Table 1. Kinetic parameter values for the in vitro biotransformation of citalopram (CIT) and desmethylcitalopram (DCIT) to DCIT and didesmethyl-CIT, respectively in human and Beagle dog microsomes.
| Substrate | Metabolite | Km1 | Vmax1 | IC1 | Km2 | Vmax2 | IC2 | References | |
| Dog liver microsomes* | |||||||||
| CIT | DCIT | 1.1 ± 0.3 | 47 ± 3 | 43 | 1 006 ± 94 | 591 ± 28 | 0.6 | this study | |
| CIT | S-DCIT | 1.0 ± 0.2 | 26 ± 1 | 27 | 848 ± 69 | 264 ± 10 | 0.3 | ||
| CIT | R-DCIT | 1.4 ± 0.5 | 21 ± 2 | 15 | 1 221 ± 161 | 338 ± 24 | 0.3 | ||
| DCIT | DDCIT | 0.6 ± 0.2 | 44 ± 4 | 73 | 137 ± 18 | 155 ± 5 | 1.0 | this study | |
| DCIT | S-DDCIT | 0.6 ± 0.1 | 31 ± 3 | 52 | 66 ± 11 | 55 ± 2 | 0.8 | ||
| DCIT | R-DDCIT | 0.3 ± 0.2 | 11 ± 2 | 37 | 212 ± 24 | 105 ± 3 | 0.5 | ||
| Human liver microsomes | |||||||||
| CIT | DCIT | 174 | – | – | – | – | – | von Moltke et al. (1999) | |
| CIT | S-DCIT | 33.8 | 20.0 | 0.6 | 202 | 220 | 1.09 | Rochat et al. (1997) | |
| CIT | R-DCIT | 17.3 | 25.0 | 1.4 | 185 | 153 | 0.83 | ||
| CIT | S-DCIT | 95 | 433 | 4.6 | – | – | – | Olesen and Linnet (1999) | |
| CIT | R-DCIT | 76 | 300 | 3.9 | – | – | – | ||
| CIT | S-DCIT | 165 | 1 007 | 6.1 | – | – | – | von Moltke et al. (2001) | |
| CIT | R-DCIT | 256 | 1 254 | 4.9 | – | – | – | ||
| DCIT | S-DDCIT | 72 | 95 | 1.3 | – | – | – | von Moltke et al. (2001) | |
| DCIT | R-DDCIT | 108 | 126 | 1.2 | – | – | – | ||
*Results are presented as means ± SD from six incubations carried out in duplicate
Intrisic clearence (IC) corresponds to the maximum velocity (Vmax) divided by the affinity constant, Km
IC = μl/(min × mg of protein); Km = μM; Vmax = pmol/(min × mg of protein)