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

Composition of cap capsule: ferric oxide black oxide - 0.53%, iron oxide red oxide - 0.93%, ferric oxide yellow oxide - 0.2%, titanium dioxide 0.3333%, gelatin up to 100%.

Dosage of 400 mg

Active substance: piracetam - 400 mg;

Excipients: croscarmellose sodium - 12.0 mg, magnesium stearate - 4.0 mg, povidone-K17- 10.0 mg.

Capsules hard gelatinous № 0.

Capsule body composition: titanium dioxide 2.0%, gelatin up to 100%.

Composition of cap capsule: dye azorubin - 0.1445%, dye blue patented - 0.002%, titanium dioxide 2.0%, gelatin up to 100%.

Description:

Dosage 200 mg

Capsule number 2: the body is white, the lid is dark brown opaque.

Dosage of 400 mg

Capsule number 0: the body is white, the lid is dark pink opaque.

The contents of the capsules are a mixture of powder and granules of white or almost white color. It is allowed to compact the contents of the capsule according to the shape of the capsule, disintegrating upon pressing.

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 the drug-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,with 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_1/2lengthened with renal failure (with terminal CRF - up to 59 hours). The pharmacokinetics of pyracetam do not change in patients with hepatic insufficiency.

Indications:

Symptomatic treatment of intellectual-mnestic disorders in the absence of an established diagnosis of dementia.
Reduction of the manifestations of cortical myoclonia in piracetam sensitive patients both as monotherapy and as part of complex therapy.
In order to determine sensitivity to pyracetam in a particular case, a trial treatment course can be conducted.

Contraindications:

Individual intolerance to piracetam or pyrrolidone derivatives, as well as other components of the drug;
Horea Huntington;
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:

Due to the antiaggregant effect, piracetam should be administered with caution to patients with severe hemorrhagic disorders, risk of bleeding, hemostasis disorders; hemorrhagic cerebrovascular disorders in the anamnesis; in patients with surgicalinterventions, including dental interventions; in patients taking anticoagulants and antiplatelet agents, including low doses of aspirin; with chronic renal failure (with a clearance of creatinine 20-80 ml / min).

Pregnancy and lactation:

Controlled studies of the use of the drug during pregnancy were not conducted. Studies in animals have not shown a direct or indirect effect on pregnancy, embryo / fetal development, childbirth or postnatal development. Pyracetam penetrates the placental barrier and into breast milk. The plasma concentration of piracetam in neonates reaches 70-90% of that of the mother. Pyracetam should not be administered during pregnancy. During the lactation period, the issue of stopping breastfeeding should be addressed.

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 begins 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, according to the following formula:

CK (ml / min) = [140 - age (years) х body weight (kg)]/[72 х КК_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 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 nervous system: motor disinhibition, irritability, drowsiness, depression, asthenia, headache, insomnia, agitation, imbalance, ataxia, exacerbation of epilepsy, anxiety, hallucinations, confusion.

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

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

From the side of metabolism: increase in body weight.

From the organs of hearing: vertigo.

From the skin: dermatitis, itching, urticaria.

Allergic reactions: angioedema, hypersensitivity, anaphylactic reactions.

Overdose:

Symptoms: diarrhea with an admixture of blood, pain in the abdomen.

Treatment: 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 piracetam is excreted unchanged by the kidneys.

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 in 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 the level of platelet aggregation, fibrinogen level, von Willebrand factors, viscosity of blood and plasma compared with the use of only indirect anticoagulants).

In vitro piracetam It does not inhibit cytochrome P450 isoenzymes such as CYP1A2, 2B6, 2C8, 2C9, 2C19, 2B6, 2E1 and 4A9 / 11 at concentrations of 142, 426 and 1422 μg / ml. At a concentration of 1422 μg / ml, slight inhibition of CYP2A6 (21%) and SA4 / 5 (11%) was noted, however, the Ki level of these two isoenzymes is sufficient when 1422 μg / ml is exceeded, and therefore metabolic interaction with other drugs is unlikely.

Admission 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, valproic acid).

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.

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 200 mg, 400 mg.

Packaging:

For 5, 10 capsules in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

By 10, 20, 30, 40, 50, 100 or 120 capsules in cans of polymeric for medicines.

One jar or 1, 2, 3, 4, 5, 6, 10 or 12 contour mesh packages together with the instruction for use are placed in a cardboard package (bundle).

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002415

Date of registration:02.04.2014

The owner of the registration certificate:ATOLL, LLC ATOLL, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Information update date: & nbsp16.09.2015

Illustrated instructions

Instructions

Pyracetam (Piracetam)