Abstract
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 language | English |
|---|---|
| Pages (from-to) | 257-265 |
| Number of pages | 9 |
| Journal | Xenobiotica |
| Volume | 15 |
| Issue number | 3 |
| DOIs | |
| Publication status | Published - 1985 |
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ASJC Scopus subject areas
- Pharmacology
- Toxicology
- Biochemistry
- Health, Toxicology and Mutagenesis
- Biochemistry, Genetics and Molecular Biology(all)
Cite this
Kinetic and pharmacological studies on estazolam in mice and man. / Mancinelli, A.; Guiso, G.; Garattini, S.; Urso, R.; Caccia, S.
In: Xenobiotica, Vol. 15, No. 3, 1985, p. 257-265.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Kinetic and pharmacological studies on estazolam in mice and man
AU - Mancinelli, A.
AU - Guiso, G.
AU - Garattini, S.
AU - Urso, R.
AU - Caccia, S.
PY - 1985
Y1 - 1985
N2 - 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.
AB - 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.
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UR - http://www.scopus.com/inward/citedby.url?scp=0021863799&partnerID=8YFLogxK
U2 - 10.3109/00498258509045357
DO - 10.3109/00498258509045357
M3 - Article
C2 - 2862746
AN - SCOPUS:0021863799
VL - 15
SP - 257
EP - 265
JO - Xenobiotica
JF - Xenobiotica
SN - 0049-8254
IS - 3
ER -