pharmachologic effect
The active component is piracetam, a cyclic derivative of gamma-aminobutyric acid (GABA).
Piracetam is a nootropic that directly affects the brain, improving cognitive processes such as learning, memory, attention, and mental performance. Piracetam affects the central nervous system in various ways: by changing the speed of propagation of excitation in the brain, improving metabolic processes in nerve cells, improving 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.
Piracetam 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 Willebrand factors by 30% - 40% and prolongs bleeding time.
Piracetam has a protective and restorative effect in cases of impaired brain function due to hypoxia and intoxication.
Piracetam reduces the severity and duration of vestibular nystagmus.
Indications for piracetam
Piracetam, the instructions for use indicate this, is in demand to combat many neurological, psychiatric and drug addiction problems. The wide scope of use is associated with the following properties:
- Positive effect on metabolic processes.
- The ability to improve blood circulation in the brain.
Indications for use are:
- Headaches and dizziness of various etiologies.
- The need to protect the brain from the effects of various damaging factors: intoxication, trauma, etc.
- The occurrence of cognitive impairment against the background of various diseases, which is manifested by memory deterioration.
The drug is used in the complex treatment of various mental illnesses and depressive conditions. It is also used in the treatment of chronic alcoholism, when persistent disorders of brain activity occur. When using the drug, it is possible to recover faster from brain injuries. This remedy improves the condition of patients with the development of dementia resulting from cerebral circulatory disorders. It is recommended for the prevention of Alzheimer's disease.
The drug is approved for the treatment of children in cases of confirmed dyslexia and other painful conditions, the symptoms of which are learning difficulties. The drug is indicated for perinatal brain damage. It is used for oligophrenia, cerebral palsy, and mental retardation.
Pharmacokinetics
The half-life of the drug from blood plasma is 4 - 5 hours and 8.5 hours from cerebrospinal fluid, which is prolonged in case of renal failure.
The pharmacokinetics of piracetam does not change in patients with liver failure.
Penetrates the blood-brain and placental barrier and membranes used in hemodialysis. In animal studies, piracetam selectively accumulates in the tissues of the cerebral cortex, mainly in the frontal, parietal and occipital lobes, in the cerebellum and basal ganglia. Does not bind to blood plasma proteins, is not metabolized in the body and is excreted unchanged by the kidneys. 80 - 100% of piracetam is excreted unchanged by the kidneys by renal filtration.
The renal clearance of piracetam in healthy volunteers is 86 ml/min.
Indications for use
- symptomatic treatment of psychoorganic syndrome, in particular in elderly patients suffering from memory loss, dizziness, decreased concentration and general activity, mood changes, behavior disorder, gait disturbance, as well as in patients with Alzheimer's disease and senile dementia of the Alzheimer's type;
- consequences of ischemic stroke (chronic stage), such as disturbances in the emotional sphere, to increase motor and mental activity;
- brain intoxication;
- dizziness of vascular origin;
— cortical myoclonus (mono- or complex therapy);
— in complex therapy of sickle cell anemia.
Contraindications
Individual intolerance to piracetam or pyrrolidone derivatives, as well as other components of the drug.
Acute stage of hemorrhagic stroke.
End-stage renal failure (with creatinine clearance less than 20 ml/min).
Psychomotor agitation.
Children's age up to 1 year.
Pregnancy, lactation period.
Use during pregnancy and lactation
No studies have been conducted in pregnant women. Piracetam penetrates the placental barrier and into breast milk. The use of the drug during pregnancy is contraindicated. When prescribing the drug, breastfeeding should be stopped.
Contraindications and side effects
Since piracetam is used in the treatment of various pathologies, the instructions focus on this, only a doctor should prescribe its use, based on the patient’s condition and the presence of contraindications. Do not use the drug if you are hypersensitive to the active substance or other components included in its composition. The medicine is not used to treat children under one year of age, as well as during pregnancy and lactation.
Piracetam tablets, the instructions indicate this, are not used in the presence of the following pathologies:
- Huntington's chorea, which is a genetic disease and is characterized at the initial stage of development by impaired coordination of movements.
- Chronic renal failure in severe form.
- Hemorrhagic stroke.
- Psychomotor agitation.
The decision to take piracetam should be made with extreme caution in case of hemostasis disorders, severe bleeding, or after major surgical operations.
Various side effects were observed when taking the drug. Patients most often experienced the following body reactions:
- Nausea and vomiting.
- Headache.
- Hives.
- Diarrhea.
As a rule, such side effects disappear on their own during therapy. More dangerous symptoms while taking the drug are decreased blood pressure, abdominal pain, depression, hallucinations, dermatitis, and confusion. Sometimes during treatment with the drug, motor disinhibition, increased libido, drowsiness or insomnia, and a constant feeling of internal anxiety occur. Overdose may increase side effects.
special instructions
Due to the effect of piracetam on platelet aggregation, caution is recommended when prescribing the drug to patients with impaired hemostasis, during major surgical operations, or to patients with symptoms of severe bleeding. When treating patients with cortical myoclonus, abrupt interruption of treatment should be avoided, which may cause resumption of attacks.
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.
Penetrates through the filter membranes of hemodialysis machines.
Considering the specifics of the disease and taking into account possible side effects, during the treatment period you should refrain from driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Instructions for use, price, reviews analogues
Piracetam must be taken in accordance with the instructions for use, as tablets and capsules are intended for internal use. The daily dosage is calculated depending on the patient’s weight and is 30-160 mg per kilogram of weight. The drug is taken 2-4 times a day, but to prevent the occurrence of insomnia, the last dose should be no later than 17 hours before bedtime.
The dosage regimen is developed by the doctor. It may vary depending on the pathology. Thus, the drug is used in complex methods of rehabilitation therapy in the treatment of serious brain damage. For recovery from complex psychotic disorders, it is used in combination with psychotropic drugs.
The price of pirocetam may vary depending on the manufacturer. But in any case, it is accessible. Today you can buy analogues of the drug in pharmacies. They are presented as single drugs and complex drugs. When prescribing such drugs, the doctor must take into account their interaction with other medications.
All nootropic drugs are highly effective, as evidenced by numerous patient reviews. First of all, they note the cumulative effect of the drug. Many note the ability to withstand heavy loads without losing concentration. You can also often find positive reviews about the treatment of children.
Directions for use and doses
Intravenously and intramuscularly.
For symptomatic treatment of chronic psychoorganic syndrome, depending on the severity of symptoms, 2–4 g are prescribed, gradually increasing the dose to 4–6 g per day, the course of treatment is 10–15 days.
When treating the consequences of stroke (chronic stage), 4.8 g/day is prescribed. The course of treatment is 10 - 15 days, if necessary, repeated courses after 6 - 8 weeks.
Treatment of dizziness and related balance disorders 2.4-4.8 g per day, course 10 - 15 days.
For cortical myoclonus, start 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 is continued throughout the entire period of the disease. Every 6 months you should try to reduce the dose or discontinue the drug by gradually reducing the dose by 1.2 g/day every 2 days. If there is little or no therapeutic effect, treatment is stopped.
For sickle cell anemia, the daily preventive dose is 160 mg/kg
body weight, divided into four equal doses. During a crisis - 300 mg/kg intravenously. This dosage can be prescribed to children from 1 year of age.
Dosing in patients with impaired renal function.
Since piracetam is excreted from the body by the kidneys, caution should be exercised when treating patients with renal failure in accordance with this dosage regimen.
In elderly patients, the dose is adjusted in the presence of renal failure and long-term therapy requires monitoring the functional state of the kidneys.
Dosing in patients with impaired liver function. Patients with impaired liver function do not need dose adjustment. For patients with impaired renal and liver function, dosing is carried out according to the scheme (see Section “Dosing for patients with impaired renal function”).
Buy Piracetam solution intravenously and intramuscularly 20% 5ml No. 10 in pharmacies
Active substance: 1 ml of solution contains: piracetam - 200.0 mg.
Release form: Solution for intravenous and intramuscular administration 200 mg/ml. Contraindications Hypersensitivity; Huntington's chorea; hemorrhagic stroke; severe chronic renal failure (creatinine clearance less than 20 ml/min); psychomotor agitation at the time of drug prescription; pregnancy, breastfeeding period. Dosage 200 mg/ml Indications for use In adults: symptomatic treatment of psychoorganic syndrome, accompanied by memory loss, decreased concentration and activity, mood changes, behavior disorder, gait disturbance; treatment of dizziness (vertigo) and related balance disorders (except for dizziness of vasomotor and psychogenic origin; cortical myoclonus (monotherapy or as part of complex therapy); relief of sickle cell vaso-occlusive crisis.
In children: treatment of dyslexia from 8 years of age in combination with other methods, including speech therapy; relief of sickle cell vaso-occlusive crisis. Interaction with other drugs When used simultaneously with iodine-containing thyroid hormones, confusion, irritability and sleep disturbance may occur.
Piracetam in high doses (9.6 g/day) increases the anticoagulant effect of indirect anticoagulants in patients with venous thrombosis (a more pronounced decrease in platelet aggregation, fibrinogen content, von Willebrand factor, blood and plasma viscosity).
The possibility of changing the pharmacodynamics of piracetam under the influence of other drugs is low, because 90% of piracetam is excreted unchanged by the kidneys.
Piracetam does not inhibit cytochrome P450 isoenzymes. Metabolic interaction with other drugs is unlikely.
Taking piracetam at a dose of 20 g/day did not change the maximum concentration and area under the concentration-time curve of antiepileptic drugs (carbamazepine, phenytoin, phenobarbital, valproic acid) in the blood serum of patients with epilepsy receiving the drug at a constant dose.
Co-administration with alcohol does not affect the serum concentration of piracetam; The concentration of ethanol in the blood serum did not change when taking 1.6 g of piracetam.
When used concomitantly with drugs that stimulate the central nervous system, excessive stimulation of the central nervous system is possible.
When used simultaneously with antipsychotics, it reduces the risk of extrapyramidal disorders. Overdose Symptoms: abdominal pain, diarrhea mixed with blood.
Treatment: symptomatic therapy, which may include hemodialysis (effectiveness 50-60%). There is no specific antidote. pharmachologic effect
Pharmacological group: Nootropic drug.
Pharmacodynamics: The active component is piracetam, a cyclic derivative of gamma-aminobutyric acid (GABA). Piracetam is a nootropic that directly affects the brain, improving cognitive abilities such as learning, memory, attention, and mental performance. Piracetam affects the central nervous system in various ways: it changes the speed of propagation of excitation in the brain, improves metabolic processes in nerve cells, improves microcirculation, affects the rheological characteristics of the blood, without having a vasodilating effect. Improves communication between the cerebral hemispheres and synaptic conduction in neocortical structures, improves cerebral blood flow. Piracetam inhibits platelet aggregation and restores the configurational properties of the outer membrane of rigid erythrocytes, as well as the ability of the latter to pass through the microvasculature. At a dose of 9.6 g, it reduces the concentration of fibrinogen and von Willebrand factor by 30-40% and prolongs bleeding time. Piracetam has a protective and restorative effect in cases of impaired brain function due to hypoxia and intoxication. Piracetam reduces the severity and duration of vestibular nystagmus.
Pharmacokinetics: The half-life of piracetam from blood plasma is 4-5 hours and 8.5 hours from cerebrospinal fluid, prolonged in chronic renal failure (in terminal chronic renal failure - up to 59 hours). Liver failure does not affect the pharmacokinetics of piracetam. Penetrates the blood-brain and placental barriers and is removed by hemodialysis. In animal experiments, it selectively accumulates in the tissues of the cerebral cortex, mainly in the frontal, parietal and occipital lobes, in the cerebellum and basal ganglia. It does not bind to plasma proteins, is not metabolized in the body and is excreted unchanged by the kidneys through glomerular filtration. The total clearance of piracetam is 80-90 ml/min. Pregnancy and breastfeeding Piracetam penetrates the placental barrier and into breast milk. The concentration of the drug in newborns reaches 70-90% of its concentration in the mother’s blood. During pregnancy, the drug is contraindicated. During the treatment period, breastfeeding should be discontinued. Conditions for dispensing from pharmacies Dispensed by prescription. Side effects From the central nervous system: motor disinhibition, irritability, drowsiness, depression, asthenia, headache, insomnia, mental agitation, imbalance, ataxia, exacerbation of epilepsy, anxiety, hallucinations, confusion.
From the digestive system: nausea, vomiting, diarrhea, abdominal pain.
Metabolism: weight gain.
From the senses: vertigo.
From the skin: dermatitis, itching, urticaria.
Allergic reactions: hypersensitivity, angioedema, anaphylactic reactions.
Local reactions: pain at the injection site, thrombophlebitis.
Other: fever, decreased blood pressure.
If any of the side effects indicated in the instructions get worse, or you notice any other side effects not listed in the instructions, tell your doctor. Special instructions Piracetam should be prescribed with caution to patients with impaired hemostasis, during major surgical operations, or to patients with symptoms of severe bleeding. When treating cortical myoclonus, abrupt interruption of treatment should be avoided, as this may cause resumption of attacks.
When stopping a veno-occlusive crisis in sickle cell anemia, a dose of less than 160 mg/kg or irregular use of the drug may cause a relapse of the crisis.
During long-term therapy in elderly patients, regular monitoring of renal function parameters is recommended; if necessary, dose adjustment is carried out depending on creatinine clearance.
Penetrates through the filter membranes of hemodialysis machines. During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions. Storage conditions: Protected from light at a temperature of 10 to 25°C. Freezing is unacceptable. Keep out of the reach of children. Method of administration and dosage: Intravenously or intramuscularly.
Parenteral administration of piracetam is prescribed when it is impossible to use oral forms of the drug (tablets, capsules, oral solution), for example, when there is difficulty swallowing or when the patient is unconscious, while intravenous administration is preferable.
Intravenous infusion of the daily dose is performed through a catheter at a constant rate for 24 hours a day (for example, in coma or in the initial stage of treatment of severe myoclonus). The drug is first diluted in one of the compatible infusion solutions: dextrose 5%, 10% or 20%, fructose 5%, 10% or 20%, sodium chloride 0.9%, hydroxyethyl starch 6% or 10%, Ringer's, mannitol 20%. The total volume of solution intended for administration is determined taking into account the clinical indications and the patient's condition.
Intravenous administration (for example, emergency treatment of sickle cell vaso-occlusive crisis) is carried out for at least 2 minutes, the daily dose is distributed over several injections at regular intervals.
The drug is administered intramuscularly if administration through a vein is difficult or the patient is overexcited. However, the amount of the drug that can be administered intramuscularly is limited, especially in children and patients with low body weight. In addition, intramuscular administration of the drug can be painful due to the large volume of fluid. The volume of solution administered intramuscularly cannot exceed 5 ml. The frequency of administration of the drug is similar to that for intravenous or oral administration.
When the opportunity arises, switch to oral administration of the drug (see instructions for medical use of the corresponding forms of release of the drug).
The duration of treatment is determined by the doctor depending on the disease and taking into account the dynamics of symptoms.
Symptomatic treatment of psychoorganic syndrome - 4.8 g / day during the first week, then switch to a maintenance dose - 1.2-2.4 g / day.
Treatment of dizziness and related balance disorders – 2.4-4.8 g/day.
Treatment of cortical myoclonus - start 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 is continued throughout the entire period of the disease. Every 6 months you should try to reduce the dose or discontinue the drug, gradually reducing the dose by 1.2 g/day every 2 days.
If there is little or no therapeutic effect, treatment is stopped.
Sickle cell vaso-occlusive crisis (in adults and children). The daily prophylactic dose is 160 mg/kg body weight, divided into 4 equal doses. During a crisis - 300 mg/kg/day intravenously, divided into 4 equal doses.
Treatment of dyslexia in children over 8 years of age (in combination with other treatment methods). The recommended daily dose is 3.2 g, divided into 2 equal doses.
Dosing in patients with impaired renal function. Since piracetam is excreted by the kidneys, caution should be exercised when treating patients with renal failure and the dose should be adjusted according to this dosing regimen:
Renal failure Creatinine clearance (ml/min) Dosage regimen
Normal > 80 - usual dose
Light 50-79-2/3 usual dose in 2-3 doses
Average 30-49-1/3 usual dose in 2 divided doses
Severe 20-30-1/6 usual dose once
End stage < 20 - contraindicated.
Side effect
They occur more often in elderly patients receiving doses above 2.4 g/day. In most cases, it is possible to achieve regression of such symptoms by reducing the dose of the drug. There are isolated reports of gastrointestinal side effects such as nausea, vomiting, diarrhea, abdominal and stomach pain; nervous system - dizziness, headaches, ataxia, imbalance, exacerbation of epilepsy, insomnia, from the psyche - confusion, excitement, anxiety, hallucinations, increased sexuality; on the part of the skin - dermatitis, itching, rashes, swelling; others - worsening of angina.
Overdose
Increased possible side effects.
First aid is taking activated carbon, symptomatic therapy, hemodialysis is possible (efficacy 50 - 60%), there is no specific antidote.
Interaction with other drugs
There was no interaction with clonazepam, phenytoin, phenobarbital, or sodium valproate.
High doses (9.6 g/day) of piracetam increased the effectiveness of acenocoumarol in patients with venous thrombosis: there was a greater decrease in platelet aggregation, fibrinogen levels, von Willebrand factor, 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, since 90% of the drug is excreted unchanged in the urine.
In vitro, piracetam does not inhibit cytochrome P450 isoforms CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 and 4 A9/11 at concentrations of 142, 426, and 1422 μg/ml. At a concentration of 1422 mcg/ml, a slight inhibition of CYP2A6 (21%) and ZA4/5 (11%) was noted. However, the Ki level of these two CYP isomers is sufficient when exceeding 1422 μg/ml. Therefore, metabolic interaction with other drugs is unlikely.
Moreover, piracetam at a dose of 20 mg/day did not change the peak and curve of the concentration level of antiepileptic drugs in the blood serum (carbamazepine, phenytoin, phenobarbital, valproate) in patients with epilepsy receiving a constant dosage.
Increases the effectiveness of antipsychotic drugs (neuroleptics).
When used concomitantly with drugs that stimulate the central nervous system, excessive stimulation of the central nervous system is possible.
When prescribed with antipsychotics, it reduces the risk of extrapyramidal disorders.
