Ламитор® DT

General characteristics. Structure:

Active ingredient: 25 mg, 50 mg or 100 mg of a lamotridzhin.

Excipients: calcium a carbonate, magnesium алюминосиликат, aspartame, carboxymethylstarch of sodium, sodium saccharinate, magnesium the stearate, talc (purified) fragrance fruit (S1038), K-30 povidone, silicon dioxide colloid.

Anticonvulsant (antiepileptic) drug.

Pharmacological properties:

Pharmacodynamics. Anticonvulsant (antiepileptic) drug. Blocker of potentsialzavisimy natrium channels. Calls the block of pulse categories in culture of neurons and inhibits excess release of a glutamate (the amino acid playing a key role in generation of epileptic seizures) along with inhibition a glutamate - the induced effector impulses.

Pharmacokinetics. Absorption. After intake ламотриджин it is quickly and completely absorbed from a GIT. Cmax in a blood plasma is observed in 2.5±1.5 h after oral administration. Time of achievement of Cmax is a little extended in case of administration of drug after food, but extent of absorption remains invariable. The pharmacokinetics has linear character up to a dose of 450 mg - the maximum single dose which was investigated. There are significant individual differences of Cmax values of drug, but individual concentration differ very little.

Distribution. Linkng with proteins of plasma makes about 55%.

Metabolism. It is metabolized in a liver with formation preferential of glucuronides.

Removal. T1/2 at healthy adults makes 24-35 h.

Average values of clearance at healthy people make 39±14 ml/min.

Lamotridzhin is brought from an organism with urine in the form of glucuronides. Less than 10% are removed in not changed view with urine. Only 2% of products of metabolism are removed with a stake.

Pharmacokinetics in special clinical cases. T1/2 of a lamotridzhin substantially depends on the accompanying medicamentous therapy.

T1/2 of a lamotridzhin decreases to 14 h at its combination with the drugs inducing activity of isoenzymes of system of P450 cytochrome such as carbamazepine and Phenytoinum, and increases on average approximately to 70 h in case of the combined use from sodium Valproatum.

T1/2 of a lamotridzhin at children is usually shorter, than at adults. T1/2 at children makes about 7 h at reception with the medicines inducing activity of isoenzymes such as carbamazepine, Phenytoinum, phenobarbital and Primidonum. T1/2 increases to 45-55 h at the combined reception from sodium Valproatum.

Studying of pharmacokinetics of a lamotridzhin in single doses at patients with diseases of kidneys demonstrate that pharmacokinetic parameters change slightly, however concentration of the main metabolite in the form of a glucuronide increase practically by 8 times in connection with decrease in renal clearance.

Indications to use:

It is recommended as monotherapy and for adults and children 12 years are more senior than auxiliary therapy:

— simple partial convulsive attacks;

— difficult partial convulsive attacks;

— for the second time generalized toniko-clonic convulsive attacks;

— initially generalized toniko-clonic convulsive attacks;

— absentias epileptica are typical;

— absentias epileptica are atypical;

— myoclonic attacks;

— attacks, resistant to other antiepileptic means of any type.

Also apply as auxiliary therapy to children aged from 2 up to 12 years.

Route of administration and doses:

The initial dose of Lamitor of DT for adults and children is more senior than 12 years which are not accepting sodium Valproatum, but accepting other antiepileptic drugs inducing isoenzymes makes 50 mg of 1 times/days within the first 2 weeks and 100 mg/days (in 2 receptions) within the next 2 weeks. Then it is necessary to increase a dose to 200-400 mg/days (in 2 receptions).

The initial dose of Lamitor of DT for the patients accepting sodium Valproatum in combination with other antiepileptic drugs inducing isoenzymes makes 25 mg every other day within the first 2 weeks and then 25 mg of 1 times/days within the next 2 weeks. Then the dose should be increased before achievement of optimum therapeutic effect. A maintenance dose - 100-200 mg (in 1 or 2 receptions).

The initial dose of Lamitor of DT for children from 2 to 12 years which are not accepting sodium Valproatum, but accepting other antiepileptic drugs inducing isoenzymes makes 2 mg/kg/days (in 2 receptions) within the first 2 weeks and 5 mg/kg/days (in 2 receptions) within the next 2 weeks. A maintenance dose - 5-15 mg/kg/days (in 2 receptions).

The initial dose of Lamitor of DT for the children accepting sodium Valproatum in combination with other antiepileptic drugs inducing isoenzymes makes 0.2 mg/kg of 1 times/days within the first 2 weeks, then 0.5 mg/kg of 1 times/days within the next 2 weeks. Then the dose should be increased before achievement of optimum therapeutic effect. A maintenance dose - 1-5 mg/kg (in 1 or 2 receptions).

Features of use:

Use during pregnancy. Inclusion in time of pregnancy is contraindicated, except for cases when the expected advantage for mother exceeds potential risk for a fruit. In view of the inhibiting impact of a lamotridzhin on reductase of dihydrofolate development of malformation of a fruit in case of treatment of pregnant women is probable, however the available data for pregnant women are insufficient for definition of degree of harmlessness of a lamotridzhin.

Category of action on a fruit on FDA — C.

According to preliminary data ламотриджин gets into breast milk, concentration in breast milk can make 40–60% of concentration in mother's plasma. Not numerous observations show that concentration of drug in serum of babies whose mothers accepted drug during breastfeeding reached therapeutic level. It is necessary to correlate potential advantage of feeding by breast milk and potential risk of development of side effects in the child.

With care apply at patients with a renal failure.

It is not necessary to apply ламотриджин at patients of advanced age.

At emergence of the expressed skin allergic reactions use of a lamotridzhin should be stopped.

At sudden cancellation of a lamotridzhin strengthening of displays of epilepsy therefore it is necessary to stop gradually treatment is possible, reducing a dose within 2 weeks.

At simultaneous use with carbamazepine dizziness, a diplopia, an ataxy, vision disorders, nausea are possible. These phenomena, as a rule, pass at reduction of a dose of carbamazepine.

It is not necessary to apply ламотриджин at children under 2 years.

Influence on ability to driving of motor transport and to control of mechanisms. During treatment delay of speed of psychomotor reactions is observed. The persons who are engaged in potentially dangerous types of activity requiring special attention and bystry psychomotor reactions need to consider it.

Side effects:

From a nervous system and sense bodys: headache, increased fatigue, dizziness, drowsiness or sleeplessness, irritability, aggression, tremor, uneasiness, confusion of consciousness, diplopia, illegibility of visual perception, conjunctivitis, balance disturbance.

From bodies of a hemopoiesis: leukopenia, thrombocytopenia.

From bodies of a GIT: nausea, vomiting.

Allergic reactions: skin rashes, are more often makulopapulezny (usually during the first 8 weeks of therapy), the drug withdrawals which are taking place later, hypersensitivity reactions (fever, a lymphadenopathy, a face edema, hematologic disturbances, including anemia, disturbance of functions of a liver, is rare — the IDCS and multiorgan insufficiency); seldom — a malignant exudative erythema (Stephens-Johnson's syndrome), a toxic epidermal necrolysis (Lyell's disease).

Interaction with other medicines:

At simultaneous use with the antiepileptic drugs inducing liver isoenzymes (Phenytoinum, carbamazepine, phenobarbital, Primidonum) Lamitor's metabolism amplifies that can demand increase in its dose.

Sodium Valproatum competing with lamotridzhiny concerning metabolizing isoenzymes of a liver oppresses it metabolism. There are no data that Lamitor is capable to induce or inhibit the liver isoenzymes metabolizing other medicines. Lamitor can induce own metabolism, but this effect is very insignificant and does not cause serious clinical manifestations.

Though at some patients changes of concentration of other antiepileptic drugs in plasma are noted, the conducted controlled researches did not confirm Lamitor's impact on levels of at the same time accepted antiepileptic drugs in a blood plasma. in vitro given researches, carried out, indicate that Lamitor does not compete with other antiepileptic drugs for places of linkng with proteins of plasma.

Contraindications:

Hypersensitivity, pregnancy, breastfeeding, children's age (up to 2 years).

Overdose:

Symptoms: nystagmus, ataxy, dizziness, drowsiness, headache, nausea, loss of consciousness, coma.

Treatment: gastric lavage, reception of absorbent carbon. If necessary carry out symptomatic therapy.

Storage conditions:

List B. To store at a temperature not above 25 °C. A period of validity - 24 months.

Issue conditions:

According to the recipe

Packaging:

- tablets the dispersed 25 mg; packaging planimetric bezjyacheykovy 10th pack cardboard 5;
- tablets the dispersed 25 mg; packaging planimetric bezjyacheykovy 10th pack cardboard 3;
- tablets the dispersed 25 mg; packaging planimetric bezjyacheykovy 10th pack cardboard 10;
- tablets the dispersed 50 mg; packaging planimetric bezjyacheykovy 10th pack cardboard 5;
- tablets the dispersed 50 mg; packaging planimetric bezjyacheykovy 10th pack cardboard 3;
- tablets the dispersed 100 mg; packaging planimetric bezjyacheykovy 10th pack cardboard 5;
- tablets the dispersed 100 mg; packaging planimetric bezjyacheykovy 10th pack cardboard 3;