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Xenobiotica
the fate of foreign compounds in biological systems
Volume 17, 1987 - Issue 10
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Original Article

Metabolism of flumecinol in humans

I. Klebovich Chemical Works of Gedeon Richter Ltd, Pharmacological Research Centre, Department of Pharmacokinetics and Drug Metabolism, Department of Organic Chemistry, H-1475, Budapest 10, Pf. 27., Hungary
,
L. Vereczkey Chemical Works of Gedeon Richter Ltd, Pharmacological Research Centre, Department of Pharmacokinetics and Drug Metabolism, Department of Organic Chemistry, H-1475, Budapest 10, Pf. 27., Hungary
,
E. Tóth Chemical Works of Gedeon Richter Ltd, Pharmacological Research Centre, Department of Pharmacokinetics and Drug Metabolism, Department of Organic Chemistry, H-1475, Budapest 10, Pf. 27., Hungary; Chemical Works of Gedeon Richter, Ltd, Budapest, Hungary
,
J. Tamás Central Research Institute for Chemistry, Hungarian Academy of Sciences, Budapest, Hungary
,
M. Mák Central Research Institute for Chemistry, Hungarian Academy of Sciences, Budapest, Hungary
,
G. Jalsovszky Central Research Institute for Chemistry, Hungarian Academy of Sciences, Budapest, Hungary
&
S. Holly Central Research Institute for Chemistry, Hungarian Academy of Sciences, Budapest, Hungary
 show all
Pages 1247-1258 | Received 28 Oct 1986, Published online: 30 Sep 2009
 
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Abstract

1. The metabolism of 14C-flumecinol (3-trifluoromethyl-α-ethyl-benzhydrol) was studied in volunteers after a single oral dose of 100mg (11.1 MBq; 300μCi). Radioactivity excreted in urine was 78.8 ± 6.0% of dose and in faeces was 12.0 ± 5.3% dose in 120h.

2. Unchanged flumecinol was not excreted in urine, but was present in faeces unconjugated (1.2% dose) and as conjugates of glucuronic and sulphuric acids (10.8% dose).

3. Enzymic hydrolysis showed that all urinary metabolites were conjugated with glucuronic and/or sulphuric acids (77.8% dose). Unconjugated urinary metabolites were not found.

4. The major route of flumecinol metabolism was hydroxylation of the alkyl side chain and/or the phenyl group followed by conjugation.

5. Both the CF3-group and the skeleton of the original compound remained intact during metabolism.

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