Lamitor, pills 100mg, 50pcs

Composition

* is a nonproprietary international name recommended by WHO; in the Russian Federation, the spelling of the international name is lamotrigine.

Pharmacological action

Anticonvulsant (antiepileptic) drug. Lamitor blocks potential-dependent sodium channels. Causes a block of pulsed discharges in the culture of neurons, inhibits the excessive release of glutamate (amino acids that play a key role in generating epileptic seizures), along with inhibiting glutamate-induced effector impulses.

Pharmacokinetics

Suction

After oral use, lamotrigine is rapidly and completely absorbed from the gastrointestinal tract. _cmax in blood plasma is observed 2.5±1.5 hours after oral use. The time to reach_cmax is slightly increased if the drug is taken after a meal, but the degree of absorption remains unchanged. The pharmacokinetics are linear up to a dose of 450 mg, the maximum single dose that has been studied. There are significant individual differences in the_{cmax values} of the drug, but individual concentrations differ very little.

Distribution

Binding to plasma proteins is approximately 55%.

Metabolism

It is metabolized in the liver to form mainly glucuronides.

Elimination

of T_1/2 in healthy adults is 24-35 hours.

The average clearance values in healthy people are 39±14 ml/min.

Lamotrigine is excreted in the urine as glucuronides. Less than 10% is excreted unchanged in the urine. Only 2% of the metabolic products are excreted in the faeces.

The pharmacokinetics

of T_1/2 lamotrigine in specific clinical cases largely depend on concomitant drug therapy.

Lamotrigine T 1/2 decreases to 14 hours when combined with drugs that induce the activity of cytochrome P450 isoenzymes, such as carbamazepine and phenytoin, and increases on average to about 70 hours when combined with sodium valproate.

Lamotrigine T 1/2 is usually shorter in children than in adults. T_1/2 in children is approximately 7 hours when taken with drugs that induce the activity of isoenzymes, such as carbamazepine, phenytoin, phenobarbital and primidone. T_1/2 increases to 45-55 hours when combined with sodium valproate.

The study of the pharmacokinetics of lamotrigine in single doses in patients with kidney disease indicates that the pharmacokinetic parameters change slightly, but the concentration of the main metabolite in the form of glucuronide increases almost 8 times due to a decrease in renal clearance.

Indications

Lamitor is recommended as monotherapy and adjunctive therapy for adults and children over 12 years of age:

• simple partial seizures;
• complex partial seizures;
• secondary generalized tonic-clonic seizures;
• primary generalized tonic-clonic seizures;
• typical absences;
• atypical absences;
• myoclonic seizures;
• seizures that are resistant to other antiepileptic drugs of any type.

Lamitor is also used as an adjunct therapy for children aged 2 to 12 years.

Use during pregnancy and lactation

The drug should not be prescribed during pregnancy and lactation, except in cases where the expected benefit of therapy for the mother exceeds the potential risk to the fetus and child.

Use in children

The initial dose of Lamitor for children from 2 to 12 years of age who are not taking sodium valproate, but are taking other antiepileptic drugs that induce isoenzymes, is 2 mg / kg / day (in 2 doses) for the first 2 weeks and 5 mg/kg/day (in 2 doses) for the next 2 weeks. The maintenance dose is 5-15 mg / kg / day (in 2 divided doses).

The initial dose of Lamitor for children taking sodium valproate in combination with other antiepileptic drugs that induce isoenzymes is 0.2 mg/kg 1 time/day for the first 2 weeks, then 0.5 mg/kg 1 time/day for the next 2 weeks. Then the dose should be increased until the optimal therapeutic effect is achieved. The maintenance dose is 1-5 mg / kg (in 1 or 2 doses).

Contraindications

• severe liver dysfunction;
• hypersensitivity to lamotrigine and other components of the drug.

Use in patients with liver function disorders

It is contraindicated in patients with severe liver function disorders.

Use in patients with impaired renal function

In patients with impaired renal function in the end stage of the disease, accumulation of the metabolite in the form of glucuronide should be expected. Therefore, caution should be exercised when prescribing to such patients.

Side effects

Side effects observed with the appointment of Lamitor as monotherapy

From the central nervous system:  dizziness, headache, drowsiness, sleep disturbance, increased fatigue.

From the digestive system:  nausea.

Allergic reactions:  macular-papular skin rash (2%), most often observed in the first 4 weeks after the start of treatment and disappears after discontinuation of the drug. In some cases – Stevens-Johnson syndrome, angioedema, toxic epidermal necrolysis.

Side effects observed with the appointment of Lamitor as an adjunct therapy to standard antiepileptic drugs

From the central nervous system:  dizziness, headache, drowsiness, balance disorders, fatigue, irritability, aggressiveness, tremor, confusion.

From the side of the visual organ:  diplopia, visual acuity disorder.

From the hematopoietic system:  neutropenia, leukopenia.

From the digestive system:  nausea, vomiting, dyspeptic symptoms.

Interaction

When used concomitantly with antiepileptic drugs that induce liver isoenzymes (phenytoin, carbamazepine, phenobarbital, primidone), the metabolism of Lamitor increases, which may require an increase in its dose.

Sodium valproate, which competes with lamotrigine for metabolizing liver isoenzymes, inhibits its metabolism. There is no evidence that Lamitor can induce or inhibit liver isoenzymes that metabolize other drugs. Lamitor can induce its own metabolism, but this effect is very small and does not cause serious clinical manifestations.

Although some patients show changes in the concentration of other antiepileptic drugs in plasma, controlled studies have not confirmed the effect of Lamitor on the levels of simultaneously taken antiepileptic drugs in blood plasma. Data from in vitro studies indicate that Lamitor does not compete with other antiepileptic drugs for plasma protein binding sites.

How to take, course of use and dosage

The initial dose of Lamitor for adults and children over 12 years of age who do not take sodium valproate, but take other antiepileptic drugs that induce isoenzymes, is 50 mg 1 time / day. during the first 2 weeks and 100 mg / day. (in 2 doses) for the next 2 weeks. Then the dose should be increased to 200-400 mg / day. (in 2 steps).

The initial dose of Lamitor for patients taking sodium valproate in combination with other antiepileptic drugs that induce isoenzymes is 25 mg every other day for the first 2 weeks and then 25 mg 1 time/day. for the next 2 weeks. Then the dose should be increased until the optimal therapeutic effect is achieved. The maintenance dose is 100-200 mg (in 1 or 2 doses).

The initial dose of Lamitor for children from 2 to 12 years of age who do not take sodium valproate, but take other antiepileptic drugs that induce isoenzymes, is 2 mg / kg / day(in 2 doses) for the first 2 weeks and 5 mg/kg/day. (in 2 doses) for the next 2 weeks. The maintenance dose is 5-15 mg / kg / day. (in 2 steps).

The initial dose of Lamitor for children taking sodium valproate in combination with other antiepileptic drugs that induce isoenzymes is 0.2 mg/kg 1 time/day. during the first 2 weeks, then 0.5 mg / kg 1 time / day. for the next 2 weeks. Then the dose should be increased until the optimal therapeutic effect is achieved. The maintenance dose is 1-5 mg / kg (in 1 or 2 doses).

Overdose

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

Treatment:  gastric lavage, taking activated charcoal. If necessary, conduct symptomatic therapy.

Special instructions

Information on the use of Lamitor in elderly patients is limited. Therefore, the drug should be prescribed with caution in this category of patients.

If the dose of Lamitor is exceeded, a skin rash may develop (in this situation, the drug should be discontinued).

In some cases, when prescribing the drug, it is possible to develop a pronounced skin rash (including Stevens-Johnson syndrome). These reactions are more common in children. Lamitor should be discontinued at the first sign of a rash. The risk of developing such complications increases when Lamitor is prescribed simultaneously with sodium valproate and if the used dose of Lamitor exceeds the recommended initial and maximum daily dose.

If a skin rash develops, the drug should be discontinued immediately.

When using Lamitor, hypersensitivity symptoms may develop (in some cases up to the development of a fatal outcome), such as fever, malaise, cold symptoms, drowsiness, lymphadenopathy, facial edema, and in very rare cases – liver function disorders, hematopoietic disorders (leukopenia and thrombocytopenia). In most patients, these symptoms disappear after discontinuation of Lamitor.

If a rash, chills, cold symptoms, drowsiness, or deterioration in the control of convulsive seizures occur during the use of the drug (especially during the first month), liver function tests, kidney function indicators, and blood clotting should be monitored.

If the Lamitor is abruptly withdrawn, seizures may become more frequent. The dose of Lamitor should be reduced gradually over 2 weeks.

In patients with impaired renal function in the end stage of the disease, accumulation of the metabolite in the form of glucuronide should be expected. Therefore, caution should be exercised when prescribing to such patients.

Influence on the ability to drive motor vehicles and manage mechanisms

The question of the ability to drive vehicles and work with moving mechanisms while taking Lamitor is decided individually, taking into account the clinical situation.

Form of production

Tablets

Storage conditions

In a place protected from light and moisture, at a temperature not exceeding 30 °C

Shelf life

3 years

Active ingredient

Lamotrigine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets