Seizar (Lamotrigin)

Active substance: one tablet contains lamotrigine 200 mg.
Excipients: low-substituted hyprolose, calcium carbonate, sodium carboxymethyl starch, colloidal silicon dioxide, magnesium aluminosilicate, magnesium stearate, sodium saccharinate, povidone, microcrystalline cellulose, blackcurrant flavoring.

 

 

Lamotrigin is a blocker of potential-dependent sodium channels. Reduces the pathological activity of neurons without oppressing their function. Stabilizes neuronal membranes by affecting the Na+ channels, blocks excess release of glutamate without reducing its normal release.

Pharmacokinetics

Suction. Lamotrigine is quickly and completely absorbed from the intestines, practically without undergoing presystem metabolism of the first passage. The maximum plasma concentration is reached approximately 2.5 hours after oral administration of the drug. The time to reach maximum concentration increases slightly after meals, but the degree of absorption remains unchanged. Pharmacokinetics has a linear character when taking a single dose of up to 450 mg (the highest studied dose). There are significant interindividual fluctuations in the maximum concentration in equilibrium state, however, with rare fluctuations in each individual.
Distribution. Lamotrigin binds to plasma proteins by about 55%. It is unlikely that the release of the drug from connection with protein can lead to the development of a toxic effect. The distribution volume is 0.92-1.22 l/kg.
Metabolism. The enzyme uridindiphosphate-glucuronyltransferase (UDP-glucuronyltransferase) takes part in the metabolism of lamotrigine. Lamotrigine slightly increases its own metabolism depending on the dose. However, there is no evidence that lamotrigine affects the pharmacokinetics of other antiepileptic drugs and that there may be interaction between lamotrigin and other drugs metabolizing the cytochrome P450 system.
Withdignment. In healthy adults, the clearance of lamotrigine in equilibrium concentrations is on average 39±14 ml/min.
Lamotrigine is metabolized to glucuronides, which are excreted by the kidneys. Less than 10% of the drug is excreted unchanged by the kidneys, about 2% by the intestines. Clearance and half-life do not depend on the dose. The half-life in healthy adults averages from 24 hours to 35 hours. Patients with Gilbert syndrome had a 32% decrease in the clearance of the drug compared to the control group, which, however, did not exceed normal values for the general population.
The half-life of lamotrigin is greatly influenced by jointly taken drugs.
The average half-life is reduced to about 14 hours with simultaneous administration with glucuronization stimulation drugs such as carbamazepine and phenytoin, and increases to an average of 70 hours when administered together with valproic acid.
Special groups of patients
Children
In children, the clearance of lamotrigine is higher than in adults; it is highest in children under 5 years of age. In children, the half-life of lamotrigine is usually shorter than in adults. Its average value is approximately 7 hours when administered simultaneously with glucuronization-enhancing drugs such as carbamazepine and phenytoin, and increases to an average of 45-50 hours when administered together with valproic acid.
Elderly patients
Clinically significant differences in lamotrigine clearance in elderly patients compared to young patients have not been found.
Patients with kidney dysfunction
In case of kidney dysfunction, the initial dose of lamothrigine is calculated in accordance with the standard prescription scheme of the antiepileptic drug. Reducing the dose may only be required if kidney function is significantly reduced.
Patients with liver disfunction
Initial, increasing and maintenance doses should be reduced by about 50% in patients with moderate liver failure (stage B in Child Pugh) and by 75% in patients with severe liver failure (stage C in Child Pugh). The dose increase and maintenance dose should be adjusted depending on the clinical effect.
Clinical efficacy in patients with bipolar disorders
Effectiveness in preventing mood disorders in patients with bipolar disorders has been demonstrated in two fundamental clinical studies.
A combined analysis of the results found that the duration of remission, determined as the time before the first episode of depression and before the first episode of mania/hypomania/mixed after stabilization, is longer in the lamothrigine group compared to placebo. The duration of remission is more pronounced for depression.

 

 

 

• Epilepsy
  Adults and children (over 12 years old)
  epilepsy (partial and generalized seizures, including tonic-clonal seizures, as well as seizures in Lennox-Gasto syndrome) as part of combination therapy or monotherapy.
  Children from 3 to 12 years old
  epilepsy (partial and generalized seizures, including tonic-clonal seizures, as well as seizures in Lennox-Gasto syndrome) as part of combination therapy. After achieving epilepsy control against the background of combined therapy, concomitant antiepileptic drugs (EPP) can be canceled and lamotrigin administration continued in monotherapy.
  Monotherapy of typical absans.
• Bipolar disorders
  Adults (18 years and older)
  to prevent mood disorders (depression, mania, hypomania, mixed episodes) in patients with bipolar disorder.

 

Clinical data on the safety of lamotrigine use during pregnancy and lactation are insufficient.

When deciding on the need for use during pregnancy, the expected benefits of therapy for the mother and the potential risk to the fetus should be compared.

Preliminary data show that lamotrigine penetrates breast milk at a concentration of 40-45% of plasma concentration. A small number of infants whose mothers received lamotrigine had no side effect.

Application in children

 

Lamotrigine should not be used in children under 2 years of age.

 

Hypersensitivity to lamotrigine or any component of the drug. Children under 3 years of age (for this dosage form).

With caution
Chronic renal failure, allergic reactions or skin rash to take other antiepileptic drugs in the history.

 

From the CNS side: headache, dizziness, drowsiness, sleep disorders, fatigue, aggressiveness, confusion.

From the digestive system: nausea, liver dysfunction.

From the hematopoietic system side: leukopenia, thrombocytopenia.

Allergic reactions: skin rash (usually macular-papulous), angioedema, Stevens-Johnson syndrome, toxic epidermal necrolysis, lymphadenopathy.

Simultaneous use with anticonvulsants - liver metabolism inductors (including phenytoin, carbamazepine, phenobarbital, primidone), the metabolism of lamotrigine accelerates.

Simultaneous use of lamotrigine and carbamazepine or phenytoin reduces T1_/2 lamotrigine. There are reports of dizziness, ataxia, diplopia, blurred vision and nausea in patients taking carbamazepine after starting treatment with lamotrigin.

Due to inhibition of microsomal liver enzymes under the influence of sodium valproate, while using simultaneously, the metabolism of lamotrigine slows down, increases T1_/2 lamotrigine.

When taken orally for adults and children over 12 years of age, the initial single dose is 25-50 mg, supporting doses - 100-200 mg/day. In rare cases, doses of 500-700 mg/day may be required.

For children aged 2 to 12 years, the initial dose is 0.2-2 mg/kg/day, the supporting dose is 1-15 mg/kg/day.

The maximum daily dose for children aged 2 to 12 years, depending on the treatment regimen used, is 200-400 mg.

The frequency of administration, the intervals between doses when the dose increases depend on the treatment regimen used, the patient's reaction to the treatment.

It was reported that doses were administered once, exceeding the maximum therapeutic doses by 10-20 times. The overdose manifested itself in symptoms, including nystagmus, ataxia, impaired consciousness to a coma.

Treatment: hospitalization and appropriate symptomatic therapy. In case of recent (less than 2 hours) administration of the drug, stomach rinsing should be carried out.

Caution is used in patients with renal failure.

Lamothrigine should not be used in elderly patients.

If there are pronounced skin allergic reactions, the use of lamotrigine should be discontinued.

In case of sudden withdrawal of lamotrigine, epilepsy may increase, so it is necessary to gradually stop treatment, reducing the dose within 2 weeks.

Simultaneous use with carbamazepine may cause dizziness, diplopia, ataxia, visual impairment, nausea. These phenomena usually occur when the dose of carbamazepine decreases.

Lamotrigine should not be used in children under 2 years of age.

Impact on the ability to drive vehicles and drive mechanisms

During treatment, there is a slowdown in the speed of psychomotor reactions. This should be taken into account by persons engaged in potentially dangerous activities that require increased attention and rapid psychomotor reactions.

Tablets

In a dark place, at a temperature of 15-25 °C

3 years