TABLE 4

Brain-to-plasma concentration or AUC ratio of several H1-antagonists after i.v. administration to mdr1a/b(-/-) mice


H1-Antagonist

Brain-to-Plasma Concentration Ratio

Brain-to-Plasma AUC Ratio

Referencea
Deslortadine 14.1b 1
Diphenhydramine 9.42b 1
Hydroxyzine 4.75b 1
Triprolidine 3.60b 1
Loratadine 3.30b 1
Ebastine 1.02c 3
Epinastine 0.70b
Fexofenadine 0.33c 2
Carebastine 0.17c 3
Cetirizine

0.08b
1
  • a 1, Chen et al. (2002); 2, Cvetkovic et al. (1999); 3, Tamai et al. (2000a)

  • b Data were obtained from mdr1a/b(-/-) mice

  • c Data were obtained from mdr1a(-/-) mice