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Active ingredients
Lamotrigine
Release form
Pills
Composition
Lamotrigine * 100 mg; * - the generic international name recommended by WHO - lamotrigine.
Pharmacological effect
Anticonvulsant (antiepileptic) drug. The blocker voltage-dependent sodium channels. Causes a block of pulsed discharges in the culture of neurons and inhibits the excessive release of glutamate (amino acids that play a key role in generating epileptic seizures) along with the inhibition of glutamate-induced effector pulses.
Pharmacokinetics
After oral administration, lamotrigine is rapidly and completely absorbed from the gastrointestinal tract. Cmax in plasma is observed 2.5 ± 1.5 h after oral administration. The time to reach Cmax is somewhat longer in the case of taking the drug after a meal, but the degree of absorption remains unchanged. Pharmacokinetics is 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; Plasma protein binding is approximately 55%; Metabolism; Metabolized in the liver to form predominantly glucuronides; Excretion; T1 / 2 in healthy adults is 24 -35 h; Average clearance values in healthy people are 39 ± 14 ml / min; Lamotrigine is excreted from the body with urine as glucuronides. Less than 10% is excreted unchanged in the urine. Only 2% of metabolic products are excreted in feces.; Pharmacokinetics in special clinical situations; Lamotrigine T1 / 2 largely depends on concomitant drug therapy.; Lamotrigine T1 / 2 decreases to 14 hours when combined with drugs that induce the activity of cytochrome P450 isoenzymes , such as carbamazepine and phenytoin, and increases to about 70 hours on average in the case of combined use with sodium valproate. T1 / 2 lamotrigine in children is usually shorter than in adults. T1 / 2 in children is approximately 7 hours when taken with drugs that induce the activity of isoenzymes, such as carbamazepine, phenytoin, phenobarbital and primidone. T1 / 2 increases to 45-55 hours when combined with sodium valproate.; A study of single-dose lamotrigine pharmacokinetics in patients with kidney disease suggests that pharmacokinetic parameters change slightly,however, 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 adjuvant therapy for adults and children over 12 years old: - simple partial seizures; - complex partial seizures; - Secondarily generalized tonic-clonic seizures; - primary generalized tonic-clonic seizures; - typical absences; - absences atypical; - myoclonic seizures; - seizures resistant to other antiepileptic drugs of any type.; Lamitor is also used as an adjuvant therapy for children aged 2 to 12 years.
Contraindications
- severe liver dysfunction; - Hypersensitivity to lamotrigine and other components of the drug.
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 outweighs the potential risk to the fetus and child.
Dosage and administration
The initial dose of Lamitor for adults and children over 12 years old, not taking sodium valproate, but taking other antiepileptic drugs that induce isoenzymes is 50 mg 1 time / day for the first 2 weeks and 100 mg / day (2 doses) for the next 2 weeks. Then the dose should be increased to 200-400 mg / day (in 2 doses). 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 to achieve the optimal therapeutic effect. Maintenance dose - 100-200 mg (in 1 or 2 doses) .; The initial dose of Lamitor for children aged 2 to 12 who do not take sodium valproate, but take other antiepileptic drugs that induce isoenzymes is 2 mg / kg / day ( 2 doses) during the first 2 weeks and 5 mg / kg / day (in 2 doses) over the next 2 weeks. Maintenance dose - 5-15 mg / kg / day (in 2 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 during the first 2 weeks, then 0.5 mg / kg 1 time / day for the next 2 weeks. Then the dose should be increased to achieve the optimal therapeutic effect.Maintenance dose - 1-5 mg / kg (in 1 or 2 doses).
Side effects
The side effects noted in the appointment of Lamitor as monotherapy; On the part of the central nervous system: dizziness, headache, drowsiness, insomnia, fatigue.; On the part of the digestive system: nausea.; Allergic reactions: maculo-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 additional therapy to standard antiepileptic drugs; CNS: dizziness, headache, drowsiness, imbalance, increased fatigue, irritability, aggressiveness, tremor, confusion. On the part of the organ of vision: diplopia, impaired visual acuity.; On the part of the hematopoietic system: neutropenia, leukopenia., C part of the digestive system: nausea, vomiting, diarrhea phenomenon.
Overdose
Symptoms: nystagmus, ataxia, dizziness, drowsiness, headache, nausea, loss of consciousness, coma.; Treatment: gastric lavage, taking activated charcoal. If necessary, conduct symptomatic therapy.
Interaction with other drugs
With simultaneous use with antiepileptic drugs that induce liver isoenzymes (phenytoin, carbamazepine, phenobarbital, primidone), Lamitor metabolism increases, which may require an increase in its dose.; There is no evidence that Lamitor is able to induce or inhibit liver isoenzymes that metabolize other drugs. Lamitor can induce its own metabolism, but this effect is very insignificant and does not cause serious clinical manifestations. Although some patients show changes in the concentration of other antiepileptic drugs in the plasma, controlled studies have not confirmed the effects of Lamitor on the levels of simultaneously taken antiepileptic drugs in the blood plasma.Data from in vitro studies indicate that Lamitor does not compete with other antiepileptic drugs for plasma protein binding sites.
special instructions
Information on the use of Lamitor in elderly patients is limited. Therefore, a drug of this category of patients should be prescribed with caution.; If you exceed the dose of Lamitor, you may develop a skin rash (in this situation, the drug should be canceled) .; In some cases, the drug may develop severe skin rash (including Stevens-Johnson syndrome). ). Such reactions often develop in children. Lamitor should be canceled at the first sign of a rash. The risk of developing such complications increases when Lamitor is prescribed concurrently with sodium valproate and if the dose of Lamitor used exceeds the recommended initial and maximum daily dose.; With the development of skin rash, use of the drug should be immediately stopped.; When using Lamitor, such hypersensitivity symptoms may develop before the development of death), such as fever, malaise, cold symptoms, drowsiness, lymphadenopathy, swelling of the face and in very rare cases - disturbed I have liver function disorders blood (leukopenia and thrombocytopenia). In most patients, these symptoms disappear after discontinuation of Lamitor. If a rash, chills, cold symptoms, drowsiness, worsening of seizure control (especially during the first month) occur during the use of the drug, liver function tests, kidney function indicators, and blood clotting should be monitored. ; With the abrupt cancellation of Lamitor may increase seizures. The dose of Lamitor should be reduced gradually over 2 weeks. In patients with impaired renal function in the terminal stage of the disease, the accumulation of the metabolite in the form of a glucuronide should be expected. Therefore, if it is necessary to appoint such patients, caution should be exercised. The effect on the ability to drive vehicles and control mechanisms; The question of the ability to drive vehicles and work with moving mechanisms while taking Lamitor is solved individually, taking into account the clinical situation.