Table 1 Pharmacology of Select Second-Generation Antihistamines ([8, 11–13])
Compound | Receptor-Binding Affinity, Ki, nmol/L (SEM) | tmax, h (SD) | Onset of Action, h | Duration of Action, h | t1/2, h (SD) | Vd, L/kg (SD) | Protein Binding, % |
|---|---|---|---|---|---|---|---|
Cetirizine | 47.2 (10) | 1.0 (0.5) | 0.7 | 324 | 6.5-10 | 0.56 | 93 |
Desloratadine | 0.87 (0.1) | 3 | 3 | 324 | 27 | > 100 | 95 |
Ebastine/carebastine | 51.7 (6.8) | 2.6 (5.7) | 1-3 | 324 | 10.3 (19.3) | 90-14 | > 95 |
Fexofenadine | 175 (68) | 2.6 | 1-2 | 24 | 14.4 | 5.8 (0.7) | 60-70 |
Levocetirizine | 2.0 (0.1) | 0.8 (0.5) | 0.5 | > 24 | 7 (1.5) | 0.33 | 96 |
Loratadine | 138 (23) | 1.2 (0.3) | 3-4 | 24 | 7.8 (4.2) | 119 | 98 |
Mizolastine | 22 (6) | 1.5 | 1 | 24 | 12.9 | 1.4 | 98 |
Rupatadine | 1.6 | 0.75 | 2 | 24 | 5.9 | 143 | > 95 |