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

active substance - piracetam 200 mg, Excipients - pregelatinized starch - 3.0 mg, croscarmellose sodium 3.0 mg, povidone (polyvinylpyrrolidone) 5.0 mg, magnesium stearate 2.0 mg. Auxiliary substances (shell): hypromellose - 3,8 mg, macrogol 4000 - 1,0 mg, titanium dioxide - 2,2 mg.

Composition per 1 tablet 400 mg:

active substance - piracetam 400 mg, Excipients - pregelatinized starch 6.0 mg, croscarmellose sodium 6.0 mg, povidone (polyvinylpyrrolidone) 10 mg, magnesium stearate 4.0 mg. Auxiliary substances (shell): hypromellose - 7.6 mg, macrogol 4000 - 2.0 mg, titanium dioxide - 4.4.

Description:

Tablets without risks are round, biconvex, with integral edges, covered with a film coat of white or almost color.Surface roughness is allowed.

Pharmacotherapeutic group:Nootropic agent.

ATX: & nbsp

N.06.B.X.03 Pyracetam

Pharmacodynamics:

Nootropic agent. Has a positive effect on brain metabolic processes: increases the concentration of ATP in the brain tissue, enhances the synthesis of RNA and phospholipids, stimulates glycolytic processes, increases the utilization of glucose. It improves the integrative activity of the brain, facilitates the consolidation of memory, facilitates the learning process.

Changes the speed of propagation of excitation in the brain, improves microcirculation, without providing a vasodilating action, suppresses the aggregation of activated platelets. Has a protective effect on brain damage caused by hypoxia, intoxication, electric shock; enhances alpha and beta activity, reduces delta activity on the electroencephalogram, reduces the severity of the vestibular nystagmus.

Improves the connection between the cerebral hemispheres and synaptic conductivity in neocortical structures, restores and stabilizes cerebral functions, especially consciousness, memory and speech, improves mental performance, improves cerebral blood flow. The effect develops gradually.Practically does not have sedative and psycho-stimulating effect.

Pharmacokinetics:

After ingestion, it is well absorbed and penetrates into various organs and tissues. Bioavailability is 95%. Time to reach the maximum concentration of 0.5-1 h. 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. Penetrates through blood-brain and placental barriers, accumulates in the brain tissue 1-4 hours after ingestion. Does not bind to blood plasma proteins, is not practically metabolized. The half-life is 4.5 hours (7.7 hours - from the brain). It is excreted by the kidneys - 2/3 unchanged for 30 hours.

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 lability, behavioral disorder, gait disorders, as well as patients with Alzheimer's disease and senile dementia of the Alzheimer's type.
The consequences of an 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.
The recovery period after craniocerebral trauma and brain intoxication.
Dizziness and related disorders of balance, with the exception of dizziness of the vasomotor and psychogenic origin.

Contraindications:

Individual intolerance to piracetam or pyrrolidone derivatives, as well as other components of the drug. The terminal stage of renal failure (with creatinine clearance less than 20 ml / min), acute cerebrovascular accident (hemorrhagic stroke), psychomotor agitation at the time of prescribing, Huntington's chorea. Children under 3 years (for this dosage form).

Carefully:

Violation of hemostasis; extensive surgical interventions; heavy bleeding.

Pregnancy and lactation:

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.During pregnancy, the prescription of the drug is only possible if the intended benefit to the mother exceeds the potential risk to the fetus. During the lactation period, the issue of stopping breastfeeding should be addressed.

Dosing and Administration:

Inside, during meals or on an empty stomach, squeezed with liquid. Attention: the last single dose should be taken no later than 17:00 to prevent sleep disturbance.

The daily dose is 30-160 mg / kg of body weight, the frequency of intake 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.

In the treatment of psycho-organic 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.

When treating the consequences of a stroke, 4.8 g / day is prescribed.

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.

With alcoholism, the maintenance dose is 2.4 g.

With dizziness and associated disorders of equilibrium, 2.4-4.8 g / day.

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 failure	Clearance creatinine (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 the section "Dosing to patients with impaired renal function").

Side effects:

From the nervous system: mental excitement, motor disinhibition, irritability, drowsiness, depression, asthenia.These side effects often occur in elderly patients who received the drug at a dose of more than 2.4 g / day. In most cases, it is possible to regress such symptoms by lowering the dose of the drug. In isolated cases - dizziness, headache, ataxia, exacerbation of epilepsy, extrapyramidal disorders, tremor, imbalance, decreased ability to concentrate, insomnia, agitation, anxiety, hallucinations, increased libido.

From the cardiovascular system: rarely - a decrease or increase in blood pressure, worsening of the course of angina pectoris.

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

From the side of metabolism: increase in body weight - more often occurs in elderly patients who received the drug at a dose of more than 2.4 g per day

Allergic reactions: dermatitis, itching, rashes, angioedema.

Overdose:

After oral administration of piracetam at a dose of 75 g, dyspeptic events such as diarrhea with blood and abdominal pain are noted.

Treatment: Immediately after taking the drug inside, you can flush the stomach or cause artificial vomiting.Symptomatic therapy is recommended, hemodialysis is possible (efficacy is 50-60%). There is no specific antidote.

Interaction:

Increases the effectiveness of thyroid hormones, antipsychotic drugs (neuroleptics).

With simultaneous use with drugs that stimulate the central nervous system, it is possible to over-stimulate it.

When administered with neuroleptics reduces the risk of extrapyramidal disorders.

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

High doses (9.6 g / day) of piracetam increase the effectiveness of indirect anticoagulants in patients with venous thrombosis (there was a greater decrease in platelet aggregation, fibrinogen levels, vWF, plasma and blood viscosity compared with only indirect anticoagulants). 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 It does not inhibit cytochrome P450 isoenzymes such as 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, however, the Ki level of these two isoenzymes is sufficient when 1422 μg / ml is exceeded, and 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:

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:

Tablets coated with a film coat of 200 mg and 400 mg.

Packaging:

For 10, 20, 30 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

By 10, 20, 30, 40, 50, 60 or 100 tablets into a polymer container for medicines. One container or 1, 2, 3,4, 5, 6, 8 or 10 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

Storage conditions:

Store in a dry, dark 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:LSR-007826/08

Date of registration:06.10.2008

The owner of the registration certificate:OZONE, LLC OZONE, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Information update date: & nbsp22.09.2015

Illustrated instructions

Instructions

Pyracetam (Piracetam)