Composition, form of production and packaging
The solution for intravenous and intravenous administration is clear, colorless or with a slight greenish tint, odorless.
1 ml of 1 amp.
piracetam 200 mg 1000 mg
Excipients: sodium acetate trihydrate - 5 mg, glacial acetic acid - up to pH 5.8, water d / u - up to 5 ml.
5 ml - ampoules of colorless glass with a break point and two red rings (5) - packings of cellular plastic (2) - packs of cardboard.
The solution for intravenous and intravenous administration is clear, colorless or with a slight greenish tint, odorless.
1 ml of 1 amp.
piracetam 200 mg 3000 mg
Excipients: sodium acetate trihydrate - 15 mg, glacial acetic acid - up to pH 5.8, water d / u - up to 15 ml.
15 ml - ampoules of colorless glass with a break point (4) - packings contour mesh (1) - packs cardboard.
15 ml - ampoules of colorless glass with a break point (4) - packings contour mesh (5) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2016.
PHARMACHOLOGIC EFFECT
Nootropic preparation. Pyracetam is a cyclic derivative of gamma-aminobutyric acid (GABA). Pyracetam directly affects the brain. Lucucim В® improves cognitive (cognitive) processes, such as learning ability, memory, attention, memory ability, and increases mental performance without developing a sedative and psychostimulating effect.
Has an influence on the central nervous system in various ways: it changes the speed of propagation of excitation in the brain, improves neuronal plasticity and metabolic processes in nerve cells. Improves the interaction between the cerebral hemispheres and synaptic conductivity in neocortical structures, increases mental performance, improves cerebral blood flow.
Lucetam В® improves microcirculation in the brain, affecting the rheological characteristics of the blood, and does not cause vasodilating action.
Lucetam В® inhibits platelet aggregation and restores the elasticity of the erythrocyte membrane, and the ability of the latter to pass through the microcirculatory bed.Reduces the adhesion of red blood cells. 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.
Lucetam В® has a protective and restorative effect in case of impaired brain function due to hypoxia, intoxication or trauma.
Reduces the severity and duration of the vestibular nystagmus.
PHARMACOKINETICS
Distribution and Metabolism
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.
Pyracetam penetrates the GEB and the placental barrier. It is not metabolized in the body.
Excretion
T 1/2 from the blood plasma is 4-5 h, T 1/2 of the cerebrospinal fluid is 8.5 h.
It is excreted by the kidneys in an unchanged form - 80-100%, by renal filtration. The renal clearance of piracetam in healthy volunteers is 86 ml / min.
Pharmacokinetics in special clinical cases
With renal failure, T 1/2 increases.
The pharmacokinetics of pyracetam does not change in patients with hepatic insufficiency.
Piracetam penetrates through membranes used in hemodialysis.
INDICATIONS
Adults
- symptomatic treatment of psycho-organic syndrome, accompanied by a decrease in memory, reduced concentration of attention and general activity, mood changes, behavioral disorder, gait disturbance;
- treatment of vertigo (vertigo) and associated disorders of balance, with the exception of dizziness of vasomotor and psychic origin;
- Cortical myoclonia as a monotherapy or as part of a complex therapy;
- cupping sickle-cell vaso-occlusive crisis.
Children and teens
- as part of the complex therapy of dyslexia in children aged 8 years, in combination with other methods, including speech therapy;
- prophylaxis and relief of sickle-cell vaso-occlusive crisis.
DOSING MODE
In / in. The daily dose is 30-160 mg / kg (3-12 g / day), the frequency of administration is 2-4 times / day. Parenteral administration of piracetam is given if oral administration of the drug is not possible, for example, with difficulty swallowing, or when the patient is in a coma.
The solution of Lutzamum is compatible with the following infusion solutions: glucose 5%, 10%, 20%; fructose 5%, 10%, 20%; levulose 5%; sodium chloride 0.9%;dextran 40 10% in a 0.9% solution of sodium chloride; dextran 100 6% in a 0.9% solution of sodium chloride; Ringer's solution; mannitol-dextran; hydroxyethyl starch 6%.
Infusion solutions with the addition of pyracetam are stable for at least 24 hours.
Adults
With symptomatic treatment of chronic psychoorganic syndrome , depending on the severity of symptoms, 2.4-4.8 g / day are prescribed, spreading over 2-3 injections.
In the treatment of vertigo and associated disorders, 2.4-4.8 g / day are prescribed for the balance , divided into 2-3 injections.
In cortical myoclonia, treatment starts at 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 is reached. Later on they switch to the oral form of Lucetam В® . Treatment continues throughout the period of the disease. To prevent the deterioration of patients should not stop using the drug.It is necessary to gradually reduce the dose of the drug. In the absence of effect or the presence of a slight therapeutic effect, treatment is discontinued.
For the treatment of sickle-cell vaso-occlusive crisis, the drug is used at a dose of 300 mg / kg of body weight, dividing into 4 doses.
Children and teens
As part of the complex therapy of dyslexia in children aged 8 years : the daily dose is 3.2 g, divided into 2 injections.
For arresting sickle-cell vaso-occlusive crisis in children over 3 years of age, 300 mg / kg of body weight is prescribed, divided into 4 doses.
Special patient groups
Since pyracetam is excreted from the body by the kidneys, caution should be exercised in the treatment of patients with renal insufficiency .
The dose is determined based on the assessment of QC in the patient, which is calculated by the formula:
CC = [140 - age (years)]? body weight (kg) / 72 - serum creatinine (mg / dL)
In women, the obtained value should be multiplied by 0.85.
Treatment for such patients is prescribed depending on the severity of renal failure, adhering to the following recommendations:
Renal failure Creatinine clearance (ml / min) Dosage
Norm> 80 Usual Dose
Light 50-79 2/3 of the usual dose in 2-3 doses
Average 30-49 1/3 of the usual dose in 2 doses
Severe <30 1/6 of the usual dose, once
The final stage <20 is contraindicated
In elderly patients, the dose is adjusted in the presence of renal failure. With prolonged therapy, monitoring of renal function is necessary.
Patients with a violation of liver function correction of the dose is not required.
In patients with impaired functions of both kidney and liver , dosing is performed according to the scheme described for patients with renal insufficiency.
SIDE EFFECT
On the part of the nervous system: hyperkinesia, irritability, drowsiness, depression, asthenia (these symptoms are more common in elderly patients receiving the drug at doses above 2.4 g / day, in most cases regress of such symptoms can be achieved by lowering the dose of the drug). Headache, dizziness, insomnia, mental arousal, anxiety, imbalance, tremor, ataxia, exacerbation of epilepsy, anxiety, hallucinations, confusion, increased libido.
From the coagulation system: bleeding.
From the side of the immune system: hypersensitivity, incl. anaphylaxis.
From the side of the hearing organ and labyrinthine disturbances: dizziness (vertigo).
From the cardiovascular system: a decrease or increase in blood pressure.
On the part of the digestive system: nausea, vomiting, diarrhea, abdominal pain, epigastric pain.
From the side of metabolism and nutrition: weight gain.
From the skin: dermatitis, itching, urticaria.
Allergic reactions: angioedema.
General disorders and disorders at the site of administration: pain at the injection site, thrombophlebitis, hyperthermia.
CONTRAINDICATIONS
- psychomotor agitation at the time of prescribing;
- Huntington's chorea;
- hemorrhagic stroke;
- chronic renal failure of severe degree (with CC less than 20 ml / min);
- children's age till 3 years;
- Pregnancy;
- lactation;
- hypersensitivity to pyracetam or pyrrolidone derivatives, as well as other components of the drug.
With caution should appoint a drug for violations of hemostasis, extensive surgical interventions, severe bleeding, chronic kidney failure (with KK 20-80 ml / min).
PREGNANCY AND LACTATION
Adequate and strictly controlled clinical studies on the safety of the drug during pregnancy have not been conducted, so Lucetam В® should not be prescribed during pregnancy.
Piracetam penetrates the placental barrier, excreted in breast milk. If it is necessary to use lactation, breastfeeding should be discontinued.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated use of the drug for chronic renal failure of a serious degree (with CC less than 20 ml / min).
With caution should prescribe the drug for chronic kidney failure (with KK 20-80 ml / min). The dose is determined based on the QA score.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
In patients with impaired liver function, correction of the dosing regimen is not required.
APPLICATION FOR CHILDREN
Contraindication: children under 3 years.
APPLICATION IN ELDERLY PATIENTS
In elderly patients, the dose is adjusted in the presence of renal failure. With prolonged therapy, monitoring of renal function is necessary.
SPECIAL INSTRUCTIONS
Due to the effect of piracetam on platelet aggregation, caution should be given to patients with hemostatic disorders, during major surgery or patients with symptoms of severe bleeding.
In the treatment of cortical myoclonia, sudden interruption in treatment should be avoided, which can lead to the resumption of seizures.
The use of the drug to stop the sickle-cell vaso-occlusive crisis in doses below 160 mg / kg / day, as well as erratic non-systemic application can cause a second crisis.
With prolonged therapy, elderly patients are recommended regular monitoring of renal function, if necessary, dose adjustment is performed depending on the results of the QC study.
It penetrates the hemodialysis apparatus through the filter membranes.
Influence on the ability to drive vehicles and work with mechanisms
Taking into account possible side effects, the patient should be careful when driving a car and working with mechanisms.
OVERDOSE
Pyracetam is not toxic even in high doses.
Symptoms: abdominal pain, diarrhea with an admixture of blood.
Treatment: symptomatic therapy, hemodialysis (efficacy 50-60%). There is no specific antidote.
DRUG INTERACTION
When used simultaneously with the thyroid extract (T 3 + T 4 ), increased irritability, disorientation and sleep disturbances are possible.
No interaction with clonazepam, phenytoin, phenobarbital, valproic acid was observed.
Pyracetam in high doses (9.6 g / day) increases the effectiveness of acenocoumarol in patients with venous thrombosis (there was a more pronounced decrease in platelet aggregation, fibrinogen, von Willebrand factors, viscosity of blood and plasma compared to acenocoumarol alone).
The possibility of changing the pharmacodynamics of piracetam under the influence of other drugs is low, because 90% of the drug is excreted unchanged in the urine.
In vitro, pyracetam does not inhibit cytochrome P450 isoenzymes CYP1A2, 2B6, 2C8, 2C19, 2D6, 2E1, 3A4 / 5 and 4A9 / 11 at a concentration of 142, 426 and 1422 Ојg / ml. At a piracetam concentration of 1422 Ојg / ml, slight inhibition of CYP2A6 (21%) and 3A4 / 5 (11%) was noted. However, the Ki value required to inhibit these two CYP isoenzymes is significantly higher than 1422 Ојg / ml. Therefore, metabolic interaction with other drugs is unlikely.
Admission piracetam at a dose of 20 mg / day did not affect C max and AUC antiepileptic drugs in the blood serum (carbamazepine, phenytoin, phenobarbital, valproate) in epilepsy patients receiving the drug in a constant dose.
The combined administration with ethanol did not affect the level of serum piracetam concentration, the concentration of ethanol in the blood serum did not change with piracetam at a dose of 1.6 g.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored at a temperature of 15 В° to 25 В° C out of the reach of children. Shelf life - 3 years.
