Lutsetam - instructions for use, doses, side effects, contraindications

1 tablet, coated, contains 400 mg, 800 mg or 1200 mg active ingredient piracetam as well as Excipients: magnesium stearate 3/6/9 mg, povidone K-30 25/50/75 mg; sheath: dibutyl sebacate 0.7 / 1.4 / 1.82 mg, ethyl cellulose (in the form of an aqueous dispersion) 3.5 / 7 / 9.1 mg, opadrai white (macrogol 6000 0.25 / 0.5 / 0.65 mg , titanium dioxide 0.75 / 1.5 / 1.95 mg, talc 1/2 / 2.6 mg, hypromellose 3.8 / 7.6 / 9.88 mg.

Description:

Tablets 400 mg: white or almost white, biconvex oval-shaped tablets, film-coated, chamfered, engraved E 241 on one side of the tablet, odorless.

Tablets 800 mg: white or almost white, biconvex oval-shaped tablets, film-coated, chamfered, with a risk on both sides, with engraved E 242 on one side of the tablet, odorless.

Tablets 1200 mg: White or almost white, oval biconvex tablets, film-coated, chamfered, engraved E 243 on one side of the tablet, and odorless.

Pharmacotherapeutic group:Nootropic remedy

ATX: & nbsp

N.06.B.X.03 Pyracetam

Pharmacodynamics:

Piracetam - nootrop, has an effect on the central nervous system in different ways: modifies neurotransmission in the brain, improves conditions conducive to neuronal plasticity, improves microcirculation by acting on the rheological properties of blood and causing vasodilation.

Application piracetam in patients with cerebral dysfunction increases concentration and improves cognitive function, as manifested by significant changes in the electroencephalogram (α and β increased activity, reduced activity of δ).

Promotes restoration of cognitive functions due to various disorders, such as hypoxia, intoxication or electroconvulsive therapy. Reduces the duration of induced vestibular neuronitis. Pyracetam inhibits increased aggregation of activated platelets and, in the case of abnormal erythrocyte rigidity,improves their deformability and ability to filter.

Pharmacokinetics:

Absorption

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

Distribution

The volume of distribution (V_d) is about 0.6 l / kg. Does not bind to plasma proteins. Pyracetam penetrates through 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.

Excretion

The half-life (T_½) from the blood is 4-5 hours and 8.5 hours for the cerebrospinal fluid. T_½ lengthened with renal failure. It is excreted unchanged by the kidneys. Excretion by the kidneys is almost complete (> 95%) for 30 hours. The total clearance of piracetam in healthy volunteers is 86 ml / min.

Indications:

Symptomatic treatment of intellectual-mnestic disorders in the absence of an established diagnosis of dementia.

Reduction of the manifestations of cortical myoclonia in piracetam sensitive patients both as monotherapy and as part of complex therapy. (In order to determine sensitivity to pyracetam in a particular case, a trial treatment course can be performed).

Contraindications:

Individual intolerance to piracetam or pyrrolidone derivatives, as well as other components of the drug.
Horea Huntington.
Hemorrhagic stroke.
Severe chronic renal failure (with creatinine clearance (CC) less than 20 mL / min).
Pregnancy and lactation period (see Section "Application during pregnancy and during lactation").

Carefully:

Violation of hemostasis, extensive surgical interventions, severe bleeding, chronic renal failure (with creatinine clearance (CC) 20-80 ml / min).

Pregnancy and lactation:

Studies on pregnant women have not been conducted, therefore piracetam should not be administered during pregnancy.

Piracetam penetrates the placental barrier and into breast milk.If you need to use the drug, you should stop breastfeeding.

Dosing and Administration:

Inside, during meals or on an empty stomach, squeezed with liquid. The last dose is taken no later than 17 hours (to prevent sleep disturbance). The daily dose is divided into 2 - 4 doses.

Symptomatic treatment of intellectual-mnestic disorders:

Depending on the severity of symptoms prescribed 2.4 - 4.8 g / day, distributing to 2-3 reception.

Treatment of cortical myoclonia:

Treatment begins with 7.2 g / day, every 3-4 days the dose increases by 4.8 g / day until the maximum dose of 24 g / day is reached. Treatment continues throughout the period of the disease. To prevent the deterioration of patients, the drug should not be discontinued drastically. It is necessary to gradually reduce the dose of the drug - by 1.2 g / day every 2 days. In the absence of effect or the presence of a slight therapeutic effect, treatment is discontinued.

Dosing to patients with impaired renal function:

Because the piracetam is excreted from the body by the kidneys, care should be taken when treating patients with renal insufficiency in accordance with the dosing regimen shown.

Calculation of the dose should be based on an assessment of creatinine clearance in a patient, which is calculated by the formula:

CK = [140-age (in years) * t (in kg)]/ [72 * With creatinine in plasma (mg / dL) ]

For women: Ccr * 0.85.

Prescribe treatment to such patients, depending on the severity of renal failure, adhering to the following recommendations:

Renal failure	Creatinine clearance (ml / min)	Dosing
Norm	>80	Usual Dose
Lightweight	50-79	2/3 of the usual dose in 2 to 3 doses
Average	30-49	1/3 of the usual dose in 2 divided doses
Heavy	<30	1/6 of the usual dose, once
The final stage	-	Contraindicated

Dosing to elderly patients:

Elderly, the dose is corrected in the presence of renal failure and with prolonged therapy requires monitoring of kidney function.

Dosing to patients with impaired liver function:

Patients with a dysfunction of the liver do not need a dose adjustment. Patients with impaired functions and kidneys and liver, dosing is carried out according to the scheme (see Section "Dosing to patients with impaired renal function") /

Side effects:

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 sense organs: dizziness (vertigo).

From the side of the cardiovascular system, decrease or increase in blood pressure.

From 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.

On the part of the immune system, hypersensitivity, anaphylactic reactions, angioedema.

Overdose:

Pyracetam is not toxic even in high doses. An isolated case of development of diarrhea in the form of diarrhea with blood and pain in the lower abdomen with the drug in the form of a drug for oral administration in a daily dose of 75 g.

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

Interaction:

When combined with an extract of the thyroid gland (triiodothyronine / T3 / + tetraiodothyronine / T4), there may be increased irritability,disorientation and sleep disorders. No interaction with clonazepam, phenytoin, phenobarbital, valproic acid was observed.

High doses (9.6 g / day) of pyracetam increased the efficacy of acenocoumarol in patients with venous thrombosis: there was a greater decrease in platelet aggregation, fibrinogen content, Willebrandt factors, viscosity of blood and plasma than with the administration of acenocoumarol alone.

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 urine.

In concentrations of 142, 426, and 1422 mg / ml piracetam does not inhibit isoenzymes of cytochrome P450 (CYP 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 and 4A9 / 11) in vitro. At a concentration of 1422 μg / ml, a minimal inhibition of the isoenzyme CYP2A6 (21%) and isoenzyme ZA4 / 5 (11%) was observed. However, the value of the inhibition constant (Ki) probably goes well beyond the concentration of 1422 μg / ml. Thus, the metabolic interactions of priracetam with other drugs are unlikely. Admission piracetam at a dose of 20 g / day did not affect the maximum concentration and area under the concentration-time curve of antiepileptic drugs in the blood serum (carbamazepine, phenytoin, phenobarbital, valproate) in patients with epilepsy receiving a constant dose.

Joint reception with alcohol did not affect the concentration of piracetam in the serum and the concentration of alcohol in the blood serum did not change with the intake of 1.6 g of piracetam.

Special instructions:

Due to the influence of piracetam on platelet aggregation, caution is recommended when administering the drug to patients with severe hemorrhagic disorders, risk of bleeding (eg, gastric ulcer), hemostasis disorders, in patients taking anticoagulants and antiaggregants, including low doses of acetylsalicylic acid.

In the treatment of patients with cortical myoclonia, sudden interruption in treatment should be avoided, which can lead to the resumption of seizures.

With prolonged therapy of elderly patients, regular monitoring of renal function indicators is recommended, if necessary, dose adjustment is performed depending on the results of the study of creatinine clearance.

It penetrates the hemodialysis apparatus through the filter membranes.

Effect on the ability to drive transp. cf. and fur:

During the period of treatment, care must be taken when driving vehicles and occupations, etc.potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Tablets, film-coated 400 mg, 800 mg and 1200 mg.

Packaging:

400 mg: 60 tablets coated in a jar of brown glass with a polyethylene stopper with the control of the first opening. 1 bottle together with instructions for use are packed in a cardboard box. Or 15 tablets in a blister of PVC / PVDC / al.foil. 4 blisters together with instructions for medical use in a cardboard box.

800 mg: 30 tablets covered with a shell in a jar of brown glass, with a polyethylene lid with the control of the first opening. 1 bottle together with instructions for use are packed in a cardboard box. Or 15 tablets in a blister of PVC / PVDC / al.foil. 2 blisters together with instructions for medical use in a cardboard box.

1200 mg: 20 or 60 tablets covered with a film shell in a jar of brown glass, with a polyethylene lid with the control of the first opening. 1 bottle together with instructions for use are packed in a cardboard box. Or 10 tablets in a blister of PVC / PVDC / al.foil.2 blisters together with instructions for medical use in a cardboard box.

Storage conditions:

Store at temperatures between 15 and 30 ° C. Keep out of the reach of children.

Shelf life:

5 years. Do not use the drug after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N013160 / 02

Date of registration:24.11.2009 / 20.10.2014

Expiration Date:Unlimited

The owner of the registration certificate:EGIS ZAO Pharmaceutical Plant EGIS ZAO Pharmaceutical Plant Hungary

Manufacturer: & nbsp

EGIS Pharmaceutical Plant, ZAO Hungary

Representation: & nbspEGIS ZAO Pharmaceutical Plant EGIS ZAO Pharmaceutical Plant Hungary

Information update date: & nbsp20.03.2018

Illustrated instructions

Instructions

Lucetam® (Lucetam®)