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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.