Seisar, 100 mg, 30 pcs.

Lamotrigine is a voltage-gated sodium channel blocker. Reduces the pathological activity of neurons without inhibiting their function. It stabilizes neuronal membranes by influencing the Na + channels, blocks the excess release of glutamate, without reducing its normal release.

 Pharmacokinetics

 Suction. Lamotrigine is rapidly and completely absorbed from the intestine, practically without undergoing a presystemic 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 slightly increases after a meal, but the degree of absorption remains unchanged. Pharmacokinetics is linear in the administration of a single dose of up to 450 mg (the largest dose studied). Significant interindividual fluctuations of the maximum concentration in the equilibrium state are observed, however, with rare fluctuations in each individual person.
Distribution. Lamotrigine binds to plasma proteins by approximately 55%. It is unlikely that the release of the drug from binding to the protein could lead to the development of a toxic effect. The volume of distribution is 0.92-1.22 l / kg.
Metabolism. The metabolism of lamotrigine involves the enzyme uridine diphosphate glucuronyl transferase (UDP-glucuronyl transferase). 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 interaction is possible between lamotrigine and other drugs metabolized by the P450 cytochrome system.
Breeding. In healthy adults, clearance of lamotrigine in a state of equilibrium concentrations averages 39 ± 14 ml / min.
Lamotrigine is metabolized to glucuronides, which are excreted by the kidneys. Less than 10% of the drug is excreted by the kidneys unchanged, about 2% - by the intestine. Ground clearance and elimination half-life are dose-independent. The half-life in healthy adults is on average from 24 hours to 35 hours. Patients with Gilbert's syndrome showed a decrease in clearance of the drug by 32% compared with the control group, which, however, did not go beyond the normal values ​​for the general population.
The half-life of lamotrigine is greatly influenced by co-administered drugs.
The average elimination half-life decreases to about 14 hours when administered concurrently with glucuronidation-stimulating drugs, such as carbamazepine and phenytoin, and rises to an average of 70 hours when used together with valproic acid.
Special groups of patients
Children
In children, the clearance of lamotrigine, based on body weight, is higher than in adults; it is highest in children under 5 years old. In children, the half-life of lamotrigine is usually shorter than in adults. Its average value is approximately 7 hours when administered concurrently with drugs that stimulate glucuronidation, such as carbamazepine and phenytoin, and increases on average up to 45-50 hours when used together with valproic acid.
Elderly patients
Clinically significant differences in lamotrigine clearance in elderly patients compared with young patients were not found.
Patients with impaired renal function
In case of impaired renal function, the initial dose of lamotrigine is calculated in accordance with the standard antiepileptic drug regimen. Dose reduction may be required only with a significant decrease in renal function.
Patients with impaired liver function
Initial, increasing, and maintenance doses should be reduced by approximately 50% in patients with moderate hepatic impairment (Child-Pugh stage B) and 75% in patients with severe hepatic insufficiency (Child-Pugh stage C). 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 basic clinical studies.
As a result of a combined analysis of the results, it was found that the duration of remission, defined as the time before the first episode of depression and before the first episode of mania / hypomania / mixed after stabilization, was longer in the lamotrigine group compared with 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-clonic seizures, as well as seizures with Lennox-Gastaut syndrome) as part of combination therapy or monotherapy.
  Children from 3 to 12 years of
  epilepsy (partial and generalized seizures, including tonic-clonic seizures, as well as seizures with Lennox-Gastaut syndrome) as part of combination therapy. After achieving control of epilepsy in combination therapy, concomitant antiepileptic drugs (PEPs) can be canceled and lamotrigine can be continued in monotherapy.
  Monotherapy of typical absences.
• Bipolar Disorders
  Adults (18 years of age and older)
  to prevent mood disorders (depression, mania, hypomania, mixed episodes) in patients with bipolar disorder.

   

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

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

Preliminary data show that lamotrigine passes into breast milk in a concentration of 40-45% of the plasma concentration.

In a small number of infants whose mothers received lamotrigine, no side effects were noted.

Use in children

Do not use lamotrigine in children under 2 years of age.

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

Precautions:
Chronic renal failure, allergic reactions, or skin rashes with a history of other antiepileptic drugs.

From the side of the central nervous system: headache, dizziness, drowsiness, sleep disturbances, feeling tired, aggressive, confused.

From the digestive system: nausea, impaired liver function.

From the hemopoietic system: leukopenia, thrombocytopenia.

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

With simultaneous use with anticonvulsants, inducers of metabolism in the liver (including phenytoin, carbamazepine, phenobarbital, primidone), lamotrigine metabolism is accelerated.

With the simultaneous use of lamotrigine and carbamazepine or phenytoin, a decrease in T _{1/2 of}  lamotrigine occurs . There are reports of dizziness, ataxia, diplopia, blurred vision and nausea in patients taking carbamazepine after starting treatment with lamotrigine.

Due to the inhibition of microsomal liver enzymes under the influence of sodium valproate, with simultaneous use, the metabolism of lamotrigine slows down, T _1/2  lamotrigine increases .

When taken orally for adults and children over 12 years of age, the initial single dose is 25-50 mg, the maintenance dose is 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 maintenance 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 with increasing doses depend on the treatment regimen used, the patient's response to the treatment.

A single dose of 10-20 times higher than the maximum therapeutic dose has been reported.

Symptoms:  nystagmus, ataxia, impaired consciousness to coma.

Treatment:  hospitalization and appropriate symptomatic therapy. In case of recent (less than 2 hours) administration of the drug, gastric lavage is necessary.

Use with caution in patients with renal failure.

Lamotrigine should not be used in elderly patients.

When severe skin allergic reactions appear, the use of lamotrigine should be discontinued.

With the sudden cancellation of lamotrigine, an increase in the manifestations of epilepsy is possible, therefore it is necessary to gradually stop treatment, reducing the dose for 2 weeks.

With simultaneous use with carbamazepine, dizziness, diplopia, ataxia, visual impairment, and nausea are possible. These phenomena, as a rule, pass with a decrease in the dose of carbamazepine.

Do not use lamotrigine in children under 2 years of age.

Influence on the ability to drive vehicles and control mechanisms

During the treatment period, a slowdown in the rate of psychomotor reactions is observed. This must be taken into account by persons involved in potentially hazardous activities that require increased attention and rapid psychomotor reactions.

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