Properties
What is it?
Piracetam 20% 5ml Composition 1 ml of the preparation contains: Active substance - piracetam 200 mg Excipients – sodium acetate trihydrate, diluted acetic acid, water for injection. Pharmacological properties The active component of the preparation is piracetam, a cyclic derivative of gamma-aminobutyric acid (GABA). Piracetam is a nootropic drug that directly affects the brain and improves its cognitive processes, such as learning ability, memory, attention, and increases mental performance. It changes the speed of excitation propagation in the brain, improves metabolic processes in nerve cells, as well as microcirculation, affects the rheological characteristics of blood, and does not cause vasodilation. It improves the interhemispheric connection of the brain and synaptic transmission in neocortical structures, increases mental performance, and improves blood circulation in the brain. Piracetam inhibits platelet aggregation and restores the elasticity of the erythrocyte membrane, reducing erythrocyte adhesion. At a dose of 9.6 g, it reduces fibrinogen levels and von Willebrand factors by 30-40%, prolonging bleeding time. Piracetam increases the resistance of brain tissue to hypoxia and intoxication, and improves reparative processes in the brain. Piracetam reduces the severity and duration of vestibular nystagmus. Pharmacokinetics The half-life of the preparation from blood plasma is 4-5 hours, from cerebrospinal fluid - 8.5 hours. Renal failure increases the half-life. The pharmacokinetics of piracetam do not change in patients with liver failure. Piracetam crosses the blood-brain barrier and membranes used during hemodialysis. In animal studies, piracetam selectively accumulates in the frontal, parietal, and occipital lobes of the cerebral cortex, cerebellum, and basal ganglia. It does not bind to blood plasma proteins and is not metabolized in the body. 80-100% of piracetam is excreted unchanged by the kidneys through filtration. The clearance of piracetam in healthy volunteers is 86 ml/min. Indications Symptomatic treatment of psychoorganic syndrome, especially in elderly patients complaining of memory impairment, dizziness, reduced concentration and general activity, mood swings, behavioral disorders, gait disturbances, as well as in patients with Alzheimer's disease and senile dementia of the Alzheimer's type. Treatment of stroke consequences (chronic stage of ischemic stroke), such as speech disorders, emotional, motor, and mental activity disorders. Chronic alcoholism – treatment of psychoorganic and abstinence syndromes. Comatose states (recovery period), including after head trauma and intoxication. Treatment of dizziness of vascular genesis. Treatment of cortical myoclonus, mono- and complex therapy. In complex therapy of sickle cell anemia. Dosage and administration Administered intravenously and intramuscularly. For symptomatic treatment of chronic psychoorganic syndrome, depending on the severity of symptoms, 2-4 g is prescribed, with a subsequent dose increase to 4-6 g per day, the course of treatment is 10-15 days. For the treatment of stroke consequences (chronic stage), 4-8 g/day is prescribed. The course of treatment is 10-15 days, if necessary, a repeated course is carried out after 6-8 weeks. For the treatment of comatose states and in individuals with perceptual difficulties after head trauma, the initial dose is 9-12 g/day, the maintenance dose is 2.4 g/day. Treatment lasts at least 3 weeks. For alcoholic abstinence syndrome – 12 g/day. The maintenance dose is 2.4 g/day. For the treatment of dizziness and related disorders, 2.4-4.8 g/day, the course of treatment is 10-15 days. For sickle cell anemia, the daily prophylactic dose is 160 mg/kg body weight, divided into four equal doses. During the crisis period – 300 mg/kg intravenously. Dosage in patients with impaired renal function: Since piracetam is excreted by the kidneys, caution should be exercised in patients with renal failure according to the following dosage regimen. Renal insufficiency | Creatinine clearance (ml/min) | Dosage Normal | > 80 | Usual dose Mild | 50-79 | 2/3 of the usual dose divided into 4 administrations Moderate | 30-49 | 1/3 of the usual dose divided into 2 administrations Severe | < 30 | 1/6 of the usual dose once End stage | - | Contraindicated In elderly patients with renal insufficiency, dose adjustment is necessary; during long-term therapy, it is necessary to monitor the functional state of the kidneys. Dosage in patients with impaired liver function: Patients with impaired liver function do not require dose adjustment. In patients with impaired renal and liver function, dosing is carried out according to the given scheme (see "Dosage in patients with impaired renal function"). Side effects Symptom | Common (1% to 10%) | Rare (0.1% to 1%) Disorders of the central and peripheral nervous system | Hyperkinesia – 1.72% | - Metabolism and nutrition disorders | Increased body weight – 1.29% | - Psychiatric disorders | Neurotic disorder – 1.13% | Somnolence - 0.96% General disorders | Asthenia – 0.23% | - Side effects are more common in elderly patients taking more than 2.4 g per day. Regression of such symptoms is achieved in most cases by reducing the dose of the preparation. There are isolated cases of side effects from the gastrointestinal tract, such as nausea, vomiting, diarrhea, abdominal and stomach pain; nervous system – dizziness, headache, ataxia, impaired balance, complications of epilepsy, insomnia; mental sphere – disorder, excitability, agitation, hallucinations, increased sexuality; skin – dermatitis, itching, rash, edema. Contraindications Individual intolerance to piracetam and pyrrolidone derivatives, as well as other components of the preparation. Acute stage of hemorrhagic stroke. End-stage renal failure (creatinine clearance not less than 20 ml/min). Children under 1 year of age. Pregnancy and lactation The use of the preparation is contraindicated during pregnancy and lactation. Special instructions Due to the effect of piracetam on platelets, it is recommended to administer the preparation with caution to patients with hemostasis disorders, during surgical operations, or in patients with severe bleeding symptoms. In patients with cortical myoclonus, abrupt discontinuation of treatment should be avoided, as it may lead to the recurrence of seizures. During long-term treatment in elderly patients, regular monitoring of kidney function is recommended; if necessary, dose adjustment is carried out based on creatinine clearance test results. It passes through the membrane of the hemodialysis filter. Effect on the ability to drive vehicles and operate machinery: There is no data on the effect of piracetam on the ability to drive vehicles and operate machinery. Considering the possible side effects, such an effect cannot be ruled out, therefore, the level of restriction or prohibition should be determined by a doctor. Overdose Piracetam is not toxic even at very high doses. There is no specific antidote. In case of suspected overdose, symptomatic treatment is carried out. The effectiveness of hemodialysis for piracetam excretion is 50-60%. Drug interactions No interactions of the preparation with clonazepam, phenytoin, phenobarbital, sodium valproate have been observed. High doses of piracetam (9.6 g/day) increase the effectiveness of acenocoumarol in patients with venous thrombosis, with a decrease in platelet aggregation and fibrinogen levels, von Willebrand factors, blood and plasma viscosity compared to acenocoumarol alone. The variability of piracetam pharmacodynamics is low under the influence of other drugs, as 90% of the preparation is excreted unchanged in the urine. In vitro, piracetam does not inhibit cytochrome P450 isoenzymes CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 4A9/11 at concentrations of 142, 426, and 1422 mcg/ml. At a concentration of 1422 mcg/ml, slight inhibition of CYP2A6 and 3A4/5 (11%) is observed. However, the clearance of these two CYP isoenzymes is sufficient when the concentration exceeds 1422 mcg/ml. Therefore, metabolic interactions of piracetam with other drugs are unlikely. In patients with epilepsy receiving a constant dose, piracetam at a dose of 20 mg/day does not change the serum concentration levels of antiepileptic drugs. Simultaneous administration with alcohol does not affect piracetam concentration in serum, nor does alcohol concentration change in serum after taking 1.6 g of piracetam. Storage conditions and shelf life Store in a place protected from light, inaccessible to children, at a temperature of 10°C to 25°C. Do not freeze. Shelf life: 5 years. Do not use after the expiry date indicated on the packaging. Dispensing from pharmacies By prescription (Group II).
