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

Pyracetam is a nootropic remedy that directly affects the brain by improving cognitive (cognitive) processes, such as learning ability, memory, attention, and mental performance. Pyracetam has an effect on the central nervous system in various ways by changing the rate of spread of excitation in the brain,improving metabolic processes in nerve cells, improving microcirculation, affecting the rheological characteristics of the blood and not causing vasodilating action.

Improves communication between the cerebral hemispheres and synaptic conductivity in neocortical structures, increases mental capacity, improves cerebral blood flow.

Pyracetam inhibits platelet aggregation and restores the elasticity of the erythrocyte membrane, reduces the adhesion of erythrocytes. In a dose of 9.6 g reduces the level of fibrinogen and von Willebrand factors, by 30% - 40% and prolongs the time of bleeding.

Piracetam has a protective and restoring effect when brain function is impaired due to hypoxia and intoxication. Pyracetam reduces the severity and duration of the vestibular nystagmus.

Pharmacokinetics:

The half-life of the drug from the blood plasma is 4-5 hours and 8.5 hours from the cerebrospinal fluid, which is prolonged with renal failure. The pharmacokinetics of pyracetam does not change in patients with hepatic insufficiency.

Penetrates through the blood-brain and placental barrier and membranes used in hemodialysis.When tested on animals piracetam selectively accumulates in the tissues of the cerebral cortex, mainly in the frontal, parietal and occipital lobes, in the cerebellum and basal ganglia. It does not bind to blood plasma proteins, is not metabolized in the body, and is excreted by the kidneys unchanged. 80-100% of piracetam is excreted by the kidneys unchanged by renal filtration. The renal clearance of piracetam in healthy volunteers is 86 ml / min.

Indications:

Symptomatic treatment of psycho-organic syndrome, in particular in elderly patients suffering from memory loss, dizziness, reduced concentration of attention and general activity, mood changes, behavioral disorders, gait disorders, as well as patients with Alzheimer's disease and senile dementia of Alzheimer's type. Treatment of the consequences of stroke (chronic stage of ischemic stroke), such as speech disorders, emotional disorders, to enhance motor and mental activity.

Chronic alcoholism - for the treatment of psycho-organic and abstinence syndromes.

Comatose conditions (and during the recovery period), including after traumas and intoxications of the brain.

Treatment of dizziness of vascular genesis.

For the treatment of cortical myoclonia as a mono- or complex therapy.

In the complex therapy of sickle-cell anemia.

Contraindications:

Individual intolerance to piracetam or pyrrolidone derivatives, as well as other components of the drug.

Acute stage of hemorrhagic stroke. Psychomotor agitation. The final stage of renal failure (with creatinine clearance less than 20 ml / min).

Children up to 1 year.

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 surgical interventions, 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:

Studies on animals have not revealed a damaging effect on the embryo and its development, including in the postnatal period,and also did not change the course of pregnancy and childbirth.

Studies on pregnant women 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. Except in special circumstances, should not be administered during pregnancy. It should be refrained from breastfeeding with the appointment of a woman piracetam.

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:

	Common (from 1% and less than 10%)	Rare (from 0.1% and less than 1%)
Disorders of the central and peripheral nervous system	Hyperkinesia 1.72%
Metabolic disorders	Weight gain of 1.29%
Mental disorders	Nervousness of 1.13%	Drowsiness 0.96% Depression of 0.83%
General disorders	Asthenia 0.23%

They are more common in elderly patients receiving doses above 2.4 g / day.In most cases, it is possible to regress such symptoms by lowering the dose of the drug. There are isolated reports of side effects from the gastrointestinal tract, such as nausea, vomiting, diarrhea, abdominal and stomach pain; nervous system - dizziness, headaches, ataxia, imbalance, exacerbation of epilepsy, insomnia; from the side of the psyche - confusion, agitation, anxiety, hallucinations, increased sexuality; from the skin - dermatitis, itching, rashes, swelling.

Overdose:

A single case of development of diarrhea in the form of diarrhea with blood and pain in the abdominal region was registered with oral administration in a daily dose of 75 g. Apparently, this was due to the use of a large total dose of sorbitol, which is part of the drug previously for the dosage form solution for reception inside.

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:

No interaction with clonazepam, phenytoin, phenobarbital, sodium valproate has been observed.

High doses (9.6 g / day) of piracetam increased the efficacy of acenocoumarol in patients with venous thrombosis: there was a greater decrease in platelet aggregation, fibrinogen, von Willebrand factors, viscosity of blood and plasma than in the administration of acenocoumarol alone.

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

In vitro piracetam does not inhibit cytochrome P450 isoforms CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 and 4A9 / 11 at a concentration 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 level Ki of these two CYP isomers is sufficient when exceeding 1422 μg / ml. Therefore, metabolic interaction with other drugs is unlikely.

The administration of piracetam at a dose of 20 mg / day did not change the peak and the concentration curve of antiepileptic drugs in serum (carbamazepine, phenytoin, phenobarbital, valproate) in patients with epilepsy receiving a constant dosage.

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

Joint intake with alcohol did not affect the level of serum piracetam concentration, 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:

Taking into account possible side effects, care should be taken when working with mechanisms and driving a car.

Form release / dosage:Capsules 400 mg.

Packaging:

For 10 capsules per package, the contour is planar, in 1, 2 packs in packs of cardboard with instructions for use.

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:

3 years.

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

Terms of leave from pharmacies:On prescription

Registration number:P N000858 / 02

Date of registration:12.05.2010

The owner of the registration certificate:MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC Russia

Manufacturer: & nbsp

MOSHIMFARM PREPARATES them. NA Semashko OJSC Russia

Information update date: & nbsp24.10.2015

Illustrated instructions

Instructions

Pyracetam (Piracetam)