Nootropil - instructions for use, dose, side effects, contraindications

Pyracetam binds to polar heads of phospholipids and forms mobile complexes of pyracetam-phospholipid. As a result, the two-layer structure of the cell membrane is restored and its stability, which in turn leads to the restoration of the three-dimensional structure of membrane and transmembrane proteins and the restoration of their function.

On the neuronal level piracetam facilitates various types of synaptic transmission, having a predominant effect on the density and activity of postsynaptic receptors (data obtained in animal studies). Pyracetam improves such functions as training, memory, attention and consciousness, without having a sedative or psychostimulating effect.

The hemorheological effects of pyracetam are related to its effect on erythrocytes, platelets and the vessel wall.

In patients with sickle-cell anemia piracetam increases the ability of erythrocytes to deform, reduces the viscosity of the blood and prevents the formation of "coins". In addition, it reduces aggregation of platelets without significantly affecting their number.

In animal studies, it has been shown that piracetam inhibits spasm of blood vessels and counteracts various vasospalic substances.

In studies on healthy volunteers piracetam reduced the adhesion of erythrocytes to the vascular endothelium and stimulated the production of prostacyclin by a healthy endothelium.

Pharmacokinetics:

Suction. After oral administration piracetam quickly and almost completely absorbed from the gastrointestinal tract. The bioavailability of piracetam is close to 100%. After a single dose at a dose of 3.2 g, the maximum concentration (C_max) is 84 μg / ml, after repeated intake of 3.2 mg 3 times a day - 115 μg / ml and is achieved after 1 hour in blood plasma and after 5 hours in cerebrospinal fluid. Eating reduces C_max by 17% and increases the time of its achievement (T_max) up to 1.5 hours. In women with piracetam at a dose of 2.4 g C_max and the area under the concentration-time curve (AUC) is 30% higher than that of men.

Distribution. The volume of distribution (V_d) is about 0.6 l / kg. Pyracetam penetrates through blood-brain and placental barriers. In animal studies, it was found that piracetam selectively accumulates in the tissues of the cerebral cortex, mainly in the frontal, parietal and occipital lobes, in the cerebellum and basal nuclei.

Metabolism. It does not bind to blood plasma proteins, it is not metabolized in the body.

Excretion. The half-life (T_1/2) is 4-5 hours from the blood plasma and 8.5 hours from the cerebrospinal fluid. The half-life does not depend on the route of administration. 80-100% of pyracetam is excreted by the kidneys unchanged by glomerular filtration. The total clearance of piracetam in healthy volunteers is 80-90 ml / min. T_1/2 lengthened with renal failure (with terminal chronic renal failure - up to 59 hours). The pharmacokinetics of pyracetam does not change in patients with hepatic insufficiency.

Indications:

In adults

Symptomatic treatment of psycho-organic syndrome, in particular in elderly patients, accompanied by a decrease in memory, dizziness, reduced concentration and decreased activity, mood changes, behavioral disorder, gait disturbance (these symptoms may be early signs of age-related diseases such as Alzheimer's and senile dementia Alzheimer's type);

Treatment of dizziness and related imbalance, with the exception of vasomotor and psychogenic dizziness;

Complex therapy and monotherapy of cortical myoclonia;

Prevention of sickle-cell vasocclusive crisis.

Children

Treatment of dyslexia (in conjunction with other methods);

Prevention of sickle-cell vasocclusive crisis.

Contraindications:

Individual intolerance to piracetam or pyrrolidone derivatives, as well as other components of the drug;
Psychomotor agitation at the time of prescribing;
Horea Gentingona;
Acute disorders of cerebral circulation (hemorrhagic stroke);
The final stage of renal failure (with creatinine clearance less than 20 ml / min);
Children under 3 years.

Carefully:

Violation of hemostasis;
Extensive surgical interventions;
Severe bleeding;
Chronic renal failure (with creatinine clearance 20-80 ml / min).

Pregnancy and lactation:

Controlled studies of the use of the drug during pregnancy were not conducted. Pyracetam penetrates the placental barrier and into breast milk. The concentration of the drug in newborns reaches 70-90 % of its concentration in the blood of the mother. Pyracetam should not be administered during pregnancy.It should be refrained from breastfeeding with the appointment of a woman piracetam.

Dosing and Administration:

Inside.

During meals or on an empty stomach, squeezed with liquid.

Symptomatic treatment of psycho-organic syndrome: 2.4 - 4.8 g / day in 2-3 divided doses.

Treatment of dizziness and associated imbalance: 2.4 - 4.8 g / day in 2-3 divided doses.

Treatment of cortical myoclonia: begin with a dose of 7.2 g / day, every 3-4 days the dose is increased by 4.8 g / day until a maximum dose of 24 g / day in 2-3 doses. Treatment continues: throughout the period of the disease. Every 6 months, attempts should be made to reduce the dose or discontinue the drug, gradually reducing the dose by 1.2 g / day every 2 days.

Prevention of sickle-cell vasocclusive crisis.

The daily preventive dose is 160 mg / kg body weight divided into 4 equal doses.

Treatment of dyslexia in children (in combination with other methods of treatment): the recommended daily dose for children from 8 years and adolescents - 3.2 g, divided into 2 doses.

Dosing to patients with impaired renal function:

the dose should be adjusted depending on the amount of creatinine clearance (CC):

The creatinine clearance for men can be calculated based on the serum creatinine concentration, according to the following formula:

CK (ml / min) = [140 - age (years) x body weight (kg)] / [72 x KK_serum (mg / ml)]

The creatinine clearance for women can be calculated by multiplying the obtained value by a factor of 0.85.

Renal insufficiency	CK (ml / min)	Dosing regimen
Norm	>80	usual dose
Lightweight	50-79	2/3 of the usual dose in 2-3 doses
Average	30-49	1/3 of the usual dose in 2 divided doses
Heavy	20-30	1/6 of the usual dose once
The final stage	<20	contraindicated

Elderly patients are adjusted the dose in the presence of renal failure, with prolonged therapy, it is necessary to monitor the functional state of the kidneys.

Dosing to patients with impaired liver function: patients with a dysfunction of the liver do not need a dose adjustment. Patients with impaired function of the kidneys and liver, dosing is carried out according to the scheme (see the section "Dosing to patients with impaired renal function").

Side effects:

From the nervous system: motor disinhibition (1.72%), irritability (1.13%), drowsiness (0.96%), depression (0.83%), asthenia (0.23%).

In postmarketing practice, the following side effects were observed: the frequency of which was not established (due to insufficient data): headache, insomnia, agitation,imbalance, ataxia, exacerbation of epilepsy, anxiety, hallucinations, confusion.

From the digestive system: nausea, vomiting, diarrhea, abdominal pain (including gastralgia).

From the side of metabolism: increase in body weight (1.29%).

From the organs of hearing: Vertigo.

From the skin: dermatitis, itching, urticaria.

Allergic reactions: angioedema, hypersensitivity, anaphylactic reactions.

Overdose:

A single case of development of diarrhea in the form of diarrhea with blood and pain in the abdominal region was registered with oral administration in a daily dose of 75 g. Apparently, this was due to the use of a large total dose of sorbitol, which is part of the drug previously for the dosage form solution for reception inside.

If there is a significant overdose, rinse the stomach or induce vomiting. It is recommended to carry out symptomatic therapy, which may include hemodialysis. There is no specific antidote. The efficacy of hemodialysis for piracetam is 50-60%.

Interaction:

The possibility of changing the pharmacokinetics of piracetam under the influence of other drugs is low, because 90% of the drug is excreted unchanged in the urine.

At simultaneous application with hormones of a thyroid gland the reports on confusion of consciousness, irritability and disturbance of a dream are marked.

According to a published study of patients with recurrent venous thrombosis piracetam in a dose of 9.6 g / day improves the effectiveness of indirect anticoagulants (there was a more pronounced decrease in platelet aggregation, fibrinogen concentration, von Willebrand factors, viscosity of blood and plasma compared with the use of only indirect anticoagulants).

Pyracetam does not inhibit cytochrome P450 isoenzymes. Metabolic interaction with other drugs is unlikely.

Receiving piracetam at a dose of 20 g / day for 4 weeks did not change the maximum concentration in the serum and the area under the concentration-time curve of antiepileptic drugs (carbamazepine, phenytoin, phenobarbital, valproate).

Joint intake with alcohol did not affect the concentration of piracetam in the serum; the concentration of ethanol in the serum did not change with the intake of 1.6 g of piracetam.

Special instructions:

In the treatment of cortical myoclonia, sudden interruption in treatment should be avoided, as this may cause the resumption of seizures.

In the treatment of sickle cell anemia, a dose of less than 160 mg / kg or an irregular intake of the drug may cause an exacerbation of the disease.

It penetrates the hemodialysis apparatus through the filter membranes.

Effect on the ability to drive transp. cf. and fur:

During the treatment period, care should be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Capsules 400 mg.

Packaging:

For 15 capsules in a planar cell package (blister) [PVC / aluminum foil]. For 4 blisters together with instructions for use in a cardboard bundle.

Storage conditions:

In a dry place, at a temperature of no higher than 25 ° C.

Keep the medicine out of the reach of children!

Shelf life:

5 years

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N014242 / 02

Date of registration:25.11.2008

The owner of the registration certificate: YUSB Farma S.A. YUSB Farma S.A. Belgium

Manufacturer: & nbsp

UCB Pharma, S.A. France

Representation: & nbspYUSB FARMA LLC YUSB FARMA LLC Russia

Information update date: & nbsp15.10.2015

Illustrated instructions

Instructions

Nootropil® (Nootropil®)