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

auxiliary substances for the preparation of a core tablet: Potato starch - 17.00 mg, povidone (polyvinylpyrrolidone, low molecular weight medical 12600 ± 2700) - 9.30 mg magnesium hydroxycarbonate (basic magnesium carbonate aq) - 21.20 mg. calcium stearate (calcium stearic acid 1-water) - 2.50 mg;

excipients for the preparation of the tablet shell: sucrose (white sugar) - 164.64 mg Povidone (polyvinylpyrrolidone, low molecular weight medical 12600 ± 2700) - 1.76 mg magnesium hydroxycarbonate (basic magnesium carbonate aq) - 24.78 mg Colloidal silicon dioxide (Aerosil) - 2.48 mg, titania (titanium dioxide) - 1.23 mg, tropeolin "O" - 0.04 mg, beeswax - 0.07 mg.

Description:

Round biconvex tablets, coated with a coat, yellow. On the cross-section, two layers with a noticeable boundary between them are visible.

Pharmacotherapeutic group:Nootropic agent.

ATX: & nbsp

N.06.B.X.03 Pyracetam

Pharmacodynamics:

Pyracetam, a cyclic derivative of gamma-aminobutyric acid, is a nootropic agent that directly affects the brain, improving cognitive processes such as learning ability, memory, attention, and mental performance. It has a positive effect on the metabolic processes of the brain, acting on the central nervous system in various ways: it changes the rate of spread of excitation in the brain, improves metabolic processes in nerve cells, improves microcirculation, influences the rheological characteristics of the blood without providing a vasodilating effect. Inhibits the aggregation of platelets and restores the elasticity of the erythrocyte membrane, and the ability of the latter to pass through the microcirculatory bed. Reduces the adhesion of red blood cells. At a dose of 9.6 g reduces the level of fibrinogen and von Willebrand factor by (30-40)% and lengthens the bleeding time.It has a protective and restorative effect when brain function is disrupted due to hypoxia, intoxication or trauma: it increases alpha and beta activity, reduces delta activity on the electroencephalogram, reduces the severity and duration of the vestibular nystagmus. Has no sedative, psycho-stimulating effect. If there is a lack of blood supply or acute cerebral ischemia in patients with dementia, local consumption of oxygen and glucose increases.

Pharmacokinetics:

After ingestion, quickly and almost completely absorbed from the gastrointestinal tract and penetrates into various organs and tissues. Bioavailability of the drug is about 100%. After ingestion of a single dose of 2 g, the maximum concentration (C_max) is 40-60 μg / ml, which is achieved in the blood after 30 minutes and after 5 hours in the cerebrospinal fluid. The apparent volume of distribution of piracetam is about 0.6 l / kg. Food intake reduces the maximum concentration by 17% and increases the time to reach it by up to 1.5 hours. It penetrates through the blood-brain and placental barriers. It accumulates in the cerebral cortex 1 to 4 hours after ingestion, mainly in the frontal, parietal and occipital lobes, the cerebellum and basal ganglia.From the cerebrospinal fluid is derived much more slowly than from other tissues. Virtually does not bind to plasma proteins and is not metabolized in the body. 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. The half-life from the plasma is 4-5 hours, from the cerebrospinal fluid - 6-8 hours, from the brain - 7.7 hours. In patients with renal insufficiency, the half-life is prolonged. Hepatic insufficiency does not affect the pharmacokinetics of piracetam.

Indications:

Symptomatic treatment of cognitive impairment not due to dementia. Short-term treatment of cortical myoclonia.

Contraindications:

Hypersensitivity; renal insufficiency (with creatinine clearance less than 20 ml / min), pregnancy, lactation, children's age (up to 3 years), hemorrhagic stroke, anxiety depression (agitated depression), Huntington's chorea, sucrose / isomaltase deficiency, fructose intolerance, glucose-galactose malabsorption.

Pregnancy and lactation:

During pregnancy and lactation, the use of the drug is contraindicated.

Dosing and Administration:

Inside, during meals or on an empty stomach, the tablets should be washed down with liquid (water, juice).

Attention: the latest single dose should be taken no later than 17:00 to prevent sleep disturbances.

The daily dose is 30-160 mg / kg of body weight, the frequency of reception is 2 times a day, if necessary 3-4 times a day. The course of treatment is from 2-3 weeks to 2-6 months. If necessary, repeat the treatment.

With symptomatic treatment of chronic psychoorganic syndrome in the elderly, the drug is prescribed at 1.2-2.4 g / day; The loading dose for the first weeks of therapy is up to 4.8 g / day. Treatment with pyracetamol, if necessary, can be combined with the use of psychotropic, cardiovascular and other drugs.

In cortical myoclonia, treatment starts at 7.2 grams per day, every 3-4 days the dose is increased by 4.8 g per day until a maximum dose of 24 g per day is reached. Treatment continues throughout the period of the illness. Every 6 months, attempts are made to reduce the dose or discontinue the drug, gradually reducing the dose by 1.2 g every 2 days. In the absence of effect or a slight therapeutic effect, treatment is discontinued.

This dosage form is recommended for children from 3 years - 1 tablet 3 times a day. The maximum daily dose is 1.8 g. The course of treatment is from 2 weeks to 2-6 months.

Dosing to patients with impaired renal function

Because the Pyracetam is excreted from the body by the kidneys, caution should be exercised in the treatment of patients with renal insufficiency, dosing is carried out in accordance with the above scheme.

Renal insufficiency	Creatinine clearance (ml / min)	Dosing
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 doses
Heavy	<30	1/6 of the usual dose, once
The final stage	-	Contraindicated

Elderly, the dose is corrected in the presence of renal failure and with prolonged therapy requires monitoring of 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 central nervous system and the peripheral nervous system: motor disinhibition, irritability, drowsiness, depression, asthenia, headache, insomnia, agitation, imbalance, ataxia, exacerbation of epilepsy, anxiety, hallucinations, confusion, convulsions, tremor;

from the digestive system: in isolated cases - nausea, vomiting, diarrhea, abdominal pain (including gastralgia);

from the skin: dermatitis, itching, hives;

from the side of metabolism: increase in body weight (1.29%);

from the organs of hearing: vertigo;

allergic reactions: angioedema, hypersensitivity, anaphylactic reactions;

Other: violation of blood coagulability, worsening of angina, increased sexual activity.

Side effects are most often observed in elderly patients at doses above 2.4 g per day. In most cases, it is possible to regress such symptoms by lowering the dose of the drug.

Overdose:

Symptoms: abdominal pain, diarrhea with an admixture of blood.

Treatment: symptomatic therapy, which may include hemodialysis (efficacy 50-60%). There is no specific antidote.

Interaction:

No interaction with clonazepam, phenytoin, phenobarbital, valproic acid was observed.

Pyracetam in high doses (9.6 g / day) increases the anticoagulant effect of indirect anticoagulants in patients with venous thrombosis (more pronounced decrease in platelet aggregation, fibrinogen content, von Willebrand factor, viscosity of blood and plasma).

Pyracetam does not inhibit cytochrome P450 isoforms CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 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. Metabolic interaction with other drugs is unlikely.

When used simultaneously with iodine-containing hormones and with thyroid extract (TZ + T4), confusion, increased irritability, disorientation and sleep disturbance can occur.

When used simultaneously with drugs that stimulate the central nervous system, excessive stimulation of the central nervous system is possible.

With simultaneous use with neuroleptics reduces the risk of extrapyramidal disorders.

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

Receiving piracetam at a dose of 20 mg / day did not change the maximum and minimum concentrations of antiepileptic drugs in serum (carbamazepine, phenytoin, phenobarbital, valproic acid) in patients with epilepsy receiving a constant dosage.

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

Special instructions:

Due to the influence of piracetam on platelet aggregation, caution is recommended when prescribing a drug to patients with hemostasis disorder, during major surgeries or patients with symptoms of severe bleeding. In the treatment of patients with cortical myoclonia, sudden interruption in treatment should be avoided, which can lead to the resumption of seizures.

With prolonged therapy of elderly patients, regular monitoring of renal function indicators is recommended, if necessary, dose adjustment is performed depending on the results of the study of creatinine clearance.

It penetrates the hemodialysis apparatus through the filter membranes.

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

During the treatment period, care must be taken when driving vehicles, performing work with mechanisms, engaging in other potentially dangerous activities requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:The tablets covered with a cover, 200 mg.

Packaging:

For 60 tablets in a can of light-protective glass or 6 contour squares for 10 tablets together with instructions for use in a pack of cardboard box.

Storage conditions:

In the dark place at a temperature of no higher than 30 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

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

Terms of leave from pharmacies:On prescription

Registration number:P N000349 / 01

Date of registration:24.12.2007

The owner of the registration certificate:ORGANICS, JSC ORGANICS, JSC Russia

Manufacturer: & nbsp

ORGANICS, JSC Russia

Information update date: & nbsp16.09.2015

Illustrated instructions

Instructions

Pyracetam (Pyracetamum)