Topalepsin, tablets 50mg 30pcs

The antiepileptic drug belongs to the class of sulfate-substituted monosaccharides.

Topiramate decreases the frequency of action potentials characteristic of the neuron in the state of persistent depolarization, indicating that the drug’s blocking effect on sodium channels depends on the state of the neuron.

Topiramate potentiates GABA activity against several GABA receptor subtypes (including GABA_A receptors) and modulates the activity of GABA_A receptors themselves, prevents kainate from activating kainate/AMPK receptor sensitivity to glutamate, and has no effect on N-methyl-D-aspartate activity against NMDA receptors. These effects of topiramate are dose-dependent at plasma concentrations of topiramate between 1 μM and 200 μM, with minimal activity between 1 μM and 10 μM.

In addition, topiramate inhibits the activity of some carboanhydrase isoenzymes, but this effect is weaker in topiramate than in acetazolamide and does not appear to be central to the antiepileptic activity of topiramate.

Indications

Partial or generalized tonic-clonic seizures in adults and children (as monotherapy or in combination with other anticonvulsants); seizures associated with Lennox-Gastaud syndrome in adults and children (as adjunctive therapy).

Active ingredient

Interaction

In concomitant use with topiramate, phenytoin and carbamazepine decrease its plasma concentrations. This is due to the induction under the influence of phenytoin and carbamazepine of enzymes involved in the metabolism of topiramate. In some cases when using topiramate an increase in plasma concentrations of phenytoin was observed.

Concomitant use of a single dose of topiramate and digoxin may decrease the AUC of digoxin.

Concomitant use of an oral contraceptive containing norethindrone and ethinylestradiol had no significant effect on norethindrone clearance, but the plasma clearance of ethinylestradiol was significantly increased. Thus, when topiramate is taken concomitantly with oral contraceptives, their efficacy may be reduced.

Concomitant administration of metformin and topiramate increases mean Cmax and AUC0-12h values of metformin by 18% and 25%, respectively, while mean clearance decreases by 20%, while plasma clearance of topiramate decreases. The clinical significance of this interaction is unclear.

In patients taking metformin, glucose levels should be monitored regularly if topiramate needs to be used or withdrawn.

Concomitant use of topiramate with drugs that predispose to nephrolithiasis may increase the risk of kidney stones.

Special Instructions

Topiramate should be withdrawn gradually to minimize the possibility of increased seizure frequency. In clinical trials, the dose of the drug was reduced by 100 mg once a week.

In order to reduce the risk of nephrolithiasis, fluid intake should be increased during treatment.

If body weight decreases with treatment, dietary adjustments should be made.

Perhaps use with caution in patients with hepatic impairment because of possible decreased clearance of topiramate.

Alcohol should be avoided during treatment.

The concomitant use of other CNS depressant drugs is not recommended.

Do not use in children under 2 years of age.

Impact on driving and operating machinery

Perhaps with caution should be used in patients engaged in potentially hazardous activities requiring increased attention and rapid psychomotor reactions, since topiramate may cause drowsiness and dizziness.

Contraindications

A hypersensitivity to topiramate

Similarities