The Disposition and Metabolism of I.C.I. 58,834 (Viloxazine) in Humans

Abstract

1. 2-(2 - Ethoxyphenoxymethyl) - 2,3,5,6 -tetrahydro - 1,4 - oxazine (I.C. I. 58,834)* in three ¹⁴C-labelled forms, given orally to two male volunteers, was completely absorbed, extensively metabolized and rapidly eliminated via the kidney.

2. O-Dealkylation, the major metabolic pathway in the rat, was not significant in man.

3. The major component in blood at all times was I.C.I. 58,834, which had a blood half-life of 4 h. The level of ¹⁴C in blood at 31 h was near the limit of detection.

4. The observed activity of the drug appears to be due to the parent compound alone.