Lutset

Active material: Piracetam
When ATH: N06BX03
CCF: Nootropics
ICD-10 codes (testimony): F00, F01, F07, F07.2, F10.2, F10.3, F80, F81, G25.3, G30, I69, R42, S06, T90
When CSF: 02.14.01
Manufacturer: EGIS PHARMACEUTICALS Plc (Hungary)

Pharmaceutical form, composition and packaging

Pills, coated white or nearly white, Oval, lenticular, without smell, chamfered, scored on both sides, Engraved “E 242” on one side of the tablet; It is seen on a break outside the ring and the core shell white or nearly white.

Excipients: magnesium stearate, povidone K-30, macrogol 6000, dybutylsebaktat, Titanium dioxide (E171), talc, ethyl cellulose, gipromelloza.

30 PC. – jars of dark glass (1) – packs cardboard.

Pills, coated white or nearly white, Oval, lenticular, without smell, Engraved “E 243” on one side of the tablet; It is seen on a break outside the ring and the core shell white or nearly white.

Excipients: magnesium stearate, povidone K-30, macrogol 6000, dybutylsebaktat, Titanium dioxide (E171), talc, ethyl cellulose, gipromelloza.

20 PC. – jars of dark glass (1) – packs cardboard.

Solution for in / and the / m completely transparent, colorless, possible slight greenish tint, without smell.

Excipients: sodium acetate, glacial acetic acid, water d / and.

5 ml – colorless glass vials (5) – packings Valium plastic (2) – packs cardboard.

Pharmacological action

Nootropics. Piracetam – cyclic derivative of GABA. A direct impact on the brain. Lutset^® improves cognitive (cognitive) processes, such as the ability to learn, memory, Attention, ability to memorize, and also enhances mental performance, without the development of sedation and psychostimulant effects.

It affects the central nervous system in different ways: It changes the propagation speed of the excitation in the brain, neuronal plasticity and improves metabolic processes in neuronal cells. It improves communication between the hemispheres of the brain and synaptic conductance in neocortical structures, enhances mental performance, improves cerebral blood flow.

Lutset^® improves microcirculation in the brain, acting on the rheological characteristics of the blood, and causes vasodilatory action. Lutset^® It inhibits platelet aggregation and restores the elastic membrane of erythrocytes, as well as the ability of the latter to the passage through the microvasculature. It reduces adhesion of red blood cells. At a dose of 9.6 Mr. reduces levels of fibrinogen and von Willebrand factor in the 30-40% and prolongs bleeding time.

Lutset^® It provides a protective and restorative effect in violation of the functions of the brain as a result of hypoxia, intoxication or injuries. It reduces the severity and duration of the vestibular nystagmus.

Pharmacokinetics

Absorption

After oral administration piracetam is rapidly and almost completely absorbed from the gastrointestinal tract, C_max plasma levels achieved after 1 no. Bioavailability is about 100%. After oral administration of a single dose 2 г C_max is 40-60 ug / ml, which is achieved in plasma 30 minutes, and after 5 h in the cerebrospinal fluid.

Distribution and metabolism

V_d is about 0.6 l / kg. Piracetam selectively accumulates in the tissues of the cerebral cortex, primarily in the frontal, parietal and occipital lobes, in the cerebellum and basal ganglia.

It binds to plasma proteins.

Piracetam penetrate the BBB and placental barrier. Do not metabolized in the body.

Deduction

T_1/2 from plasma is 4-5 no, T_1/2 from cerebrospinal fluid – 8.5 no.

Excreted by the kidneys in unchanged form – 80-100%, by renal filtration. Renal clearance of piracetam in healthy volunteers is 86 ml / min.

Pharmacokinetics in special clinical situations

In renal insufficiency T_1/2 increases.

The pharmacokinetics of piracetam is not changed in patients with hepatic insufficiency.

Piracetam permeates through the membrane, used in hemodialysis.

Testimony

- Symptomatic treatment of psycho-organic syndrome, particularly in elderly patients, accompanied by memory loss, dizziness, low concentration and total activity, change in mood, conduct disorder, gait disturbance, as well as in patients with Alzheimer's disease and senile dementia of the Alzheimer type;

- The effects of treatment of ischemic stroke, such as speech disorders, violation of the emotional sphere, motor and mental activity;

- Alcoholism – for the treatment of withdrawal symptoms and psychoorganic;

- In the period of recovery after injury and intoxication of the brain;

- Treatment of vertigo and associated balance disorders, with the exception of dizziness mental origin;

- In the complex treatment of low learning in children, especially in cases of the acquisition of specific reading skills, letters, accounts, that can not be explained by mental retardation, inadequate training, or features of a family environment;

- For the treatment of cortical myoclonus as mono- or combination therapy.

Dosage regimen

Inside drug administered in a daily dose 30-160 mg / kg, the multiplicity of reception – 2-4 times / day.

B / or / m administered in a daily dose of 30-160 mg / kg (3-12 g / day), multiplicity of introduction – 2-4 times / day.

At symptomatic treatment of chronic psycho-organic syndrome depending on the severity of symptoms prescribe 1.2-2.4 g / day, and during the first week – 4.8 g / day.

At the treatment of the effects of stroke appointed 4.8 g / day.

At alcohol withdrawal syndrome – 12 g / day. Maintenance dose – 2.4 g / day.

Treatment vertigo and associated balance disorders appointed 2.4-4.8 g / day.

At cortical myoclonus Treatment begins with a dose of 7.2 g / day, every 3-4 increase the dose of the day 4.8 g / d to a maximum dose 24 g / day. Treatment continued throughout the period of illness. Every 6 months should attempt to reduce the dose or stop the drug, gradually reducing the dose by 1.2 g every 2 day in order to prevent attack. If there is no effect or a minor therapeutic effect of treatment is stopped.

When treating comatose states, and the difficulties of perception in people with injuries introducing drug / m or in / at an initial dose of 9-12 g / day, maintenance dose - 2.4 g / day. Treatment continues for at least 3 weeks.

Babies to correcting learning disabilities administered orally at a dose 3.2 g / day. Treatment continues throughout the school year.

In patients with impaired renal function requires correction mode depending on the spacecraft.

In elderly patients correcting the dose in the presence of renal failure and prolonged treatment is necessary to monitor renal function.

In patients with impaired liver function correction dosing regime is not required.

Tablets Lutsetama^® taken during meals or on an empty stomach, with some liquid (water, juice).

The solution Lutsetama^® for the / m or / in the introduction is compatible with the following infusion solutions: dextrose 5%, 10%, 20%; fructose 5%, 10%, 20%; levuloza 5%; sodium chloride 0.9%; dextran 40 – 10% in 0.9% sodium chloride solution; dextran 100 – 6% in 0.9% sodium chloride solution; Ringer; Ringer lactated; mannitol dextran; gidroksietilkraxmal 6%. Infusion solutions are stable for at least pyracetam 24 no.

Side effect

From the central and peripheral nervous system: 1.72% – giperkineziya; 1.13% – nervousness; 0.96% – drowsiness; 0.83% – depression; in rare cases - dizziness, headache, ataxia, disequilibrium, exacerbation of epilepsy, insomnia, confusion, excitation, alarm, hallucinations, increased sexual.

Metabolism: 1.29% – weight gain.

From the digestive system: in a few cases – nausea, vomiting, diarrhea, pain in the stomach.

Dermatological reactions: dermatitis, itch, rashes, edema.

Other: 0.23% – asthenia.

Side effects are more common in elderly patients, receiving the drug in a dose of 2.4 g / day, and disappear in most cases at lower doses.

Contraindications

- Hemorrhagic stroke;

- End-stage renal failure (at least QC 20 ml / min);

- Children up to age 1 year;

- Pregnancy;

- Lactation;

- Hypersensitivity to piracetam or pyrrolidone derivatives, as well as other components of the drug.

Pregnancy and lactation

There are no adequate and well-controlled clinical studies on the safety of the drug during pregnancy has not been.

Lutset^® should not be administered during pregnancy except in cases of emergency.

Piracetam crosses the placental barrier, excreted in breast milk. Concentration piracetam blood reaches neonates 70-90% on its concentration in the blood of the mother.

If necessary, use during lactation should stop breastfeeding.

Cautions

Due to the influence of piracetam on platelet aggregation, caution should be prescribed to patients with impaired hemostasis, during major surgery or in patients with symptoms of severe bleeding.

In the treatment of cortical myoclonus should avoid abrupt discontinuation, which may cause the resumption of seizures.

When long-term therapy in elderly patients is recommended regular monitoring of renal function, If necessary to adjust the dose depending on the results of research QC.

It penetrates through the filter membrane devices for hemodialysis.

Effects on ability to drive and operate machinery

Taking into account the possible side effects, the patient should be careful when driving or operating machinery.

Overdose

Treatment: immediately after oral administration can wash out the stomach or cause an artificial vomiting. Symptomatic therapy, which may include hemodialysis. No specific antidote. The effectiveness of hemodialysis for piracetam 50-60%.

Drug Interactions

While the use of thyroid extract can be increased irritability, disorientation and sleep disorders.

There was no interaction with clonazepam, phenytoin, fenoʙarʙitalom, sodium valproate.

Piracetam high doses (9.6 g / day) acenocoumarol improves patients with venous thrombosis (It noted a marked reduction in the level of platelet aggregation, fibrinogen level, von Willebrand factor, blood and plasma viscosity in comparison with the use of only acenocoumarol).

The ability to change under the influence of piracetam pharmacodynamics of other drugs is low, tk. 90% the drug is excreted unchanged in the urine.

In vitro пирацетам не угнетает изоферменты CYP1A2, 2AT 6, 2C8, 2C9, 2C19, 2D6, 2E1 and 4A9 / 11 in a concentration of 142, 426 and 1422 ug / ml. At a concentration of piracetam 1422 ug / ml was a slight inhibition of CYP2A6 (21%) and 3A4 / 5 (11%). However, the level of the two isoenzymes Ki sufficient in excess 1422 ug / ml. Therefore, metabolic interaction with other drugs is unlikely.

Receiving a dose of piracetam 20 mg / day did not change the level of the peak curve and the concentration of antiepileptic drugs in serum (Carbamazepine, phenytoin, phenobarbital, valproate) in patients with epilepsy, receiving the drug at constant dose.

Joint reception with ethanol had no effect on the level of concentration in the serum of piracetam, ethanol concentration in serum did not change when receiving 1.6 g piracetam.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

List B. The drug should be stored at a temperature of 15 ° to 30 ° C out of reach of children. Shelf life of the drug in tablet form – 5 years, in the form of solution for injection - 2 year.