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Related Experiment Videos

Interaction study between fluvoxamine and quazepam.

Hideto Kanda1, Norio Yasui-Furukori, Takashi Fukasawa

  • 1Department of Neuropsychiatry, Yamagata University School of Medicine, Yamagata 990-9585, Japan.

Journal of Clinical Pharmacology
|November 15, 2003
PubMed
Summary
This summary is machine-generated.

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Fluvoxamine, a cytochrome P450 inhibitor, slightly reduced quazepam metabolism in healthy volunteers. This drug interaction showed minimal clinical significance for quazepam (QZ) and its metabolites.

Area of Science:

  • Pharmacology
  • Drug Metabolism
  • Clinical Pharmacology

Background:

  • Fluvoxamine is a potent inhibitor of cytochrome P450 enzymes.
  • Drug interactions involving fluvoxamine can alter the metabolism of co-administered medications.
  • Quazepam is a benzodiazepine used for insomnia, metabolized by cytochrome P450 enzymes.

Purpose of the Study:

  • To investigate the pharmacokinetic interaction between fluvoxamine and quazepam.
  • To assess the impact of fluvoxamine on quazepam and its active metabolites' plasma concentrations.
  • To evaluate the effect of this interaction on psychomotor function.

Main Methods:

  • Double-blind, randomized, crossover study in 12 healthy male volunteers.
  • Administration of fluvoxamine (50 mg/day) or placebo for 14 days.

Related Experiment Videos

  • Single oral dose of quazepam (20 mg) on day 4, with blood sampling up to 240 hours.
  • High-performance liquid chromatography (HPLC) for quantifying quazepam and metabolites (2-oxoquazepam [OQ] and N-desalkyl-2-oxoquazepam [DOQ]).
  • Psychomotor function assessed using Digit Symbol Substitution Test and Stanford Sleepiness Scale.

    • Main Results:

    • Fluvoxamine did not alter quazepam plasma concentrations.
    • Fluvoxamine significantly reduced plasma concentrations of OQ (6-12 hours) and DOQ (3-48 hours).
    • The AUC ratio of OQ to quazepam was significantly lower during fluvoxamine co-administration.
    • No significant impact on psychomotor function was observed at most time points.

    Conclusions:

    • Fluvoxamine exhibits a slight inhibitory effect on quazepam metabolism to OQ.
    • The observed drug interaction between fluvoxamine and quazepam appears to have minimal clinical significance.
    • Further research may be warranted to confirm long-term implications.