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

Pyracetam is a nootropic remedy that directly affects the brain, improving cognitive (cognitive) processes, such as learning ability, memory, attention, and mental performance. Pyracetam affects 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. At a dose of 9.6 g reduces fibrinogen and von Willebrand factor at 30% -40% and prolongs bleeding time. Pyracetam has a protective and restorative effect in the violation of brain function due to hypoxia and intoxication.

Pyracetam reduces the severity and duration of the vestibular nystagmus.

Pharmacokinetics:

The half-life of the drug from plasma is 4.5 hours, and 8.5 hours from the cerebrospinal fluid, which is elongated in 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, low concentration and general activity, mood changes, behavioral disorders, gait disorders, as well as patients with Alzheimer's disease and senile dementia such as Alzheimer's;
the consequences of ischemic stroke (chronic stage), such as emotional disorders, to enhance motor and mental activity;
intoxication of the brain;
dizziness of vascular genesis;
cortical myoclonia (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.
The final stage of renal failure (with creatinine clearance less than 20 ml / min).
Psychomotor agitation.
Children up to 1 year.
Pregnancy, lactation.

Pregnancy and lactation:

Studies on pregnant women were not conducted. Pyracetam penetrates the placental barrier and into breast milk. The use of the drug during pregnancy is contraindicated. When prescribing the drug, breastfeeding should be discontinued.

Dosing and Administration:

Intravenous and intramuscular.

With symptomatic treatment of chronic psychoorganic syndrome, depending on the severity of symptoms, 2-4 g are prescribed, gradually increasing the dose to 4-6 g per day, the course of treatment is 10-15 days.

When treating the consequences of a stroke (chronic stage), 4.8 g / day is prescribed. The course of treatment is 10-15 days, if necessary, repeated courses in 6-8 weeks.

Treatment of dizziness and associated disorders of equilibrium 2,4-4,8 g per day, course 10-15 days.

With cortical myoclonia begin with a dose of 7.2 g / day every 3-4 days a dose, increase by 4.8 g / day until a maximum dose of 24 g / day. 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.

With sickle cell anemia, the daily prophylactic dose is 160 mg / kg body weight divided into four equal doses. During the crisis - 300 mg / kg intravenously. This dosage can be given to children from 1 year of age.

Dosing to patients with impaired renal function

Because the piracetam is excreted from the body by the kidneys, care should be taken when treating patients with renal insufficiency in accordance with this dosing regimen:

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	30-19	1/3 of the usual dose in 2 divided 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 impaired functions and 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 psyche - confusion, agitation, anxiety, hallucinations, increased sexuality; from the skin - dermatitis, itching, rashes, swelling; other - worsening of the course of angina pectoris.

Overdose:

Strengthening of possible side effects.

First aid - reception of activated charcoal, symptomatic therapy; hemodialysis is possible (efficacy 50-60%), there is no specific antidote.

Interaction:

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

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

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.

In vitro piracetam does not inhibit the cytochrome P450 of the 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 Ki level of these two CYP isomers is sufficient when 1422 μg / ml is exceeded. Therefore, metabolic interaction with other drugs is unlikely.

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

Increases the effectiveness of antipsychotic drugs (neuroleptics). With simultaneous use with drugs that stimulate the central nervous system, excessive stimulation of the central nervous system is possible.

When administered with neuroleptics reduces the risk of extrapyramidal disorders.

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. When treating patients with cortical myoclonia, sudden interruption in treatment should be avoided; which can cause 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 the specific nature of the diseases and taking into account possible side effects, during the treatment period one should refrain from driving vehicles and practicing other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Solution for intravenous and intramuscular injection 200 mg / ml.

Packaging:

5 ml in ampoules.

5 ampoules of 5 ml are placed in a contour mesh package made of a polyvinyl chloride film.

2 contour mesh packages are placed in a pack of cardboard.

In each pack put the instructions for use, a knife ampoule or scarifier. At packing of ampoules with a ring of a break, points and notches the knife ampullum or skarifikator do not put.

Storage conditions:

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

Keep out of the reach of children.

Shelf life:

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

Terms of leave from pharmacies:On prescription

Registration number:LS-002391

Date of registration:28.12.2011

The owner of the registration certificate:BIOSINTEZ, PAO BIOSINTEZ, PAO Russia

Manufacturer: & nbsp

BIOSINTEZ, PAO Russia

Information update date: & nbsp17.09.2015

Illustrated instructions

Instructions

Pyracetam (Piracetam)