TABLE 1

Observed in vivo AUCi/AUC ratios for 37 CYP3A4 time-dependent interactions

Interaction
Mean AUCi/AUC
fmCYP3A4
Reference
Erythromycin
1 + Alprazolam 2.5 0.8 Yasui et al. (1996)
2 + Buspirone 5.9 0.99 Kivisto et al. (1997)
3 + Carbamazepine 1.4 0.6 Barzaghi et al. (1987)
4 + Cerivastatin 1.21 0.37 Muck et al. (1998)
5 + Cyclosporinea 2.15 0.71 Gupta et al. (1989)
6 + Cyclosporinea 2.22 0.71 Freeman et al. (1987)
7 + Felodipine 2.5 0.81 Bailey et al. (1996)
8 + Loratadine 1.5 0.6 Brannan et al. (1995)
9 + Midazolam 4.11 0.94 Olkkola et al. (1993); Zimmermann et al. (1996)
10 + Nitrazepam 1.25 0.6 Luurila et al. (1995)
11 + Quinidine 1.2 0.76 Damkier et al. (1999a)
12 + Simvastatin 6.2 0.99 Kantola et al. (1998)
13 + Terfenadine 2.1 0.74 Honig et al. (1994)
14 + Triazolam 2.06 0.92 Phillips et al. (1986)
15 + Triazolam 3.36 0.92 Greenblatt et al. (1998)
Clarithromycin
16 + Cisapride 3.16 0.95 van Haarst et al. (1998)
17 + Midazolam 3.6 0.94 Yeates et al. (1996)
18 + Midazolam 7 0.94 Gorski et al. (1998)
19 + Pimozide 2.12 0.4 Desta et al. (1999)
20 + Terfenadine 2.5 0.74 Honig et al. (1994)
21 + Triazolam 5.1 0.92 Greenblatt et al. (1998)
Azithromycin
22 + Midazolam 0.87 0.94 Backman et al. (1995)
23 + Midazolam 1.23 0.94 Zimmermann et al. (1996)
24 + Triazolam 1.03 0.92 Greenblatt et al. (1998)
Diltiazem
25 + Cyclosporinea 1.49 0.71 Asberg et al. (1999)
26 + Cyclosporinea 1.57 0.71 Foradori et al. (1998)
27 + Cyclosporinea 1.25 0.71 Brockmoller et al. (1990)
28 + Lovastatin 3.6 0.99 Azie et al. (1998)
29 + Midazolam 3.75 0.94 Backman et al. (1994)
30 + Nifedipine 2.22 0.71 Tateishi et al. (1989)
31 + Nifedipine 3.11 0.71 Tateishi et al. (1989)
32 + Nifedipine 2.39 0.71 Ohashi et al. (1990)
33 + Simvastatin 4.82 0.99 Mousa et al. (2000)
34 + Triazolam 3.38 0.92 Varhe et al. (1996)
35 + Triazolam 2.3 0.92 Kosuge et al. (1997)
36 + Buspirone 5.5 0.99 Lamberg et al. (1998)
37
+ Quinidine
1.53
0.76
Laganiere et al. (1996)

  • ↵ a fmCYP3A4 values obtained by regression analysis using eq. 1.