Relative amounts of unchanged galantamine (UD) and its major metabolites in deproteinized 1-h plasma samples of rats and of three healthy male dogs after single oral administration of [3H]galantamine hydrobromide at 2.5 mg base-Eq/kg body weight and of four healthy male subjects after a single oral dose of 4 mg base-Eq [3H]galantamine hydrobromide
| Metabolite Code | Rats | Male Dogs | Human Subjects | ||
|---|---|---|---|---|---|
| Male | Female | Poor Metabolizers | Extensive Metabolizers | ||
| UD | 43.9 | 83.2 | 22.6 | 68.4 | 62.1 |
| 2 | 3.5 | 3.9 | — | — | 13.4 |
| 3 | 7.9 | 3.2 | — | — | — |
| 5 | 14.3 | 11.4 | 23.3 | 20.3 | 23.8 |
| 8 | 5.9 | 2.4 | 3.8 | — | — |
| 10 | 4.1 | 0.8 | 47.5 | — | — |
| 13 | 10.6 | 2.8 | — | — | — |
| 14 | 2.6 | 0.9 | 0.6 | — | — |
| 15 | — | 6.9 | — | — | — |
| P96-a | — | — | 2.2 | — | — |
| Sum | 92.8 | 115.5 | 100.0 | 88.7 | 99.3 |
The data for human subjects are separately presented for poor and extensive metabolizers of CYP2D6. Figures represent the percentage of sample radioactivity.
—, not detected or below the limit of quantification.
↵6-a Metabolite fraction comprising 1 or 2 metabolites.