Nootropil 200 mg-ml 125 ml oral solution

Nosological classification (ICD-10)

• F03 Dementia, unspecified
• F06.6 Organic emotionally labile [asthenic] disorder
• F06.7 Mild cognitive impairment
• F10.2 Alcohol dependence syndrome
• F10.3 Withdrawal state
• F70-F79 Mental retardation
• G81 Hemiplegia
• H81.4 Dizziness of central origin
• I63 Cerebral infarction
• I67.2 Cerebral atherosclerosis
• I67.9 Cerebrovascular disease, unspecified
• I69 Consequences of cerebrovascular diseases
• R40.2 Coma, unspecified
• R41.8.0* Intellectual-mnestic disorders
• R63.0 Anorexia
• S06 Intracranial injury
• T90.5 Consequences of intracranial injury

Nootropil solution for internal use 20% fl 125ml

Compound

Active substance: piracetam 200 mg.
Excipients: glycerol 85% 27 g, sodium saccharinate 300 mg, sodium acetate 200 mg, methyl parahydroxybenzoate 135 mg, propyl parahydroxybenzoate 15 mg, apricot flavor 30 mg, caramel flavor 15 mg, glacial acetic acid 16 mg ± 5%, purified water 62.1 g ±5%.

Pharmacokinetics

Suction

After taking the drug orally, piracetam is quickly and almost completely absorbed from the gastrointestinal tract. After a single dose of the drug in a dose of 3.2 g, Cmax is 84 mcg/ml, after repeated doses of 3.2 mg 3 times a day - 115 mcg/ml and is achieved after 1 hour in the blood plasma and after 5 hours in the cerebrospinal fluid. Food intake reduces Cmax by 17% and increases Tmax by up to 1.5 hours. In women, when taking piracetam at a dose of 2.4 g, Cmax and AUC are 30% greater than in men.

Distribution and metabolism

Does not bind to blood plasma proteins.

Vd of piracetam is about 0.6 l/kg.

In animal studies, it was found that piracetam selectively accumulates in the tissues of the cerebral cortex, mainly in the frontal, parietal and occipital lobes, in the cerebellum and basal ganglia.

Not metabolized in the body.

Penetrates the BBB and placental barrier.

Removal

T1/2 from blood plasma is 4-5 hours, from cerebrospinal fluid - 8.5 hours. T1/2 does not depend on the route of administration.

80-100% of piracetam is excreted unchanged by the kidneys by renal filtration. The total clearance of piracetam in healthy volunteers is 80-90 ml/min.

Pharmacokinetics in special clinical situations

T1/2 is prolonged in renal failure; for end-stage chronic renal failure - up to 59 hours.

The pharmacokinetics of piracetam does not change in patients with liver failure.

Penetrates through the filter membranes of hemodialysis machines.

Indications for use

Adults

• symptomatic treatment of psychoorganic syndrome, in particular in elderly patients, accompanied by memory loss, dizziness, decreased concentration and decreased activity, mood changes, behavior disorder, gait disturbance (these symptoms may be early signs of age-related diseases such as Alzheimer's disease and senile dementia Alzheimer's type);
• treatment of dizziness and associated imbalance, with the exception of vasomotor and psychogenic dizziness;
• treatment of cortical myoclonus (as monotherapy or as part of complex therapy);
• prevention of sickle cell vaso-occlusive crisis.

Children

• treatment of dyslexia (as part of complex therapy);
• prevention of sickle cell vaso-occlusive crisis.

Contraindications

• Psychomotor agitation at the time of drug prescription;
• Huntington's chorea;
• acute cerebrovascular accident (hemorrhagic stroke);
• end stage of chronic renal failure (with CC < 20 ml/min);
• children under 1 year of age (for oral solution);
• children under 3 years of age (for tablets);
• hypersensitivity to the components of the drug;
• hypersensitivity to pyrrolidone derivatives.

The drug should be used with caution in cases of impaired hemostasis, extensive surgical interventions, severe bleeding, and chronic renal failure (creatinine clearance 20-80 ml/min).

Directions for use and doses

The drug is prescribed orally, during meals or on an empty stomach, with liquid.

Symptomatic treatment of psychoorganic syndrome: 2.4-4.8 g/day in 2-3 doses.

Treatment of dizziness and associated imbalance: 2.4-4.8 g/day in 2-3 divided doses.

Treatment of cortical myoclonus begins with a dose of 7.2 g/day, every 3-4 days the dose is increased by 4.8 g/day until a maximum dose of 24 g/day is reached in 2-3 doses. Treatment is continued throughout the entire period of the disease. Every 6 months, attempts should be made to reduce the dose or discontinue the drug, gradually reducing the dose by 1.2 g/day every 2 days.

Prevention of sickle cell vaso-occlusive crisis: the daily dose is 160 mg/kg body weight, divided into 4 equal doses.

Treatment of dyslexia in children (as part of complex therapy): the recommended daily dose for children from 8 years of age and adolescents is 3.2 g, divided into 2 doses.

For patients with impaired renal function, the dose should be adjusted depending on the value of CC.

CC can be calculated based on serum creatinine concentration using the following formula:

For men, CC (ml/min) = [140 - age (years)] x body weight (kg)/72 x serum creatinine (mg/dl);

CC for women can be calculated by multiplying the resulting value by a coefficient of 0.85.

Patients with renal failure require dose adjustment of the drug in accordance with the following regimen.

In elderly patients, the dose is adjusted in the presence of renal failure; with long-term therapy, monitoring of the functional state of the kidneys is necessary.

Patients with impaired liver function do not require dose adjustment.

For patients with impaired renal and liver function, the drug is prescribed in the same way as for patients with only impaired renal function.

Storage conditions

The drug should be stored out of the reach of children, in a dry place at a temperature not exceeding 25°C.

Best before date

4 years. Do not use after the expiration date stated on the package.

special instructions

Due to the effect of piracetam on platelet aggregation, the drug should be prescribed with caution to patients with impaired hemostasis, during extensive surgery, or to patients with symptoms of severe bleeding.

When treating cortical myoclonus, abrupt interruption of treatment should be avoided, because this may cause the attacks to recur.

When treating sickle cell anemia, a dose of less than 160 mg/kg or irregular use of the drug may cause an exacerbation of the disease.

During long-term therapy in elderly patients, regular monitoring of renal function indicators is recommended; if necessary, dose adjustment is carried out depending on the results of the QC study.

When treating patients on a hyposodium diet, it is recommended to take into account that piracetam oral solution at a dose of 24 g contains 80.5 mg of sodium.

Piracetam penetrates through the filter membranes of hemodialysis machines.

Description

Nootropic drug.

Pharmacodynamics

Nootropic drug, cyclic derivative of gamma-aminobutyric acid (GABA).

Available evidence suggests that the primary mechanism of action of piracetam is not cell-specific or organ-specific.

Piracetam binds to the polar heads of phospholipids and forms mobile piracetam-phospholipid complexes. As a result, the two-layer structure of the cell membrane and its stability are restored, which in turn leads to the restoration of the three-dimensional structure of membrane and transmembrane proteins and the restoration of their function.

At the neuronal level, piracetam facilitates various types of synaptic transmission, having a predominant effect on the density and activity of postsynaptic receptors (data obtained from animal studies).

Piracetam improves functions such as learning, memory, attention and consciousness without causing sedation or psychostimulant effects.

The hemorheological effects of piracetam are associated with its effect on red blood cells, platelets and the vascular wall.

In patients with sickle cell anemia, piracetam increases the ability of red blood cells to deform, reduces blood viscosity and prevents the formation of coin columns. In addition, it reduces platelet aggregation without significantly affecting platelet count.

Animal studies have shown that piracetam prevents vasospasm and counteracts various vasospastic substances.

In studies in healthy volunteers, piracetam reduced the adhesion of red blood cells to the vascular endothelium and stimulated the production of prostacyclins by healthy endothelium.

Side effects

From the nervous system: motor disinhibition (1.72%), irritability (1.13%), drowsiness (0.96%), depression (0.83%), asthenia (0.23%); in isolated cases - dizziness, headaches, ataxia, imbalance, exacerbation of epilepsy, insomnia, confusion, agitation, anxiety, hallucinations, increased sexuality. In post-marketing practice, the following side effects have been observed, the frequency of which has not been established (due to insufficient data): headache, insomnia, agitation, imbalance, ataxia, exacerbation of epilepsy, anxiety, hallucinations, confusion.

From the digestive system: nausea, vomiting, diarrhea, abdominal pain (including gastralgia).

From the metabolic side: increase in body weight (1.29%).

On the part of the organ of hearing and balance: vertigo.

From the skin: dermatitis, itching, urticaria.

Allergic reactions: angioedema, hypersensitivity, anaphylactic reactions.

Other: in rare cases - pain at the injection site, thrombophlebitis, hyperthermia, arterial hypotension (with intravenous administration).

In most cases, it is possible to achieve regression of such symptoms by reducing the dose of the drug.

Use during pregnancy and breastfeeding

Adequate and strictly controlled studies of the safety of Nootropil during pregnancy have not been conducted. There have been no controlled studies of the use of the drug during pregnancy.

Piracetam penetrates the placental barrier. The concentration of the drug in newborns reaches 70-90% of its concentration in the mother's blood. Nootropil® should not be prescribed during pregnancy.

Piracetam is excreted in breast milk. When prescribing the drug during lactation, you should refrain from breastfeeding.

Interaction

The possibility of changes in the pharmacokinetics of piracetam under the influence of other drugs is low, because 90% of the drug is excreted unchanged in the urine.

When used concomitantly with thyroid hormones, there have been reports of confusion, irritability, and sleep disturbances.

According to a published study of patients with recurrent venous thrombosis, piracetam at a dose of 9.6 g/day increases the effectiveness of indirect anticoagulants (there was a more pronounced decrease in platelet aggregation, fibrinogen concentration, von Willebrand factors, blood and plasma viscosity compared with the use of indirect anticoagulants only).

Piracetam does not inhibit cytochrome P450 isoenzymes. Metabolic interaction with other drugs is unlikely.

Taking piracetam at a dose of 20 g/day for 4 weeks did not change the serum Cmax and AUC of antiepileptic drugs (carbamazepine, phenytoin, phenobarbital, valproate).

Co-administration with alcohol did not affect serum concentrations of piracetam; The concentration of ethanol in the blood serum did not change when taking 1.6 g of piracetam.

Overdose

Symptoms: a single case of the development of dyspeptic symptoms in the form of diarrhea with blood and pain in the abdominal area was registered when taking the drug orally at a daily dose of 75 g. Apparently, this was associated with the use of a large total dose of sorbitol, previously included in the dosage form solution for ingestion.

Treatment: immediately after a significant overdose when taken orally, you can rinse the stomach or induce artificial vomiting. There is no specific antidote. The effectiveness of hemodialysis is 50-60%.

Impact on the ability to drive vehicles and operate machinery

During the treatment period, care should be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Indications of the drug Nootropil®

Involution syndrome in the elderly (memory impairment, difficulty remembering and reproducing, adaptation disorders), asthenic syndrome, post-traumatic syndrome due to traumatic brain injury (headache and dizziness, motor disorders, asthenia), acute cerebrovascular accident, cerebral vascular sclerosis, hemiplegia, chronic alcoholism (preliminary states, delirium tremens, intellectual impairment, withdrawal syndrome, anorexia), impaired consciousness or coma of traumatic or toxic origin, mental retardation and learning disorders in children.

Nootropil 200 mg/ml 125 ml oral solution

Latin name

Nootropil

Release form

Oral solution

Package

Bottle 125 ml.

pharmachologic effect

Nootropil is a nootropic drug.

The active component is piracetam, a cyclic derivative of gamma-aminobutyric acid (GABA).

Improves cognitive (cognitive) processes such as learning ability, memory, attention, and mental performance.

Nootropil affects the central nervous system in various ways: it changes the rate of spread of excitation in the brain, improves metabolic processes in nerve cells, improves microcirculation, affecting the rheological characteristics of the blood and without causing a vasodilator effect.

Improves connections between the cerebral hemispheres and synaptic conduction in neocortical structures, increases mental performance, and improves cerebral blood flow.

Inhibits platelet aggregation and restores the elasticity of the erythrocyte membrane, reduces the adhesion of erythrocytes. At a dose of 9.6 g, it reduces the level of fibrinogen and von Willibrand factors by 30%-40% and prolongs bleeding time.

Nootropil has a protective and restorative effect in cases of impaired brain function due to hypoxia and intoxication.

Reduces the severity and duration of vestibular nystagmus.

Indications

– symptomatic treatment of psychoorganic syndrome (including in elderly patients with memory loss, dizziness, decreased ability to concentrate, mood changes, behavior disorder, gait disturbance, as well as in patients with Alzheimer’s disease and senile dementia of the Alzheimer’s type);

– treatment of the consequences of ischemic stroke, such as speech disorders, emotional disturbances, to increase motor and mental activity;

– for the treatment of withdrawal syndrome and psychoorganic syndrome in chronic alcoholism;

– comatose states (and during the recovery period), incl. after brain injuries and intoxications;

– for the treatment of dizziness and related balance disorders (except for cases of dizziness of vasomotor and psychogenic origin);

– as part of complex therapy for learning disabilities in children with psychoorganic syndrome;

– treatment of cortical myoclonus (both in the form of monotherapy and as part of combination therapy);

– sickle cell anemia (as part of combination therapy).

Contraindications

— Acute cerebrovascular accident (hemorrhagic stroke).

— End-stage renal failure (with creatinine clearance (CC)) — Children under 1 year of age (for oral solution).

— Children under 3 years of age (for tablets and capsules).

— Hypersensitivity to the components of the drug.

Use during pregnancy and breastfeeding

Adequate and strictly controlled studies of the safety of Nootropil during pregnancy have not been conducted. The drug should not be prescribed during pregnancy unless absolutely necessary.

Piracetam penetrates the placental barrier and is excreted in breast milk. The concentration of piracetam in newborns reaches 70-90% of its concentration in the mother’s blood. If it is necessary to use the drug during lactation, you should refrain from breastfeeding.

Experimental studies on animals did not reveal any damaging effects on the embryo and its development, incl. in the postnatal period, as well as changes in the course of pregnancy and childbirth.

special instructions

Caution should be exercised when prescribing the drug to patients with impaired hemostasis, during major surgery, or to patients with symptoms of severe bleeding.

When treating patients with cortical myoclonus, abrupt discontinuation of therapy should be avoided, because this may cause the attacks to recur.

During long-term therapy in elderly patients, regular monitoring of renal function indicators is recommended; if necessary, dose adjustment is carried out depending on the results of a creatinine clearance study.

Nootropil penetrates through the filter membranes of hemodialysis machines.

Impact on the ability to drive vehicles and operate machinery

Taking into account possible undesirable effects, the patient should be careful when operating machinery and driving a car.

Compound

1 ml of oral solution contains: piracetam 200 mg

Excipients: glycerol, sodium saccharin, sodium acetate, methyl parahydroxybenzoate, propyl parahydroxybenzoate, apricot flavor, caramel flavor, glacial acetic acid, water.

Directions for use and doses

Daily doses vary in the range of 30-160 mg/kg body weight. Frequency of administration 2-4 times/day.

When treating chronic psychoorganic syndrome, the drug is prescribed at a dose of 4.8 g/day during the first week, and then switched to a maintenance dose of 1.2-2.4 g/day.

When treating the consequences of ischemic stroke, Nootropil should be prescribed at a dose of 4.8 g/day.

When treating comatose states, as well as difficulties in perception in people with brain injuries, the initial dose is 9-12 g/day, maintenance - 2.4 g/day. Treatment should be continued for at least 3 weeks.

For abstinence in chronic alcoholism, the dose of the drug reaches 12 g/day during the period of manifestation of alcohol withdrawal syndrome. The maintenance dose is 2.4 g/day.

For the treatment of dizziness and associated imbalances, the dose is 2.4-4.8 g/day.

When correcting learning disabilities, Nootropil is prescribed in a daily dose of 3.3 g (approximately 8 ml of a 20% solution for oral administration 2 times a day). Treatment should continue throughout the school year.

For cortical myoclonus, treatment begins with a dose of 7.2 g/day, every 3-4 days the dose is increased by 4.8 g/day until a maximum dose of 24 g/day is reached. Treatment with Nootropil continues throughout the entire period of the disease. Every 6 months, attempts should be made to reduce the dose or discontinue the drug, gradually reducing the dose by 1.2 g/day every 2 days. If there is no effect or insignificant therapeutic effect, treatment is stopped.

For sickle cell anemia, the daily preventive dose is 160 mg/kg body weight, divided into 4 doses. During a crisis – up to 300 mg/kg IV. This dose can be given to children over 1 year of age.

Side effects

From the side of the central nervous system:

hyperkinesia (1.72%), nervousness (1.13%), drowsiness (0.96%), depression (0.83%), asthenia (0.23%). These side effects occur more often in elderly patients receiving the drug at a dose of more than 2.4 g/day. In some cases - dizziness, headache, ataxia, imbalance, exacerbation of epilepsy, insomnia, confusion, agitation, anxiety, hallucinations, increased sexuality.

From the side of metabolism:

increase in body weight (1.29%).

From the digestive system:

in some cases - nausea, vomiting, diarrhea, abdominal pain.

Dermatological reactions:

dermatitis, itching, rash, swelling.

Drug interactions

There was no interaction of Nootropil with clonazepam, phenytoin, phenobarbital, or sodium valproate.

Piracetam in high doses (9.6 g/day) increased the effectiveness of acenocoumarol in patients with venous thrombosis: there was a greater decrease in platelet aggregation, fibrinogen levels, von Willebrand factors, blood and plasma viscosity than when acenocoumarol was prescribed alone.

The possibility of changing the pharmacodynamics of piracetam under the influence of other drugs is low, because 90% of its dose is excreted unchanged in the urine.

Piracetam at concentrations of 142, 426 and 1422 μg/ml does not inhibit the activity of isoenzymes CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 and 4A9/11. At a concentration of 1422 μg/ml, a slight inhibition of the activity of CYP2A6 (21%) and 3A4/5 (11%) isoenzymes was noted. However, the Ki level of these two isoenzymes is sufficient when exceeding 1422 μg/ml. Therefore, metabolic interaction with other drugs is unlikely.

When taking piracetam at a dose of 20 mg/day, C max in the blood plasma and the nature of the pharmacokinetic curve of anticonvulsants (carbamazepine, phenytoin, phenobarbital, valproic acid) in patients with epilepsy receiving constant doses of these drugs do not change. When taking piracetam at a dose of 1.6 g with alcohol, the serum concentrations of piracetam and ethanol did not change.

Overdose

Symptoms:

When using piracetam at a dose of 75 g in the form of an oral solution, dyspeptic symptoms such as bloody diarrhea and abdominal pain were noted. No other special symptoms of piracetam overdose were noted.

Treatment:

immediately after a significant overdose when taken orally, you can rinse the stomach or induce artificial vomiting. Symptomatic therapy is indicated, which may include hemodialysis. There is no specific antidote. The effectiveness of hemodialysis is 50-60%.

Storage conditions

The drug should be stored in a dry place at a temperature not exceeding 25°C.