TABLE 3

Classification of drugs based on discrepancies between in vivo P-gp efflux ratio and [plasma],u/[brain],uratio

The classification for each drug was assigned according to the scheme in Fig. 1. Additional evidence from the literature is provided to support the classification of each drug.


Class Ib: P-gp Efflux + Additional Mechanism

Class II: Weak or No P-gp Efflux + Additional Impairment

Class IV: P-gp Efflux - Compensatory Mechanism(s)
Drug
Additional Evidence
Drug
Additional Evidence
Drug
Additional Evidence
Cetirizine (C) Very low permeability (Mahar Doan et al., 2002) Cimetidine (Ci) Non-P-gp efflux transporter(s) (www.tp-search.jp) Methadone (M) Active uptake (Chi and Dixit, 1977)
Digoxin (Dg) Additional efflux transporter(s) (www.tp-search.jp) Dexamethasone (Dex) Steroid transporter (Pariante et al., 2001) Ritonavir (Rit) Active uptake (Anthonypillai et al., 2004)
Doxorubicin (Dox) Additional efflux transporter(s) (www.tp-search.jp) Fexofenadine (Fex) Reduced CNS activity (Hindmarch et al., 2002) Saquinavir (Sq) Active uptake (Su et al., 2004)
Ivermectin (Iv) Additional efflux transporter(s) (Lespine et al., 2006) Ranitidine (Ra) Non-P-gp efflux transporter(s) (Bourdet et al., 2005)
Sumatriptan (Sum) Very low permeability (Mahar Doan et al., 2002)


Zolmitriptan (Z)
Very low permeability (Mahar Doan et al., 2002)