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

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 1200 mg n20 tablet

Indications: symptomatic treatment of psychoorganic syndrome, in particular in elderly patients, accompanied by memory loss, dizziness, decreased concentration and general activity, mood changes, behavior disorder, gait disturbance, as well as in patients with Alzheimer's disease and senile dementia of the Alzheimer's type;

- treatment of the consequences of ischemic stroke, such as speech disorders, disturbances in the emotional sphere, motor and mental activity;

— chronic alcoholism — for the treatment of psychoorganic and withdrawal syndromes;

— during the recovery period after brain injuries and intoxications;

- treatment of dizziness and related balance disorders, with the exception of dizziness of mental origin;

- as part of complex therapy for learning disabilities in children, especially in cases of acquisition of specific reading, writing, and counting skills that cannot be explained by mental retardation, inadequate training or characteristics of the family environment;

— for the treatment of cortical myoclonus as mono- or complex therapy.

pharmachologic effect

Nootropic drug. Piracetam is a cyclic derivative of GABA. Directly affects the brain. Lucetam improves cognitive (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. Lucetam inhibits platelet aggregation and restores the elasticity of the erythrocyte membrane, as well as the ability of the latter 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, Cmax in blood plasma is reached after 1 hour. The bioavailability of the drug is about 100%. After oral administration of a single dose of 2 g, Cmax is 40-60 mcg/ml, which is achieved in the blood plasma after 30 minutes and after 5 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 - 80-100%, by renal filtration. The renal clearance of piracetam in healthy volunteers is 86 ml/min.

Pharmacokinetics in special clinical situations

In renal failure, T1/2 increases.

The pharmacokinetics of piracetam does not change in patients with liver failure.

Piracetam penetrates membranes used in hemodialysis.

Instructions for use / dosage

Inside

the drug is prescribed in a daily dose of 30-160 mg/kg, the frequency of administration is 2-4 times/day.

IV or IM

prescribed in a daily dose of 30-160 mg/kg (3-12 g/day), frequency of administration - 2-4 times/day.

For symptomatic treatment of chronic psychoorganic syndrome

depending on the severity of symptoms, 1.2-2.4 g/day is prescribed, and during the first week - 4.8 g/day.

When treating the consequences of a stroke

4.8 g/day is prescribed.

For alcohol withdrawal syndrome

- 12 g/day. Maintenance dose - 2.4 g/day.

Treatment of dizziness and related balance disorders

Prescribe 2.4-4.8 g/day.

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 the maximum dose of 24 g/day is reached. Treatment is continued throughout the entire period of the disease. Every 6 months, an attempt should be made to reduce the dose or discontinue the drug, gradually reducing the dose by 1.2 g every 2 days in order to prevent an attack. If there is no effect or insignificant therapeutic effect, treatment is stopped.

In the treatment of comatose states, as well as difficulties of perception in persons with injuries

the drug is administered intramuscularly or intravenously at an initial dose of 9-12 g/day, maintenance dose – 2.4 g/day. Treatment is continued for at least 3 weeks.

For children

to
correct learning disabilities,
it is prescribed orally at a dose of 3.2 g/day. Treatment continues throughout the academic year.

In patients with impaired renal function

correction of the dosage regimen is required depending on the QC.

In elderly patients

the dose is adjusted in the presence of renal failure and with long-term therapy, monitoring of the functional state of the kidneys is necessary.

In patients with impaired liver function

no dosage regimen adjustment is required.

Lucetam tablets are taken with meals or on an empty stomach with liquid (water, juice).

Lucetam solution for IM or IV administration is compatible with the following infusion solutions: dextrose 5%, 10%, 20%; fructose 5%, 10%, 20%; levulose 5%; sodium chloride 0.9%; dextran 40 - 10% in 0.9% sodium chloride solution; dextran 100 – 6% in 0.9% sodium chloride solution; Ringer's solution; lactated Ringer's solution; mannitol-dextran; hydroxyethyl starch 6%. Piracetam infusion solutions are stable for at least 24 hours.

Side effect

From the central nervous system and peripheral nervous system:

1.72% - hyperkinesia; 1.13% - nervousness; 0.96% - drowsiness; 0.83% - depression; in isolated cases - dizziness, headache, ataxia, imbalance, exacerbation of epilepsy, insomnia, confusion, agitation, anxiety, hallucinations, increased sexuality.

From the side of metabolism:

1.29% - increase in body weight.

From the digestive system:

in isolated cases - nausea, vomiting, diarrhea, pain in the stomach.

Dermatological reactions:

dermatitis, itching, rashes, swelling.

Other:

0.23% - asthenia.

Side effects occur more often in elderly patients receiving the drug at a dose of more than 2.4 g / day, and in most cases disappear when the dose is reduced.

Contraindications

- hemorrhagic stroke;

— end-stage renal failure (with CC less than 20 ml/min);

- children under 1 year of age;

- pregnancy;

- lactation;

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

Use during pregnancy and breastfeeding

Adequate and strictly controlled clinical studies on the safety of the drug during pregnancy have not been conducted.

Lucetam should not be used during pregnancy unless absolutely necessary.

Piracetam penetrates the placental barrier and is excreted in breast milk. The concentration of piracetam in the blood of newborns reaches 70-90% of its concentration in the blood of the mother.

If use is necessary during lactation, breastfeeding should be discontinued.

Use for liver dysfunction

In patients with impaired liver function

no dosage regimen adjustment is required.
Use for impaired renal function
In patients with impaired renal function

correction of the dosage regimen is required depending on the QC.

Special instructions
Due to the effect of piracetam on platelet aggregation, the drug should be prescribed with caution to patients with impaired hemostasis, during major surgical operations or to patients with symptoms of severe bleeding.

When treating cortical myoclonus, abrupt interruption of treatment should be avoided, which may cause resumption of attacks.

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

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

Overdose

Treatment:

immediately after taking the drug orally, you can rinse the stomach or induce artificial vomiting.
Conducting symptomatic therapy, which may include hemodialysis. There is no specific antidote. The effectiveness of hemodialysis for piracetam is 50-60%. Drug interactions
When used simultaneously with thyroid extract, increased irritability, disorientation and sleep disturbances are possible.

There was no interaction with clonazepam, phenytoin, phenobarbital, or sodium valproate.

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 of these two isoenzymes is sufficient when exceeding 1422 μg/ml. Therefore, metabolic interaction with other drugs is unlikely.

Taking piracetam at a dose of 20 mg/day. did not change the peak and curve of the concentration level 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 1.6 g of piracetam.

Conditions for dispensing from pharmacies

The drug is available with a prescription.

Storage conditions and periods

List B. The drug should be stored at a temperature of 15° to 30°C out of the reach of children. The shelf life of the drug in the form of tablets is 5 years, in the form of an injection solution – 2 years.

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.