Active substancePyracetamPyracetam
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  • Dosage form: & nbspCapsules.
    Composition:

    Composition per 1 capsule:

    Active substance: piracetam (in terms of 100% substance) - 400 mg. Excipients: calcium stearate - 4.3 mg, magnesium hydroxycarbonate - up to the contents of the capsule 430 mg.

    Composition of hard gelatin capsule: gelatin - 61.289 mg, glycerol 0.193 mg, purified water 10.585 mg, methyl parahydroxybenzoate 0.268 mg, propyl parahydroxybenzoate 0.067 mg, sodium lauryl sulfate 0.049 mg, dye quinoline yellow E-104 0.042 mg, dye sunset yellow E-110 - 0.01 mg, titanium dioxide E-171 - 0.497 mg.

    Description:

    Hard gelatin capsules No. 1 yellow. The contents of capsules are white or almost white powder.

    Pharmacotherapeutic group:Nootropic agent.
    ATX: & nbsp

    N.06.B.X.03   Pyracetam

    Pharmacodynamics:

    Pyracetam - nootropic agent, has an effect on the central nervous system in various ways: it modifies neurotransmission in the brain; improves the conditions conducive to neuronal plasticity; improves microcirculation, affecting the rheological characteristics of the blood and not causing vasodilation. The use of piracetam in patients with cerebral dysfunction increases concentration and improves cognitive function, which is accompanied by changes in the electroencephalogram (increase in α and β activity, decrease δ activity). Promotes restoration of cognitive functions due to various disorders, such as hypoxia, intoxication or electroconvulsive therapy.

    Pyracetam is indicated for the treatment of cortical myoclonus both as monotherapy and as part of complex therapy.

    Reduces the duration of induced vestibular neuronitis. Pyracetam inhibits increased aggregation of activated platelets and, in the case of abnormal rigidity of erythrocytes, improves their deformability and ability to filter.

    Pharmacokinetics:

    Absorption

    After oral administration piracetam quickly and almost completely absorbed from the gastrointestinal tract. Bioavailability is about 100%.

    After a single dose of piracetam at a dose of 2 g, the maximum concentration (Cmax) is reached in 30 minutes and is 40-60 μg / ml, after 2-8 hours it is found in the cerebrospinal fluid.

    Distribution

    The volume of distribution (Vd) is about 0.6 l / kg. Does not bind to plasma proteins. Pyracetam penetrates through blood-brain and placental barriers, as well as hemodialysis membranes. In an animal study, 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.

    Metabolism

    It is not metabolized.

    Excretion

    The half-life of blood (T1) is 4-5 hours and 8.5 hours of cerebrospinal fluid. T1 is prolonged with renal failure. It is excreted unchanged by the kidneys. Excretion by the kidneys is almost complete (> 95%) for 30 hours.

    The total clearance of piracetam in healthy volunteers is 86 ml / min.

    Indications:

    Symptomatic treatment of intellectual-mnestic disorders in the absence of an established diagnosis of dementia.Reduction of the manifestations of cortical myoclonias in piracetam sensitive patients both as monotherapy and as part of complex therapy (in order to determine sensitivity to pyracetam, a trial course of treatment can be conducted in a specific case).

    Contraindications:

    Individual intolerance to piracetam or pyrrolidone derivatives, as well as other components of the drug; Huntington's chorea; hemorrhagic stroke; terminal stage of chronic renal failure; pregnancy, the period of breastfeeding.

    Carefully:

    Violation of hemostasis, extensive surgical interventions, heavy bleeding, chronic renal failure (KK - 20-80 ml / min).

    Pregnancy and lactation:

    Pregnancy

    Sufficient data on the use of piracetam during pregnancy are absent. Studies in animals have not shown a direct or indirect effect on pregnancy, embryo / fetal development, childbirth or postnatal development.

    Piracetam penetrates the placental barrier. The plasma concentration of piracetam in neonates reaches 70-90% of that of the mother. Pyracetam should be prescribed during pregnancy only in exceptional cases if the benefit to the mother exceeds the potential risk to the fetus, and the clinical condition of the pregnant woman requires treatment with piracetam.

    Lactation

    Piracetam penetrates into breast milk. Pyracetam should not be used during breastfeeding or should stop breastfeeding while treating piracetam. When deciding whether to quit breastfeeding or refuse treatment with piracetam, the benefits of breastfeeding for a child and the benefits of therapy for a woman should be correlated.

    Dosing and Administration:

    Inside. Capsules are swallowed, not liquid, squeezed with water. During a meal or on an empty stomach.

    In memory disorders, intellectual disorders:

    On 2,4-4,8 g / day in several receptions during the first several weeks, then pass to supporting therapy of 2,4 g / day in 2-3 receptions, reception of 1,2 g / day is possible.

    Treatment of cortical myoclonia:

    Treatment begins with 7.2 grams per day, increasing it by 4.8 g every 3-4 days up to 24 g, divided into 2-3 injections. The dose of other drugs for the treatment of myoclonus does not change.Further on the results of treatment, it is necessary, if possible, to reduce the dose of other drugs for the treatment of myoclonus. After initiation of piracetam treatment, treatment is continued as long as the symptoms of the disease persist. In patients with acute episodes, the course of the disease may change with time, therefore every 6 months, attempts should be made to reduce the dose or to cancel the drug. To avoid sudden relapse, the dose is reduced by 1.2 g every 2 days (to prevent the possibility of sudden recurrence of seizures in the Lansa-Adams syndrome - every 3-4 days).

    If oral administration is not possible, the drug is administered intravenously at the same dose.

    Elderly patients

    Elderly patients with renal insufficiency should be corrected for the dose (see below "Renal failure"). With long-term treatment to assess the need for dose adjustment, creatinine clearance should be assessed regularly.

    Renal insufficiency

    Piracetam is excreted almost exclusively by the kidneys, care should be taken when treating patients with renal insufficiency or requiring renal function control.

    The elimination half-life increases in direct proportion to the impairment of kidney function and creatinine clearance; this is also true for the elderly, in whom the excretion of creatinine depends on age.

    The dose should be adjusted depending on the creatinine clearance (CK).

    The creatinine clearance for men can be calculated based on the serum creatinine concentration (Kserum), 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.

    Kidney function

    CK (ml / min)

    Dosing regimen

    Norm

    >80

    The standard dose of 2-4 admission

    Mild renal insufficiency

    50-79

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

    Mean renal insufficiency

    30-49

    1/3 of the standard dose in 2 divided doses

    Severe renal insufficiency

    <30

    1/6 of the standard dose, once

    Terminal Renal Failure

    -

    Contraindicated

    Liver failure

    Patients with isolated dysfunction of the liver do not need correction of the dose. Patients with impaired function and kidney and liver dosing is carried out according to the scheme (see above "Renal failure").

    Side effects:

    The undesirable drug reactions listed below were detected in clinical trials and post-detection observations and grouped according to system-organ classes. The frequency gradient is defined as follows: very often (≥1 / 10), often (≥1 / 100 to <1/10), infrequently (≥1 / 1000 to <1/100), rarely (≥1 / 10000 to <1 / 1000), very rarely (<1/10000) and the frequency is unknown (it is impossible to estimate based on the available clinical trial data).

    From the side of the blood and lymphatic system:

    The frequency is unknown: bleeding.

    From the immune system:

    The frequency is unknown: anaphylactoid reactions, hypersensitivity.

    From the side of the psyche:

    Often: nervousness. Infrequently: depression.

    The frequency is unknown: agitation, anxiety, confusion, hallucinations.

    From the nervous system:

    Often: hyperactivity. Infrequently: drowsiness. The frequency is unknown: ataxia, imbalance, exacerbation of epilepsy, headache, insomnia, tremor.

    From the side of the organ of hearing and labyrinth:

    Frequency unknown: vertigo.

    From the side of the vessels:

    Rarely: thrombophlebitis, arterial hypotension (only with parenteral administration).

    From the digestive system:

    The frequency is unknown: abdominal pain (including in the upper parts), nausea, vomiting, diarrhea.

    From the skin and subcutaneous tissues:

    The frequency is unknown: angioedema, dermatitis, itching, urticaria.

    On the part of the reproductive system:

    Frequency unknown: increased sexual desire.

    Common disorders and disorders at the site of administration:

    Infrequently: asthenia.

    Rarely: pain at the injection site, fever (only with parenteral administration).

    Laboratory and instrumental data:

    Often: weight gain.

    Overdose:

    Symptoms: abdominal pain, diarrhea with an admixture of blood.

    A case is described when, after taking piracetam at a dose of 75 g / day, the patient developed diarrhea with blood, accompanied by pain in the abdomen, which was explained by the effect of a significant amount of sorbitol.

    Treatment: induction of vomiting, gastric lavage, symptomatic therapy, hemodialysis (efficacy 50-60%). There is no specific antidote.
    Interaction:

    Thyroid hormones

    With the simultaneous use of pyracetam and thyroid extract (triiodothyronine + thyroxine), confusion, irritability and sleep disturbance were noted.

    Acenocoumarol

    According to a published blind clinical trial in patients with recurrent venous thrombosis, piracetam at a dose of 9.6 g / day does not affect the dose of acenocoumarol necessary to achieve an international normalized ratio of 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, the release of P-thromboglobin, the concentration of fibrinogen and von Willebrand factor (VIII: C; VIII: vW: Ag; VIII: vW: RCo), and the viscosity of whole blood and plasma.

    Pharmacokinetic interactions

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

    In concentrations of 142, 426 and 1422 mg / ml piracetam does not inhibit cytochrome P450 isoenzymes (CYP 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 and 4A9 / 11) in vitro.

    At a concentration of 1422 mg / ml, the minimal inhibition of the isoenzyme CYP 2A6 (21%) and SA4 / 5 (11%) was observed. However, the values ​​of the inhibition constant (K;) probably go well beyond the concentration of 1422 mg / ml. Thus, the metabolic interactions of piracetam with other drugs are unlikely.

    Anticonvulsants

    Admission piracetam at a dose of 20 g / day for 4 weeks in patients with epilepsy, taking a constant dose of antiepileptic drugs (carbamazepine, phenytoin, phenobarbital and valproic acid), did not change their maximum and minimum concentrations. Alcohol Simultaneous reception with alcohol did not affect the concentration of pyracetam in plasma; when taking 1.6 g of pyracetam, the concentration of ethanol in the plasma did not change.

    Pharmaceutical compatibility

    There is no information on pharmaceutical compatibility.

    Special instructions:

    Effect on platelet aggregation

    Due to the antiaggregant effect (see the section "Pharmacodynamics"), patients should be administered with caution to patients with severe hemorrhagic disorders, risk of bleeding (eg, gastric ulcer), hemostasis disorders, in patients with surgical interventions, including dental interventions, in patients taking anticoagulants and antiaggregants, incl. low doses of acetylsalicylic acid.

    Renal insufficiency

    Because the piracetam is excreted by the kidneys, care should be taken when prescribing the drug to patients with renal insufficiency.See section "Dosing and Administration").

    Elderly patients

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

    Abolition of therapy

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

    It penetrates the hemodialysis apparatus through the filter membranes.
    Effect on the ability to drive transp. cf. and fur:

    Given the profile of adverse reactions, during the treatment period, care must be taken when driving vehicles, working with mechanisms and engaging in other potentially hazardous activities requiring increased concentration and speed of psychomotor reactions.

    Form release / dosage:Capsules 400 mg.
    Packaging:

    10 capsules per contour cell packaging made of polyvinylchloride film and aluminum foil.

    By 3 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

    Storage conditions:

    Store in a dry, dark place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years.

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

    Terms of leave from pharmacies:On prescription
    Registration number:П N015341 / 01
    Date of registration:27.07.2010
    The owner of the registration certificate:BELMEDPREPARATY, RUP BELMEDPREPARATY, RUP Republic of Belarus
    Manufacturer: & nbsp
    BELMEDPREPARATY, RUP Republic of Belarus
    Information update date: & nbsp22.09.2015
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