Active substancePyracetamPyracetam
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  • Dosage form: & nbsp
    Solution for intravenous and intramuscular injection.
    Composition:

    1 ml of the solution contains:

    active substance - Piracetam 200 mg;

    Excipients - water for injection up to 1 ml.

    Description:Transparent colorless liquid.
    Pharmacotherapeutic group:Nootropic agent.
    ATX: & nbsp

    N.06.B.X.03   Pyracetam

    Pharmacodynamics:

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

    Pyracetam is a nootropic remedy that directly affects the brain, improving cognitive (cognitive) processes, such as learning ability, memory, attention, and mental performance. Pyracetam affects the central nervous system in various ways: by changing the rate of spread of excitation in the brain, improving metabolic processes in nerve cells, improving microcirculation, affecting the rheological characteristics of the blood and not causing vasodilating action.

    Improves communication between the cerebral hemispheres and synaptic conductivity in neocortical structures, increases mental capacity, improves cerebral blood flow.

    Pyracetam inhibits platelet aggregation and restores the elasticity of the erythrocyte membrane, reduces the adhesion of erythrocytes. In a dose of 9.6 g reduces the level of fibrinogen and von Willebrand factors by 30-40% and lengthens the time of bleeding. Pyracetam has a protective and restorative effect in the violation of brain function due to hypoxia and intoxication.

    Pyracetam reduces the severity and duration of the vestibular nystagmus.

    Pharmacokinetics:

    The half-life of the drug from the blood plasma is 4-5 hours and 8.5 hours from the cerebrospinal fluid; the half-life is prolonged with renal failure.The pharmacokinetics of pyracetam does not change in patients with hepatic insufficiency.

    Penetrates through the blood-brain and placental barrier and membranes used in hemodialysis. When tested on animals 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, it is not metabolized in the body and excreted by the kidneys in unchanged form by renal filtration. The renal clearance of piracetam in healthy volunteers is 86 ml / min.

    Indications:

    Symptomatic treatment of psycho-organic syndrome, particularly in elderly patients, accompanied by a decline in memory, reduced concentration and a decrease in general activity, mood changes, conduct disorder, gait disorder, as well as in patients with Alzheimer's disease and dementia of the Alzheimer type.

    Treatment effects of acute stroke (ischemic stroke) such as speech disorders, disorders of the emotional sphere, decrease in motor and mental activity.

    Chronic alcoholism - for the treatment of psycho-organic and abstinence syndromes. Comatose conditions (and during the recovery period), including after traumas and intoxications of the brain.

    Treatment of dizziness and related disorders of balance, with the exception of dizziness of vascular genesis and psychogenic dizziness.

    For the treatment of cortical myoclonia as a mono- or complex therapy.

    In the complex therapy of sickle cell anemia.

    Contraindications:

    • Individual intolerance to piracetam or pyrrolidone derivatives, as well as other components of the drug.
    • Psychomotor agitation at the time of prescribing.
    • Horea Huntington.
    • The final stage of renal failure (with creatinine clearance less than 20 ml / min).
    • Acute disturbance of cerebral circulation (hemorrhagic stroke).
    • Children under 3 years.

    Carefully:

    Violation of hemostasis; extensive surgical interventions; heavy bleeding.

    Pregnancy and lactation:

    There were no controlled studies in pregnant women. Pyracetam penetrates the placental barrier and into breast milk.The concentration of the drug in newborns reaches 70-90% of its concentration in the blood of the mother. Except in special circumstances piracetam should not be administered during pregnancy. It should be refrained from breastfeeding with the appointment of a woman piracetam.

    Dosing and Administration:

    The drug is administered intravenously or intramuscularly.

    Parenteral administration of piracetam is given when oral administration of the drug is not possible (tablets, capsules, oral solution), for example, if swallowing is difficult or when the patient is in a coma, with intravenous administration being preferred.

    If there is an opportunity, they switch to oral administration of the drug (see the instructions for the medical use of the respective forms of the drug release).

    Intravenous infusion of the daily dose is performed through a catheter at a constant rate for 24 hours a day (for example, coma or at the initial stage of treatment with severe myoclonia). Preliminary preparation is diluted in one of the compatible infusion solutions: dextrose 5%, 10% or 20%, fructose 5%, 10% or 20%, sodium chloride 0.9%, dextran 40 (10% in sodium chloride solution 0.9% ), Ringer, mannitol 20%.The total volume of solution intended for administration is determined taking into account the clinical indications and the patient's condition.

    Bolus intravenous administration (for example, with the withdrawal of withdrawal syndrome with alcoholism, emergency treatment of sickle cell anemia, etc.) is performed for at least 2 minutes, the daily dose is then divided into several injections (2-4) at regular intervals so , so that the dose per injection does not exceed 3 g. Intramuscularly the drug is administered if the introduction through the 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 a reduced body weight. In addition, the administration of the drug intramuscularly can be painful because of the large volume of fluid. The volume of the solution administered intramuscularly can not exceed 5 ml. The frequency of administration of the drug is similar to that of its intravenous or oral administration.

    The duration of treatment is determined by the doctor depending on the disease and taking into account the dynamics of the symptoms.

    Symptomatic treatment of chronic psychoorganic syndrome. 2.4-4.8 g.

    Treatment of cerebrovascular disorders (stroke). 4.8-12 g / day.

    Treatment of coma, as well as the difficulties of perception in people with brain trauma. The initial dose is 9-12 g / day, supporting - 2 g / day. Treatment lasts no less than 3 weeks.

    Alcohol withdrawal syndrome. 12 g / day. Supportive dose of 2.4 g / day.

    Treatment of dizziness and related disorders of balance. 2,4-4,8 g per day.

    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 the maximum dose of 24 g / day is reached. Treatment continues throughout the 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. In the absence of effect or a slight therapeutic effect, treatment is discontinued.

    Sickle cell anemia. The daily preventive dose is 160 mg / kg of body weight divided into four equal doses. During the crisis - 300 mg / kg intravenously, divided into four equal doses.

    Dosing to patients with impaired renal function.

    Because the piracetam is excreted from the body by the kidneys, caution should be exercised in the treatment of patients with renal insufficiency and appropriate dosage in accordance with this dosing regimen.

    Renal failure

    Clearance creatinine (ml / min)

    Dosing

    Norm

    >80

    Usual Dose

    Lightweight

    50-79

    2/3 of the usual dose in 2-3 doses

    Average

    30-49

    1/3 of the usual dose in 2 divided doses

    Heavy

    <30

    1/6 of the usual dose, once

    The final stage

    -

    contraindicated

    Elderly, the dose is corrected in the presence of renal failure, with prolonged therapy requires monitoring of the functional state of the kidneys.

    Dosing to patients with impaired liver function

    Patients with a dysfunction of the liver do not need a dose adjustment. Patients with impaired functions and kidneys and liver dosing is carried out according to the scheme (see the section "Dosing to patients with impaired renal function").

    Side effects:

    From the nervous system: motor disinhibition, irritability, drowsiness, depression, asthenia. These side effects often occur in elderly patients who received the drug at a dose of more than 2.4 g / day. In most cases, it is possible to regress such symptoms by lowering the dose of the drug. In isolated cases - dizziness, headache, ataxia, exacerbation of epilepsy, extrapyramidal disorders, tremor, imbalance, decreased ability to concentrate, insomnia, agitation, anxiety,hallucinations, increased libido.

    From the cardiovascular system: rarely - a decrease or increase in blood pressure.

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

    From the side of metabolism: an increase in body weight - often occurs in elderly patients who received the drug at a dose of more than 2.4 g / day.

    From the skin: dermatitis, itching, rashes.

    Allergic reactions: angioedema.

    Overdose:

    Symptoms of overdose for this dosage form are not described in the literature. Treatment: in case of an overdose, symptomatic therapy is recommended, which may include hemodialysis. There is no specific antidote. The efficacy of hemodialysis for piracetam is 50-60%.

    Interaction:

    Piracetam improves the effectiveness of thyroid hormones, antipsychotic drugs (neuroleptics).

    With simultaneous appointment with neuroleptics piracetam reduces the risk of extrapyramidal disorders. When used simultaneously with drugs that have a stimulating effect on the central nervous system (CNS), it is possible to enhance the stimulating effect on the central nervous system.

    No interaction with clonazepam, phenytoin, phenobarbital, valproic acid was observed.

    High doses (9.6 g / day) of piracetam increase the effectiveness of indirect anticoagulants in patients with venous thrombosis (there was a greater decrease in platelet aggregation, fibrinogen levels, vWF, plasma and blood viscosity compared with only indirect anticoagulants). Changeable pharmacodynamics piracetam under the influence of other drugs is low, since 90% of the drug is excreted unchanged in the urine.

    In vitro piracetam It does not inhibit cytochrome P450 isoenzymes such as CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 and 4A9 / 11 at concentrations of 142, 426 and 1422 μg / ml. At a concentration of 1422 μg / ml, slight inhibition of CYP2A6 (21%) and SA4 / 5 (11%) was noted, but the Ki level of these two isoenzymes is sufficient when exceeding 1,422 μg / ml, in connection with which metabolic interaction with other drugs is unlikely. The administration of piracetam at a dose of 20 mg / day did not change the peak and the concentration curve of antiepileptic drugs in serum (carbamazepine, phenytoin, phenobarbital, valproic acid) in patients with epilepsy receiving a constant dosage.

    Joint intake with alcohol did not affect the level of serum piracetam concentration, and the serum concentration of alcohol did not change with the intake of 1.6 g of piracetam.

    Special instructions:

    Due to the effect of piracetam on platelet aggregation, caution is recommended when administering the drug to patients with hemostasis disorder, during major surgeries or patients with symptoms of severe bleeding. When treating patients with cortical myoclonia, sudden interruption in treatment should be avoided, as this may cause a resumption of seizures.

    With prolonged therapy of elderly patients, regular monitoring of renal function indicators is recommended, if necessary, dose adjustment is performed depending on the results of the study of creatinine clearance.

    It penetrates the hemodialysis apparatus through the filter membranes.

    Effect on the ability to drive transp. cf. and fur:

    During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

    Form release / dosage:

    Solution for intravenous and intramuscular injection 200 mg / ml.

    Packaging:5 ml per ampoule of neutral glass with a break point. 10 ampoules per contour cell package. One contour pack with instructions for use in a pack of cardboard.
    Storage conditions:

    Store in a dark place at a temperature of no higher than 30 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years. Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-009001/09
    Date of registration:09.11.2009
    The owner of the registration certificate:VIAL, LLC VIAL, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp23.09.2015
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