are observed with the same frequency), blood pressure lability, hot flashes .
From the central nervous system: sleep disturbances (insomnia, increased drowsiness), dizziness, headache, general weakness (these symptoms may be manifestations of the underlying disease).
From the digestive system: dry mouth, nausea, heartburn.
Other: allergic skin reactions, increased sweating.
Contraindications for use
acute phase of hemorrhagic stroke, severe ischemic heart disease, severe arrhythmias, pregnancy, lactation (breastfeeding), childhood and adolescence under 18 years of age, hypersensitivity to vinpocetine or other components of the drug.
Use during pregnancy and breastfeeding
Cavinton® Forte is contraindicated for use during pregnancy, because Vinpocetine penetrates the placental barrier. Moreover, its concentration in the placenta and in the blood of the fetus is lower than in the blood of a pregnant woman. When taken in high doses, placental bleeding and spontaneous abortion may develop, probably as a result of increased placental blood supply.
Within 1 hour, 0.25% of the administered dose of the drug is excreted in breast milk. If it is necessary to use the drug during lactation, breastfeeding should be stopped.
Use for liver dysfunction If liver function is impaired, no dosage adjustment is required.
Use for impaired renal function In case of impaired renal function, no adjustment of the dosage regimen is required; the absence of accumulation allows for long courses of treatment.
special instructions
The presence of long QT interval syndrome and simultaneous use of drugs that cause prolongation of the QT interval require periodic ECG monitoring. In case of lactose intolerance, please note that one tablet of Cavinton® Forte contains 83 mg of lactose monohydrate.
Use in pediatrics
The drug Cavinton® Forte should not be prescribed to children and adolescents under the age of 18 years due to insufficient data on its use in this category of patients.
Impact on the ability to drive vehicles and operate machinery
There is no data on the effect of taking Cavinton® Forte on the ability to drive a car or operate machinery.
Overdose
Currently, data on overdose of vinpocetine are limited.
Treatment: gastric lavage, taking activated carbon, symptomatic therapy.
Drug interactions
No interaction is observed when used simultaneously with beta-blockers (chloranolol, pindolol), clopamide, glibenclamide, digoxin, acenocoumarol and hydrochlorothiazide, imipramine.
The simultaneous use of Cavinton® Forte and methyldopa sometimes caused a slight increase in the hypotensive effect, therefore, when using this combination, regular blood pressure monitoring is required.
Despite the lack of data confirming the possibility of interaction, it is recommended to exercise caution when prescribing Cavinton Forte simultaneously with centrally acting drugs, antiarrhythmics and anticoagulants.
Storage conditions for the drug Cavinton® forte
The drug should be stored out of the reach of children, protected from light at a temperature of 15° to 30°C.
Shelf life of the drug Cavinton® forte Shelf life - 5 years.
Terms of sale The drug is available with a prescription.
Interactions
The simultaneous use of vinpocetine with beta-adrenergic blockers (cloranolol, pindolol), clopamide, glibenclamide, digoxin, acenocoumarol or hydrochlorothiazide in clinical studies was not accompanied by any interaction between them. simultaneous use of vinpocetine and α-methyldopa sometimes caused a slight increase in the hypotensive effect, therefore, regular monitoring of blood pressure is necessary during the use of this combination of drugs. Despite the lack of clinical trial data confirming the possibility of interaction, caution is recommended when prescribing vinpocetine simultaneously with drugs that affect the central nervous system, as well as in the case of concomitant antiarrhythmic and anticoagulant therapy.
Cavinton® forte
Suction
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.
Distribution
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 ingestion. 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 plasma volume of the liver (50 l/h), metabolism is predominantly extrahepatic.
Metabolism
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. Preclinical studies revealed that vinpocetine is excreted unchanged in small quantities.
For liver and kidney diseases, no dose adjustment is required due to the peculiarity of the metabolism of vinpocetine - the absence of cumulation.
Removal
With repeated doses of 5 and 10 mg, the kinetics of vinpocetine is linear. Steady-state concentrations 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 radioactive label, the drug was excreted by the kidneys and through the intestines in a ratio of 60:40. In preclinical studies, a significant portion of the radioactivity was detected in bile, but significant enterohepatic circulation was not 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.
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.
Note!
Description of the drug Cavinton forte table. 10mg No. 90 on this page is a simplified author’s version of the apteka911 website, created on the basis of the instructions for use.
Before purchasing or using the drug, you should consult your doctor and read the manufacturer's original instructions (attached to each package of the drug). Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.
