Zonisamide: chemistry, mechanism of action, and pharmacokinetics

@article{Leppik2004ZonisamideCM,
  title={Zonisamide: chemistry, mechanism of action, and pharmacokinetics},
  author={Ilo E. Leppik},
  journal={Seizure},
  year={2004},
  volume={13},
  pages={S5-S9}
}
  • I. Leppik
  • Published 1 December 2004
  • Biology
  • Seizure

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References

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Reductive metabolism of the anticonvulsant agent zonisamide, a 1,2-benzisoxazole derivative.
TLDR
Metabolism of zonisamide in vitro by hepatic subcellular fractions and cultured gastrointestinal flora produced a single metabolite, 2-(sulphamoylacetyl)-phenol (2-SMAP), by reductive cleavage of the 1,2-benzisoxazole ring.
Steady‐State Pharmacokinetics of Zonisamide, an Antiepileptic Agent for Treatment of Refractory Complex Partial Seizures
TLDR
A 56‐day pharmacokinetic study of zonisamide was conducted in 24 healthy volunteers, and steady state was achieved in 29 days including two dose escalations, and in an average of 15 days from the last dose adjustment, demonstrating that zonisamia is not an autoinducer.
Formation of 2-sulphamoylacetylphenol from zonisamide under aerobic conditions in rat liver microsomes.
TLDR
The results imply that zonisamide is metabolized reductively to SMAP by a cytochrome P450 belonging to the 3A subfamily under aerobic conditions as well as anaerobic conditions.
The necessity of adjusting the dosage of zonisamide when coadministered with other anti-epileptic drugs.
TLDR
Findings show that when ZNS is administered concomitantly with these anti-epileptic drugs, it is necessary to monitor the plasma concentration of ZNS in order to adjust its dosage.
Reductive metabolism of the anticonvulsant agent zonisamide, a 1,2-benzisoxazole derivative
TLDR
The metabolism of zonisamide in vitro was characterized through aerobic and anaerobic incubations with rat liver subcellular fractions and cultured gastrointestinal microflora and produced a single metabolite, 2-(sulphamoylacetyl)-phenol (2-SMAP), by reductive cleavage of the 1,2-benzisoxazole ring.
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