Piracetam Bufus

General characteristics. Structure:

Active ingredient: 200 mg of piracetam.

Excipients: sodium acetate, acetic acid, water for injections.

Pharmacological properties:

Pharmacodynamics. Active component is piracetam, cyclic derivative piperidic acid (GAMK).

Piracetam is nootropic means which directly influences a brain, improving cognitive (cognitive) processes, such as ability to training, memory, attention, and also intellectual working capacity. Piracetam exerts impact on the central nervous system (CNS) in various ways: change of speed of spread of activation in a brain, improving metabolic processes in nervous cells, improving microcirculation, influencing rheological characteristics of blood, not having vasodilating effect.

Improves bonds between cerebral hemispheres and synaptic conduction in neocortical structures, increases intellectual working capacity, improves a brain blood stream.

Piracetam inhibits aggregation of thrombocytes and recovers elasticity of a membrane of erythrocytes, reduces adhesion of erythrocytes. In a dose of 9,6 g reduces the level of fibrinogen and Villebrand's factor by 30-40% and extends a bleeding time. Piracetam has the tire-tread and recovering effect at dysfunction of a brain owing to a hypoxia and intoxication.

Piracetam reduces expressiveness and duration of a vestibular nystagmus.

Pharmacokinetics. The drug elimination half-life from a blood plasma makes 4-5 hours and 8,5 hours of cerebrospinal fluid which is extended at a renal failure.

The pharmacokinetics of piracetam does not change at patients with a liver failure. Gets through the hematoencephalic and placental barriers and membranes used at a hemodialysis. At a research on animals piracetam selectively collected in tissues of a cerebral cortex, is preferential in frontal, parietal and occipital lobes in a cerebellum and basal gangliya. Does not contact proteins of a blood plasma, it is not metabolized in an organism and allocated with kidneys in not changed look by renal filtering. The renal clearance of piracetam at healthy volunteers makes 86 ml/min.

Indications to use:

Symptomatic treatment of the psychoorganic syndrome, in particular, at elderly patients which is followed by decrease in the memory lowered by concentration of attention and decrease in the general activity, change of mood, disorder of behavior, gait disturbance and also at patients with Alzheimer's disease and dementia of altsgeymerovsky type.

Treatment of dizziness (вертиго) and the related disorders of balance, except for dizziness of vascular genesis and psychogenic dizziness.

Complex therapy and monotherapy of a cortical myoclonia.

Complex therapy of a sickemia.

Treatment of a dyslexia at children of 8 years is also more senior in a complex with other methods.

Route of administration and doses:

Intravenously or intramusculary. Parentalny administration of piracetam is appointed at impossibility of use of peroral forms of production of drug (a tablet, capsules, solution for intake), for example, at difficulty of swallowing or when the patient is in a coma, at the same time intravenous administration is preferable.

Intravenous infusion of a daily dose is carried out through a catheter with a constant speed throughout the 24th hour a day (for example, at a coma or in an initial stage of treatment of a heavy myoclonia). Previously drug is dissolved in one of compatible infusion solutions: a dextrose of 5%, 10% or 20%, fructose of 5%, 10% or 20%, sodium of chloride of 0,9%, a dextran 40 (10% in solution of sodium of chloride of 0,9%), Ringera, Mannitolum of 20%. The total amount of the solution intended for introduction is defined with clinical testimonies and a condition of the patient.

Bolyusny intravenous administration (for example, urgent treatment of a sickemia) is carried out within not less than 2 min., the daily dose at the same time is distributed on several introductions (2-4) with equal intervals so that the dose on one introduction did not exceed 3 g.

Intramusculary the drug is administered if introduction through a vein is complicated or the patient is overexcited. However amount of drug which can be entered intramusculary, limited especially children and patients with an underweight have bodies. Besides, administration of drug intramusculary can be painful because of the large volume of liquid. The volume of the solution entered intramusculary cannot exceed 5 ml. Frequency rate of administration of drug is similar that at its intravenous or oral administration.

At emergence of an opportunity pass to oral administration of drug (see instructions on a medical use of the corresponding forms of production of drug).

Duration of treatment is defined by the doctor depending on a disease and with dynamics of symptoms.

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

Treatment of dizziness and the related disorders of balance – 2,4-4,8 g/days.

Cortical myoclonia. Treatment begin with a dose 7,2 g / суг, each 3-4 days increase a dose by 4,8 g/days before achievement of the maximum dose of 24 g/days. Treatment is continued throughout the entire period of a disease. Each months it would be necessary to make attempts of reduction of a dose or drug withdrawal, gradually reducing a dose by 1,2 g/days each 2 days. In the absence of effect or insignificant therapeutic effect of treatment stop.

Sickemia. The daily preventive dose makes – 160 mg/kg of body weight, divided into 4 equal portions. During crisis – to 300 mg/kg intravenously, divided into 4 equal doses.

Treatment of a dyslexia at children. The daily dose for children of 8 years and teenagers – 3,2 g, divided into 2 introductions is recommended.

Dosing to patients with a renal failure. As piracetam is removed from an organism by kidneys, it is necessary to be careful at treatment of patients with a renal failure and to select a dose according to this scheme of dosing:

Renal failure	KK (ml/min.)	Dosing mode
Norm	> 80	usual dose
Easy	50-79	2/3 usual doses in 2-3 receptions
Average	30-49	1/3 usual doses in 2 receptions
Heavy	<30	1/6 usual doses once
Final stage	<20	contraindicated

The dose korrigirutsya by the elderly patient in the presence of a renal failure, and at long therapy control of a functional condition of kidneys is necessary.

Dosing to patients with an abnormal liver function. Patients with an abnormal liver function do not need dose adjustment. The patient with disturbance of functions and kidneys and a liver, dosing is carried out according to the scheme (see the section "Dosing to Patients with a Renal Failure").

Features of use:

Use during pregnancy and breastfeeding. Controlled researches on pregnant women were not conducted. Piracetam gets through a placental barrier and into breast milk. Concentration of drug at newborns reaches 70-90% of concentration it in blood at mother. Except for special circumstances it should not be appointed during pregnancy. It is necessary to refrain from breastfeeding at appointment to the woman of piracetam.

Patients should appoint piracetam with care with disturbance of a hemostasis, during extensive surgeries or the patient with symptoms of heavy bleeding.

At treatment of a cortical myoclonia it is necessary to avoid sharp interruption of treatment as it can cause resuming of attacks.

At treatment of a sickemia the dose is less than 160 mg/kg or irregular administration of drug can cause a crisis recurrence.

At long therapy regular control of indicators of function of kidneys is recommended to patients of advanced age, if necessary carry out dose adjustment depending on results of a research of creatinine.

During treatment it is necessary to be careful during the driving of motor transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Gets through the filtering membranes of devices for a hemodialysis.

Side effects:

From the central nervous system and peripheral nervous system: motive disinhibition (1,72%), irritability (1,13%), drowsiness (0,96%), depression (0,83%), adynamy (0,23%).

In isolated cases – a headache, sleeplessness, excitement, balance disturbance, an ataxy, an aggravation of a course of epilepsy, alarm, hallucinations, confusion of consciousness.

From cardiovascular system: increase or lowering of arterial pressure.

From the alimentary system: in isolated cases – nausea, vomiting, diarrhea, abdominal pains (including a gastralgia).

From a metabolism: increase in body weight (1,29%).

From integuments – dermatitis, an itch, rashes.

Allergic reactions: hypersensitivity, Quincke's disease, anaphylactoid reactions.

Interaction with other medicines:

Giovyshayet efficiency of hormones of a thyroid gland.

Piracetam in high doses (9,6 g/days) increases efficiency of indirect anticoagulants at patients with venous thrombosis (bigger decrease in aggregation of thrombocytes, concentration of fibrinogen, Villebrand's factors, viscosity of blood and plasma in comparison with use only of indirect anticoagulants was noted). The possibility of change of a pharmacodynamics of piracetam under the influence of other medicines is low as 90% of drug are removed in not changed view with urine. Piracetam does not oppress P450 cytochrome isoenzymes. Metabolic influence by other drugs is improbable.

Reception of piracetam in a dose of 20 g/days did not change the maximum concentration and the area under a curve "concentration time" of antiepileptic drugs (carbamazepine, Phenytoinum, phenobarbital, valproic acid) in blood serum at the patients with epilepsy receiving drug in a constant dose.

Joint reception with alcohol does not influence concentration of piracetam in serum, concentration of ethanol in blood serum did not change at reception of 1,6 g of piracetam.

Contraindications:

- Individual intolerance of piracetam or derivatives of a pirrolidon, and also other components of drug.
- Chorea of Gentington.
- Acute disorder of cerebral circulation (hemorrhagic stroke).
- A final stage of a renal failure (at clearance of creatinine less than 20 ml/min.).
- Psychomotor excitement at the time of purpose of drug.
- Children's age up to 3 years.

With care:
• disturbance of a hemostasis;
• extensive surgical interventions;
• heavy bleeding.

Overdose:

The isolated case of development of the dispeptic phenomena in the form of diarrhea with blood and pains in a stomach at administration of drug is registered inside in a daily dose to the 75th Mr. Povidimy, it was connected with the use of a high total dose of the sorbitol which is a part of drug earlier for a dosage form solution for intake. Other cases of overdose of drug are not revealed.

Treatment: in case of overdose performing symptomatic therapy which can include a hemodialysis is recommended. There is no specific antidote. Efficiency of a hemodialysis for piracetam makes 50-60%.

Storage conditions:

List B. In the place protected from light at a temperature not above 25 °C. To store in the place, unavailable to children. A period of validity - 5 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Solution for intravenous and intramuscular administration of 200 mg/ml. On 5 ml in ampoules polymeric, from polyethylene of high pressure or from polyethylene of low pressure, or from polyethylene for the medical purposes, or from polyethylene, or polypropylene for infusion solutions and injection drugs. On 10 ampoules with the application instruction place in a pack from a cardboard.