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

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 pyracetam in patients with cerebral dysfunction increases concentration and improves cognitive function, which is accompanied by changes in the electroencephalogram (increase α and β activity, decrease δ activity). Promotes restoration of cognitive functions due to various disorders, such as hypoxia, intoxication or electroconvulsive therapy. Pyracetam is indicated for the treatment of cortical myoclonia both as monotherapy and as part of complex therapy. Reduces the duration of induced vestibular neuronitis.

Piracetam inhibits increased aggregation of activated platelets and, in the case of abnormal rigidity of erythrocytes, improves their deformability and ability to filter.

Pharmacokinetics:

Distribution

Volume of 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 / 2) is 4-5 hours and 8.5 hours of cerebrospinal fluid. T1 / 2 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:

Symptomatic treatment of intellectual-mnestic disorders in the absence of an established diagnosis of dementia.

Reduction of the manifestations of cortical myoclonia in piracetam sensitive patients both as monotherapy and as part of complex therapy. (In order to determine sensitivity to pyracetam in a particular case, a trial treatment course can be performed).

Contraindications:

Hypersensitivity to piracetam or other components of the drug; severe chronic renal failure (creatinine clearance less than 20 ml / min); hemorrhagic stroke; psychomotor agitation; Huntington's chorea; pregnancy, lactation, children under 1 year.

Carefully:

Violation of hemostasis; extensive surgical interventions; heavy bleeding; chronic renal failure (creatinine clearance 20-80 ml / min).

Pregnancy and lactation:

Pregnancy

Sufficient data on the use of piracetam during pregnancy are absent. Studies in animals have not shown a direct or indirect effect on pregnancy, embryo / fetal development, childbirth or postnatal development.

Piracetam penetrates the placental barrier. The plasma concentration of piracetam in neonates reaches 70-90% of that of the mother. Pyracetam should be prescribed during pregnancy only in exceptional cases if the benefit to the mother exceeds the potential risk to the fetus, and the clinical condition of the pregnant woman requires treatment with piracetam.

Lactation

Piracetam penetrates into breast milk. Pyracetam should not be used during breastfeeding or should stop breastfeeding while treating piracetam. When deciding whether to quit breastfeeding or refuse treatment with piracetam, the benefits of breastfeeding for a child and the benefits of therapy for a woman should be correlated.

Dosing and Administration:

In memory disorders, intellectual violations

At 2.4-4.8 g / day for the first few weeks, then go on maintenance therapy 2.4 g / day in 2-3 doses, taking 1.2 g / day.

If you can take the drug inside, go to oral dosage forms.

Treatment of cortical myoclonia

Treatment begins with 7.2 g / day, increasing it by 4.8 g every 3-4 days up to 24 g divided into 2-3 injections. The dose of other drugs for the treatment of myoclonus does not change. Further on the results of treatment, it is necessary, if possible, to reduce 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. In patients with acute episodes, the course of the disease may change with time, therefore every 6 months, attempts should be made to reduce the dose or to cancel the drug. To avoid sudden relapse, the dose is reduced by 1.2 g every 2 days.

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.

Elderly patients

Elderly patients with renal insufficiency should be corrected for the dose (see below "Renal failure"). With long-term treatment to assess the need for dose adjustment, creatinine clearance should be assessed regularly.

Renal insufficiency

Piracetam is excreted almost exclusively by the kidneys, care should be taken when treating patients with renal insufficiency or requiring renal function control.

The half-life (T1 / 2) increases in direct proportion to the impairment of kidney function and creatinine clearance; this is also true for the elderly, in whom the excretion of creatinine depends on age.

The dose should be adjusted depending on the creatinine clearance (CK). The creatinine clearance for men can be calculated based on the serum creatinine concentration (Xyvorot), according to the following formula:

CK (ml / min) = [140 - age (years) x body weight (kg)] / [72 x KSvorot (mg / ml)]

The creatinine clearance for women can be calculated by multiplying the obtained value by a factor of 0.85.

Kidney function	CK (ml / min)	Dosing regimen
Norm	>80	The standard dose of 2-4 admission
Mild renal insufficiency	50-79	2/3 of the standard dose in 2-3 doses
Mean renal insufficiency	30-49	1/3 of the standard dose in 2 divided doses
Severe renal insufficiency	<30	1/6 of the standard dose once
Terminal Renal Failure	-	Contraindicated

Liver failure

Patients with isolated dysfunction of the liver do not need correction of the dose. Patients with impaired function and kidney and liver dosing is carried out according to the scheme (see above "Renal failure").

Side effects:

The undesirable drug reactions listed below were detected in clinical trials and post-detection observations and grouped according to system-organ classes. The frequency gradient is defined as follows: very often (≥ 1/10), often (≥ 1/100 to <1/10), infrequently (≥ 1/1000 to <1/100), rarely (≥ 1/10 000 to < 1/1000), very rarely (up to <1/10 000) and the frequency is unknown (it is impossible to evaluate based on the available clinical trial data).

On the part of the blood and lymphatic system

The frequency is unknown: bleeding.

From the immune system

The frequency is unknown: anaphylactoid reactions, hypersensitivity.

From the side of the psyche

Often: nervousness. Infrequently: depression. The frequency is unknown: agitation, anxiety, confusion, hallucinations.

From the nervous system

Often: hyperactivity. Infrequently: drowsiness. The frequency is unknown: ataxia, imbalance, exacerbation of epilepsy, headache, insomnia, tremor.

From the side of the hearing and labyrinth organs

Frequency unknown: vertigo.

From the side of the vessels

Rarely: thrombophlebitis, arterial hypotension (only with parenteral administration).

From the digestive system

The frequency is unknown: abdominal pain (including in the upper divisions), diarrhea, nausea, vomiting.

From the skin and subcutaneous tissues

The frequency is unknown: angioedema, dermatitis, itching, urticaria.

From the side of the reproductive system

Frequency unknown: increased sexual desire.

General disorders and disorders at the site of administration

Infrequently: asthenia. Rarely: pain at the injection site, fever (only with parenteral administration).

Laboratory and instrumental data

Often: weight gain.

Overdose:

Data on overdose with intravenous administration of the drug are absent. When symptoms of an overdose occur, symptomatic therapy is recommended, which may include hemodialysis. The efficiency of hemodialysis for the removal of piracetam is 50-60%. There is no specific antidote.

Interaction:

Thyroid hormones

With the simultaneous use of pyracetam and thyroid extract (triiodothyronine + thyroxine), confusion, irritability and sleep disturbance were noted.

Acenocoumarol

According to a published blind clinical trial in patients with recurrent venous thrombosis piracetam at a dose of 9.6 g / day does not affect the dose of acenocoumarol necessary to achieve an international normalized ratio of 2.5-3.5, but compared with the effects of acenocoumarol alone, the addition of pyracetam at a dose of 9.6 g / day significantly reduces platelet aggregation, β-thromboglobin release, fibrinogen concentration and von Willebrand factor (VIII: C; VIII: vW: Ag; VIII: vW: RCo), and the viscosity of whole blood and plasma.

Pharmacokinetic interactions

The possibility of changing the pharmacokinetics of pyracetam under the influence of other drugs is low, since 90% of pyracetam is excreted unchanged in urine.

In concentrations of 142, 426 and 1422 mg / ml piracetam does not inhibit cytochrome P450 isoenzymes (CYP 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 and 4A9 / 11) in vitro. At a concentration of 1422 mg / ml, a minimal inhibition of the isoenzyme CYP2A6 (21%) and SA4 / 5 (11%) was observed. However, the values of the inhibition constant (Ki) probably go well beyond the concentration of 1422 mg / ml. Thus, the metabolic interactions of piracetam with other drugs are unlikely.

Anticonvulsants

Admission piracetam at a dose of 20 g / day for 4 weeks in patients with epilepsy, taking a constant dose of antiepileptic drugs (carbamazepine, phenytoin, phenobarbital and valproic acid), did not change their maximum and minimum concentrations.

Alcohol

Simultaneous reception with alcohol did not affect the concentration of pyracetam in plasma; when taking 1.6 g of pyracetam, the concentration of ethanol in the plasma did not change.

Pharmaceutical incompatibility

There is no information on pharmaceutical incompatibility.

Special instructions:

Effect on platelet aggregation

Due to the antiaggregant effect (see the section "Pharmacodynamics"), piracetam should be administered with caution to patients with severe hemorrhagic disorders, risk of bleeding (eg, gastric ulcer), hemostasis disorders, in patients with surgical interventions, including dental interventions, in patients taking anticoagulants and antiaggregants, incl. low doses of acetylsalicylic acid.

Renal insufficiency

Because the piracetam is excreted by the kidneys, care should be taken when prescribing the drug to patients with renal insufficiency.section "Method of administration and dose"),

Elderly patients

Long-term treatment of elderly patients requires regular monitoring of creatinine clearance, since dose adjustment may be required.

Abolition of therapy

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

It penetrates the hemodialysis apparatus through the filter membranes.

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

Given the profile of adverse reactions, during the treatment period, care must be taken when driving vehicles, working with mechanisms and engaging in other potentially hazardous activities requiring increased concentration and speed of psychomotor reactions.

Form release / dosage:

Solution for intravenous administration 200 mg / ml.

Packaging:

5 ml into neutral glass ampoules.

5 or 10 ampoules per contour cell pack of a polyvinyl chloride film.

1 circuit cell pack of 10 ampoules or 2 contour packs of 5 ampoules with instructions for use, a scarifier or a knife ampoule in a pack of cardboard.

When using ampoules with a kink ring or with a notch and a point, the scarifier or knife is not ampouled.

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 expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-000649

Date of registration:23.07.2010

The owner of the registration certificate:Company DEKO, LLC Company DEKO, LLC Russia

Manufacturer: & nbsp

Company DEKO, LLC Russia

Information update date: & nbsp16.09.2015

Illustrated instructions

Instructions

Pyracetam (Piracetam)