Piracetam

General characteristics. Structure:

Active ingredient: 400 mg of piracetam.

Excipients: calcium stearate, magnesium hydroxycarbonate. Gelatinous solid capsules: gelatin, the water purified methylparahydroxybenzoate (нипагин), пропилпарагидроксибензоат (нипазол), titanium dioxide.

The medicine which is favorably influencing vascular brain characteristics.

Pharmacological properties:

Pharmacodynamics. Piracetam is nootropic means. Exerts positive impact on exchange processes of a brain: increases concentration of ATP in brain fabric, strengthens biosynthesis of RNA (RNA) and phospholipids, stimulates glycoclastic processes, strengthens glucose utilization.

Improves integrative activity of a brain, promotes memory consolidation, facilitates training process.

Pharmacodynamics. Drug changes the speed of spread of activation in a brain, improves microcirculation, without having at the same time vasodilating effect, suppresses aggregation of the activated thrombocytes. Has protective action at the injuries of a brain caused by a hypoxia, intoxications, an electroshock; the alpha strengthens - and beta activity, reduces delta activity on EEG, reduces expressiveness of a vestibular nystagmus.

Improves bonds between cerebral hemispheres and synaptic conduction in neocortical structures, increases intellectual working capacity, improves a brain blood stream. Practically has no sedative and psychogogic influence.

Pharmacokinetics. After intake it is well soaked up and gets into various bodies and fabrics. Bioavailability makes about 95%. Time of achievement of the maximum concentration in a blood plasma makes 30-60 min.

Gets through hematoencephalic and placental barriers, and also through the membranes used at a hemodialysis. At a research on animals it is revealed that piracetam selectively collects in tissues of a cerebral cortex, it is preferential in frontal, parietal and occipital lobes, in a cerebellum and basal gangliya.

Practically it is not metabolized in an organism, does not contact proteins of a blood plasma. Out of cerebrospinal fluid it is brought much more slowly, than out of other fabrics that testifies to high tropism to brain fabric. The elimination half-life (T1/2) makes 4,5 h (7,7 h - of a brain). 2/3 piracetams are removed by kidneys in not changed look by renal filtering during 30 h. The elimination half-life is extended at a renal failure. The pharmacokinetics of piracetam does not change at patients with a liver failure.

Indications to use:

Piracetam is applied generally in neurologic, psychiatric and narcological practice.
• A symptomatic treatment of a psychoorganic syndrome, in particular at the elderly patients suffering from decrease in the memory, dizziness lowered by concentration of attention and the general activity, lability of mood, disorders of behavior, gait disturbance, and also at patients with Alzheimer's disease and senile dementia like Alzheimer.
• Effects of an ischemic stroke, such as disturbances of the speech, disturbances of the emotional sphere, for increase in motor and mental performance.
• An alcoholism — for treatment of psychoorganic and abstinent syndromes.
• The recovery period after craniocereberal injuries and intoxications of a brain.
• Dizzinesses and the related disorders of balance, except for dizziness of a vasculomotor and psychogenic origin.
• As a part of complex therapy of low learnability at children with a psychoorganic syndrome.

Route of administration and doses:

Piracetam is accepted inside during meal or on an empty stomach, washing down with liquid. Attention: to accept the last single dose no later than 17:00 for prevention of sleep disorders.

Daily dose — 30 — 160 mg/kg of body weight, frequency rate of reception — 2 times a day, if necessary — 3 — 4 times a day. 

The course of treatment is continued from 2-3 weeks to 2-6 months. If necessary the course of treatment is repeated.

At therapy of a psychoorganic syndrome at elderly appoint 1,2-2,4 g/days (3-6 capsules/days). A load dose within the first weeks of therapy - to 4,8 g/days (the 12th capsules/days). Treatment by piracetam, if necessary, can be combined using psychotropic, is warm — vascular and other medicines. 

At treatment of effects of a stroke: appoint piracetam in a dose of 4,8 g/days.

At treatment of dizziness appoint 2,4-4,8 g/days (6-12 capsules/days in 2-3 receptions).

At alcoholism: A maintenance dose — 2,4 g/days (6 capsules a day).

At dizziness and the related disorders of balance — 2,4 — 4,8 g/days.

To children for correction of low learnability - treatment appoint 3,3 g/days in a dose. Treatment is continued during all academic year.

Dosing by the patient with a renal failure. As piracetam is removed from an organism by kidneys, at purpose of drug patients with a renal failure and to patients of advanced age should be careful and korrigirovat a dose depending on the size of clearance of creatinine, according to the provided scheme:

Is absent (norm)	More than 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	20-30	1/6 usual doses, once
End-stage	Less than 20	Contraindicated

The dose korrigirutsya by the elderly patient in the presence of a renal failure. At long therapy it is necessary to control a functional condition of kidneys. Dosing by the patient with an abnormal liver function.

Patients with an abnormal liver function do not need dose adjustment. Patients with an abnormal liver function and kidneys — dosing is carried out according to the scheme (cm the section "Dosing 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 hemostasis, during big surgeries or the patient with symptoms of heavy bleeding.

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 of 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 creatinine.

Gets through the filtering membranes of devices for a hemodialysis.

Influence on control of vehicles and 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.

Use at pregnancy and in the period of a lactation. 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, drug should not be appointed during pregnancy. It is necessary to refrain from breastfeeding at appointment to the woman of piracetam.

Side effects:

Side effects are most often noted at elderly patients at doses higher than 2,4 g/days.

From TsNS and peripheral nervous system: motive disinhibition (1,72%), irritability (1,13%), drowsiness (0,96%), depression (0,83%), adynamy (23%). These side effects arise at the patients of advanced age receiving drug in a dose more 2,4g/days more often. In most cases it is possible to achieve regress of similar symptoms, having lowered a drug dose. In isolated 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 sexuality.

From outside warmly — vascular system: seldom — decrease or increase in arterial pressure, deterioration in a course of stenocardia.

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

From a metabolism — increase in body weight (1,29%) — arises at the patients of advanced age receiving drug in a dose more 2,4g/days more often.

From integuments — dermatitis, an itch, rashes, a Quincke's disease.

Interaction with other medicines:

Increases efficiency of hormones of a thyroid gland, antipsychotic medicines (neuroleptics).

At simultaneous use with the medicines stimulating the central nervous system excessive stimulation of the central nervous system is possible.

At appointment with neuroleptics reduces danger of emergence of extrapyramidal disturbances.

Therapy by piracetam if necessary can be combined using psychoactive, cardiovascular and other medicines.

Interaction with klonazepany, Phenytoinum, phenobarbital, sodium Valproatum is noted.

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

In vitro piracetam does not oppress P450 cytochrome isoenzymes, such as CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 and 4A9/11 in concentration of 142, 426 and 1422 mkg/ml. at concentration of 1422 mkg/ml small oppression of CYP2A6 (21%) and 3A4/5 is noted (11%), however the Ki level of these two isoenzymes is sufficient at exceeding of 1422 mkg/ml in this connection metabolic interaction with other drugs is improbable.

Reception 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, фетионин, phenobarbital, Valproatum) at the patients with epilepsy receiving a constant dosage.

Joint reception with alcohol did not influence the level of 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 or derivatives of pyrrolidine, and also other components of drug.
• Chorea of Gentington.
• Final stage of a renal failure (clearance of creatinine less than 20 ml/min.).
• Acute disorder of cerebral circulation (hemorrhagic stroke).
• 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:

After oral administration of piracetam in a dose of 75 g the dispeptic phenomena, such as diarrhea with blood, abdominal pains are noted.

Treatment: Right after administration of drug inside it is possible to wash out a stomach or to cause artificial vomiting. 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 dry, protected from light place, at a temperature not over 25 ºС. To store in the place, unavailable to children. Period of validity 3,5 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Capsules on 400 mg. On 10 capsules in a blister strip packaging. 6 blister strip packagings together with the application instruction in a pack from a cardboard.