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How does stiripentol s impact on gaba differ from fenfluramine?

See the DrugPatentWatch profile for stiripentol

Stiripentol and fenfluramine are two drugs that have been associated with the modulation of gamma-aminobutyric acid (GABA), an important neurotransmitter in the brain. However, their mechanisms of action and impacts on GABA differ significantly.

Stiripentol is an anticonvulsant drug primarily used in the treatment of Dravet syndrome, a severe form of epilepsy. It is believed to exert its effects by enhancing GABAergic neurotransmission [1]. Specifically, stiripentol increases GABA levels in the brain by inhibiting GABA transaminase, an enzyme responsible for breaking down GABA [1]. This results in an increase in GABA-mediated inhibitory neurotransmission, which can help reduce seizure activity.

On the other hand, fenfluramine is a drug that was initially used as an appetite suppressant but was later withdrawn from the market due to safety concerns. Fenfluramine has been found to increase serotonin levels in the brain by promoting serotonin release and inhibiting its reuptake [2]. However, it also has an impact on GABA, although this effect is less well-studied. Fenfluramine has been shown to decrease GABA levels in certain brain regions, which could potentially contribute to its adverse effects [3].

In summary, stiripentol increases GABA levels in the brain by inhibiting its breakdown, while fenfluramine has been found to decrease GABA levels. These differences in mechanisms of action and impacts on GABA likely contribute to the distinct therapeutic and adverse effects of these two drugs.

Sources:
[1] https://www.drugpatentwatch.com/drugs/diacomit
[2] https://www.ncbi.nlm.nih.gov/books/NBK537035/
[3] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2676430/


Other Questions About Stiripentol :  In which cases is stiripentol preferred for seizure control? In what dravet syndrome stage is stiripentol primarily used unlike fenfluramine? What are the distinct side effects of stiripentol compared to fenfluramine?





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