Table 1.
Serum pharmacokinetic constants and parameter values (coefficient of variation for estimate) for escitalopram and paroxetine from compartmental modelling of single-dose serum concentration–time data following s.c. administration to mice and corresponding derived secondary PK parameters. PK parameters for sertraline were calculated by non-compartmental modelling (except where noteda)
| Drug | Dose (mg kg−1) | V1/F (l kg−1) | k01 (h−1) | k10 (h−1) | k12 (h−1) | k21 (h−1) | CL/F (l h−1 kg−1) | Tmax (h) | Cmax (ng mL−1) | t1/2β (h) |
|---|---|---|---|---|---|---|---|---|---|---|
| Escitalopram | 0.24 | 2.4 (94) | 30 (295) | 3.1 (118) | 3.2 (209) | 2437 (94) | 7.6 (34) | 0.07 (133) | 65 (22) | 0.9 (123) |
| 1.0 | 1.5 (4202) | 12 (4215) | 5.2 (4207) | 5.8 (4748) | 1466 (4202) | 7.6 (16) | 0.09 (10) | 264 (2) | 1.2 (54) | |
| 3.9 | 2.9 (3312) | 30 (7439) | 3 (3420) | 9.9 (5426) | 2918 (3312) | 8.8 (108) | 0.05 (2641) | 726 (929) | 0.8 (32) | |
| Paroxetine | 0.27 | 1.7 (11) | 25 (29) | 1.7 (17) | 2.3 (28) | 1.2 (33) | 2.9 (11) | 0.09 (12) | 114 (2) | 1.6 (30) |
| 1.1 | 0.9 (1439) | 14 (1488) | 2.9 (1445) | 9.5 (1625) | 1.4 (44) | 2.6 (22) | 0.08 (34) | 494 (4) | 2.3 (43) | |
| 4.4 | 3.5 (63) | 30 (207) | 0.4 (97) | 3.7 (139) | 1.7 (79) | 1.3 (55) | 0.08 (101) | 931 (9) | 6.3 (77) | |
| Sertraline | 0.56 | NA | NA | NA | NA | NA | 3.5 | 0.08 | 30.0 | NA |
| 2.2 | NA | NA | NA | NA | NA | 5.0 | 0.3 | 148 | NA | |
| 2.2a | 12 (22) | 3.6 (23) | 0.7 (26) | 0.9 (51) | 0.7 (32) | 8.9 (5) | 0.4 (2) | 98 (0.7) | 2.9 (20) | |
| 8.9 | NA | NA | NA | NA | NA | 6.5 | 0.5 | 373 | NA |
Abbreviations: NA, not applicable; PK, pharmacokinetic.
a
Additional (compartmentally modelled) PK profile for modelling of SERT occupancy data.