Lamitrile

Lamitril is an anticonvulsant often used when other medications used to treat a variety of seizures have failed.

Indications Lamitrile

Indications include: generalized and focal tonic-clonic seizures (mainly used in the presence of resistance to other anticonvulsants).

[ 1 ]

Release form

It is available in the form of tablets of 25 mg (30 tablets in a bottle) or 100 and 150 mg (60 tablets in a bottle).

Pharmacodynamics

Lamotrigine blocks potential-dependent sodium channels located in presynaptic neuronal membranes. This occurs through slow deactivation and suppression of excess released glutamate (this amino acid is one of the main factors that provoke the development of an epileptic seizure).

[ 2 ], [ 3 ], [ 4 ], [ 5 ], [ 6 ], [ 7 ], [ 8 ]

Pharmacokinetics

After oral administration, the drug is absorbed from the gastrointestinal tract quite quickly, and reaches peak concentration in the blood plasma after 2.5 hours.

The active substance is actively metabolized, the main decay product is N-glucuronide. The average half-life is 29 hours. Excretion occurs mainly in the form of metabolites, and some is excreted unchanged (mainly with urine). The half-life in children is shorter than in adult patients.

[ 9 ], [ 10 ], [ 11 ]

Dosing and administration

The initial single dose for oral administration (for children aged 12+ and adults) is 25-50 mg. For maintenance treatment – 100-200 mg per day. Rarely, it is necessary to prescribe doses of 500-700 mg per day.

The initial dosage for children aged 2-12 years is 0.2-2 mg/kg per day, and for maintenance treatment - 1-15 mg/kg per day. Children aged 2-12 years are allowed to consume no more than 200-400 mg per day (the exact dosage depends on the treatment regimen used).

The frequency of use, as well as the intervals between doses in the event of an increase in dosage, depend on the treatment regimen used, as well as the patient's response to therapy.

[ 17 ], [ 18 ]

Use Lamitrile during pregnancy

It is not recommended to prescribe Lamitril during pregnancy. It is allowed to use it only in cases where the possible benefit to the woman exceeds the possibility of negative consequences for the fetus. During the period of breastfeeding, the drug should also be used with caution.

Contraindications

Among the contraindications:

• severe liver dysfunction;
• individual intolerance to the active component of the drug;
• children under 2 years of age, as well as elderly people.

[ 12 ], [ 13 ], [ 14 ], [ 15 ]

Side effects Lamitrile

Side effects include:

• CNS organs: dizziness with headaches, sleep disorders or, on the contrary, a feeling of drowsiness, fatigue, confusion, and also aggressiveness;
• digestive system organs: liver dysfunction and nausea;
• organs of the hematopoietic system: leukopenia or thrombocytopenia;
• allergy: skin rashes (usually measles-like), Quincke's edema, malignant exudative erythema, Lyell's syndrome, and in addition lymphadenopathy.

[ 16 ]

Overdose

Overdose of lamotrigine results in dizziness, ataxia, and nystagmus, as well as headaches, drowsiness, widening of the QRS interval on the ECG, vomiting, and coma. In some cases, this has resulted in death.

Therapy includes gastric lavage and activated carbon. In addition, hospitalization of the patient is mandatory for symptomatic and supportive therapy.

[ 19 ], [ 20 ], [ 21 ]

Interactions with other drugs

Valproates (including valproic acid) are competitive blockers of liver enzymes, and in addition, they suppress the process of glucuronidation of the active substance. As a result, the rate of metabolism decreases and the average half-life of lamotrigine increases (up to 70 hours).

Anticonvulsants that induce metabolizing liver enzymes (including carbamazepine with phenytoin, as well as primidone with phenobarbital, etc.), and also paracetamol increase the rate of metabolism and glucuronidation of the active substance. When combined with them, the average half-life of lamotrigine is reduced by about 2 times (to 14 hours).

The combined use of carbamazepine with lamotrigine often leads to the appearance of negative manifestations from the central nervous system (dizziness, ataxia, nausea, and in addition to this, loss of visual acuity and diplopia). These symptoms disappear soon after reducing the dosage of carbamazepine. A similar effect develops in the case of prescribing oxcarbazepine with lamotrigine to a healthy person (without studying the results of reducing the dosage).

Oral contraceptives containing ethinyl estradiol (30 mcg) and levonorgestrel (150 mcg) approximately double the clearance rate of lamotrigine, as a result of which its peak concentration and AUC decrease by 39 and 52 percent, respectively. During the week free from taking OCs, the concentration of lamotrigine in the serum increases, and at the time of taking a new dose it becomes approximately 2 times higher than during the treatment course.

Rifampicin increases the clearance rate of lamotrigine and also reduces its half-life (stimulates the activity of liver enzymes involved in the glucuronidation process).

[ 22 ], [ 23 ]

Storage conditions

The medicine must be kept in a place protected from sunlight and inaccessible to children. Temperature conditions – no more than 25°C.

[ 24 ], [ 25 ]

Shelf life

Lamitril is permitted to be used for 5 years from the date of manufacture of the drug.

[ 26 ]