Examples of active metabolites formed by hydroxylation
Drug | Metabolite | In Vitro Activity Ratio with Parenta | Reference |
|---|---|---|---|
| Acetohexamide | Hydroxyacetohexamide | 2.5 | Harrower et al. (1996) |
| Carteolol | 8-Hydroxycarteolol | 1.0 | Watanabe et al. (1989) |
| Darifenacin | Hydroxydarifenacin | 0.1 | Kerbusch et al. (2004) |
| Propranolol | 4-Hydroxypropranolol | 0.8 | Oatis et al. (1981) |
| Proprafenone | 5-Hydroxypropafenone | 0.25 | Cahill and Goss (2004) |
| Risperidone | 9-Hydroxyrisperidone | 1.0 | Yamada et al. (2002) |
| Tolazamide | Hydroxytolazamide | 0.4 | Harrower et al. (1996) |
| Tolbutamide | 5-Hydroxytolbutamide | 0.25 | Nilvebrant (2002) |
| Zatosetron | 3-Hydroxyzatosetron | 0.1 | Cohen et al. (1993) |
↵ a This value is calculated as in vitro potency (e.g., Ki) of parent drug/in vitro potency of metabolite for the target receptor