Lucetam, 1200 mg 20 pcs

Pharmacotherapeutic group: nootropic agent

ATX code: [N06BX03].

Pharmacodynamics

Piracetam is a nootropic that affects the central nervous system in different ways: it modifies neurotransmission in the brain, improves conditions that promote neuronal plasticity, improves microcirculation, affecting blood rheological characteristics without causing vasodilation.
Administration of piracetam in patients with cerebral dysfunction increases attention concentration and improves cognitive functions, which is manifested by significant changes on the electroencephalogram (increased α and β activity, reduced δ activity).

It helps to restore cognitive function due to various disorders such as hypoxia, intoxication or electroconvulsive therapy. Reduces the duration of induced vestibular neuronitis. Piracetam inhibits increased aggregation of activated platelets and, in case of pathological erythrocyte stiffness, improves their deformability and filtration capacity.

Pharmacokinetics

Absorption.

After oral administration, piracetam is rapidly and almost completely absorbed from the gastrointestinal tract. Bioavailability is about 100%. After a single dose of 2 g, maximum concentration (Cmax) is reached within 30 minutes and is 40-60 mcg/ml, after 2-8 hours it is detected in cerebrospinal fluid.

Distribution

The volume of distribution (Vd) is about 0.6 l/kg. It does not bind with plasma proteins. Piracetam penetrates through the blood-brain and placental barriers, as well as hemodialysis membranes. In animal studies it was found that piracetam selectively accumulates in the tissues of the cerebral cortex, mainly in the frontal, parietal and occipital lobes, in the cerebellum and basal nuclei.

Biotransformation

It is not metabolized.

Elimination

The elimination half-life (T1/2) from blood is 4-5 h and 8.5 h for cerebrospinal fluid. T1/2 is prolonged in renal insufficiency. It is excreted unchanged by the kidneys. Renal excretion is almost complete (>95%) within 30 hours. Total clearance of piracetam in healthy volunteers is 86 ml/min.

Indications

Attention and memory disorders, Mental retardation in children, Alzheimer’s disease, Dizziness, Headache, Learning disabilities, Alcoholism, Impaired cerebral circulation, Tinnitus, Stroke after-effects, Disorientation, Hangover, Concussion and other brain injuries, Acquired dementia<> Symptomatic treatment of intellectual and mental disorders in the absence of diagnosed dementia.p> Symptomatic treatment of intellectual and mental disorders in the absence of an established diagnosis of dementia.

The reduction of manifestations of cortical myoclonias in patients sensitive to piracetam both as monotherapy and as part of complex therapy. (A trial course of treatment may be conducted to determine sensitivity to piracetam in a particular case).

Active ingredient

Piracetam

Composition

1 coated tablet contains:

active ingredient:

piracetam – 1200 mg,

excipients:

magnesium stearate 9 mg,

povidon K-30 75 mg;

shell:

dibutylsebakat 1.82 mg,

ethylcellulose (in the form of aqueous dispersion) 9.1 mg,

opadray white (macrogol 6000 0.65 mg, titanium dioxide 1.95 mg, talc 2.6 mg, hypromellose 9.88 mg).

How to take, the dosage

The drug is administered by mouth in a daily dose of 30-160 mg/kg, 2-4 times a day.

Lucetam tablets are taken with a meal or on an empty stomach with fluids (water, juice).

In symptomatic treatment of chronic psychorganic syndrome 1.2-2.4 g/day is prescribed depending on the severity of symptoms, and for the first week – 4.8 g/day.

In treatment of the consequences of stroke 4.8 g/day is prescribed.

In case of alcohol withdrawal syndrome – 12 g/day. Maintenance dose is 2.4 g/day.

For treatment of dizziness and related balance disorders 2.4-4.8 g/day are prescribed.

For cortical myoclonias, 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 duration of the disease. Every 6 months an attempt should be made to reduce the dose or cancel the drug, gradually reducing the dose by 1.2 g every 2 days in order to prevent seizure. If there is no effect or little therapeutic effect, treatment should be discontinued.

In children for correction of learning disabilities, the drug is administered orally at a dose of 3.2 g/day. Treatment continues throughout the school year.

In patients with hepatic impairment no dosage adjustment is required.

In patients with impaired renal function, dosage regimen adjustment is required depending on creatinine clearance (CK). Grade of renal insufficiency CK (ml/min) Dose Normal > 80 Normal dose Mild 50-79 2/3 of normal dose in 2 – 3 doses Moderate 30-49 1/3 of normal dose in 2 doses Severe < 30 1/6 of normal dose, single dose Terminal stage – contraindicated

In patients with renal impairment/p>

In elderly patients the dose is corrected in the presence of renal insufficiency and during long-term therapy it is necessary to control the functional state of the kidneys.

Interaction

When co-administration with thyroid extract (triiodothyronine /TZ/ + tetraiodothyronine /T4/) increased irritability, disorientation and sleep disorders are possible. No interaction with clonazepam, phenytoin, phenobarbital, valproic acid was noted.

High doses (9,6 g/day) of piracetam increased efficacy of acenocoumarol in patients with venous thrombosis: a greater decrease of platelet aggregation, fibrinogen, Willibrandt factors, blood and plasma viscosity was noted than when administering acenocoumarol alone.

The possibility of changes of piracetam pharmacodynamics under the influence of other drugs is low because 90% of the drug is excreted unchanged in the urine.

At concentrations of 142, 426 and 1422 mg/ml piracetam does not inhibit cytochrome P450 isoenzymes (CYP 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 and 4A9/11) in vitro. At a concentration of 1422 µg/ml, minimal inhibition of CYP2A6 isoenzyme (21%) and 3A4/5 isoenzyme (11%) was observed. However, the value of the inhibition constant (Ki) probably goes far beyond the 1422 µg/ml concentration. Thus, metabolic interactions of priracetam with other drugs are unlikely.

Administration of piracetam at a dose of 20 g/day had no effect on the maximum concentration and area under the concentration-time curve of antiepileptic drugs in serum (carbamazepine, phenytoin, phenobarbital, valproate) in epilepsy patients receiving a constant dose.

Co-administration with alcohol did not affect the serum concentration of piracetam and the serum concentration of alcohol did not change with 1.6 g of piracetam.

Special Instructions

Due to the effect of Piracetam on platelet aggregation, caution should be exercised when prescribing the drug in patients with impaired hemostasis, during major surgery or in patients with symptoms of severe bleeding.

In the treatment of cortical myoclonias, abrupt interruption of treatment should be avoided, which may cause recurrence of seizures.

In long-term therapy in elderly patients, regular monitoring of renal function parameters is recommended; if necessary, dose adjustments are made depending on the results of CK tests.

It penetrates through the filter membranes of hemodialysis machines.

Impact on driving and operating machinery

With due regard to possible side effects, the patient should exercise caution when driving and operating machinery.

Contraindications

• Individual intolerance to piracetam or pyrrolidone derivatives or other drug components.
• Hemorrhagic stroke.
• Severe chronic renal failure (with creatinine clearance (CK) less than 20 ml/min).
• Pregnancy and lactation (see section “Use during pregnancy and lactation”).

With caution

Hemostasis disorders, major surgical interventions, severe bleeding, chronic renal failure (when creatinine clearance (CK) is 20-80 ml/min).

Side effects

Nervous system disorders: hyperkinesias, irritability, somnolence, depression, asthenia: these symptoms occur more frequently in elderly patients receiving doses over 2.4 g/day, in most cases it is possible to achieve regression of such symptoms by reducing the drug dose. Headache, dizziness, insomnia, mental agitation, restlessness, balance disorders, tremor, ataxia, worsening of epilepsy, anxiety, hallucinations, confusion, increased libido.

Blood and lymphatic disorders: bleeding

Immune system disorders: hypersensitivity, including anaphylaxis

Hearing and labyrinth disorders: Dizziness (vertigo)

Cardiovascular system disorders: decreased or increased blood pressure.

Digestive system disorders: nausea, vomiting, diarrhea, abdominal pain, epigastric pain.

Metabolic and nutrition disorders: weight gain.

Skin disorders: dermatitis, itching, urticaria.

Allergic reactions: angioedema.

General disorders and disorders at the injection site: pain at the injection site, thrombophlebitis, hyperthermia.

Overdose

Treatment: Gastric lavage or induced vomiting may be performed immediately after ingestion. Conduct symptomatic therapy, which may include hemodialysis.

There is no specific antidote. The effectiveness of hemodialysis for piracetam is 50-60%.

Pregnancy use

There have been no studies on pregnant women, so piracetam should not be prescribed during pregnancy.

Piracetam passes through the placental barrier and into the breast milk. If it is necessary to use the drug, breastfeeding should be stopped.

Similarities

Nootropil, Piracetam, Piracetam bufus, Notrocetam