Sazar, pills 50mg, 30pcs

Composition

• Active ingredient:  one tablet contains 50 mg of lamotrigine.
• Auxiliary substances:  low-substituted hyprolose, calcium carbonate, sodium carboxymethyl starch, colloidal silicon dioxide, magnesium aluminosilicate, magnesium stearate, sodium saccharinate, povidone, microcrystalline cellulose, blackcurrant flavor.

Pharmacological action

Lamotrigine is a potential-dependent sodium channel blocker. Reduces the pathological activity of neurons without inhibiting their function. Stabilizes neuronal membranes by influencing Na+channels, blocks excessive release of glutamate, without reducing its normal release. Pharmacokinetics Suction. Lamotrigine is rapidly and completely absorbed from the intestine, with virtually no first-pass presystemic metabolism. The maximum plasma concentration is reached approximately 2.5 hours after oral use of the drug. The time to reach the maximum concentration slightly increases after ingestion, but the degree of absorption remains unchanged. The pharmacokinetics are linear when taking a single dose of up to 450 mg (the highest dose studied). There are significant inter-individual fluctuations in the maximum concentration at equilibrium, however, with rare fluctuations in each individual. Distribution. Lamotrigine binds to plasma proteins by approximately 55%. It is unlikely that the release of the drug from the protein bond can lead to the development of a toxic effect. The volume of distribution is 0.92-1.22 l / kg. Metabolism. The enzyme uridine diphosphate-glucuronyltransferase (UDP-glucuronyltransferase) is involved 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 an interaction between lamotrigine and other drugs metabolized by the cytochrome p450 system. Output. In healthy adults, the clearance of lamotrigine at steady-state 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 unchanged by the kidneys, about 2% – by the intestines. Clearance and half-life are independent of the dose. The elimination half-life in healthy adults is on average from 24 hours to 35 hours. Patients with Gilbert’s syndrome showed a 32% decrease in drug clearance compared to the control group, which, however, did not exceed the limits of normal values for the general population. The half-life of lamotrigine is greatly affected by co-administered medications. The mean elimination half-life is reduced to approximately 14 hours when co-administered with glucuronidation-promoting drugs such as carbamazepine and phenytoin, and increases to an average of 70 hours when co-administered with valproic acid. Special patient groups Children have a higher clearance of lamotrigine based on body weight than 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 concomitantly with drugs that stimulate glucuronidation, such as carbamazepine and phenytoin, and increases on average to 45-50 hours when co-administered 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 functionin case of impaired renal function, the initial dose of lamotrigine is calculated in accordance with the standard scheme for prescribing an antiepileptic drug. A dose reduction may only be necessary if there is a significant decrease in renal function. Patients with impaired liver function The initial, increasing and maintenance dose should be reduced by approximately 50% in patients with moderate hepatic insufficiency (Child-Pugh stage B) and by 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 disorder: Efficacy in preventing mood disorders in patients with bipolar disorder has been demonstrated in two basic clinical studies. As a result of the combined analysis of the results obtained, it was found that the duration of remission, defined as the time to the first episode of depression and to the first episode of mania/hypomania/mixed after stabilization, was longer in the lamotrigine group compared to placebo. The duration of remission is more pronounced for depression.

Indications

Use during pregnancy and lactation

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

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

Preliminary data indicate that lamotrigine passes into breast milk at concentrations of 40-45% of the plasma concentration. In a small number of children whose mothers received lamotrigine, no side effects were observed.

Use in children

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

Contraindications

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

Use caution if you have a history of chronic renal failure, allergic reactions, or skin rash when taking other antiepileptic drugs.

Side effects

From the central nervous system:  headache, dizziness, drowsiness, sleep disorders, fatigue, aggressiveness, confusion.

From the digestive system:  nausea, impaired liver function.

From the hematopoietic system:  leukopenia, thrombocytopenia.

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

Interaction

When used concomitantly with anticonvulsants – inducers of metabolism in the liver (including phenytoin, carbamazepine, phenobarbital, primidone), lamotrigine metabolism accelerates.

With simultaneous use of lamotrigine and carbamazepine or phenytoin, a decrease in T_1/2 of lamotrigine occurs. Dizziness, ataxia, diplopia, blurred vision, and nausea have been reported in patients taking carbamazepine after starting lamotrigine treatment.

Due to the inhibition of microsomal liver enzymes under the influence of sodium valproate, when used simultaneously, lamotrigine metabolism slows down, and lamotrigine T_{1/2 increases}.

How to take, course of use and dosage

When taken orally for adults and children over 12 years of age, the initial single dose is 25-50 mg, maintenance doses are 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 use, the intervals between doses when increasing the dose depend on the treatment regimen used, the patient’s reaction to the treatment.

Overdose

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

Symptoms:  nystagmus, ataxia, loss of consciousness before coma.

Treatment:  hospitalization and appropriate symptomatic therapy. In case of recent (less than 2 hours) use of the drug, gastric lavage should be performed.

Special instructions

Use with caution in patients with renal insufficiency.

Lamotrigine should not be used in elderly patients.

If severe allergic skin reactions occur, the use of lamotrigine should be discontinued.

If lamotrigine is suddenly discontinued, it is possible to increase the manifestations of epilepsy, so it is necessary to gradually stop treatment, reducing the dose over 2 weeks.

When used concomitantly with carbamazepine, dizziness, diplopia, ataxia, visual disturbances, nausea are possible. These symptoms usually disappear with a decrease in the dose of carbamazepine.

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

Influence on the ability to drive motor vehicles and manage mechanisms

During the treatment period, the rate of psychomotor reactions slows down. This should be taken into account by people who engage in potentially dangerous activities that require increased attention and rapid psychomotor reactions.

Form of production

Tablets

Storage conditions

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

Shelf life

3 years

Active ingredient

Lamotrigine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets