Kinetic and pharmacological studies on estazolam in mice and man

A. Mancinelli, G. Guiso, S. Garattini, R. Urso, S. Caccia

Research output: Contribution to journalArticlepeer-review


1. After i.v. and oral doses of estazolam (5 mg/kg) to mice, the drug was rapidly cleared with a half-life (t1/2 of 0.7 h. 2. The active metabolite, 1-oxo-estazolam, was present in traces in mouse plasma and brain. Its elimination t1/2 ( determined after i.v. injection of 1-oxo-estazolam (5 mg/kg) to mice, was similar to that of the parent drug in both plasma and brain. 3. After a single oral dose of estazolam (4mg) to four human volunteers the drug was rapidly absorbed and reached maximum plasma concentrations in one to three hours. Elimination t1/2 of estazolam in humans was 19 h. 4. The metabolite was undetectable in human plasma after either single or multiple doses of estazolam. 5. These results, together with the finding that 1-oxo-estazolam was less effective than estazolam, in terms of ED50 and brain concentrations necessary to antagonize leptazol convulsions and disrupt rota-rod performance in mice, indicate that the metabolite does not contribute significantly to the pharmacological effects of its parent drug.

Original languageEnglish
Pages (from-to)257-265
Number of pages9
Issue number3
Publication statusPublished - 1985

ASJC Scopus subject areas

  • Pharmacology
  • Toxicology
  • Biochemistry
  • Health, Toxicology and Mutagenesis
  • Biochemistry, Genetics and Molecular Biology(all)


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