Piracetam

General characteristics. Structure:

Active agent piracetam - 1000 mg;
excipients: dihydrophosphate sodium a dihydrate - 4,00 mg, hydrophosphate potassium trihydrate - 0,25 mg, water for injections - to 5,0 ml.
Description: transparent colourless or with slightly brownish shade solution.

Pharmacological properties:

Pharmacodynamics. Nootropic means. Piracetam is to the cyclic derivatives of piperidic acid (GAMK) which are directly influencing a brain. Improves cognitive (cognitive) processes (ability to training, memory, attention), intellectual working capacity. Piracetam exerts impact on the central nervous system in various ways: izmenyav-the speed of spread of activation in a brain, improves microcirculation and metabolic processes in nervous cells, influences rheological characteristics of blood and does not cause vasodilating action. Mose improves bonds between hemispheres head (and and synaptic conduction in neocourt hiccuped ny struk1urakh, increases intellectual working capacity, improves a brain blood stream. Reduces expressiveness and duration of a vestibular nystagmus.

Pharmacokinetics. The elimination half-life (T1/2) from a blood plasma makes 4-5 h and 8.5 h of cerebrospinal fluid. T1/2 is extended at a renal failure. The pharmacokinetics of piracetam does not change at patients with a liver failure.

Gets through the hematoencephalic, placental barriers and membranes used at a hemodialysis. Selectively collects in tissues of a cerebral cortex, it is preferential in frontal, parietal and occipital lobes, and also in a cerebellum and basal gangliya. Does not contact proteins of a blood plasma and not мегаболизируегся in an organism. 80-100% of piracetam are removed by kidneys in an invariable look by renal filtering. The renal clearance of piracetam at healthy volunteers makes 86 ml/min.

Indications to use:

- A symptomatic treatment of a psychoorganic syndrome (including at elderly patients with decrease is the memory reduced by concentration of attention and the general activity, changes of mood, disorder of behavior, gait disturbance, and 1akzhe at patients with Alzheimer's disease and senile dementia of altsgeymerovsky type);
- treatment of effects of an ischemic stroke, such as disturbances of the speech, disturbances of the emotional sphere, for increase in motor and mental performance;
- for treatment of an abstinence syndrome and a psychoorganic syndrome at an alcoholism;
- comas (and during recovery), including after injuries and intoxications of a brain;
- for treatment of dizziness and the related disorders of balance (except for cases of dizziness vasculomotor and psychogenic origins);
- treatment of a cortical myoclonia (both in the form of monotherapy, and as a part of a combination therapy);
- a sickemia (as a part of a combination therapy);
- treatment of a dyslexia at children (in a complex with other methods).

Route of administration and doses:

Intravenously or intramusculary.

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%. a dextran (average molecular weight 35000-45000) (10% in solution of sodium of chloride of 0,9%), Ringera, the radio tape recorder of 20%.

The total amount of solution intended for introduction is defined with clinical testimonies and a condition of the patient.

Bolyusny intravenous administration (for example, at removal of an abstinence syndrome at alcoholism, urgent treatment of a sickemia, etc.) is carried out within not less than 2 min., the daily dose at the same time is distributed on several introductions (2-4) with uniform 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 at children and patients with reduced body weight. 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 it intravenous use.

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

At treatment of a chronic psychoorganic syndrome appoint drug in a dose of 2,4-4,8 g/days.

At treatment of effects of an ischemic stroke piracetam it is necessary to appoint 4,8-12 g/days in a dose.

At treatment of comas, and also difficulties perception at persons with brain grams the initial dose makes 9-12 g/days supporting — 2 g/days. It is necessary to continue treatment not less than 3 weeks.

At treatment of an alcoholic abstinence syndrome the dose of drug reaches 12 g/days. The maintenance dose makes 2,4 g/days. At treatment of dizziness and the related disturbances of balance the dose makes 2.D-4.8 g/days.

At treatment of a cortical myoclonia treatment 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.

Further pass to a peroral form of a tiratsetam. Treatment by piracetam is continued throughout the entire period of a disease. Each 6 months it is 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.

At treatment of a sickemia in the period of crisis the dose makes up to 300 mg/kg intravenously, divided into 4 equal doses. The daily preventive dose makes 160 mg/kg of body weight, divided into 4 equal doses.

At treatment of a dyslexia the recommended daily dose for children of 8 years and teenagers - 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 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 creatine (ml/min.)              Dosing
          norm                                         > 80th                                  usual dose
          easy                                                                  50-79 2/3 usual doses on 2-3 introductions
          average                                                             30-49 1/3 usual doses on 2 introductions
          heavy                                                               20-29 1/6 usual doses once
          final stage                             <20                                   it is 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 abnormal liver functions do not need dose adjustment. To patients 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:

Due to the influence of piracetam on aggregation of thrombocytes, care at purpose of drug is recommended to patients with disturbance of a temostaz, during big hirur! ichesky operations or to patients with symptoms heavy bleedings. At treatment of patients with a cortical myoclonia it is necessary to avoid sharp interruption of treatment that can cause resuming of attacks.

At long therapy at elderly patients regular control of indicators of function of kidneys is recommended, if necessary carry out dose adjustment depending on results of a research of clearance of creatine. Gets through the filtering membranes of devices for a hemodialysis.

Influence on ability to manage the vehicle or potentially dangerous mechanisms

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.

Side effects:

From the central nervous system (CNS) and peripheral nervous system: motive disinhibition, irritability, drowsiness, depression, adynamy. These side effects arise at the patients of advanced age receiving drug in a dose more than 2,4 g/days more often, In most cases it is possible to achieve regress of similar symptoms, having lowered a drug dose. In some cases dizziness, a headache, an ataxy, an aggravation of a course of epilepsy, extrapyramidal disturbances, a tremor, disbalance, decline in the ability to concentration of attention, sleeplessness, excitement, alarm, hallucinations, increase in a libido can be noted.

From cardiovascular system: in some cases decrease or increase in arterial pressure.

From a metabolism: increase in body weight (there are at patients elderly age, more than 2,4 g/days receiving drug in a dose more often).

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

From integuments: dermatitis, itch, rash. Allergic reactions: Quincke's disease.

Interaction with other medicines:

At combined use with hormones of a thyroid gland and antipsychotic drugs (neuroleptics) increases their efficiency. At co-administration with neuroleptics piracetam reduces danger of emergence of extrapyramidal disturbances. At simultaneous use with the medicines exerting the stimulating impact on TsNS strengthening of the stimulating influence on TsNS is possible.

Interaction with clonazepam, Phenytoinum, phenobarbital, valproic acid is noted.

High doses (9,6 g/days) of piracetam increase efficiency of indirect anticoagulants at patients with venous thrombosis (big braking of aggregation of thrombocytes, decrease in concentration of fibrinogen, Villibrand'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.

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

Joint reception with alcohol did not influence concentration of piracetam in serum and concentration of alcohol in blood serum did not change at reception of 1.6 g of piracetam.

Contraindications:

- Hypersensitivity to piracetam, derivatives of a pirrolidon and other components of drug;
- acute phase of a hemorrhagic stroke;
- the expressed renal failures (at clearance of creatine less than 20 ml/min.);
- psychomotor excitement at the time of purpose of drug;
- chorea of Gentington;
- children's возрасг up to 3 years.

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

Use at pregnancy and during breastfeeding

Controlled researches on drug use piracetam at 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 piracetam should not be appointed during pregnancy. It is necessary to refrain from breastfeeding at purpose of drug in the period of a lactation.

Overdose:

Symptoms: strengthening of expressiveness of dozozavisimy side effects.

Treatment: symptomatic which can include a hemodialysis.

Efficiency of a hemodialysis makes 50-60%.

There is no specific antidote.

Storage conditions:

At a temperature not above 25 °C. To store in the place, unavailable to children. A period of validity - 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 200 mg/ml. On 5 ml in ampoules of colourless glass. On 5 ampoules in a blister strip packaging. On 1 or 2 blister strip packagings together with the application instruction in a pack from a cardboard.