A tofizopam (Grandaxin) farmakokinetikája és metabolizmusa.

Translated title of the contribution: Pharmacokinetics and metabolism of tofizopam (Grandaxin)

I. Klebovich, M. Abermann

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

Present publication summarizes the pharmacokinetics and metabolism investigations of anxiolytic tofizopam (Grandaxin) carried out in Hungary and in other countries. The pharmacokinetics and metabolism of tofizopam were studied in animals (mice, rat, rabbit, dog, monkey) and humans. The pharmacokinetics profile of the compound can be described by a two-compartment open model, where the absorption and distribution phase were found to be rapid (tmax 0.5-1.0 hour in rats and 1.0-1.5 hours in humans). The unchanged tofizopam and 14C-total radioactivity were eliminated from human plasma with a biological half-life (t beta 1/2) of 2.7-3.5 hours and 15-21 hours, respectively, which show a slower elimination of the metabolites. The main route of elimination was the excretion of the mainly conjugated metabolites after the intensive first-pass metabolism in urine and/or faeces, depends on the species. The major route of biotransformation was mono-, di-, tri- and tetra-o-demethylation in the various degree and positions of aromatic ring(s).

Original languageHungarian
Pages (from-to)83-90
Number of pages8
JournalActa Pharmaceutica Hungarica
Volume63
Issue number2
Publication statusPublished - Mar 1993

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Pharmacokinetics
Hungary
Anti-Anxiety Agents
Biotransformation
Feces
Radioactivity
Haplorhini
Half-Life
Urine
Dogs
Rabbits
tofisopam

ASJC Scopus subject areas

  • Pharmaceutical Science

Cite this

A tofizopam (Grandaxin) farmakokinetikája és metabolizmusa. / Klebovich, I.; Abermann, M.

In: Acta Pharmaceutica Hungarica, Vol. 63, No. 2, 03.1993, p. 83-90.

Research output: Contribution to journalArticle

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