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Benzodiazepine: Bedeutung der Kinetik für die Therapie

Benzodiazepines: Pharmacokinetic properties

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Summary

The onset and duration of action of benzodiazepines after single oral doses depend largely on absorption rate and the rate and extent of distrubion. The rate and extent of accumulation during multiple dosage depend on elimination half-life and clearance. A framework is proposed for classification of benzodiazepines according to elimination half-life. Long acting benzodiazepines have half-life values usually exceeding 24 h. Drugs in this category have long-acting pharmacologically active metabolites, often desmethyldiazepam, accumulate extensively during multiple dosage, and may have impaired clearance in the elderly and those with liver disease. Intermediate and short-acting benzodiazepines have half-life values from 5–24 h and active metabolites are uncommon. Accumulation during multiple dosage is less extensive than with the long-acting group and diminishes as the half-life becomes shorter. Age and liver disease have a small influence on metabolic clearance. The half-life of ultrashort-acting benzodiazepines is less than 5 h. These drugs are essentially non-accumulating. Pharmacokinetic classification may assist in understanding differences among benzodiazepines, but does not explain all of their clinical actions.

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Abbreviations

DZ:

Diazepam

DMDZ:

Desmethyldiazepam

DMDZ (CZP):

Desmethyldiazepam (gebildet aus Clorazepat)

DMDZ (PRZ):

Desmethyldiazepam (gebildet aus Prazepam)

DAFLZ:

Desalkylflurazepam (gebildet aus Flurazepam)

OXZ:

Oxazepam

LRZ:

Lorazepam

TMZ:

Temazepam

CBZ:

Clobazam

TRZ:

Triazolam

ALPRZ:

Alprazolam

MDZ:

Midazolam

t1/2El :

Eliminationshalbwertzeit

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Authors and Affiliations

  1. Medizinische Universitätsklinik, Bonn-Venusberg

    Hermann R. Ochs

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Mit Unterstützung der Deutschen Forschungsgemeinschaft (Az Oc 10/6-3), Kennedyallee 40, D-5300 Bonn 2

Diese Arbeit enthält wesentliche Teile der Dissertation D. Saur, Bonn, 1983.

Frau Monika Linden, Elke Moritz, D.J. Greenblatt sei für die freundliche Mitarbeit gedankt.

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Ochs, H.R. Benzodiazepine: Bedeutung der Kinetik für die Therapie. Klin Wochenschr 61, 213–224 (1983). https://doi.org/10.1007/BF01496127

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