Pyracetam-Ferein - 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 piracetam in patients with cerebral dysfunction increases concentration and improves cognitive function, which is accompanied by changes in encephalogram (increase of α and β activity, decrease of 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 cytological rigidity of erythrocytes, improves their deformability and ability to filter.

Pharmacokinetics:

The pharmacokinetic profile of piracetam is linear and does not depend on time. Characteristic of low variability in a large range of doses. Constant concentration in the plasma is achieved after 3 days from the beginning of the reception.

The volume of the distribution (Vd) 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.

It does not bind to blood plasma proteins, it is not metabolized in the body. The half-life (T_1/2) is 4 to 5 hours for blood serum and 8.5 hours for cerebrospinal fluid. The half-life does not depend on the route of administration. 80 - 100% of piracetam 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 does not change in patients with hepatic insufficiency.

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.
Horea Huntington.
Acute disturbance of cerebral circulation (hemorrhagic stroke).
The final stage of renal failure (with creatinine clearance less than 20 ml / min).
Age to 3 years.

Pregnancy and lactation:

Studies in animals showed no damaging effects on the embryo and its development, including in the postnatal period, and also did not change the course of pregnancy and childbirth.

Controlled studies of the use of the drug during pregnancy were not conducted.

Piracetam penetrates the placental barrier and into breast milk. The concentration of the drug in newborns reaches 70-90% of its concentration in the mother's blood. Pyracetam should not be administered during pregnancy. It is necessary to refrain from breastfeeding while prescribing a piracetam to a woman.

Dosing and Administration:

Intravenously sprayed or drip, intramuscularly. The daily dose is divided into 2-4 admission.

Parenteral administration of piracetam is prescribed when it is not possible to use oral forms of the drug (unconsciousness, difficulty swallowing). Intravenous administration is preferred. Intravenous infusion of the drug in a daily dose is performed through a catheter at a constant rate for 24 hours (for example, in the initial stage of treatment with severe myoclonus).Pre-drug diluted in a compatible infusion solutions: dextrose 5%, 10% or 20%; fructose 5%, 10%, 20%; sodium chloride 0.9%; dextran 40 10%; in 0.9% sodium chloride solution; Ringer's solution; solution of mannitol 20%. The total volume of solution intended for administration is determined taking into account the clinical indications and the patient's condition.

Bolus intravenous injection is performed for at least 2 minutes, wherein the daily dose divided into multiple administrations (2 - 4) at regular intervals so that the dose per administration is less than 3, the drug is administered intramuscularly, if the introduction through the vein is difficult. The volume of the solution administered intramuscularly can not exceed 5 ml.

The frequency of administration of the drug is similar to that of its intravenous or oral administration.

When the opportunity arises, they switch to oral administration of the drug (see instructions for the medical use of the respective forms of the drug). The duration of treatment is determined by the doctor depending on the disease and taking into account the dynamics of the symptoms.

Symptomatic treatment of intellectually-mnestic disorders without diagnosis of dementia: 2,4 - 4,8 g / day (2 or 3 sub-doses).

To reduce manifestations of cortical myoclonus treatment starts with a dose of 7.2 g / day, every 3-4 days the dose is increased by 4.8 g / day (2 or 3 sub-doses) until the maximum dose of 24 g / day is reached. 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.

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

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) x body weight (kg)] / [72 x KK_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	usual dose
Lightweight	50-79	2/3 of the usual dose in 2 to 3 doses
Average	30-49	1/3 of the usual dose in 2 divided doses
Heavy	20-30	1/6 of the usual dose once
The final stage	<20	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 a dose adjustment. Patients with impaired functions and kidneys and liver, dosing is carried out according to the scheme (see the section "Dosing to patients with impaired renal function").

Side effects:

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

From the immune system: anaphylactoid reactions, hypersensitivity.

Metabolic disorders and eating disorders: weight gain.

From the side of the psyche: drowsiness, nervousness, agitation, anxiety, depression, hallucinations, confusion.

From the nervous system: insomnia, headache, asthenia, hyperkinesia, ataxia, imbalance, tremor.

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

From the organs of hearing: Vertigo.

From the skin: angioedema, dermatitis, itching, urticaria.

From the side of the reproductive system: increased sexual desire.

Other: thrombophlebitis, pain in the area of injection, hyperthermia, hypotension (after intravenous administration).

Overdose:

A single case of development of diarrhea in the form of diarrhea with blood and pain in the abdomen with taking the drug inside at a daily dose of 75 g. It seems that this was due to the use of a large total dose of sorbitol, which was previously part of the solution for oral administration.

In case of a significant overdose, rinse the stomach or induce vomiting.

It is recommended to carry out symptomatic therapy, which may include hemodialysis. There is no specific antidote. The efficacy of hemodialysis for piracetam is 50 - 60%.

Interaction:

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

According to a published study of patients with recurrent venous thrombosis piracetam in a dose of 9.6 g / day does not change the dose

asynocoumarol necessary to achieve the INR (international normalized ratio) 2.5 to 3.5, but compared to 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 factor of von Willebrand (VIII: C; VIII: vW: Ag; VIII: vW: RCo), as well as viscosity of blood and serum.

In vitro piracetam does not inhibit cytochrome P450 isoenzymes such as CUR1A2, 2B6, 2C8, 2C9, 2CI9, 2D6, 2E1 and 4A9 / 11 at concentrations 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 level of inhibition constant (Ki) of these two isoenzymes is sufficient when exceeding 1422 μg / ml. Therefore, metabolic interaction with other drugs is unlikely.

Admission of piracetam at a dose of 20 g / day for 4 weeks in patients with epilepsy who received stable doses of antiepileptic drugs did not change the maximum serum concentration and AUC (area under the curve) of antiepileptic drugs (carbamazepine, phenytoin, phenobarbital and valproate.)

At simultaneous application with hormones of a thyroid gland the reports on confusion of consciousness, irritability and disturbance of a dream are marked. Joint reception with alcohol does not affect the concentration of piracetam in the serum; the concentration of the standard in the serum did not change with the intake of 1.6 g of piracetam.

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

Special instructions:

Due to the antiaggregant effect (section pharmacodynamics), piracetam should be administered with caution to patients with severe hemorrhagic disorders, the risk of bleeding (eg, gastric ulcer), hemostasis disorders, haemorrhagic cerebrovascular disorders in the history, in patients with surgical interventions, including dental interventions, in patients taking anticoagulants and antiplatelet agents, including low dose of aspirin.

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

24 mg of the drug contains about 1 mmol (23 mg) of sodium.

Because the piracetam is excreted through the kidneys, care should be taken when prescribing the drug to patients with renal insufficiency.

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

Piracetam penetrates the filtration membranes of hemodialysis apparatus.

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,requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Solution for intravenous and intramuscular injection 200 mg / ml.

Packaging:

5 ml into neutral glass ampoules.

5 ampoules are placed in a contour mesh package made of a polyvinyl chloride film.

For 1.2 contour mesh packages together with instructions for use and a knife ampoule or scarifier in a cardboard bundle.

For 5, 10 ampoules together with the instruction for use and a knife ampoule or scarifier in a pack with an insert with cells from cardboard box.

For 25, 50, 100 contour cell packs of 5 ampoules together with an equal number of instructions for use in a box of corrugated cardboard.

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 expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N000577 / 01

Date of registration:10.09.2008

The owner of the registration certificate:BRYNTSALOV-A, CJSC BRYNTSALOV-A, CJSC Russia

Manufacturer: & nbsp

BRYNTSALOV-A, CJSC Russia

Information update date: & nbsp23.09.2015

Illustrated instructions

Instructions

Piracetam-Ferein® (Piracetam-Ferein®)