New range of products: Topiramate by ALSI Pharma.

In August 2014 the Russian Ministry of healthcare approved production of a new medicine named “Topiramate” in the form of film-coated tablets for a producer “ALSI Pharma” (registration certificate number ЛП-002577 from 13.08.2014). This preparation is our recent development, although this product has been awaited and planned to extend our product portfolio in a “Neurology and Psychiatry” range. As far as our product “Carbamazepine” has been a success for many years, we decided to follow the recommendations of our clients to broaden a product trend, connected with antiepileptic remedies. So, both products “Topiramate” and “Carbamazepine” belong to antiepileptic drugs.

Topiramate

A chemical structure of Topiramate is rather unusual for its expected pharmacological effect. It means that being a sulfate derivate of monosaccharide named fructopyranose (fructose), this substance possesses antiepileptic activity. In addition to this, Topiramate was considered useful for prevention of migraine attacks.

Topiramate is a novel agent classified as a sulfamate substituted monosaccharide. Three pharmacological properties of topiramate are believed to contribute to its anticonvulsant activity. First, topiramate reduces the frequency at which action potentials are generated when neurons are subjected to a sustained depolarization indicative of a state-dependent blockade of voltagesensitive sodium channels. Second, topiramate markedly enhances the activity of GABA at some types of GABA receptors. Because the antiepileptic profile of topiramate differs markedly from that of the benzodiazepines, it may modulate a benzodiazepine-insensitive subtype of GABAA receptor. Third, topiramate antagonizes the ability of kainate to activate the kainate/AMPA subtype of excitatory amino acid (glutamate) receptors but has no apparent effect on the activity of N-methyl-D-aspartate (NMDA) at the NMDA receptor subtype. There are also alternative explanations of pharmacodynamics of this drug. We should take into account that the mechanism of action for Topiramate is still under discussion and research, in spite of widespread usage of the drug in medical practice (since 24 December 1996 in USA, for example).

Topiramate is rapidly and well absorbed. Following oral administration of 100 mg topiramate to healthy subjects, a mean peak plasma concentration (Cmax) of 1.5 Fg/mL was achieved within 2 to 3 hours (Tmax). The mean extent of absorption from a 100 mg oral dose of 14C-topiramate was at least 81% based on the recovery of radioactivity from the urine. There was no clinically significant effect of food on the bioavailability of topiramate.

The preparation “Topiramate”, manufactured by “ALSI Pharma”, has passed all the necessary procedures for the state registration, i.e. confirmation and approval of quality, safety and bioequivalence. This trials and research testing were assigned by the Russian Ministry of healthcare and were carried out in comparison with the original preparation “Topamax ®” (JANSSEN-CILAG, Switzerland).

Topiramate by “ALSI Pharma” is going to be manufactured in the form of film-coated tablets 25 mg or 100 mg, packed into a carton box with the quantity of 30 tablets (3 blisters, 10 tablets in each). There is also possible an optional package, which consists of 100 tablets in one polymer jar. Topiramate is a prescription only product in the vast majority of countries. The specialists, who can prescribe this medicine, are mainly doctors, such as neurologists or specialists in epileptology or psychiatry. They can practice in hospitals or ambulances. Read carefully the specialist’s or patient’s leaflet, attached to any drug’s package, before prescribing or taking these tablets. Seek for your doctor’s or pharmacist’s advice in case you have any doubts or don’t feel confident about this remedy.