Piracetam (solution)

General characteristics. Structure:

Active ingredient: piracetam; 1 ml of solution contains piracetam 200 mg;

excipients: sodium acetate trihydrate, ice acetic acid, water for injections.

Pharmacological properties:

Pharmacodynamics. Active component of drug is piracetam, cyclic derivative piperidic acid. Drug positively influences exchange processes and blood circulation of a brain, stimulates oxidation-reduction processes, increases glucose utilization, improves a regional blood stream in ischemic sites of a brain, increases energy potential of an organism with the participation of ATP and adenylatecyclase. Optimization of power processes promotes increase in resistance of the central nervous system to a hypoxia and various toxic factors. Piracetam improves integrative activity of a brain, promotes memory consolidation, improves training processes.

Piracetam oppresses 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 Villibrand's factors by 30-40% and prolongs a bleeding time. Piracetam reduces expressiveness and duration of a vestibular nystagmus.

Pharmacokinetics. The maximum concentration after intravenous administration is reached in blood in 30 minutes, and in cerebrospinal fluid – in 5 minutes and makes 40-60 mkg/ml. Honor the volume of distribution of piracetam – 0,6 l/kg. The drug elimination half-life from a blood plasma makes 4-5 hours and 8,5 hours of cerebrospinal fluid. This period is extended at a renal failure. Does not contact proteins of a blood plasma, it is not metabolized in an organism. 80-100% of piracetam are removed from an organism in not changed look by kidneys by glomerular filtering. The renal clearance of piracetam at healthy volunteers makes 86 ml/min. The pharmacokinetics of piracetam does not change at patients with a liver failure. Piracetam gets through hematoencephalic and placental barriers and membranes which are used at a hemodialysis. At a research on animals it is established that piracetam selectively collects in tissues of a cerebral cortex, it is preferential in frontal, parietal and occipital zones, a cerebellum and basal gangliya.

Pharmaceutical characteristics.

Main physical and chemical properties: transparent colourless liquid.

Indications to use:

Adults.
Simtomatichesky treatment of a psychoorganic syndrome which is followed by decrease in memory, dizziness, decrease in concentration of attention.
Treatment of dizziness and the related disorders of balance, except for dizziness of a vasculomotor and psychogenic origin.
Treatment of a cortical myoclonia as monodrug or in complex therapy.
Treatment of an alcoholism and alcoholic abstinence.

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

Route of administration and doses:

Appoint intravenously 2 - 3 times a day. The daily dose for adults varies in the range of 30-160 mg/kg of body weight. The drug is administered in a vein, slowly, since 2 - 4 g, and quickly bringing a dose to 4 - 6 g a day. After clinical improvement the dose is gradually reduced and passed to oral administration of drug. The course of treatment and the choice of a dose depend on weight of a state and speed of reversible dynamics of a disease.

Treatment of a psychoorganic syndrome.

The recommended daily dose makes 2,4-4,8 g, divided into 2-3 introductions.

Treatment of a cortical myoclonia.

The initial dose makes 24 g a day for 3 days, divided into 2-3 introductions. If the therapeutic effect is absent or weak, continue use up to 7 days. If in 7 days did not gain desirable therapeutic effect, Piracetam stop treatment. At achievement of desirable therapeutic effect treatment is continued before disappearance of symptoms of a disease. Stop treatment by a gradual dose decline each 2-3 days on 1-2 g (in case of Lantsa-Adams's syndrome each 3-4 days). At use during treatment of other myoclonic means of their dose can decrease if it is possible. The patient with bad spontaneous attacks courses of treatment repeat each 6 months, adjusting at the same time a dose depending on a condition of the patient and displays of a disease.

Treatment of dizziness and related disorders of balance.

The recommended daily dose makes 2,4-4,8 g, divided into 2-3 introductions.

Treatment of alcoholism, including chronic.

During the acute period the daily dose makes 12 g, a maintenance dose – 2,4 g a day.

Treatment of a dyslexia at children is more senior than 8 years.

The daily dose makes 3,2 g, divided into 2 introductions.

Dosing by the patient with a renal failure.

As Piracetam is removed from an organism by kidneys, it is necessary to appoint carefully to patients with a renal failure, according to the table below:

 

Degree of a renal failure         Clearance of creatinine (ml/min.)                Dosage
Normal                                                          ≥ 80th                               usual dose,

                                                                                                                   divided into 2-4 receptions
Easy                                                                                          50 - 79 2/3 usual doses on 2-3 receptions
Average                                                                                       30 - 49 1/3 usual doses on 2 receptions
Heavy                                                                <                           30 1/6 usual doses once
Terminal                                                          -                                     it is contraindicated

 Dose adjustment is not necessary to patients with an abnormal liver function.

Features of use:

Due to the influence of piracetam on aggregation of thrombocytes patients should appoint drug with care with disturbance of a hemostasis, at volume surgeries, against the background of heavy bleedings.

At treatment of patients with a cortical myoclonia it is necessary to avoid the sharp termination of treatment, the risk of resuming of attacks is high.

At prolonged use regular control of function of kidneys is recommended to patients of advanced age, if necessary carry out correction of a dose depending on indicators of clearance of creatinine. Piracetam nestles close through the filtering membranes of devices for a hemodialysis.

Ability to influence speed of response at control of motor transport or work with other mechanisms. Considering possible side effects, the patient should be careful during the work with mechanisms and control of motor transport.

Side effects:

From the central nervous system: often - a hyperkinesia; seldom – an ataxy, a headache, sleeplessness, balance disturbance, increase in frequency of attacks of epilepsy, drowsiness.

From digestive tract: single - nausea, vomiting, a diarrhea, an abdominal pain and/or epigastric area.

From skin: rare: dermatitis, itch, rash, urticaria, Quincke's disease.

From immune system: anaphylactoid reactions, hypersensitivity reactions.

Mental disorders: often – a hyperexcitability, a depression, sometimes – uneasiness, confusion of consciousness, a hallucination.

Others: often - increase in body weight; seldom – an adynamy; very seldom – arterial hypertension, pain in a drug injection site, thrombophlebitis, a hyperthermia.

Interaction with other medicines:

Possibility of change of a pharmacodynamics of piracetam under the influence of other drugs low as 90% of drug are removed in not changed view with urine. At the combined use with thyroid hormones (T3+T4) the acrimony, a disorientation and sleep disorders is possible. Interaction with clonazepam, Phenytoinum, phenobarbital, sodium Valproatum is noted.

High doses of piracetam (9,6 g a day) increase efficiency of an atsenokumarol at patients with venous thrombosis: considerable decrease in level of aggregation of thrombocytes, level of fibrinogen, Villebrand's factors, viscosity of blood and plasma was noted.

In experiences of in vitro piracetam does not oppress P450 cytochrome of the CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 and 4A9/11 isoform in concentration 142, 426, 1422 mkg/ml. At concentration of 1422 mkg/ml small oppression of CYP2A6 (21%) and 3A4/5 is noted (11%). Metabolic interaction with drugs which give in to biotransformation these enzymes it is improbable. Use of piracetam in a dose of 20 mg/days did not change peak and a curve of level of concentration of antiepileptic drugs in blood serum (carbamazepine, Phenytoinum, phenobarbital, Valproatum) at patients with epilepsy.

The concomitant use of drug and alcohol intake do not influence the level of concentration of piracetam in serum.

Contraindications:

Individual intolerance of piracetam or derivatives of a pirrolidon, and also other components of drug, an acute disorder of cerebral circulation (a hemorrhagic stroke), an end-stage of a renal failure (the clearance of creatinine is less than 20 ml/min.), Huntington chorea, children's age up to 8 years, pregnancy and the period of a lactation.

Overdose:

Symptoms: strengthening of manifestations of side effects of drug.

Treatment: the specific antidote does not exist, use of a hemodialysis (removal of 50-60% of piracetam) is possible. Symptomatic treatment.

Use during pregnancy and feeding by a breast.

It is impossible to appoint piracetam during pregnancy.

Drug is emitted in breast milk therefore in need of drug use women who nurse for treatment by a breast need to stop feeding.

Children. 

Use drug for treatment of a dyslexia at children 8 years are more senior.

Storage conditions:

Period of validity. 4 years. Not to use drug after the termination of the period of validity specified on packaging. To store in protected from light and the place, unavailable to children, at a temperature from 15 ºС to 25 ºС.

Issue conditions:

According to the recipe

Packaging:

On 5 ml or 10 ml, or 20 ml in an ampoule. On 10 ampoules in a pack.