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

Excipients of the core tablet: povidone -10,10 mg, potato starch - 17,15 mg, magnesium hydroxycarbonate (magnesium carbonate basic) - 20.35 mg, calcium stearate monohydrate (calcium stearate 1-water) - 2.40 mg.

Shell accessories: sugar - 118.768 mg, povidone - 1.402 mg, magnesium hydroxycarbonate (magnesium carbonate basic) - 23.80 mg, silicon dioxide colloid (aerosil) - 1.78 mg, talcum - 0.044 mg, titanium dioxide - 3.93 mg , beeswax - 0.028 mg, paraffin liquid (liquid petroleum jelly) - 0,028 mg, quinoline yellow colorant - 0,22 mg.

Description:Round tablets, biconvex, coated with yellow color.

Pharmacotherapeutic group:Nootropic agent.

ATX: & nbsp

N.06.B.X.03 Pyracetam

Pharmacodynamics:

Cyclic derivative of gamma-aminobutyric acid, nootropic agent; acts directly on the brain, improving cognitive (cognitive) processes, such as learning ability, memory, attention, and mental performance. It influences 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.

Improves the connection between the cerebral hemispheres and synaptic conductivity in neocortical structures, improves cerebral blood flow.

Inhibits the aggregation of platelets and restores the configuration properties of the outer membrane of rigid red blood cells, as well as the ability of the latter to pass through the vessels of the microcirculatory bed. At a dose of 9.6 g reduces the concentration of fibrinogen and von Willebrand factor by 30-40% and prolongs the time of bleeding. It has a protective and restoring effect when the brain function is impaired due to hypoxia and intoxication.

Reduces the severity and duration of the vestibular nystagmus.

Pharmacokinetics:

Absorption at ingestion is fast and complete. Bioavailability is about 100%. After a single oral dose of 3.2 g, the maximum concentration (C_max) - 84 mcg / ml, after repeated (3.2 g 3 times a day) - 115 mcg / ml, the time required to reach the maximum concentration (TC_max) in plasma - 1 hour, cerebrospinal fluid (CSF) - 5 hours. Food intake reduces C_max by 17% and increases the TCA to 1.5 h. In women C_max and the area under the "concentration time" (AUC) curve after taking 2.4 g is 30% higher than in men.

The apparent volume of distribution is about 0.6 l / kg. Penetrates through blood-brain and placental barriers; is removed during hemodialysis. In animal experiments, it selectively accumulates in the tissues of the cerebral cortex, mainly in the frontal, parietal and occipital lobes, in the cerebellum and basal nuclei.

Does not bind to plasma proteins, it is not metabolized. The half-life (T_1/2) - 4-5 hours from the blood plasma and 8.5 hours - from the CSF. 80-100 % Piracetam is excreted by the kidneys in an unchanged form by glomerular filtration. The total clearance is 80-90 ml / min. T_1/2prolonged with chronic renal failure (with terminal chronic renal failure - up to 59 hours).Hepatic insufficiency does not affect the pharmacokinetics of piracetam.

Indications:

In adults: symptomatic treatment of psycho-organic syndrome, accompanied by a decrease in memory, a decrease in concentration and activity, mood changes, behavioral disorder, gait disturbance; treatment of dizziness (vertigo) and associated disorders of equilibrium (with the exception of vertigo of the vasomotor and psychogenic origin); cortical myoclonus (monotherapy or as part of complex therapy); prophylaxis of sickle-cell vaso-occlusive crisis.

In children: dyslexia in children from the age of 8 in combination with other methods, including speech therapy.

Contraindications:

Hypersensitivity, severe chronic renal failure (creatinine clearance less than 20 ml / min), hemorrhagic stroke, psychomotor agitation, Huntington's chorea, pregnancy, lactation.

Carefully:

Violation of hemostasis, extensive surgical interventions, severe bleeding, chronic renal failure (creatinine clearance 20-80 ml / min).

Pregnancy and lactation:

Without the doctor's instructions, the drug should not be administered to pregnant women and nursing mothers.

Dosing and Administration:

Inside (during meals or on an empty stomach, squeezed with liquid).

The last dose is taken no later than 17 hours (to prevent sleep disturbance). The daily dose is divided into 2-4 admission.

Symptomatic treatment of psycho-organic syndrome: 4.8 g / day during the first week, then pass to the maintenance dose - 1.2-2.4 g / day.

Treatment of dizziness and related imbalances: 2.4-4.8 g / day. 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 is reached. Treatment continues throughout the period of the disease. Every 6 months, you should try to reduce the dose or cancel the drug, gradually reducing the dose by 1.2 g / day every 2 days. With little or no therapeutic effect, treatment is discontinued. In the sickle-cell vaso-occlusive crisis (in adults and children): prophylaxis - inside at 160 mg / kg / day, divided into 4 equal doses. Dose less than 160 mg / kg / day or an irregular intake of the drug. can cause an exacerbation of the disease.Treatment of dyslexia in children older than 8 years (in conjunction with other methods of treatment) - 3.2 grams, divided into 2 equal doses.

For chronic mild renal insufficiency (creatinine clearance 50-79 ml / min) - 2/3 dose divided into 2-3 doses; average (creatinine clearance 30-49 ml / min) - 1/3 dose divided into 2 doses; severe (creatinine clearance 20-30 ml / min) -1/6 dose once.

Side effects:

From the central nervous system: motor disinhibition, irritability, drowsiness, depression, asthenia, headache, insomnia, mental agitation, imbalance, ataxia, exacerbation of epilepsy, anxiety, hallucinations, confusion.

From the digestive system: nausea, vomiting, diarrhea, abdominal pain.

From the side of metabolism: weight gain.

From the sense organs: Vertigo.

From the skin: dermatitis, itching, urticaria.

Allergic reactions: hypersensitivity, anaphylactic reactions, angioedema.

Other: fever, lowering blood pressure.

Overdose:

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

Treatment: induction of vomiting, gastric lavage, symptomatic therapy, hemodialysis (efficacy 50-60%). There is no specific antidote.

Interaction:

When used simultaneously with iodine-containing hormones of the thyroid gland, confusion, irritability and sleep disturbance may occur. In high doses (9.6 g / day) in patients with venous thrombosis increases the anticoagulant effect of indirect anticoagulants (more pronounced decrease in platelet aggregation, fibrinogen content, von Willebrand factor, viscosity of blood and plasma).

Pharmaceutically compatible with dextrose solutions (5%, 10%, 20%), fructose (5%, 10%, 20%), 0.9% sodium chloride solution, Ringer's solution, 20% mannitol solution, hydroxyethyl starch (6%, 10%) .

Special instructions:

Be wary appoint patients with hemostasis, before the forthcoming extensive surgical interventions or in patients with symptoms of severe bleeding.

In the treatment of cortical myoclonia, sudden cessation of treatment should be avoided, this can cause a resumption of seizures.

When treating a veno-occlusive crisis with sickle-cell anemia, a dose of less than 160 mg / kg or an irregular intake of the drug may cause a recurrence of the crisis.With prolonged therapy in elderly patients, regular monitoring of kidney function is recommended, if necessary, dose adjustment is performed depending on the creatinine clearance.

It penetrates the hemodialysis apparatus through the filter membranes.

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

During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

The tablets covered with a cover of 200 mg.

Packaging:

For 10 tablets, coated with a shell, into the contour cell packaging of a polyvinyl chloride film and aluminum foil.

For 60 tablets, coated with a shell, in cans of polymer material.

Each jar, 3 or 6 contour squares, together with the instruction for use, is placed in a pack of cardboard for consumer containers.

Storage conditions:

In a dry, protected from light 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:P N000377 / 01

Date of registration:02.06.2011

The owner of the registration certificate:MARBIOFARM, OJSC MARBIOFARM, OJSC Russia

Manufacturer: & nbsp

MARBIOFARM, OJSC Russia

Information update date: & nbsp16.09.2015

Illustrated instructions

Instructions

Pyracetam (Piracetam)