TABLE 3

Four general patterns observed between in vitro unbound fractions and in vivo exposure ratios for 33 drugs in mice

A, represents the degree to which B/P was over- or under-predicted by fuplasma/fubrain ratio. B represents the degree by which CSF/B was over- or under-predicted by fubrain. C, representsthe degree by which CSF/P was over- or under-predicted by fuplasma. In every case, the reported number represents the fold difference determined by ratio of mean values rounded to the nearest whole number. Numbers in parentheses represent fold under-predictions.

Class 1
Class 2
Class 3
Class 4
Drug
A
B
C
Drug
A
B
C
Drug
A
B
C
Drug
A
B
C
Carisoprodol 3 (2) 1 Risperidone 4 3 11 Carbamazepine 4 (4) (1) Buspirone (1) 7 5
Chlorpromazine 2 (1) 1 Sulpiride 16 1 20 Midazolam 7 (9) 1 Caffeine 2 6 14
Citalopram 1 (3) (2) Thiopental 6 1 7 Phenytoin 4 (3) 1 9-OH-Risperidone 64 (9) 7
Clozapine (1) (2) (2) Zolpidem 4 (7) (2)
Cyclobenzaprine (2) 1 (1)
Diazepam (1) 1 1
Fluoxetine 1 (1) (1)
Fluvoxamine (1) (1) (1)
Haloperidol (1) (2) (2)
Hydrocodone (2) 2 1
Hydroxyzine (2) 1 (1)
Lamotrigine 2 2 3
Meprobamate 2 (1) 2
Methylphenidate (3) 2 (1)
Metocloperamide 2 (1) 2
Morphine 1 (3) (2)
Nortriptyline (2) 2 1
Paroxetine 1 (1) 1
Propoxyphene 1 (2) (2)
Selegiline (1) (2) (3)
Sertraline (1) 3 2
Trazodone 2 (1) 1
Venlafaxine
1
2
2