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Topiramate

CAS No.

97240-79-4

Innovator/marketer

Topamax

Polymorphic form

Orthorhombic structure

Therapeutic Area

Nervous system

Status

Commercial

EU DMF readiness

US DMF readiness

020581

Other documentation

Korean DMF

Drug description:

Topiramate is a dioxolopyrans derivative acts as an anticonvulsant agent.
Topiramate is indicated for monotherapy in adults, adolescents and children over 6 years of age with partial seizures with or without secondary generalized seizures, and primary generalized tonic-clonic seizures. Topiramate is indicated for adjunctive therapy in children aged 2 years and above, adolescents and adults with partial onset seizures with or without secondary generalization or primary generalized tonic-clonic seizures and for the treatment of seizures associated with Lennox-Gastaut syndrome. Topiramate is indicated in adults for the prophylaxis of migraine headache after careful evaluation of possible alternative treatment options.
It is formulated as tablets for oral route of administration.

Mechanism of action:

Topiramate blocks the action potentials elicited repetitively by a sustained depolarization of the neurons in a time-dependent manner, suggesting a state-dependent sodium channel (voltage dependent sodium channel) blocking action. Topiramate increased the frequency at which GABA-activated chloride channels (GABAA receptors) and enhances the ability of GABA to induce a flux of chloride ions into neurons, suggesting that topiramate potentiates the activity of this inhibitory neurotransmitter.
Topiramate antagonizes the ability of kainate to activate the kainate/AMPA subtype of excitatory amino acid (glutamate) receptor, but had no apparent effect on the activity of N-methyl-D-aspartate (NMDA) at the NMDA receptor subtype and it also inhibits the carbonic anhydrase enzyme, particularly isozymes II and IV.

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Products protected by valid patents are not offered for commercial sale in countries where the sale of such products constitutes patent infringement but are offered solely for uses reasonably related to the development and submission of information under a law regulating the manufacture, use or sale of drugs. It is within the buyer’s responsibility and liability to check the patent situation of the product in the imported market(s).

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