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

Pyracetam is a nootropic drug that directly affects the brain, improving cognitive (cognitive) processes, such as learning ability, memory, attention, and mental performance. Pyracetam affects the central nervous system (DPS) in various ways: changing the speed of propagation of excitation in the brain, improves metabolic processes in nerve cells, improves microcirculation, affects the rheological characteristics of the blood without providing a vasodilating effect. 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 factor by 30-40% and lengthens the time of bleeding. Pyracetam has a protective and restorative action in cases of impaired brain function due to hypoxia and intoxication.

Pyracetam reduces the 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 blood-brain and placental barriers 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 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:

Individual intolerance to piracetam or pyrrolidone derivatives, as well as other components of the drug.
Acute stage of hemorrhagic stroke.
Severe renal dysfunction (with creatinine clearance (CC) less than 20 mL / min). Psychomotor agitation.
Children up to 1 year.
Pregnancy and the period of breastfeeding.

Carefully:

violation of hemostasis;
extensive surgical interventions;
heavy bleeding;
impaired renal function (KK 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:

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

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 begins with 7.2 grams per 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 (to prevent the possibility of sudden recurrence of seizures in the Lansa-Adams syndrome - every 3-4 days). If oral administration is not possible, the drug is administered intravenously at the same dose. Intravenous administration is carried out for several minutes; for intravenous infusion, the daily dose is administered for 24 hours through a 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 determine the need for dose adjustment, regular QC evaluation should be performed.

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 elimination half-life increases in direct proportion to the impairment of kidney function and QC; this is also true of the elderly, in whom the excretion of creatinine depends on the age of a.

In this regard, the dose is adjusted in accordance with the table below:

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

The creatinine clearance for men can be calculated based on the serum creatinine concentration, according to the following formula:

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

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

Liver failure

Patients with isolated dysfunction of the liver do not need correction of the dose. Patients with impaired function and nights, 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 estimate based on the available clinical trial data).

The data of post-registration observations are not sufficient to determine the frequency of undesired reactions.

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.

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. hives.

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.

Laboratory and instrumental data

Often: weight gain.

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 was noted. phenytoin, phenobarbital, sodium valproate.

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 cytochrome P450 isoforms CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 2121 and 4 A9 / 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 g / day did not change the peak and the curve of the concentration level of antiepileptic drugs in blood serum (carbamazepine, phenytoin, phenobarbital, valproate) in patients with epilepsy receiving a constant dosage. Increases the effectiveness of antipsychotic drugs (neuroleptics). When used simultaneously with drugs that stimulate the central nervous system, excessive stimulation of the DSP is possible.

When administered with neuroleptics reduces the risk of extrapyramidal disorders.

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

There is no information on pharmaceutical incompatibility.

Special instructions:

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.

Because the piracetam is excreted by the kidneys, care should be taken when prescribing the drug to patients with renal insufficiency (see section "Dosing and Administration").

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

With prolonged therapy in elderly patients, regular monitoring of renal function indicators is recommended, if necessary, dose adjustment is performed depending on the results of the QC study.

It penetrates the hemodialysis apparatus through the filter membranes.

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

During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Solution for intravenous and intramuscular injection 200 mg / ml.

Packaging:

By 5 or 10 ml into ampoules of low-density polyethylene or polypropylene.

For 5 or 10 ampoules together with instructions for use in a pack of cardboard.

Storage conditions:

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:LP-002909

Date of registration:13.03.2015

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

Manufacturer: & nbsp

GROTEKS, LLC Russia

Information update date: & nbsp22.09.2015

Illustrated instructions

Instructions

Pyracetam (Piracetam)