TABLE 4.
Predicted geometric mean peak RO and, t onset, and duration of TAT on day 1 and day 7 of 30 mg IR trazodone and on day 7 of 300 mg OAD trazodone administration
| Target | K i (nM) | Mean peak RO | t onset (h) | TAT (h) | ||||||
|---|---|---|---|---|---|---|---|---|---|---|
| 30 mg IR, s.d. | 30 mg IR, q.d. | 300 mg OAD | 30 mg IR, s.d. | 30 mg IR, q.d. | 300 mg OAD | 30 mg IR, s.d. | 30 mg IR, q.d. | 300 mg OAD | ||
| 5‐HT2A | 14 | 0.91 | 0.92 | 0.97 | 0.07 | 0.09 | 0.42 | 27.0 | >24.0 | >24.0 |
| α1B | 15 | 0.90 | 0.92 | 0.97 | 0.07 | 0.09 | 0.42 | 26.0 | >24.0 | >24.0 |
| 5‐HT1D | 26 | 0.84 | 0.87 | 0.95 | 0.07 | 0.09 | 0.50 | 18.3 | 18.2 | >24.0 |
| α1D | 27 | 0.84 | 0.86 | 0.95 | 0.10 | 0.09 | 0.50 | 17.7 | 17.7 | >24.0 |
| 5‐HT2B | 48 | 0.75 | 0.78 | 0.91 | 0.12 | 0.17 | 0.67 | 9.36 | 9.32 | >24.0 |
| 5‐HT1A | 81.8 | 0.63 | 0.68 | 0.86 | 0.19 | 0.25 | 0.76 | 3.29 | 3.11 | >24.0 |
| α1A | 98 | 0.59 | 0.64 | 0.84 | 0.22 | 0.25 | 0.84 | 2.18 | 2.1 | >24.0 |
| H1 | 190 | – | – | 0.73 | – | – | 1.43 | – | – | 16.6 |
| α2C | 240 | – | – | 0.68 | – | – | 2.18 | – | – | 11.9 |
| SERT | 280 | – | – | 0.76 | – | – | 2.94 | – | – | 8.40 |
| 5‐HT2C | 307 | – | – | 0.63 | – | – | 3.44 | – | – | 6.30 |
| 5‐HT7 | 406 | – | – | 0.56 | – | – | 27.05 | – | – | 5.88 |
| α2A | 430 | – | – | 0.55 | – | – | 27.64 | – | – | 4.28 |
| α2B | 460 | – | – | 0.53 | – | – | 28.39 | – | – | 2.19 |
| D3 | 490 | – | – | 0.52 | – | – | 52.42 | – | – | 2.01 |
| D2 | 560 | – | – | 0.48 | – | – | – | – | – | – |
Abbreviations: IR, immediate release; OAD, once a day; RO, receptor occupancy; TAT, time above the RO threshold; t onset, onset time.