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. 1981;11(Suppl 1):11S–16S. doi: 10.1111/j.1365-2125.1981.tb01833.x

Benzodiazepines

A summary of pharmacokinetic properties

D J Greenblatt, R I Shader, M Divoll, J S Harmatz
PMCID: PMC1401650  PMID: 6133528

Abstract

1 The onset and duration of action of benzodiazepines after single oral doses depend largely on absorption rate and the rate and extent of distribution, respectively.

2 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.

3 Long-acting benzodiazepines have half-life values usually exceeding 24 hours. 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.

4 Intermediate and short-acting benzodiazepines have half-life values from 5-24 hours. 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.

5 The half-life of ultrashort acting benzodiazepines is less than 5 hours. These drugs are essentially non-accumulating.

6 Pharmacokinetic classification may assist in understanding of differences among benzodiazepines, but does not explain all of their clinical actions.

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

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