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

Composition per ml: active substance: piracetam - 0.2 g; Excipients: sodium acetate trihydrate 0.001 g, acetic acid diluted to pH 5.8, water for injection up to 1 ml.

Description:

Transparent colorless or slightly colored liquid.

Pharmacotherapeutic group:Nootropic agent.

ATX: & nbsp

N.06.B.X.03 Pyracetam

Pharmacodynamics:

Pyracetam - nootropic agent, has an effect on the central nervous system in various ways: it modifies neurotransmission in the brain; improves the conditions conducive to neuronal plasticity; improves microcirculation, affecting the rheological characteristics of the blood and not causing vasodilation.The use of piracetam in patients with cerebral dysfunction increases attention concentration and improves cognitive function, which is accompanied by changes in the electroencephalogram (increase in α and β activity, decrease in δ activity).

Promotes restoration of cognitive functions due to various disorders, such as hypoxia, intoxication or electroconvulsive therapy.

Reduces the duration of induced vestibular neuronitis. Pyracetam inhibits increased aggregation of activated platelets and, in the case of abnormal rigidity of erythrocytes, improves their deformability and ability to filter.

Pharmacokinetics:

Distribution

The volume of the distribution (Vd) is about 0.6 l / kg. Does not bind to plasma proteins. Pyracetam penetrates through blood-brain and placental barriers, as well as hemodialysis membranes. In an animal study, it was found that piracetam selectively accumulates in the tissues of the cerebral cortex, mainly in the frontal, parietal and occipital lobes, in the cerebellum and basal nuclei.

Metabolism

It is not metabolized.

Excretion

The half-life of blood (T1) is 4-5 h and 8.5 h from cerebrospinal fluid. T1 is prolonged with renal failure. It is excreted unchanged by the kidneys. Excretion by the kidneys is almost complete (> 95%) for 30 hours.

The total clearance of piracetam in healthy volunteers is 86 ml / min.

Indications:

Pyracetam is indicated for the symptomatic treatment of memory disorders, intellectual disorders in the absence of a diagnosis of dementia (symptomatic treatment of chronic psychoorganic syndrome). Pyracetam can reduce manifestations of cortical myoclonus. To determine the effect of piracetam in a patient with cortical myoclonia, a trial course of treatment is necessary.

Contraindications:

Individual intolerance to piracetam or pyrrolidone derivatives, as well as other components of the drug; Huntington's chorea; acute violation of cerebral circulation (hemorrhagic stroke); terminal stage of chronic renal failure; childhood.

Carefully:

violation of hemostasis;
extensive surgical interventions;
heavy bleeding.

Pregnancy and lactation:

Pregnancy

Studies in animals have not revealed any adverse effects on the course of pregnancy and childbirth, embryonic fetal development. There were no controlled studies on pregnant women. Pyracetam penetrates the placental barrier and into breast milk. The concentration of pyracetam in newborns reaches 70-90% of its concentration in the blood of the mother.

Application during pregnancy is possible in exceptional cases, if the expected benefit for a woman exceeds the potential risk to the fetus.

Breastfeeding period

Pyracetam is excreted in breast milk. If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.

Dosing and Administration:

Intravenous (if oral administration is not possible). In the future, when an opportunity arises, it is advisable to switch to oral dosage forms.

Intramuscularly the drug is administered, if the introduction through the vein is difficult. The volume of the solution administered intramuscularly can not exceed 5 ml. The multiplicity of intramuscular injection is similar to that of intravenous or oral administration.

In memory disorders, intellectual disorders

At 2.4-4.8 g / day for the first few weeks, then go on maintenance therapy 2.4 g / day, you can take 1.2 g / day.

Treatment of cortical myoclonia

Treatment is started from 7.2-24 g per day, with little therapeutic effect or its absence, treatment is stopped on the 7th day, in case of a positive response to treatment, a dose of 24 g is reduced by 1.2 g every 2 days, until the appearance of myoclonus . This allows you to know the average effective dose. Intravenous administration is carried out for several minutes; for intravenous infusion, the daily dose is administered for 24 hours through the catheter at a constant rate.

The dose of other drugs for the treatment of myoclonus does not change. Then, later on the results of treatment, it is allowed to review the dose of other drugs for the treatment of myoclonus.

After initiation of piracetam treatment, treatment is continued as long as the symptoms of the disease persist.

However, every 6 months, attempts should be made to reduce the dose or cancel the drug. To avoid sudden relapse, the dose is reduced by 1.2 g every 2 days.

Because the piracetam is excreted from the body by the kidneys,when the drug is prescribed for patients with renal insufficiency and elderly patients, the dose should be adjusted depending on the amount of creatinine clearance (CC).

Patients with renal insufficiency a dose adjustment is required in accordance with the following scheme:

Degree of kidney failure	CK (ml / min)	Dose
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

In elderly patients dose adjusted for renal failure; with prolonged therapy, it is necessary to monitor the functional state of the kidneys.

Patients with impaired hepatic function correction of the dose is not required.

Patients with impaired functions of both kidney and liver the drug is prescribed in the same way as patients only with impaired renal function.

Side effects:

Information on adverse reactions was obtained on the basis of the results of double-blind placebo-controlled clinical trials and clinical pharmacological studies (manufacturer's data of the original drug).

The frequency of adverse reactions is determined as follows: very often (≥1 / 10), often (≥1 / 100 to <1/10), infrequently (≥1 / 1000, <1/100), rarely (≥1 / 10000, < 1/1000), very rarely (<1/10000), is unknown (the frequency can not be estimated based on available data).

From the nervous system:

Often: hyperactivity infrequent: drowsiness. Unknown: ataxia, imbalance, worsening of epilepsy, headaches, sleep disorders, tremor.

From the side of the hearing organ and labyrinthine disorders:

Unknown: dizziness.

Mental disorders:

Often: anxiety. Infrequently: depression. Unknown: agitation, anxiety, confusion, hallucinations.

From the digestive system:

Unknown: gastralgia, nausea, vomiting, constipation or diarrhea, decreased appetite.

From the cardiovascular system:

Rarely: arterial hypotension, thrombophlebitis. Unknown: worsening of angina, hypertension.

From the skin and subcutaneous tissue:

Unknown: dermatitis, itching, hives, angioedema

From the immune system:

Unknown: anaphylactoid reactions, hypersensitivity reactions.

From the genitals and the breast:

Unknown: sexual arousal.

General disorders and disorders at the site of administration:

Often: weight gain. Infrequently: asthenia. Rarely: pain at the injection site, hyperthermia.

Overdose:

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

A case when, after receiving a dose of piracetam to 75 g / day, the patient developed diarrhea with blood, accompanied by abdominal pain, which was explained by the effect of a significant amount of sorbitol.

No other symptoms of overdose have been reported.

Treatment: Induction of emesis, gastric lavage, symptomatic therapy, hemodialysis (efficiency 50-60%, as piracetam penetrates the filtration membranes of hemodialysis apparatus). There is no specific antidote.

Interaction:

While the use of thyroid hormones are marked individual reports of confusion, irritability and sleep disorders.

Piracetam in high doses (9.6 g / d) increases the effectiveness of indirect anticoagulants in patients with venous thrombosis (noted a more pronounced reduction of platelet aggregation, fibrinogen, von Willebrand factor, blood viscosity and plasma as compared to using only acenocoumarol).

The possibility of changing the pharmacodynamics of piracetam under the influence of other drugs is low, because 90% of the drug is excreted unchanged in the urine.

In concentrations of 142, 426 and 1422 μg / ml piracetam does not inhibit cytochrome P450 isoenzymes such as CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, 4A9 / 11. For a concentration of 1422 μg / ml, a minimal inhibition of CYP 2A6 (21%) and SA4 / 5 (11%) was observed. However, the normal values of the inhibition constant can probably be achieved at a higher concentration. Thus, the metabolic interaction of piracetam with other drugs is unlikely.

Receiving piracetam at a dose of 20 g / day did not change the maximum concentration and area under the concentration-time curve of antiepileptic drugs in (carbamazepine, phenytoin, phenobarbital, valproic acid) in the serum of patients with epilepsy who receive the drug in a constant dose.

Joint intake with alcohol did not affect the concentration of piracetam in the serum; the concentration of ethanol in the serum did not change with the intake of 1.6 g of piracetam.

Special instructions:

Due to the influence of piracetam on platelet aggregation, care should be taken when prescribing the drug to patients with hemostasis, bleeding symptoms,before the forthcoming surgical intervention, postponed surgical intervention (including dental surgery), risk factors for bleeding (eg peptic ulcer disease of the stomach and duodenum), previous intracerebral hemorrhage, anticoagulant or antiplatelet therapy, including low doses of aspirin.

During the period of taking the drug, it is recommended that the kidney function be monitored continuously.

In the treatment of cortical myoclonia, sudden interruption in treatment should be avoided, as this may cause the resumption of seizures.

With prolonged therapy, elderly patients are recommended regular monitoring of renal function, if necessary, adjust the dose depending on the results of the study of creatinine.

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

During the treatment period, care should be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Solution for intravenous and intramuscular injection 200 mg / ml.

Packaging:

5 ml per ampoule.

For 10 ampoules, together with the instructions for use and the ampoule scarifier, are placed in a pack of cardboard with partitions or special nests.

5 ampoules are placed in a contour mesh package.

For 1 or 2 contour mesh packages together with the instruction for medical use and the ampoule scarifier are placed in a pack of cardboard.

When using ampoules with a break ring, it is allowed to pack the ampoules without an ampoule scarifier.

Storage conditions:

Store in a dark place at a temperature of no higher than 25 ° C. Do not freeze.

Keep out of the reach of children.

Shelf life:

5 years.

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

Terms of leave from pharmacies:On prescription

Registration number:П N015341 / 02

Date of registration:31.08.2010

The owner of the registration certificate:BELMEDPREPARATY, RUP BELMEDPREPARATY, RUP Republic of Belarus

Manufacturer: & nbsp

BELMEDPREPARATY, RUP Republic of Belarus

Information update date: & nbsp22.09.2015

Illustrated instructions

Instructions

Pyracetam (Piracetam)