Abstract
Tolcapone is a catechol‐O‐methyl transferase inhibitor. It is used in the treatment of Parkinson's disease as an adjunct to levodopa/carbidopa medication. The excretion and metabolism of [ 14 C]‐tolcapone were examined in six healthy male volunteers after an oral administration. Results showed that tolcapone was completely metabolized and excreted in urine (57% of the administered radioactivity) and feces (41%). Only 0.5% of the administered tolcapone was excreted unchanged. Glucuronide conjugation was the major metabolic reaction observed to form 2 as the major metabolite in plasma within 2 h after dosing, whereas 3‐O‐methyl tolcapone was the major terminal metabolite in plasma. Metabolite 2 was also the most abundant metabolite in urine and feces, accounting for 27 and 33%, respectively, of the total radioactivity excreted by these routes.
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