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

1 ml of the solution contains 200 mg of pyracetam as the active substance; auxiliary substances: sodium acetate, acetic acid diluted, water for injection.

Description:

Transparent colorless or slightly colored liquid.

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).

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 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 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.
The final stage of renal failure (with creatinine clearance less than 20 ml / min).
Children up to 1 year.
Psychomotor agitation.

Carefully:Violation of hemostasis, extensive surgical intervention, heavy bleeding.

Pregnancy and lactation:

Studies in animals showed no damaging effects 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 piracetam should not be administered during pregnancy. It should be refrained from breastfeeding with the appointment of a woman piracetam.

Dosing and Administration:

Intravenous or 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.

In the treatment of coma, as well as difficulties in perception in people with brain injuries, the initial dose is 9-12 g / day, supporting - 2 g / day. Treatment lasts no less than 3 weeks.

With alcohol withdrawal syndrome - 12 g / day. Maintenance dose of 2.4 g / day.

Treatment of dizziness and related disorders of equilibrium 2.4-4.8 g per day, the course 10-15 days.

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 Pyracetam 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	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 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 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 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 pain, incl. in the epigastric region; 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.

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.

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 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.

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:

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.

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. It penetrates the hemodialysis apparatus through the filter membranes.

Form release / dosage:Solution for intravenous and intramuscular injection of 200 mg / ml in ampoules from neutral glass to 5 ml.

Packaging:

10 ampoules per box or a pack of cardboard.

5 or 10 ampoules per contour cell package. For 1 or 2 contour packs in a pack of cardboard.

In the package or box, insert instructions for use, a knife for opening ampoules or a scarifier ampoule.

Storage conditions:

List B. In sheltered from light, inaccessible to children at a temperature of no higher than 30 ° C.

Shelf life:

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

Terms of leave from pharmacies:On prescription

Registration number:P N000387 / 01

Date of registration:17.08.2007

The owner of the registration certificate:VEROPHARM SA VEROPHARM SA Russia

Manufacturer: & nbsp

VEROPHARM SA Russia

Information update date: & nbsp16.09.2015

Illustrated instructions

Instructions

Pyracetam (Piracetam)