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

    Composition per 1 ampoule 1 g / 5 ml and 3 g / 15 ml

    active substance: piracetam - 1.0 g or 3.0 g; Excipients: sodium acetate trihydrate 0, 005 g or 0.015 g, glacial acetic acid 0, 000245 g or 0.000735 g, water for injection 4,195 g or 12,585 g.

    Description:

    A clear, colorless solution.

    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).

    The available data indicate that the main mechanism of action of pyracetam is not cell-specific or organ-specific.

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

    On the neuronal level piracetam facilitates various types of synaptic transmission, having a predominant effect on the density and activity of postsynaptic receptors (data obtained in animal studies). Pyracetam improves cognitive functions such as learning, memory, attention and cognitive abilities without exerting sedative or psychostimulating effects.

    The hemorheological effects of pyracetam are related to its effect on erythrocytes, platelets and the vessel wall.

    In patients with sickle-cell anemia piracetam increases the ability of erythrocytes to deform, reduces the viscosity of the blood and prevents the formation of "coins". In addition, it reduces aggregation of platelets without significantly affecting their number.

    In animal studies, it has been shown that piracetam inhibits spasm of blood vessels and counteracts various vasospalic substances.

    In studies on healthy volunteers piracetam reduced the adhesion of erythrocytes to the vascular endothelium and stimulated the production of protacyclines by a healthy endothelium.

    Pharmacokinetics:

    The pharmacokinetic profile of piracetam is linear and does not depend on time. Characteristic of low variability in a large range of doses. Constant concentration in the plasma is achieved after 3 days from the beginning of the reception.

    The volume of distribution (Vd) is about 0.6 l / kg. Pyracetam penetrates through blood-brain and placental barriers. 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 nuclei.

    It does not bind to blood plasma proteins, it is not metabolized in the body. The half-life (T1) is 4-5 hours for serum and 8.5 h for cerebrospinal fluid. The half-life does not depend on the route of administration. 80- 100% of pyracetam is excreted by the kidneys unchanged by glomerular filtration. The total clearance of piracetam in healthy volunteers is 80-90 ml / min. T1 elongates with renal failure (with terminal chronicrenal failure-up to 59 hours). The pharmacokinetics of pyracetam does not change in patients with hepatic insufficiency.

    Indications:

    In adults

    Symptomatic treatment of psycho-organic syndrome, in particular in elderly patients, accompanied by a decrease in memory, dizziness, reduced concentration and decreased activity, mood changes, behavioral disorder, gait disturbance (these symptoms may be early signs of age-related diseases such as Alzheimer's and senile dementia Alzheimer's type);

    Treatment of dizziness and related imbalance, with the exception of vasomotor and psychogenic dizziness;

    Treatment of cortical myoclonus as a monotherapy or as part of a complex therapy;

    Prevention of sickle-cell vasocclusive crisis.

    Children

    Prevention of sickle-cell vasocclusive crisis.

    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;
    • Acute disorders of cerebral circulation (hemorrhagic stroke);
    • The final stage of renal failure (with creatinine clearance less than 20 ml / min);
    • Age to 3 years.

    Pregnancy and lactation:

    Studies in animals have not shown a direct or indirect effect on pregnancy, embryo / fetal development, childbirth or postnatal development.

    Controlled studies of the use of the drug during pregnancy were not conducted. 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. Pyracetam should not be administered during pregnancy. It is necessary to refrain from breastfeeding while prescribing a piracetam to a woman.

    Dosing and Administration:

    Intravenously. Intramuscularly.

    Parenteral administration of piracetam is prescribed when it is not possible to use oral forms of the drug (unconsciousness, difficulty swallowing). Intravenous administration is preferred.

    Intravenous infusion of a daily dose is performed through a catheter at a constant rate for 24 hours a day (for example, in the initial stage of treatment with severe myoclonia).

    Preliminarily the drug is diluted in one of the compatible infusion solutions: dextrose 5%, 10% or 20%; fructose 5%, 10%, 20%; sodium chloride 0.9%; dextran 40 10% (in a solution of sodium chloride 0.9%); Ringer's solution; solution of 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, emergency treatment of crisis in sickle cell anemia) is performed for at least 2 minutes, the daily dose is then divided into several injections (2-4) at regular intervals so that the dose per injection does not exceed 3 g .

    Intramuscularly the drug is administered, if the introduction through the vein is difficult. The volume of the solution administered intramuscularly can not exceed 5 ml. Multiplicity of administration of the drug is similar to that for its intravenous or oral administration.

    When the opportunity arises, they switch to oral administration of the drug (see instructions for the medical use of the respective forms of the drug). 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 / day (2 or 3 sub-doses)

    Treatment of dizziness and associated imbalance. 2,4-4,8 g / day (2 or 3 sub-doses).

    Cortical myoclonus. Treatment starts with a dose of 7.2 g / day, every 3-4 days the dose is increased by 4.8 g / day (2 or 3 sub-doses) 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. Sickle-cell anemia. During the crisis - 300 mg / kg intravenously, divided into 4 equal doses.

    Dosing to patients with impaired renal function. The dose should be adjusted depending on the amount of creatinine clearance (CC):

    The creatinine clearance for men can be calculated based on the serum creatinine concentration, according to the following formula:

    CK (ml / min) = [140 - age (years) x body weight (kg)] / [72 x KKserum (mg / ml)]

    The creatinine clearance for women can be calculated by multiplying the obtained value by a factor of 0.85.

    Renal insufficiency

    CK (ml / min)

    Dosing regimen

    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

    20-30

    1/6 of the usual dose once

    The final stage

    <20

    contraindicated

    Elderly patients are adjusted the dose in the presence of renal failure, with prolonged therapy, it is necessary to monitor 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 side of the blood and lymphatic system: hemorrhagic disorders.

    From the immune system: anaphylactoid reactions, hypersensitivity.

    Metabolic disorders and eating disorders: increase in body weight (1.29%).

    From the side of the psyche: excitement, nervousness (1.13%), anxiety, depression (0.83%), hallucinations, confusion, drowsiness (0.96%).

    From the nervous system: hyperkinesis (1.72%), ataxia, imbalance, exacerbation of epilepsy, headache, insomnia, asthenia (0.23%).

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

    From the organs of hearing: vertigo.

    From the skin: dermatitis, itching, hives, angioedema.

    Others: rarely - pain in the area of ​​injection, thrombophlebitis, hyperthermia, hypotension (after intravenous administration).

    Overdose:

    A single case of development of diarrhea in the form of diarrhea with blood and pain in the abdomen with taking the drug inside at a daily dose of 75 g. It seems that this was due to the use of a large total dose of sorbitol, which was previously part of the solution for oral administration.

    In case of a significant overdose, rinse the stomach or induce vomiting.

    It is recommended to carry out symptomatic therapy, which may include hemodialysis. There is no specific antidote. The efficacy of hemodialysis for piracetam is 50-60%.

    Interaction:

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

    At simultaneous application with hormones of a thyroid gland the reports on confusion of consciousness, irritability and disturbance of a dream are marked.

    According to a published study of patients with recurrent venous thrombosis piracetam in a dose of 9.6 g / day does not change the dose of acenocumarol necessary to achieve INR (international normalized ratio) 2.5-3.5, but compared with the effects of acenocoumarol alone, the addition of pyracetam at a dose of 9.6 g / day significantly reduces platelet aggregation, P-thromboglobin release, fibrinogen concentration and von Willebrand factor (VIII: C; VIII: vW: Ag; VIII: vW: RCo), and blood and serum viscosity.

    In concentrations of 142, 426 and 1422 mg / ml piracetam does not inhibit cytochrome P450 isoenzymes.

    For the concentration of 1422 mg / ml, minimal inhibition of CYP 2A6 (21%) and SA4 / 5 (11%) was observed. However, the normal values ​​of the inhibition constant (Ki) can probably be achieved at a higher concentration. Thus, the metabolic effect of piracetam with other drugs is unlikely. Admission of piracetam at a dose of 20 g / day for 4 weeks in patients with epilepsy who received stable doses of antiepileptic drugs did not change the maximum serum concentration and AUC (area under the curve) of antiepileptic drugs (carbamazepine, phenytoin, phenobarbital and valproate).

    Joint intake with alcohol did not affect the concentration of piracetam in the serum; the concentration of ethanol in the serum did not change with the intake of 1.6 g of piracetam.

    Special instructions:

    Due to the antiaggregant effect (section pharmacodynamics), piracetam should be administered with caution to patients with severe hemorrhagic disorders, risk of bleeding (eg, gastric ulcer), haemostasis disorders, hemorrhagic cerebrovascular disorders in the history, in patients with surgical interventions, including dental interventions, in patients taking anticoagulants and antiplatelet agents, including low doses of aspirin.

    In the treatment of cortical myoclonia, sudden interruption in treatment should be avoided, as this may cause the resumption of seizures.

    In the treatment of sickle cell anemia, a dose of less than 160 mg / kg or an irregular intake of the drug may cause an exacerbation of the disease.

    24 mg of the drug contains about 1 mmol (23 mg) of sodium.

    Because the piracetam is excreted via the kidneys, caution should be exercised when prescribing the drug to patients with renal insufficiency.

    Long-term treatment of elderly patients requires regular monitoring of creatinine clearance, a dose adjustment may be required.

    Piracetam penetrates the filtration membranes of hemodialysis apparatus.

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

    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.

    Form release / dosage:Solution for intravenous and intramuscular injection 200 mg / ml.
    Packaging:

    For 5 or 15 ml of solution in ampoules of colorless glass (type I, Hebrew F.). By 4 (15 ml each) or 6 (5 ml) ampoules on cardboard or plastic pallets. For 1 (4 ampoules each) or 2 (6 ampoules) a pallet together with instructions for use in a cardboard bundle.

    Storage conditions:

    At a temperature of no higher than 30 ° C.

    Keep the medicine out of the reach of children!

    Shelf life:

    5 years in the original packaging.

    Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:П N014242 / 01
    Date of registration:28.05.2009
    The owner of the registration certificate: YUSB Farma S.A. YUSB Farma S.A. Belgium
    Manufacturer: & nbsp
    Representation: & nbspYUSB FARMA LLC YUSB FARMA LLC Russia
    Information update date: & nbsp15.10.2015
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