Pharmacokinetic parameters of six H1-antagonists in mdr1a/b KO and WT mice after a 5-mg/kg i.v. bolus dose (parameters were estimated based on mean concentration-time data; each data point was the mean of three animals)
| H1-Antagonists | PK Parameters | |||||
|---|---|---|---|---|---|---|
| CL | Vss | Terminalt1/2 | ||||
| KO | WT | KO | WT | KO | WT | |
| ml/min/kg | l/kg | h | ||||
| Cetirizine | 5.4 | 7.5 | 1.1 | 0.9 | 7.8 | 3.6 |
| Loratadine | 83 | 99 | 2.1 | 2.2 | 0.5 | 0.4 |
| Desloratadine | 20 | 23 | 3.2 | 3.0 | 3.2 | 2.8 |
| Hydroxyzine | 70 | 80 | 2.4 | 3.7 | 2.2 | 1.7 |
| Diphenhydramine | 62 | 66 | 1.6 | 1.3 | 0.8 | 0.6 |
| Triprolidine | 134 | 119 | 2.3 | 2.0 | 0.5 | 0.3 |
PK, pharmacokinetic.