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The concentrations of diazepam and its metabolites in the plasma after an acute and chronic administration

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Abstract

The plasma diazepam, N-demethyldiazepam, and free oxazepam concentrations were studied in 12 neurotic outpatients during subchronic use, in 14 outpatients after chronic use, and in 8 test subjects after an acute intravenous administration. There are several reasons for believing that diazepam may induce its own metabolism in man:

  1. 1.

    The decrease in diazepam and N-demethyldiazepam concentrations in the plasma after 1–6 weeks therapy.

  2. 2.

    Comparatively low plasma diazepam concentrations in patients who had taken diazepam for several months or years.

  3. 3.

    Much higher concentrations of N-demethyldiazepam, the main metabolite, after intravenously given diazepam in chronic users of diazepam as compared to controls.

  4. 4.

    The decrease in the ability to form N-demethyldiazepam after abstinence, when diazepam was administered intravenously to a chronic user of diazepam before and after the abstinence of the drug.

Diazepam should be administered in small doses and for short periods of time only, or intermittently.

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Kanto, J., Iisalo, E., Lehtinen, V. et al. The concentrations of diazepam and its metabolites in the plasma after an acute and chronic administration. Psychopharmacologia 36, 123–131 (1974). https://doi.org/10.1007/BF00421784

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  • DOI: https://doi.org/10.1007/BF00421784

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