Epitomax is an antiepileptic drug, belongs to the class of sulfate-substituted monosaccharides. It blocks sodium channels and suppresses the occurrence of repetitive action potentials against the background of prolonged depolarization of the neuron membrane. Epitomax increases the activity of gamma-aminobutyric acid (GABA) against several subtypes of GABA receptors (including GABA receptors), as well as modulates the activity of GABA receptors themselves, prevents activation of kainate/AMPK (a-amino-3-hydroxy-5-methylisoxazole-4-propionic acid)-receptors to glutamate, does not affect N-methyl-D-aspartate (NMDA) activity against the NMDA-receptor subtype. These effects of Epitomax are dose-dependent at plasma concentrations of Epitomax of 1 to 200 μmol/L, with minimal activity between 1 and 10 μmol/L.
In addition, Epitomax inhibits the activity of certain carboanhydrase isoenzymes (II-IV). Epitomax is significantly inferior to acetazolamide, a known carbohydrase inhibitor, in terms of the severity of this pharmacological effect, so this action of Epitomax is not a major component of its antiepileptic activity.
Indications for use of Epitomax
- in monotherapy in adults and children over 6 years of age with partial (with or without secondary generalization) or primary generalized tonic-clonic seizures;
- as part of complex therapy in adults and children over 3 years of age with partial, with or without secondary generalization, or generalized tonic-clonic seizures, and also for treatment of seizures caused by Lennox-Gastaud syndrome;
- Prevention of migraine attacks in adults after careful evaluation of all possible alternatives. Epitomax is not intended to treat acute migraine attacks.
Orally, regardless of meals. Tablets should not be divided.
For optimal seizure control, it is recommended that treatment begin with a low dose followed by an increase to an effective dose. When used as monotherapy, the possible effect of withdrawal of concomitant antiepileptic drugs on seizure frequency should be considered. In cases where there is no need to abruptly cancel antiepileptic drugs, it is recommended to reduce their doses gradually, reducing doses by 1/3 every 2 weeks. When drugs that are inducers of microsomal liver enzymes are withdrawn, the concentration of Epitomax in plasma will increase, which should be taken into account in the ongoing therapy.
In adults at the beginning of monotherapy – 25 mg 1 time per night for 1 week. Then the dose is increased at 1-2 week intervals by 25-50 mg/day (the daily dose is divided into 2 doses). If intolerant to this therapy regimen, the dose is increased by a smaller amount or at longer intervals. The dose is adjusted depending on the effectiveness and tolerability of the therapy. The recommended initial target dose is 100-200 mg/day, the maximum daily dose should not exceed 500 mg in monotherapy. Dosing recommendations apply to all adults, including elderly patients without kidney disease.
For children over 6 years old in monotherapy in the first week of treatment, 0.5-1 mg/kg body weight before bedtime. Then the dose is increased at 1-2 week intervals by 0.5-1 mg/kg/day (daily dose is divided into two doses). If this therapy regimen is intolerant, the dose is increased more gently or at longer intervals between dose increases. The size of the dose and the rate of dose increase are determined by clinical efficacy and tolerability of therapy. The recommended dose range for Epitomax monotherapy in children is 100 mg/day and depends on clinical efficacy (in children aged 6-16 years, it is about 2 mg/kg/day).