Piracetam

General characteristics. Structure:

Active agent: piracetam - 200 mg. Excipients: acetate sodium trihydrate (sodium acetic 3-water) – 1 mg, acetic acid of divorced 30% - to рН 5,8, water for injections – to 1 ml.

Pharmacological properties:

Pharmacodynamics. Active component is piracetam, cyclic derivative piperidic acid (GAMK). Piracetam is nootropic means which directly influences a brain, improving cognitive (cognitive), such as ability to training, memory, attention, and also intellectual working capacity. Piracetam exerts impact on the central nervous system in various ways: changes the speed of spread of activation in a brain, improves metabolic processes in nervous cells, improves microcirculation, influences rheological characteristics of blood, without having at the same time vazodilatiruyushchy effect. Improves communication between cerebral hemispheres and synaptic conduction in neocortical structures, improves a brain blood stream. Piracetam inhibits aggregation of thrombocytes and recovers configuration properties of an outer membrane of rigid erythrocytes, and also ability of the last to a passage through vessels of a microcirculator bed. In a dose of 9,6 g reduces concentration 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 piracetam elimination half-life from a blood plasma makes 4-5 h and 8,5 h of cerebrospinal fluid, is extended at a chronic renal failure (at a terminal chronic renal failure – to 59 h). The liver failure does not influence piracetam pharmacokinetics. Gets through hematoencephalic and placental barriers, is removed at a hemodialysis. In experiments on animals selectively collects in tissues of a cerebral cortex, it is preferential in frontal, parietal and occipital lobes, in a cerebellum and basal kernels. Does not contact proteins of a blood plasma, it is not metabolized in an organism and removed by kidneys in not changed look by glomerular filtering. The general clearance of piracetam makes 80-90 ml/min.

Indications to use:

At adults: a symptomatic treatment of the psychoorganic syndrome which is followed by decrease in memory, decrease in concentration of attention and activity, change of mood, disorder of behavior, gait disturbance;
- treatment of dizziness (вертиго) and the related disorders of balance (except for dizzinesses of a vasculomotor and psychogenic origin;
- a cortical myoclonia (monotherapy or as a part of complex therapy);
- stopping of drepanocytic vazookklyuzionny crisis.
At children: treatment of a dyslexia since 8 years in a complex with other methods, including logopedic treatment;
- stopping of drepanocytic vazookklyuzionny crisis.

Route of administration and doses:

Intravenously or intramusculary. Parenteral 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 unconsciousness, at the same time intravenous administration is preferable. Intravenous infusion of a daily dose is carried out through a catheter with a constant speed for 24 h 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: Dextrosums of 5%, 10% or 20%, fructose of 5%, 10% or 20%, sodium of chloride of 0,9%, hydroxyethylstarch of 6% or 10%, Ringera, Mannitolum of 20%. The total amount of solution intended for introduction is defined with clinical testimonies and a condition of the patient. Intravenous administration (for example, urgent treatment of drepanocytic vazookklyuzionny crisis) is carried out within not less than 2 min., the daily dose at the same time is distributed on several introductions with uniform intervals. 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. A symptomatic treatment of a psychoorganic syndrome – 4,8 g/days within the first week, then pass to a maintenance dose – 1,2-2,4 g/days. Treatment of dizziness and the related disturbances of balance – 2,4 - 4,8 g/days. Treatment of a cortical myoclonia – begin 7,2 g/days with a dose, 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 6 months it is necessary to try to reduce a dose or to cancel drug, gradually lowering a dose by 1,2 g/days each 2 days. At insignificant therapeutic effect or its absence treatment is stopped. Drepanocytic vazookklyuzionny crisis (at adults and children). The daily preventive dose makes 160 mg/kg of body weight, divided into 4 equal doses. In the period of crisis – 300 mg/kg/days intravenously, divided into 4 equal doses. Treatment of a dyslexia at children is more senior than 8 years (in a complex with other methods of treatment). The recommended daily dose – 3,2 g, divided into 2 equal doses. Dosing by the patient 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   Clearance of creatinine (ml/min.)        dosing Mode

Norm                                                               >                        80th usual dose
Easy                                                                                50-79 2/3 usual doses in 2-3 receptions
Average                                                                              30-49 1/3 usual doses in 2 receptions
Heavy                                                                              20-30 1/6 usual doses once
Final stage                                              <                           20 it is contraindicated

Features of use:

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, so кат it can cause resuming of attacks.
When stopping venookklyuzionny crisis at a sickemia the dose is less than 160 mg/kg or irregular administration of drug can cause a crisis recurrence.
At long therapy at patients of advanced age regular control of indicators of function of kidneys is recommended, if necessary carry out dose adjustment depending on clearance of creatinine.
Gets through the filtering membranes of devices for a hemodialysis.
During treatment it is necessary to be careful at control of vehicles and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

From the central nervous system: motive disinhibition, irritability, drowsiness, depression, adynamy, headache, sleeplessness, hyperphrenia, balance disturbance, ataxy, aggravation of a course of epilepsy, alarm, hallucinations, confusion of consciousness.
From the alimentary system: nausea, vomiting, diarrhea, abdominal pain.
From a metabolism: increase in body weight.
From sense bodys: вертиго.
From integuments: dermatitis, itch, urticaria.
Allergic reactions: hypersensitivity, Quincke's disease, anaphylactic reactions.
Local reactions: pain in an injection site, thrombophlebitis.
Others: fever, lowering of arterial pressure.
If any of the side effects specified in the instruction are aggravated, or you noticed any other side effects which are not specified in the instruction, report about it to the doctor.

Interaction with other medicines:

At simultaneous use with iodinated hormones of a thyroid gland there can be a confusion of consciousness, irritability and a sleep disorder.
Piracetam in high doses (9,6 g/days) increases anticoagulating effect of indirect anticoagulants at patients with venous thrombosis (more expressed decrease in aggregation of thrombocytes, contents of fibrinogen, Villebrand's factor, viscosity of blood and plasma).
Possibility of change of a pharmacodynamics of piracetam under the influence of other medicines low since 90% of piracetam are removed in not changed look by kidneys.
Piracetam does not oppress P450 cytochrome isoenzymes. Metabolic interaction with 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.
At simultaneous use with the medicines stimulating the central nervous system excessive stimulation of the central nervous system is possible.
At simultaneous use with neuroleptics reduces danger of emergence of extrapyramidal disturbances.

Contraindications:

- hypersensitivity;
- chorea of Gentington;
- gemmoragichesky stroke;
- heavy chronic renal failure (clearance of creatinine less than 20 ml/min.);
- psychomotor excitement at the time of purpose of drug;
- pregnancy, breastfeeding period. 
Use at pregnancy 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. During pregnancy drug is contraindicated.
During treatment it is necessary to cancel breastfeeding.

Overdose:

Symptoms: abdominal pain, diarrhea with blood impurity.
Treatment: symptomatic therapy which can include a hemodialysis (efficiency of 50-60%). There is no specific antidote.

Storage conditions:

In the place protected from light at a temperature from 10 to 25 °C. Freezing is inadmissible. To store in the places unavailable to children. 
Period of validity of 5 years. Not to use after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Solution for intravenous and intramuscular administration of 20%; an ampoule of 5 ml with a knife ampoule, a pack cardboard 10.