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

In 1 tablet, coated with a coating, contains: active substance: piracetam - 800 mg or 1200 mg; Excipients: silicon dioxide (14.7 mg or 22.05 mg), magnesium stearate (2.0 mg or 3.0 mg), macrogol 6,000 (20.00 mg or 30.00 mg), croscarmellose sodium (16.70 m or 25.05 mg); opadrai Y-1-7000 (25.6 mg or 38.4 mg) [titanium dioxide (E171) (8.00 mg or 12.00 mg), macrogol 400 (1.60 mg or 2.40 mg), hypromellose 2910 5sP (E464) (16.00 mg or 24.00 mg)], opedrai OY-S-29019 (1.0 mg or 1.50 mg) [hypromellose 2910 50 cP (0.95 mg or 1.425 mg), macrogol 6000 (0.05 mg or 0.75 mg)].

Description:

Oblong white or almost white coated tablets, with a cross-sectional dividing risk on both sides; on one side of the tablet to the right and left of the risks of engraving "N".

Pharmacotherapeutic group:Nootropic agent.

ATX: & nbsp

N.06.B.X.03 Pyracetam

Pharmacodynamics:

Pyracetam is a nootropic drug that directly improves the functions performed by the brain. The drug has an effect on the central nervous system in various ways: it modifies neurotransmission in the brain, improves metabolic conditions that promote neuronal plasticity, improves microcirculation, influencing the rheological characteristics of the blood and not causing vasodilation.

Prolonged or short-term use of piracetam in patients with cerebral dysfunction increases attention concentration and improves cognitive function, which is manifested by significant changes in the electroencephalogram (increase in α and β-activity, decrease in δ-activity).

The drug helps restore cognitive abilities after various cerebral injuries due to hypoxia, intoxication or electroconvulsive therapy.

Pyracetam is indicated for the treatment of cortical myoclonus both as monotherapy and as part of complex therapy.

Reduces the duration of the provoked vestibular neuronitis. Pyracetam inhibits increased aggregation of activated platelets and, in the case of abnormal rigidity of erythrocytes, improves their deformability and ability to filter.

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 (AUC) is 30% larger 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 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:

Symptomatic treatment of memory disorders, intellectual disorders in the absence of a diagnosis of dementia.
Nootropil has the ability to reduce manifestations of cortical myoclonus in sensitive patients.

To determine the sensitivity to pyracetam in a particular case, a trial treatment course can be performed.

Contraindications:

Hypersensitivity to pyracetam or pyrrolidone derivatives, as well as other components of the drug.
Horea Huntington.
Acute disturbance of cerebral circulation (hemorrhagic stroke).
The final stage of chronic renal failure.

Pregnancy and lactation:

Preclinical studies did not show 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.

In memory disorders, intellectual disorders: 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.

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 (K_serum), 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	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	<30	1/6 of the usual dose once
The final stage	-	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 dysfunction 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: hyperkinesia (1.72%), ataxia, imbalance, exacerbation of epilepsy, headache, insomnia, asthenia (0.23%), trembling.

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

From the organs of hearing: Vertigo.

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

On the part of the reproductive system: increased sexual desire.

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.

When treating patients on a hyponatrial diet, it is recommended that the piracetam tablets in a dose of 24 g contain 46 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:

The tablets covered with a cover. 800 mg and 1200 mg.

Packaging:

Tablets coated with 800 mg.

15 tablets in a PVC blister / aluminum foil. 2 blisters with instructions for use in a cardboard pack.

The tablets covered with a cover of 1200 mg.

10 tablets in a PVC blister / aluminum foil. 2 blisters with instructions for use in a cardboard pack.

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:

4 years.

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

Terms of leave from pharmacies:On prescription

Registration number:П N011926 / 03

Date of registration:18.03.2009

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

Manufacturer: & nbsp

UCB Pharma, S.A. Belgium

Representation: & nbspYUSB FARMA LLC YUSB FARMA LLC Russia

Information update date: & nbsp15.10.2015

Illustrated instructions

Instructions

Nootropil® (Nootropil®)