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

1 ml of the solution contains: active substance: piracetam - 200 mg; auxiliary substances: sodium acetate - 1 mg, acetic acid - up to pH 5.8, water for injection - up to 1 ml.

Description:

Transparent colorless or slightly colored liquid.

Pharmacotherapeutic group:Nootropic agent.

ATX: & nbsp

N.06.B.X.03 Pyracetam

Pharmacodynamics:

The active component is piracetam, a cyclic derivative of gamma-aminobutyric acid (GABA).

Pyracetam is a nootropic remedy that directly affects the brain, improving cognitive (cognitive) processes, such as learning ability, memory, attention, and mental performance. Pyracetam affects the central nervous system (CNS) in various ways: by changing the speed of propagation of excitation in the brain, improving metabolic processes in nerve cells, improving microcirculation, affecting the rheological characteristics of the blood, without providing vasodilating action. Improves connectivity between 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 effect in the violation of brain function due to hypoxia and intoxication.

Pyracetam reduces the severity and duration of the vestibular nystagmus.

Pharmacokinetics:

The half-life of the drug from plasma is 4.5 hours, and 8.5 hours from the cerebrospinal fluid, which is elongated in renal failure.

The pharmacokinetics of pyracetam do not change in patients with hepatic insufficiency. Penetrates through the blood-brain and placental barriers and membranes used in hemodialysis. When tested on animals piracetam selectively accumulated 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 secreted by the kidneys in an unchanged form 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;

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:

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).
Psychomotor agitation at the time of prescribing.
Children under 3 years.

Carefully:

violation of hemostasis;
extensive surgical interventions;
heavy bleeding.

Pregnancy and lactation:

Studies in animals have not shown a 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. The concentration of the drug in newborns reaches 70-90% of its concentration in the blood 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.

Piracetam penetrates into breast milk. Pyracetam should not be used during breastfeeding, or breastfeeding should be discontinued when treated with piracetam.When deciding whether to abort breastfeeding or refusing 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. Intramuscularly. 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 a daily dose is performed through a catheter at a constant rate for 24 hours a day. The total volume of the solution intended for administration is determined taking into account the clinical indications and the patient's condition.

Bolus intravenous administration is performed for at least 2 minutes, the daily dose is then divided into several injections (2-4) at regular intervals so that the dose per administration does not exceed 3 g.

Intramuscularly the drug is administered, 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.If there is an opportunity, they switch to oral administration of the drug (see instructions for the medical use of the appropriate forms of release 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 intellectual-mnestic disorders. 2,4-4,8 g / day (2 or 3 sub-doses).

Cortical myoclonus. Treatment begins with a dose of 7.2 g / day, every 3-4 days the dose is increased by 4.8 g / day until the maximum dose of 24 g / day (2 or 3 sub-doses) 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 failure	QC (ml / min)	Dosing regimen
Norm	>80	usual dose
Lightweight	50-79	2/3 of the usual dose in 2-3 times of admission
Average	30-49	1/3 of the usual dose in 2 divided doses
Heavy	<30	1/6 of the usual dose once
The final stage	-	contraindicated

Older patients are given a dose adjustment in the presence of kidney failure, prolonged therapy requires monitoring of 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 "Dosing to patients with impaired renal function").

Side effects:

Frequency of occurrence: very often more than 1/10, often more than 1/100 and less than 1/10, infrequently more than 1/1000 and less than 1/100, rarely more than 1/10000 and less than 1/1000, very rarely - less than 1/10000, the frequency is unknown - insufficient data available to estimate the incidence of side effects. Side effects identified in clinical trials:

From the side of the psyche: often - nervousness (1.13%); infrequently, depression (0.83%).

From the nervous system: often - hyperkinesis (1.72%); infrequently - drowsiness (0,96%), asthenia (0,23%).

From the side of metabolism and nutrition: often - an increase in body weight (1.29%).

Side effects, revealed by the results of post-registration observation:

From the side of the psyche: frequency unknown - excitation, anxiety, hallucinations, confusion.

From the side of the nervous system, frequency unknown - ataxia, imbalance, exacerbation of epilepsy, headache, insomnia, tremor.

From the digestive system. frequency unknown - nausea, vomiting, diarrhea, abdominal pain (including gastralgia).

From the skin: frequency unknown - dermatitis, itching, urticaria.

Allergic reactions: frequency unknown - hypersensitivity, angioedema, anaphylactoid reactions.

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

From the organs of hearing: frequency unknown - vertigo.

On the part of the reproductive system: frequency unknown - increased sexual desire.

Others: rarely - pain in the area of injection, thrombophlebitis, 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 the intake of the drug inside a daily dose of 75 g; Apparently, this was due to the use of a large total dose of sorbitol,which is part of the drug earlier for the dosage form solution for oral administration. There were no other cases of drug overdose.

Treatment: In case of an overdose, symptomatic therapy is recommended, 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, since 90% of the drug is excreted unchanged by the kidneys.

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 at a dose of 9.6 g / day does not change the dose of acenocoumarol necessary to achieve INR (international normalized ratio) 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, beta-thromboglobin release, fibrinogen and vWF, as well as blood and serum viscosity.

In concentrations of 142, 426 and 1422 mg / ml piracetam does not inhibit cytochrome P450 isoenzymes. For a concentration of 1422 mg / ml, a minimal inhibition of AMS 2A6 (21%) and SA4 / 5 (11%) was observed. However, the normal values of the inhibition constant (Ki), it is possible to achieve at a higher concentration. Thus, the metabolic interaction of piracetam 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).

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.

Special instructions:

Due to the antiaggregant effect, piracetam should be administered with caution to patients with severe hemorrhagic disorders, a risk of bleeding (eg, gastric ulcer), including hemostasis disorders, haemorrhagic cerebrovascular disorders in the anamnesis,in patients with surgical interventions, dental interventions, in patients taking anticoagulants and antiaggregants, including 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 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, since 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 that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Solution for intravenous and intramuscular injection 200 mg / ml.

Packaging:

By 5 ml per ampoule polymer from high-density polyethylene or from low-pressure polyethylene,or from polyethylene for medical purposes, or from polyethylene or polypropylene for infusion solutions and injections.

On polymer ampoules paste labels from paper label, writing or

The text of the label is applied directly to the ampoule by a polymer method of drop-jet printing.

For 10, 100 ampoules of polymer with instructions for use are placed in a pack of 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.

Not. apply at the expiration date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-003631/10

Date of registration:30.04.2010

The owner of the registration certificate:UPDATE OF PFC, CJSC UPDATE OF PFC, CJSC Russia

Manufacturer: & nbsp

UPDATE, PFC CJSC Russia

Information update date: & nbsp23.09.2015

Illustrated instructions

Instructions

Pyracetam Beefus (Piracetam bufus)