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Clinical Trial
. 2011 Mar;71(3):403-10.
doi: 10.1111/j.1365-2125.2010.03843.x.

Riluzole pharmacokinetics in young patients with spinal muscular atrophy

Chadi Abbara  1 , Brigitte Estournet, Lucette Lacomblez, Benedicte Lelièvre, Amal Ouslimani, Blandine Lehmann, Louis Viollet, Annie Barois, Bertrand Diquet
Affiliations
Clinical Trial

Riluzole pharmacokinetics in young patients with spinal muscular atrophy

Chadi Abbara et al. Br J Clin Pharmacol. 2011 Mar.

Abstract

Aims: The objective of the present study was to assess the pharmacokinetics of riluzole in patients with spinal muscular atrophy (SMA).

Methods: Fourteen patients were enrolled in an open-label, nonrandomized and repeat-dose pharmacokinetic study. All participants were assigned to receive 50mg riluzole orally for 5 days. Riluzole plasma concentrations were determined from samples obtained at day 5.

Results: The pharmacokinetic analysis demonstrated that a dose of 50mg once a day was sufficient to obtain a daily total exposure [AUC(0,24h)=2257ng ml(-1) h] which was comparable with results obtained in adult healthy volunteers or ALS patients in whom a dose of 50mg twice a day is recommended. The pharmacokinetic simulation demonstrated that the administration of 50mg twice a day could result in higher concentrations, hence reduced safety margin.

Conclusion: The dose of 50mg once a day was chosen for the clinical trial evaluating the efficacy of riluzole in SMA patients.

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Figures

Figure 1
Figure 1
Mean pharmacokinetic profile of riluzole at steady state
Figure 2
Figure 2
Plot of time course of riluzole plasma concentrations in a typical subject after oral administration of 50 mg once daily. Solid lines represent the pharmacokinetic curve predicted by the one compartment model with zero order absorption. Observed (formula image); Predicted (formula image)
Figure 3
Figure 3
Simulated pharmacokinetic profiles following the oral administration of 50 mg riluzole once daily and twice daily in a typical subject. once daily (formula image); twice daily (formula image)
See this image and copyright information in PMC

References

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