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High-throughput Fluorometric Measurement of Potential Soil Extracellular Enzyme Activities
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[Not Available].

Danièle Bentué-Ferrer1, Olivier Tribut1, Marie-Clémence Verdier1

  • 1Laboratoire de Pharmacologie Biologique, CHU Pontchaillou, Rennes, France.

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Summary

Clobazam, an anticonvulsant, has an active metabolite, norclobazam, with a longer half-life. Therapeutic drug monitoring for clobazam is considered largely ineffective due to complex factors.

Keywords:
clobazamsuivi thérapeutique pharmacologiquetherapeutic drug monitoring

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Area of Science:

  • Pharmacology
  • Clinical Pharmacy

Context:

  • Clobazam is a 1,5-benzodiazepine used as adjunctive therapy for refractory epilepsies and adult anxiety.
  • It is metabolized into an active metabolite, norclobazam, with significantly higher plasma concentrations and a longer elimination half-life than the parent drug.

Purpose:

  • To evaluate the utility of therapeutic drug monitoring (TDM) for clobazam and its active metabolite, norclobazam.
  • To understand the pharmacokinetic and pharmacodynamic complexities influencing clobazam efficacy and safety.

Summary:

  • Clobazam exhibits substantial inter-individual variability in plasma concentrations.
  • The concentration-effect relationship is challenging to establish due to add-on therapy and dose-response complexities.
  • Adverse reactions and tolerance are more frequent at higher concentrations, but TDM is deemed 'rather useless' due to lack of validated therapeutic ranges and kinetic interactions.

Impact:

  • Highlights the challenges in optimizing clobazam therapy due to its complex pharmacokinetics and metabolism.
  • Suggests that current evidence does not support routine therapeutic drug monitoring for clobazam.
  • Underscores the need for further research to establish clear guidelines for clobazam dosing and monitoring.