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Xenobiotica
the fate of foreign compounds in biological systems
Volume 9, 1979 - Issue 5
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Original Article

Metabolic fate of 3-(3-methylphenyl)-5-hydroxymethyl-2-oxazolidinone (toloxatone), a new antidepressant agent, in man

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Pages 281-288 | Received 21 Nov 1977, Accepted 11 Dec 1978, Published online: 30 Sep 2009
 

Abstract

1. In man, the antidepressant agent 3-(3-methylphenyl)-5-hydroxymethyl-2-oxazolidinone (toloxatone) on oral dosing was mainly eliminated in urine (80% dose in 12h).

2. Plasma concn. of total radioactivity was max (5·8 μg equiv./ml) at 30 min to 1 h after administration and declined rapidly (t1/2, 1·25 h). Unchanged drug accounted for 48, 32 and 13% of plasma radioactivity at 15 min, 1 h and 6h, respectively.

3. The drug was extensively metabolized. The major urinary metabolites were 3-(3-carboxyphenyl)-5-hydroxymethyl-2-oxazolidinone and a glucuronide of toloxatone. A minor urinary metabolite, characterized as a phenolic derivative, was also excreted conjugated.

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