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

In 100 ml solution for oral administration contains: active substance: piracetam - 20.0 g; Excipients: glycerol 85% 27.0 g, sodium saccharinate 0.300 g, sodium acetate 0.200 g, methyl parahydroxybenzoate 0.135 g, propyl parahydroxybenzoate 0.015 g, apricot flavor 0.030 g, caramel flavor 0, 015 g, acetic glacial acid 0, 016 g + -5%, water purified 62.10 g + - 5%.

Description:

Transparent colorless liquid.

Pharmacotherapeutic group:Nootropic agent.

ATX: & nbsp

N.06.B.X.03 Pyracetam

Pharmacodynamics:

The active component is piracetam, a cyclic derivative of gamma-aminobutyric acid (GABA).

The available data indicate that the main mechanism of action of pyracetam is not cell-specific or organ-specific.

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 cognitive functions such as learning, memory, attention and cognitive abilities without exerting sedative or psychostimulating effects.

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 g 3 times a day - 115 μg / ml and is achieved after 1 hour in the serum and after 5 hours in the 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 (AIJC) at 30 % more than 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 h for serum and 8.5 h for 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;

Treatment of cortical myoclonus as a monotherapy or as part of a complex therapy;

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 Huntington;
Acute disorders of cerebral circulation (hemorrhagic stroke);
The final stage of renal failure (with creatinine clearance less than 20 ml / min);
Age before 1 year.

Pregnancy and lactation:

Studies in animals have not shown a direct or indirect effect on pregnancy, embryo / fetal development, childbirth or postnatal development. 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 is necessary to refrain from breastfeeding while prescribing a piracetam to a woman.

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: treatment starts 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: dose should be adjusted depending on the amount of creatinine clearance (CC): Creatinine clearance for men can be calculated based on the serum creatinine concentration (K_serum), according to the following formula: [140 - age (years)] х mass

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	the usual dose of 2-4 admission
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 side of the blood and lymphatic system: hemorrhagic disorders.

From the immune system: anaphylactoid reactions, hypersensitivity.

Metabolic disorders and eating disorders: increase in body weight (1.29%).

From the side of the psyche: excitement, nervousness (1.13%), anxiety, depression (0.83%), hallucinations, confusion, drowsiness (0.96%).

From the nervous system: hyperkinesis (1.72%), ataxia, imbalance, exacerbation of epilepsy, headache, insomnia, asthenia (0.23%).

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

From the organs of hearing: Vertigo.

From the skin: dermatitis, itching, hives, angioedema.

Overdose:

A single case of development of diarrhea in the form of diarrhea with blood and pain in the abdomen with taking the drug inside at a daily dose of 75 g. It seems that this was due to the use of a large total dose of sorbitol, which was previously part of the solution for oral administration.

In case of 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 does not change the dose of acenocumarol necessary to achieve INR (international normalized ratio) 2.5-3.5, but compared with the effects of acenocoumarol alone, the addition of pyracetam at a dose of 9.6 g / day significantly reduces platelet aggregation, p-thromboglobin release, fibrinogen concentration and von Willebrand factor (VIII: C; VIII: vW: Ag; VIII: vW: RCo), and blood and serum viscosity.

In concentrations of 142, 426 and 1422 mg / ml piracetam does not inhibit cytochrome P450 isoenzymes.

For the concentration of 1422 mg / ml, minimal inhibition of CYP 2A6 (21%) and SA4 / 5 (11%) was observed. However, the normal values of the inhibition constant (Ki) can probably be achieved at a higher concentration. Thus, the metabolic effect of piracetam with other drugs is unlikely. Admission of piracetam at a dose of 20 g / day for 4 weeks in patients with epilepsy who received stable doses of antiepileptic drugs did not change the maximum serum concentration and AUC (area under the curve) of antiepileptic drugs (carbamazepine, phenytoin, phenobarbital and 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:

Due to the antiaggregant effect (section pharmacodynamics), piracetam should be administered with caution to patients with severe hemorrhagic disorders, risk of bleeding (eg, gastric ulcer), haemostasis disorders, hemorrhagic cerebrovascular disorders in the history, in patients with surgical interventions, including dental interventions, in patients taking anticoagulants and antiplatelet agents, including low doses of aspirin.

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.

When treating patients on a hyponatrial diet, it is recommended that the solution of piracetam for oral administration at a dose of 24 g contains 80.5 mg of sodium.

Because the piracetam is excreted via the kidneys, caution should be exercised when prescribing the drug to patients with renal insufficiency.

Long-term treatment of elderly patients requires regular monitoring of creatinine clearance, a dose adjustment may be required.

Piracetam penetrates the filtration membranes of hemodialysis apparatus.

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:

Solution for oral administration 200 mg / ml.

Packaging:

125 ml in a vial of transparent dark glass (type 3), sealed with a tamper-proof polypropylene with a plastic measuring cup. The bottle is enclosed in a cardboard box together with instructions for use.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep the medicine out of the reach of children!

Shelf life:

4 years.

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

Terms of leave from pharmacies:On prescription

Registration number:П N011926 / 02

Date of registration:25.06.2007

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

Manufacturer: & nbsp

NEXTPHARMA, SAS France

Representation: & nbspYUSB FARMA LLC YUSB FARMA LLC Russia

Information update date: & nbsp15.10.2015

Illustrated instructions

Instructions

Nootropil® (Nootropil®)