Stiripentol, a Putative Antiepileptic Drug, Enhances the Duration of Opening of GABAA‐Receptor Channels

  title={Stiripentol, a Putative Antiepileptic Drug, Enhances the Duration of Opening of GABAA‐Receptor Channels},
  author={Pascale P. Quilichini and Catherine Chiron and Yehezkel Ben-Ari and Henri Gozlan},
Summary:  Purpose: Stiripentol (STP) is currently an efficient drug for add‐on therapy in infantile epilepsies because it improves the efficacy of antiepileptic drugs (AEDs) through its potent inhibition of liver cytochromes P450. In addition, STP directly reduces seizures in several animal models of epilepsy, suggesting that it might also have anticonvulsive effects of its own. However, its underlying mechanisms of action are unknown. 

Stiripentol in the Management of Epilepsy

Stiripentol is a structurally unique antiepileptic drug that has several possible mechanisms of action, including diverse effects on the gamma-aminobutyric acid (GABA)-A receptor and novel inhibition

Interactions between modulators of the GABA(A) receptor: Stiripentol and benzodiazepines.

  • J. Fisher
  • Biology, Medicine
    European journal of pharmacology
  • 2011

Stiripentol – characteristic of a new antiepileptic drug

Stiripentol represents a group of drugs indirectly enhancing GABA-ergic neurotransmission and it exerts a protective activity in some experimental seizure models, including maximal electroshock (MES)-, pentylenetetrazol-, bicuculline-, strychnine-, and cocaine-induced convulsions.

Mechanisms of action of antiepileptic drugs

The proposed mechanisms of action of marketed AEDs in the US are reviewed, the future of Aeds in development is discussed and the proposed targets of action at more than one molecular target are discussed.

Mechanisms of action of currently used antiseizure drugs

Stiripentol exhibits higher anticonvulsant properties in the immature than in the mature rat brain

After the first positive experimental data in rodents in the early 1970s demonstrating the anticonvulsant effect of stiripentol (STP), in vitro studies showed that STP acts directly on γ‐aminobutyric acid A (GABAA) receptors, leading to the hypothesis thatSTP might exhibit higher efficacy in the immature brain.

Stiripentol: an example of antiepileptic drug development in childhood epilepsies.

  • R. NabboutC. Chiron
  • Biology
    European journal of paediatric neurology : EJPN : official journal of the European Paediatric Neurology Society
  • 2012

Stiripentol in refractory status epilepticus

It is suggested that STP, either alone or as add‐on therapy, may prove useful in treating established and BZD‐resistant status epilepticus and may be particularly effective in terminating SE in children when SE is most prevalent.



Effects of Clobazam and Its Active Metabolite on GABA‐Activated Currents in Rat Cerebral Neurons in Culture

The purpose of this study was to learn how clobazam and its active metabolite modulate γ‐aminobutyric acid (GABA)‐activated currents in rat cerebral neurons in culture.

Stiripentol: Efficacy and Tolerability in Children with Epilepsy

Stiripentol (STP) is a new antiepileptic drug (AED) that inhibits cytochrome P450′ resulting in increased plasma concentrations of concomitant AEDs.

A new type of anticonvulsant, stiripentol. Pharmacological profile and neurochemical study.

Findings suggest that the anticonvulsant activity of stiripentol involves two aspects of the GABAergic mechanism in which the metabolic transamination and synaptosomal uptake of this neurotransmitter are inhibited.

Neurosteroids: endogenous regulators of the GABAA receptor

GABAA (γ-aminobutyric acid type A) receptors mediate most of the 'fast' synaptic inhibition in the mammalian brain and are targeted by many clinically important drugs. Certain naturally occurring

A Mechanistic Approach to Antiepileptic Drug Interactions

  • G. Anderson
  • Biology, Medicine
    The Annals of pharmacotherapy
  • 1998
By understanding the mechanisms of drug interactions, the pharmacist can play a key role in patient care by anticipating and preventing AED drug interactions.

Preclinical evaluation of newly approved and potential antiepileptic drugs against cocaine-induced seizures.

This study provides the first description of the effectiveness of new antiepileptic drugs against experimentally induced cocaine seizures and points to several drugs that deserve clinical scrutiny for this indication.

Neurosteroids and GABA, receptor function

The therapeutic potential of this novel, non-genomic effect of steroids is discussed and whether they may influence behaviour under physiological, or pathophysiological, conditions is investigated.

When antiepileptic drugs aggravate epilepsy

  • P. Genton
  • Medicine, Psychology
    Brain and Development
  • 2000