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

Pyracetam is a nootropic drug that directly improves the functions performed by the brain. Pyracetam has an effect on the central nervous system in various ways: it modifies neurotransmission in the brain, improves metabolic conditions,promoting neutral plasticity, improves microcirculation, affecting the rheological characteristics of the blood and not causing vasodilation.

Prolonged or short-term use of piracetam in patients with cerebral dysfunction increases attention concentration and improves cognitive functions, which is manifested by significant changes in the electroencephalogram (increase in α and β activity, decrease in δ activity).

Piracetam promotes restoration of cognitive abilities after various cerebral injuries due to hypoxia, intoxication or electroconvulsive therapy.

Reduces the duration of the provoked vestibular neuronitis.

The drug is indicated for the treatment of cortical myoclonus both as monotherapy and as part of complex therapy.

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

Pharmacokinetics:

Suction. After oral administration piracetam quickly and almost completely absorbed from the gastrointestinal tract. Bioavailability is about 100%.After a single dose at a dose of 3.2 g, the maximum concentration (C_max) is 84 μg / ml, after repeated intake of 3.2 g 3 times a day - 115 μg / ml and is achieved after 1 hour in the blood serum and after 5 hours in the cerebrospinal fluid. Eating reduces C_max by 17% and increases the time of its achievement (T_max) up to 1.5 hours. At women at reception of a preparation in a dose of 2,4 g С_max and the area under the concentration-time curve (AUC) is 30% higher than that of men.

Distribution. The volume of distribution is about 0.6 l / kg. Pyracetam penetrates through blood-brain and placental barriers. In animal studies, 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. Does not bind to blood plasma proteins.

Metabolism. It is not metabolized.

Excretion. The half-life (T_1/2) is 4-5 hours for blood serum and 8.5 hours for cerebrospinal fluid. 80-100% of pyracetam is excreted by the kidneys unchanged by glomerular filtration. The total clearance of piracetam in healthy volunteers is 80-90 ml / min. T_1/2lengthened with renal failure (with terminal chronic renal failure - up to 59 hours).The pharmacokinetics of pyracetam do not change in patients with hepatic insufficiency.

Indications:

symptomatic treatment of intellectual-mnestic disorders in the absence of an established diagnosis of dementia;
a decrease in 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, a trial course of treatment can be conducted in a specific case).

Contraindications:

hypersensitivity to pyracetam or pyrrolidone derivatives, as well as other components of the drug;
hemorrhagic stroke;
Huntington's chorea;
the final stage of renal failure;
childhood;
pregnancy and lactation.

Carefully:

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

In case of deterioration of the patient should stop treatment with the drug.

If you have any of these diseases, consult a doctor before taking the drug.

Pregnancy and lactation:

In experimental animal studies, there was no direct or indirect effect on pregnancy, embryo / fetal development, childbirth, or postnatal development.

Controlled studies of the use of the drug during pregnancy 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. The drug should not be administered during pregnancy.

During breastfeeding should refrain from taking the drug, if the expected benefits of using the drug exceeds the risk of abandoning breastfeeding.

Dosing and Administration:

Inside, during meals or on an empty stomach, squeezed with liquid.

Symptomatic treatment of intellectual-mnestic disorders: 2,4-4,8 g / day in 2-3 hours. Treatment lasts at least 3 weeks.

Treatment of cortical myoclonia: begin with a dose of 7.2 g / day and every 3-4 days the dose is increased by 4.8 g / day until a maximum dose of 24 g / day in 2-3 doses. Treatment continues throughout the period of the disease. Every 6 months, attempts should be made to reduce the dose or discontinue the drug,gradually reducing the dose by 1.2 g / day every 2 days. Treatment continues throughout the period of the disease. In the absence of effect or the presence of a slight therapeutic effect, treatment is discontinued.

Dosing to patients with impaired renal function: the dose should be adjusted depending on the amount of creatinine clearance (CC):

The creatinine clearance for men is 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

Elderly patients are adjusted the dose in the presence of renal failure, with prolonged therapy, it is necessary to monitor the functional state of the kidneys.

Dosing to patients with impaired liver function: patients with a dysfunction of the liver do not need correction of the dose.Patients with dysfunction of the kidneys and liver dosing is carried out according to the scheme (see the section "Dosing to patients with impaired renal function").

Side effects:

The frequency of unwanted reactions is given in accordance with the following scale: very often (≥ 10%); often (≥ 1% and <10%); infrequently (≥ 0.1% and <1%); rarely (≥ 0.01% and <0.1%); very rarely (<0.01%).

From the side of the blood and lymphatic system: very rarely - hemorrhagic disorders.

From the immune system: very rarely - hypersensitivity, anaphylactoid reactions.

From the side of metabolism and nutrition: often - an increase in body weight.

From the side of the psyche: often - arousal, nervousness, depression; infrequently - anxiety, confusion; very rarely - drowsiness, hallucinations.

From the nervous system: often hyperkinesis, irritability; infrequently - asthenia; very rarely - ataxia, headache, imbalance, insomnia, exacerbation of epilepsy, tremor.

From the organ of hearing: very rarely - vertigo.

From the digestive system: very rarely - nausea, vomiting, diarrhea, abdominal pain (including gastralgia).

From the skin: very rarely - dermatitis, itching, hives, angioedema.

From the side of the reproductive system: very rarely - increased sexual desire.

If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose:

When 75 g of piracetam was taken, dyspeptic phenomena such as diarrhea with blood and abdominal pain were noted. No other symptoms of piracetam overdose have been observed.

Treatment: induction of vomiting, gastric lavage. Symptomatic therapy, hemodialysis (efficacy 50-60%). There is no specific antidote.

Interaction:

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

At simultaneous application with hormones of a thyroid gland the reports on confusion of consciousness, irritability and disturbance of a dream are marked.

According to a published study of patients with recurrent venous thrombosis piracetam in a dose of 9.6 g / day improves the effectiveness of indirect anticoagulants (there was a more pronounced decrease in platelet aggregation,concentration of fibrinogen, von Willebrand factors, viscosity of blood and plasma in comparison with the use of only indirect anticoagulants).

In vitro piracetam It does not inhibit the isoenzymes CYP1A2, 2B6, 2C8, 2C19, 2D6, 2E1, 4A4 / 5 and 4A9 / 11 of cytochrome P 450 at a concentration of 142, 426 and 1422 μg / ml. For a concentration of 1422 μg / ml, a minimal inhibition of the isoenzyme CYP 2A6 (21%) and isoenzyme ZA4 / 5 (11%) was observed. However, the value of the inhibition constant (Ki) required to inhibit these two isoenzymes is significantly higher than 1422 μg / ml. Thus, metabolic interaction with other drugs is unlikely.

Receiving piracetam at a dose of 20 g / day for 4 weeks did not change the maximum concentration in the serum and AUC of antiepileptic drugs (carbamazepine, phenytoin, phenobarbital, valproate).

Joint reception with alcohol did not affect the concentration of piracetam in the blood serum; the concentration of ethanol in the serum did not change with the intake of 1.6 g of piracetam. You should inform your doctor about all the medications that you are taking.

Special instructions:

Due to the influence of piracetam on platelet aggregation, caution is recommended when administering the drug to patients with hemostasis disorder, during major surgeries or patients with symptoms of severe bleeding.

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, dose adjustment is performed depending on the results of the study of creatinine clearance.

Piracetam penetrates the filtration membranes of hemodialysis apparatus.

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:

Capsules 400 mg.

Packaging:

For 60 capsules in a can of polymer, 10 capsules per circuit cell packaging.

One can of polymer or 6 contour mesh packages together with instructions for medical use in a pack of cardboard.

Storage conditions:

In dry, the 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 expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N001713 / 01

Date of registration:09.09.2008

The owner of the registration certificate:FARMPROJECT, CJSC FARMPROJECT, CJSC Russia

Manufacturer: & nbsp

FARMPROJECT, CJSC Russia

Information update date: & nbsp16.09.2015

Illustrated instructions

Instructions

Pyracetam (Piracetam)