Active substancePyracetamPyracetam
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  • Dosage form: & nbsp

    Solution for intravenous and intramuscular injection.

    Composition:

    Composition per 1 ml

    Active substance:

    Piracetam 200.0 mg 1 mg

    Excipients:

    Sodium acetate trihydrate (sodium acetate, acetic acid, 3-water) - 1 mg, acetic acid diluted 30% to pH 5.6-5.8, water for injection up to 1.0 ml.

    Description:

    Transparent colorless or slightly colored 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).

    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 the drug-phospholipid. As a result, the two-layer structure of the cell membrane is restored and its stability, which in turn leads to the restoration of the three-dimensional structure of membrane and transmembrane proteins and the 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 such functions as training, memory, attention and consciousness, without having a sedative or psychostimulating effect.

    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 prostacyclin by a healthy endothelium.

    Pharmacokinetics:

    The pharmacokinetic profile of pyracetam 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 the 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 (T1/2) is 4-5 hours from the blood plasma and 8.5 hours from the 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. T1/2 lengthened with renal failure (with terminal CRF - 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;

    Complex therapy and monotherapy of cortical myoclonia;

    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);
    • Children under 3 years.

    Carefully:

    Risk of bleeding, violation of hemostasis; hemorrhagic cerebrovascular disorders in history, surgical interventions (including extensive dental interventions), in patients taking anticoagulants and antiaggregants, including low doses of aspirin, chronic renal failure (with creatinine clearance 20-80 ml / min).

    Pregnancy and lactation:

    Controlled studies of the use of the drug during pregnancy were not conducted. Studies in animals have not shown a direct and indirect effect on pregnancy, embryo development, childbirth and postnatal development.

    Piracetam 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.During the lactation period, the issue of stopping breastfeeding should be addressed.

    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).

    Preliminary preparation 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 sodium chloride solution 0.9%); Ringer's solution; A 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 or the patient is overexcited. 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.

    If there is an opportunity, they switch to oral administration of the drug (see instructions for the medical use of the appropriate 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 the symptoms.

    Symptomatic treatment of chronic psychoorganic syndrome - 2,4-4,8 g / day.

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

    Cortical myoclonia

    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 body weight divided into 4 equal doses. 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) х body weight (kg)]/[72 х ККserum (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 function of the 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 and mental sphere: motor disinhibition, nervousness, irritability, drowsiness, depression, asthenia, headache, insomnia, agitation, imbalance, ataxia, hyperkinesia, exacerbation of epilepsy, anxiety, hallucinations, confusion.

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

    From the side of metabolism: increase in body weight.

    From the organs of hearing: Vertigo.

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

    Allergic reactions: hypersensitivity, anaphylactic reactions.

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

    Overdose:

    Symptoms: diarrhea with an admixture of blood, pain in the abdomen.

    Treatment: Symptomatic therapy is recommended, 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, because90% of piracetam is excreted unchanged by the kidneys.

    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 in patients with recurrent venous thrombosis piracetam at a dose of 9.6 g / day dose does not alter acenocoumarol, but significantly reduces platelet aggregation (indicated a greater reduction in the level of platelet aggregation, release of β-tromboglobina, fibrinogen, von Willebrand factor, blood viscosity and plasma as compared to using only indirect anticoagulants) .

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

    Receiving piracetam at a dose 20 g / day for 4 weeks did not alter the maximum concentration in serum and area under the curve "concentration - time" epileptic patients taking stable doses of antiepileptic drugs (carbamazepine, phenytoin, phenobarbital, valproic acid).

    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:

    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.

    In the treatment of patients on a hyponatrial diet, it is recommended that the solution of piracetam at a dose of 2.4 g contain 12 mg of sodium.

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

    It penetrates the hemodialysis apparatus through the filter membranes.

    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:

    5 ml in ampoules of colorless neutral glass type I with a colored break ring or with a colored dot and a notch or without a kink ring, a colored dot and a notch.One, two or three color rings and / or a two-dimensional bar code, and / or alphanumeric coding or without additional color rings, a two-dimensional bar code, and alphanumeric coding can additionally be applied to the ampoules.

    5 ampoules per circuit cell packaging made of polyvinylchloride film and aluminum foil foil or polymer film or without foil and without film. Or 5 ampoules in a prefabricated form (tray) made of cardboard with cells for laying ampoules. One or two contour squares or cardboard trays, together with an instruction for use and a scarifier or knife, ampoule or without a scarifier or a knife ampoule in a cardboard package (bundle).

    Storage conditions:

    In the dark place at a temperature of no higher than 25 ° C. Do not freeze.

    Keep out of the reach of children.

    Shelf life:

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

    Terms of leave from pharmacies:On prescription
    Registration number:LP-002053
    Date of registration:16.04.2013
    The owner of the registration certificate:ATOLL, LLC ATOLL, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp17.09.2015
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