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

Composition per ml: active substance: piracetam - 200 mg; Excipients: sodium acetate trihydrate (sodium acetate, 3-led) - 1 mg, acetic acid diluted 30% to pH 5.8, water for injection up to 1 ml.

Description:Transparent colorless or slightly yellowish 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, without 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 βactivity, 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 myoclonus 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:

The half-life of piracetam from plasma is 4-5 h and 8.5 h from cerebrospinal fluid, which is prolonged in chronic renal failure (in terminal chronic renal failure, up to 59 h). The pharmacokinetics of pyracetam does not change in patients with hepatic insufficiency. Penetrates through blood-brain and placental barriers, is removed during 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 nuclei. It does not bind to blood plasma proteins, it is not metabolized in the body. 80-100% of pyracetam is excreted by the kidneys unchanged by glomerular filtration. The apparent volume of distribution (Vd) is about 0.6 l / kg. The total clearance is 80-90 ml / min.

Indications:

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

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

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);
severe renal dysfunction;
psychomotor agitation at the time of prescribing.

Carefully:

violation of hemostasis;
extensive surgical interventions;
heavy bleeding;
impaired renal function.

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, the development of the embryo / fetus. 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:

Intravenously.

In memory disorders, intellectual disorders

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

Treatment of cortical myoclonia

Treatment begins with 7.2 grams per day, increasing the total of 4.8 g every 3-4 days up to 24 grams 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 should try to reduce the dose or 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, with intravenous infusion introduction, 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 elimination half-life 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 (K_serum), 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.

Renal insufficiency	CK (ml / min)	Dosing regimen
Norm	>80	the usual dose of 2-4 admission
Lightweight	50-79	2/3 of the usual dose in 2-3 doses
Average	30-19	1/3 of the usual dose in 2 divided doses
Heavy	<30	1/6 of the usual dose once
The final stage	-	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"). "

The procedure for working with a polymer ampoule:

Take the ampoule and shake it. holding at the neck
Press the ampoule with your hand, while the preparation should not be isolated, and turn and rotate the valve and separate the valve.
Through the formed hole, immediately connect the syringe with the ampoule.
Turn the ampoule over and slowly put the contents into the syringe.
Put the needle on the syringe.

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).

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 parts); 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.

Laboratory and instrumental data

Often: weight gain.

Overdose:

An isolated case of development of diarrheal phenomena in the form of diarrhea with blood and abdominal pain was registered with piratsetam administered inside at a daily dose of 75 g, presumably because of the large total dose of sorbitol. In this preparation sorbitol There is no, but you should be careful. Other symptoms of overdose are not registered.

Interaction:

When used simultaneously with thyroid hormones, confusion, irritability and sleep disturbance may occur.

According to a published blind clinical trial in patients with recurrent venous thrombosis piracetam in 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, the release of β-thromboglobin. concentration of fibrinogen and von Willebrand factor (VIII: C; VIII: vW: Ag; VIII: vW: RCo). as well as the viscosity of whole blood and plasma. The possibility of changing the pharmacodynamics of piracetam under the influence of other drugs is low, because90% of the drug is excreted unchanged in the urine.

In concentrations of 142, 426 and 1422 mg / ml piracetam does not inhibit cytochrome P450 isoenzymes (CYP 1A2, 2B6, 2CS, 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 far beyond the concentration of 1422 mg / ml. Thus, the metabolic interactions of piracetam with other drugs are 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 (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.

When used simultaneously with drugs that stimulate the central nervous system, excessive stimulation of the central nervous system is possible.

With simultaneous use with neuroleptics reduces the risk of extrapyramidal disorders.

It is pharmaceutically compatible with solutions of dextrose (5%, 10%, 20%), fructose (5%, 10%.20%), 0.9% solution of sodium chloride, Ringer's solution, 20% mannitol solution. hydroxyethyl starch (6%, 10%).

Special instructions:

Due to the antiaggregant effect, 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.

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

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").

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.

It penetrates the hemodialysis apparatus through the filter membranes.

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

During the treatment period, 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 administration 200 mg / ml.

Packaging:

By 5 or 10 ml in polymeric ampoules made by technology blow-fill-seal "blow-fill-seal".

For 5 or 10 polymer ampoules, along with the instructions for medical use, put in a pack of cardboard.

Storage conditions:

3 years.

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

Shelf life:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Terms of leave from pharmacies:On prescription

Registration number:LP-002972

Date of registration:23.04.2015

The owner of the registration certificate:SLAVYANSKAYA APTEKA, LLC SLAVYANSKAYA APTEKA, LLC Russia

Manufacturer: & nbsp

SLAVYANSKAYA APTEKA, LLC Russia

Information update date: & nbsp22.09.2015

Illustrated instructions

Instructions

Pyracetam (Piracetam)