TABLE 2

Unbound fractions and Kp,brain values for 34 drugs

Kp,brain values were determined experimentally or obtained from the cited reference. Free fractions are reported as mean ± S.D. (n = 6, unless otherwise indicated by an = 5, bn = 4, cn = 18, or dn = 16).

Drug
fu,plasma
fu,brain
Kp,brain-/-
Kp,brain+/+
Reference for Kp,brain
Alfentanil (Al) 0.26 ± 0.04 0.32 ± 0.11 0.53 0.19
Amprenavir (A) 0.075 ± 0.008 0.091 ± 0.005 1.0 0.072 Polli et al., 1999
Cetirizine (C) 0.160 ± 0.009 0.072 ± 0.007 0.080 0.020 Chen et al., 2003
Cimetidine (Ci) 0.81 ± 0.07 0.53 ± 0.10 0.031 0.033
Desloratadine (Dl) 0.055 ± 0.002 0.0071 ± 0.0008 14 <1.0 Chen et al., 2003
Dexamethasone (Dex) 0.272 ± 0.014 0.098 ± 0.010a 0.70 0.30 Schinkel et al., 1995b
Digoxin (Dg) 0.33 ± 0.02 0.0156 ± 0.0011 1.5 0.08 Schinkel et al., 1995b
Diphenhydramine (D) 0.33 ± 0.02 0.058 ± 0.003 0.70 9.0 Chen et al., 2003
Doxorubicin (Dox) 0.22 ± 0.03 0.0014 ± 0.0005 0.0025 0.00077 Kusuhara and Sugiyama, 2001
Eletriptan (Ele) 0.28 ± 0.03 0.055 ± 0.004 14 0.30 Evans et al., 2003
Fentanyl (F) 0.17 ± 0.04 0.07 ± 0.005 4.5 2.4
Fexofenadine (Fex) 0.35 ± 0.03 0.077 ± 0.014 0.30 0.17 Cvetkovic et al., 1999
Hydroxyzine (H) 0.062 ± 0.008 0.014 ± 0.002 4.8 3.8 Chen et al., 2003
Indinavir (I) 0.058 ± 0.007 0.100 ± 0.008 0.81 0.084 Kim et al., 1998
Ivermectin (Iv) 0.024 ± 0.008a 0.00009 ± 0.00007b 2.5 0.094 Schinkel et al., 1995a
Loperamide (Lop) 0.023 ± 0.005c 0.0046 ± 0.0005d 5.7 0.096
Loratadine (L) 0.0045 ± 0.00017 0.00178 ± 0.00015 3.3 1.6 Chen et al., 2003
Meperidine (Me) 0.38 ± 0.03 0.13 ± 0.019 7.0 6.8
Methadone (M) 0.147 ± 0.007 0.029 ± 0.002 20 4.0
Morphine (Mor) 0.50 ± 0.04 0.41 ± 0.11 0.72 0.49 Schinkel et al., 1995b
Naratriptan (N) 0.58 ± 0.03 0.23 ± 0.02 1.1 0.42 Evans et al., 2003
Nelfinavir (Nel) 0.0010 ± 0.0004 0.00053 ± 0.00004 2.6 0.086 Kim et al., 1998
Peclitaxel (Pax) 0.021 ± 0.002 0.0028 ± 0.0004 4.0 0.50 Kemper et al., 2004
Quinidine (Q) 0.16 ± 0.03 0.037 ± 0.003 4.8 0.20 Kusuhara et al., 1997
Ranitidine (Ra) 0.96 ± 0.05 0.96 ± 0.13 0.039 0.022
Ritonavir (Rit) 0.0027 ± 0.0005 0.0106 ± 0.0016 2.3 0.17 Yamazaki et al., 2001
Rizatriptan (Riz) 0.62 ± 0.02 0.348 ± 0.014 0.85 0.20 Evans et al., 2003
Saquinavir (Sq) 0.00043 ± 0.00007 0.00190 ± 0.00016 0.88 0.13 Kim et al., 1998
Sufentanil (Su) 0.054 ± 0.014 0.034 ± 0.010 4.8 1.6
Sumatriptan (Sum) 0.63 ± 0.03 0.36 ± 0.03 0.22 0.13 Evans et al., 2003
Triprolidine (T) 0.31 ± 0.02 0.092 ± 0.002 3.6 5.9 Chen et al., 2003
Verapamil (V) 0.11 ± 0.03 0.033 ± 0.02 3.3 0.43 Hendrikse et al., 1998
Vinblastine (Vi) ≥ 0.09 0.0046 ± 0.0004 19 1.7 Schinkel et al., 1994
Zolmitriptan (Z)
0.98 ± 0.11a
0.54 ± 0.08
0.085
0.038
Evans et al., 2003