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Xenobiotica
the fate of foreign compounds in biological systems
Volume 15, 1985 - Issue 3
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Original Article

Kinetic and pharmacological studies on estazolam in mice and man

, , , &
Pages 257-265 | Received 02 Feb 1984, Published online: 30 Sep 2009
 

Abstract

1. After i.v. and oral doses of estazolam (5 mg/kg) to mice, the drug was rapidly cleared with a β half-life (t1/2β) of 0.7 h.

2. The active metabolite, 1-oxo-estazolam, was present in traces in mouse plasma and brain. Its elimination t1/2 (β), 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.

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