Lucetam, 200 mg/ml, solution for intravenous and intramuscular administration, 5 ml, 10 pcs.

Pharmacological properties of the drug Lucetam

The active component of Lucetam is piracetam, a cyclic derivative of γ-aminobutyric acid. Piracetam is a nootropic drug that has a positive effect on metabolic processes and blood circulation in the brain, improving cognitive processes such as learning ability, memory, attention, and mental performance. The drug affects the central nervous system 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 and without having a vasodilating effect. Improves connections between the cerebral hemispheres and synaptic conduction in neocortical structures. Piracetam inhibits platelet aggregation and restores the elasticity of the erythrocyte membrane, reduces the adhesion of erythrocytes. At a dose of 9.6 g, it reduces the level of fibrinogen and von Willibrand factors by 30–40% and increases bleeding time. Piracetam has a protective and restorative effect in cases of impaired brain function due to hypoxia and intoxication. Piracetam reduces the severity and duration of vestibular nystagmus. After oral administration, piracetam is quickly and almost completely absorbed, the maximum concentration is reached 1 hour after administration. Bioavailability is about 100% after taking a single dose of 2 g. The volume of distribution of piracetam is about 0.6 l/kg body weight. The half-life of the drug from blood plasma is 4–5 hours and 8.5 hours from cerebrospinal fluid; this period increases with renal failure. Does not bind to blood plasma proteins and is not metabolized in the body. 80–100% of piracetam is excreted unchanged by the kidneys through renal filtration. The renal clearance of piracetam in healthy volunteers is 86 ml/min. The pharmacokinetics of piracetam does not change in patients with liver failure. Piracetam penetrates the blood-brain and placental barriers and membranes used in hemodialysis. In animal studies, piracetam selectively accumulates in the tissues of the cerebral cortex, mainly in the frontal, parietal and occipital lobes, in the cerebellum and basal ganglia. IV administration When administered IV, the effect of piracetam begins quickly. Bioavailability - 100%. The maximum concentration in the cerebrospinal fluid is achieved within 2-8 hours. The half-life from the blood plasma is 4-5 hours, from the cerebrospinal fluid - 6-8 hours. High concentrations of the drug are determined in the cerebral cortex and cerebellum, in some basal ganglia. The drug penetrates the placenta and into breast milk and is not metabolized in the body. Piracetam is excreted by the kidneys mainly unchanged. Within 24–30 hours after a single dose, 90–100% of the administered dose of piracetam is eliminated. About 1–2% are detected in feces.

Lucetam 800 mg 30 pcs. film-coated tablets

pharmachologic effect

Nootropic drug.
It has an effect on the central nervous system in various ways: it modifies neurotransmission in the brain, improves conditions conducive to neuronal plasticity, improves microcirculation, affecting the rheological characteristics of the blood and without causing vasodilation. The use of piracetam in patients with cerebral dysfunction increases concentration and improves cognitive function, which is manifested by significant changes in the EEG (increased α and β activity, decreased δ activity).

Promotes the restoration of cognitive functions due to various disorders, such as hypoxia, intoxication or electroconvulsive therapy. Reduces the duration of vestibular neuronitis.

Piracetam inhibits increased aggregation of activated platelets and, in the case of pathological rigidity of red blood cells, improves their deformability and filtration ability.

Composition and release form Lucetam 800 mg 30 pcs. film-coated tablets

Tablets - 1 tablet:

• Active substance: piracetam 800 mg.
• Excipients: magnesium stearate, povidone K-30.
• Shell composition: dibutyl sebacate, ethylcellulose (in the form of an aqueous suspension), opadry white (macrogol 6000, titanium dioxide, talc, hypromellose).

10 pieces. - blisters (3) - cardboard packs.

20 pcs. - dark glass jars (1) - cardboard packs.

Description of the dosage form

White or almost white, film-coated tablets, oval, biconvex, chamfered, engraved “E 243” on one side, odorless.

Characteristic

Cyclic derivative of GABA.

Directions for use and doses

The drug is taken orally, during meals or on an empty stomach, with liquid. The daily dose is divided into 2-4 doses. The last dose should be taken no later than 17:00 (to prevent sleep disturbances).

For the symptomatic treatment of intellectual-mnestic disorders, depending on the severity of symptoms, 2.4-4.8 g/day is prescribed, dividing the dose into 2-3 doses.

For 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 a maximum dose of 24 g/day is reached. Treatment is continued throughout the entire period of the disease. To prevent deterioration of the patient's condition, do not abruptly stop using the drug. It is necessary to gradually reduce the dose of the drug - by 1.2 g / day every 2 days. If there is no effect or there is an insignificant therapeutic effect, treatment is stopped.

Since piracetam is excreted by the kidneys, caution should be exercised when treating patients with renal failure.

The dose calculation should be based on an assessment of the patient's CC, which is calculated using the formula:

CC = [140 - age (years)] × body weight (kg)/72 - serum creatinine (mg%)

For women, the resulting figure is multiplied by 0.85.

Treatment for such patients is prescribed depending on the severity of renal failure, adhering to the following recommendations:

In elderly patients, the dose should be adjusted in the presence of renal failure. With long-term therapy, monitoring of renal function is necessary.

In patients with impaired liver function, no dose adjustment is required.

For patients with impaired renal and hepatic function, dosing is carried out according to the scheme described for patients with impaired renal function.

Pharmacodynamics

Lucetam® is a nootropic drug that directly affects the brain. Improves cognitive processes such as learning ability, memory, attention, memorization ability, and also increases mental performance, without developing a sedative and psychostimulating effect. It affects 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 interaction between the hemispheres of the brain and synaptic conduction in neocortical structures, increases mental performance, improves cerebral blood flow. Lucetam® improves microcirculation in the brain, affecting the rheological characteristics of the blood and does not cause a vasodilator effect. Inhibits platelet aggregation and restores the elasticity of the red blood cell membrane, as well as their ability to pass through the microvasculature. Reduces red blood cell adhesion. At a dose of 9.6 g, it reduces the level of fibrinogen and von Willebrand factor by 30-40% and prolongs bleeding time. Lucetam® has a protective and restorative effect in cases of impaired brain function due to hypoxia, intoxication or injury. Reduces the severity and duration of vestibular nystagmus.

Pharmacokinetics

Suction

After taking the drug orally, piracetam is quickly and almost completely absorbed from the gastrointestinal tract. The bioavailability of the drug is about 100%. After a single dose of 2 g, Cmax is reached in the blood plasma after 30 minutes and is 40-60 mcg/ml, after 2-8 hours - in the cerebrospinal fluid.

Distribution and metabolism

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

Does not bind to blood plasma proteins.

Piracetam penetrates the BBB and the placental barrier. Not metabolized in the body.

Removal

T1/2 from blood plasma is 4-5 hours, T1/2 from cerebrospinal fluid is 8.5 hours.

It is excreted unchanged by the kidneys. Excretion by the kidneys is almost complete (>95%) within 30 hours. The total clearance of piracetam in healthy volunteers is 86 ml/min.

Pharmacokinetics in special clinical situations

In renal failure, T1/2 increases.

Indications for use Lucetam 800 mg 30 pcs. film-coated tablets

• Symptomatic treatment of intellectual-mnestic disorders in the absence of an established diagnosis of dementia;
• in order to reduce the manifestations of cortical myoclonus in patients sensitive to piracetam, both as monotherapy and as part of complex therapy (a trial course of treatment can be carried out to determine sensitivity to piracetam in a particular case).

Contraindications

• Huntington's chorea;
• hemorrhagic stroke;
• severe chronic renal failure (with CC less than 20 ml/min);
• pregnancy;
• lactation period;
• hypersensitivity to piracetam or pyrrolidone derivatives, as well as other components of the drug.

The drug should be prescribed with caution in case of hemostasis disorders, extensive surgical interventions, severe bleeding, chronic renal failure (creatinine clearance 20-80 ml/min).

Application of Lucetam 800 mg 30 pcs. film-coated tablets during pregnancy and breastfeeding

Adequate and strictly controlled clinical studies on the safety of the drug during pregnancy have not been conducted, therefore Lucetam® should not be used during pregnancy. Piracetam penetrates the placental barrier and is excreted in breast milk. If it is necessary to use the drug during lactation, breastfeeding should be discontinued.

special instructions

Due to the effect of piracetam on platelet aggregation, the drug should be prescribed with caution to patients with hemorrhagic disorders, risk of bleeding (for example, with gastric ulcer), impaired hemostasis, in patients taking anticoagulants and antiplatelet agents, incl. acetylsalicylic acid in low doses.

When treating cortical myoclonus, abrupt interruption of treatment should be avoided, because this may cause the attacks to recur.

During long-term therapy in elderly patients, regular monitoring of renal function indicators is recommended; if necessary, dose adjustment is carried out depending on the results of the QC study.

Penetrates through the filter membranes of hemodialysis machines.

Impact on the ability to drive vehicles and operate machinery

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Overdose

Piracetam is not toxic even in high doses. A single case of the development of dyspeptic symptoms in the form of diarrhea with blood and pain in the lower abdomen was registered when taking the drug in the dosage form of an oral solution in a daily dose of 75 g.

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

Side effects Lucetam 800 mg 30 pcs. film-coated tablets

From the central nervous system: hyperkinesis, irritability, drowsiness, depression, asthenia, headache, dizziness, insomnia, mental agitation, anxiety, imbalance, tremor, ataxia, exacerbation of epilepsy, anxiety, hallucinations, confusion, increased libido.

From the senses: dizziness (vertigo).

From the cardiovascular system: decrease or increase in blood pressure.

From the digestive system: nausea, vomiting, diarrhea, abdominal pain, epigastric pain.

Metabolism and nutrition: weight gain.

From the skin: dermatitis, itching, urticaria.

From the immune system: hypersensitivity, anaphylactic reactions, angioedema.

Drug interactions

When used simultaneously with thyroid extract (T3+T4), increased irritability, disorientation and sleep disturbances are possible.

There was no interaction with clonazepam, phenytoin, phenobarbital, or valproic acid.

Piracetam in high doses (9.6 g/day) increases the effectiveness of acenocoumarol in patients with venous thrombosis (a more pronounced decrease in platelet aggregation, fibrinogen levels, von Willebrand factors, blood and plasma viscosity was observed compared with the use of acenocoumarol alone).

The possibility of changes in 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, piracetam does not inhibit the isoenzymes CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 and 4A9/11 at concentrations of 142, 426 and 1422 μg/ml. At a piracetam concentration of 1422 mcg/ml, a slight inhibition of CYP2A6 (21%) and 3A4/5 (11%) was noted. However, the Ki level is likely to be well beyond the concentration of 1422 μg/ml. Therefore, metabolic interaction with other drugs is unlikely.

Taking piracetam at a dose of 20 mg/day did not affect the Cmax and AUC of antiepileptic drugs in the blood serum (carbamazepine, phenytoin, phenobarbital, valproate) in patients with epilepsy receiving the drug at a constant dose.

Co-administration with ethanol did not affect the level of piracetam concentration in the serum; the concentration of ethanol in the blood serum did not change when taking piracetam at a dose of 1.6 g.

Indications for use of the drug Lucetam

Tablets Symptomatic treatment for psychoorganic syndrome in elderly patients with memory loss, dizziness, decreased concentration and general activity, mood changes, behavioral disorders, gait disorders, including Alzheimer's disease and senile dementia of the Alzheimer's type. Therapy for the consequences of stroke (chronic stage of ischemic stroke), traumatic brain injury. As part of complex therapy for low learning ability in children with psychoorganic syndrome. For the treatment of cortical myoclonus both in mono- and complex therapy. Solution for injection The drug Lucetam is used to treat patients with different types of dementia, that is, with loss or deterioration of memory, loss of concentration and/or agility in movements, diseases of the nervous system, especially caused by cerebrovascular disorders in elderly and senile people, with aphasia as a result of cerebral hypoxia, cortical myoclonus, organic mental syndrome in elderly people. It improves intellectual functions such as thinking, learning, and mastering previously learned habits. Used as an adjuvant in the treatment of symptoms arising from brain damage and operations on it (for example, dizziness, involuntary movements of the eyeballs, loss of the ability to speak and/or write). Lucetam can be used to treat deterioration of cognitive functions in people who abuse alcohol. The drug can also be used in them to treat symptoms of alcohol withdrawal.

Use of the drug Lucetam

Tablets Use internally. Daily dose - 30-160 mg/kg body weight, frequency of administration - 2-4 times a day, with meals or on an empty stomach; The tablets should be taken with liquid (water, juice). For symptomatic treatment of chronic psychoorganic syndrome, depending on the severity of symptoms, 4.8 g / day is prescribed (12 tablets of 400 mg or 6 tablets of 800 mg or 4 tablets of 1200 mg) for the first few weeks, followed by a reduction in the maintenance dose within 1.2– 2.4 g/day (3–6 tablets 400 mg or 11/2–3 tablets 800 mg or 1–2 tablets 1200 mg). For the consequences of a stroke (chronic stage), 4.8 g/day is prescribed. For difficulties in perception for persons with brain injuries, the initial dose is 9–12 g/day, maintenance dose is 2.4 g/day. The duration of treatment is at least 3 weeks. For children over 7 years of age, 3.3 g/day is prescribed to correct reduced learning ability. The treatment is long-term, throughout the entire academic year. For cortical myoclonus, treatment begins with 7.2 g/day, every 3–4 days the dose is increased by 4.8 g/day until a maximum dose of 24 g/day is reached. Therapy is continued throughout the entire period of the disease. Every 6 months the dose is gradually reduced or the drug is discontinued. In order to prevent an attack, the dose is reduced gradually, by 1.2 g every 2 days. If there is no effect or in case of insignificant therapeutic effect, treatment is stopped. Daily doses for children aged:

• 1 year–3 years – 400 mg/day;
• 3–7 years – 400–800 mg/day;
• 7–12 years – 400–2000 mg/day;
• 12–16 years – 800–2400 mg/day.

Dosing for patients with impaired renal function Since Lucetam is excreted from the body by the kidneys, the drug should be prescribed according to the following treatment regimen.

Patients with impaired liver function do not require dose adjustment. Solution for injection Treatment can be carried out over several weeks, months and even years (the tablet form of Lucetam is used). The duration of therapy depends on the patient's condition and response to it. The drug is administered intravenously as an infusion. Solvents used:

• 0.9% sodium chloride solution;
• 5; 10; 20% fructose solution;
• 5; 10; 20% glucose solution;
• 5% levulose solution;
• 10% solution of Dextran 40 in 0.9% solution of sodium chloride;
• 6% solution of Dextran 100 in 0.9% solution of sodium chloride;
• Ringer solution;
• Ringer's solution Lactate;
• solution Mannitol - Dextran;
• 6% solution of hydroxethyl starch (HES).

Adults

Typically, the initial dose is 2400 mg/day, maintenance - 1200–2400 mg/day. The initial and maintenance doses are distributed in several doses (for example, 2 doses per day). The daily dose is 4800 mg.

• Patients during the period of alcohol withdrawal can receive 12 g, then they are transferred to a maintenance dose of 2400 mg/day;
• patients with sudden contraction of muscles of cerebral origin: initial dose - 2-4 g / day, gradually increasing over several weeks to a daily dose - 9-12 g;
• organic mental syndrome in elderly people: 4800 mg/day for several weeks with the following reduction to a maintenance dose of 1200–2400 mg/day;
• cerebrovascular lesions, cognitive deficits after head injuries: daily dose of 9–12 g in the first 2 weeks, then a maintenance dose of 2400 mg/day for at least 3 weeks.

Children aged 8–12 years with childhood dyslexia The maximum daily dose is 3200 mg of Lucetam or 0.03–0.16 g/kg body weight. Doses for patients with renal impairment

Elderly patients can take the drug in doses prescribed for adults without their correction.

Compound

Side effects of the drug Lucetam

Tablets There are isolated reports of side effects from the gastrointestinal tract: nausea, vomiting, diarrhea, abdominal and stomach pain; from the nervous system: dizziness, headache, ataxia, imbalance, exacerbation of epilepsy, insomnia; from the psyche: excitement, anxiety, nervousness, hallucinations, increased sexuality, rarely - drowsiness and depression; from the skin: dermatitis, itching, skin rashes, swelling. Solution Complaints such as nervousness, irritability, fear, anxiety, aggressiveness, sleep disturbance, increased excitability and increased motor activity most often occur in older people, as well as with daily administration of the drug in doses exceeding 2400 mg. Nausea, dizziness, headache, hand tremors, increased sexuality and allergic reactions are rare.

Special instructions for the use of the drug Lucetam

Due to the effect of piracetam on platelet aggregation, caution is required when prescribing the drug to patients with impaired hemostasis, during major surgical operations, or to patients with symptoms of severe bleeding. When treating patients with cortical myoclonus, abrupt interruption of therapy should be avoided, as this may cause resumption of attacks. During long-term therapy in the elderly, regular monitoring of renal function parameters is recommended; if necessary, dose adjustment is carried out depending on the results of a creatinine clearance study. Considering the possible side effects, the patient should be careful when driving vehicles and operating machinery. Penetrates through the filter membranes of hemodialysis machines. Pregnancy and lactation period Animal studies have not revealed any negative effects on the embryo and its development, including in the postnatal period; piracetam did not affect the course of pregnancy and childbirth. There is no experience in using the drug for treatment in pregnant women. Piracetam penetrates the placental barrier and into breast milk. The concentration of the drug in the blood of newborns reaches 70–90% of its concentration in the mother’s blood. Except in special circumstances, Lucetam is not used during pregnancy. You should refrain from breastfeeding during treatment with the drug.

Drug interactions Lucetam

When combined with thyroid hormones (T3+T4), increased irritability, disorientation and sleep disturbance are possible. There was no interaction with clonazepam, phenytoin, phenobarbital, or sodium valproate. Piracetam in high doses (9.6 g/day) increased the effectiveness of acenocoumarol in patients with venous thrombosis: a significant decrease in the level of platelet aggregation, fibrinogen level, Villibran factors, blood viscosity and blood plasma was noted. The possibility of changing the pharmacodynamics of piracetam under the influence of other drugs is low, since 90% of the drug is excreted unchanged in the urine. In vitro, piracetam does not inhibit cytochrome P450 isoforms CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 and 4A9/11 at a concentration of 142; 426; 1422 mcg/ml. Therefore, metabolic interaction with drugs that undergo biotransformation by these enzymes is unlikely. Taking piracetam at a dose of 20 mg/day did not change the maximum and curve of the concentration level of antiepileptic drugs in the blood serum (carbamazepine, phenytoin, phenobarbital, valproate) in patients with epilepsy. In patients with epilepsy receiving appropriate therapy for this reason, it may be necessary to adjust the treatment and conduct a course of IV therapy with Lucetam. Concomitant use of the drug and alcohol consumption did not affect the level of piracetam concentration in the blood serum - the concentration of alcohol in the blood serum did not change when taking 1.6 g of piracetam.

Release form

Film-coated tablets, 400 mg. 60 tab. in a brown glass jar with a PE stopper with tamper evident. 1 jar is packed in a cardboard box or 15 tablets. in a blister made of PVC/PVDC/aluminum foil. 4 blisters in a cardboard box.

Film-coated tablets, 800 mg. 30 tab. in a brown glass jar, with a PE lid with tamper evident. 1 jar is packed in a cardboard box or 15 tablets. in a blister made of PVC/PVDC/aluminum foil. 2 blisters in a cardboard box.

Film-coated tablets, 1200 mg. 20 or 60 tablets in a brown glass jar, with a PE lid with tamper evident. 1 jar is packed in a cardboard box. Or 10 tablets. in a blister made of PVC/PVDC/aluminum foil. 2 blisters in a cardboard box.

Solution for intravenous and intramuscular administration, 200 mg/ml. In colorless glass ampoules with a break point and two red rings, 5 ml each. A label is attached to the ampoule. 5 amp. placed in a plastic cell package sealed with transparent film. 2 packages (10 amps) are placed in a cardboard box. Or in 15 ml ampoules made of colorless glass with a break point. A label is attached to the ampoule. 4 amp. placed in a blister pack sealed with transparent film. 1 or 5 packages (4 or 20 amps) are placed in a cardboard box.