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. 2004 Apr;57(4):473–486. doi: 10.1111/j.1365-2125.2003.02041.x

Table 3.

In vivo database for the interactions involving CYP3A4

Substrate Inhibitor AUC ratio Ki* (µm) [I]av/Ki [I]av,u/Ki [I]max/Ki [I]in/Ki Reference
Midazolam Azithromycin  0.87  30  0.0046  0.0033  0.0056   0.71 3.01
Midazolam Azithromycin  1.19  30  0.0092  0.0066  0.011   1.4 3.02
Midazolam Clarithromycin  3.57  57  0.0087  0.0047  0.024   0.37 3.02
Triazolam Azithromycin  1.03  30  0.0092  0.0066  0.01   0.71 3.03
Triazolam Clarithromycin  5.06  57  0.017  0.0094  0.048   0.74 3.03
 Triazolam Erythromycin  3.65  77  0.0068  0.0011  0.035   0.56 3.03
Midazolam Azithromycin  1.27  30  0.0092  0.0066  0.011   1.4 3.04
Midazolam Erythromycin  3.81 170  0.0046  0.0004  0.016   0.25 3.04
Alprazolam Cimetidine  1.58 140  0.034  0.028  0.081   0.56 3.05
Triazolam Cimetidine  1.54  99  0.048  0.039  0.11   0.8 3.05
Alprazolam Cimetidine  1.73 140  0.028  0.023  0.067   0.38 3.06
Triazolam Cimetidine  2.20  99  0.04  0.033  0.096   0.54 3.06
Midazolam Cimetidine  2.02 180  0.022  0.0089  0.052   0.29 3.07
Midazolam Ranitidine  1.66 170  0.0027  0.0012  0.011   0.17 3.07
Midazolam Cimetidine  1.35 180  0.018  0.0071  0.074   0.56 3.08
Midazolam Ranitidine  1.23 170  0.0027  0.0012  0.011   0.17 3.08
Nifedipine Cimetidine  1.60 140  0.028  0.023  0.24   1.8 3.09
Nifedipine Ranitidine  1.22 170  0.0027  0.0023  0.011   0.17 3.09
Nifedipine Cimetidine  2.01 140  0.023  0.018  0.19   1.4 3.10
Nifedipine Ranitidine  1.06 170  0.0055  0.0047  0.022   0.35 3.10
Nimodipine Cimetidine  1.74 140  0.028  0.023  0.067   0.38 3.11
Nimodipine Ranitidine  0.99 170  0.0027  0.0023  0.022   0.35 3.11
Nisoldipine Cimetidine  1.49 140  0.028  0.023  0.067   0.38 3.12
Nitrendipine Cimetidine  2.41 140  0.027  0.022  0.057   0.38 3.13
Triazolam Cimetidine  1.55  99  0.048  0.039  0.11   0.8 3.14
Triazolam Cimetidine  1.32  99  0.048  0.039  0.11   0.8 3.15
Midazolam Clarithromycin  7.00    57  0.017  0.0094  0.048   0.74 3.16
Lovastatin Cyclosporin  1.89   2  0.059  0.0041  0.11   3.7 3.17
Buspirone Diltiazem  5.50  65  0.0024  0.0005  0.0047   0.14 3.18
Buspirone Verapamil  3.40  16  0.0047  0.0005  0.0087   0.68 3.18
Cyclosporin Diltiazem  1.49  63.0  0.0033  0.0007  0.0084   0.29 3.19
Cyclosporin Diltiazem  1.57  63.0  0.0025  0.0006  0.0063   0.22 3.20
Cyclosporin Ketoconazole  4.39   0.37  1.2  0.012  6.2   66 3.20
Lovastatin Diltiazem  3.57  65  0.0032  0.0007  0.0081   0.28 3.21
Midazolam Diltiazem  3.75  54  0.0029  0.0003  0.0056   0.17 3.22
Midazolam Verapamil  2.92  13  0.0061  0.0003  0.011   0.87 3.22
Nifedipine Diltiazem  2.22  65  0.0012  0.0003  0.0023   0.07 3.23
Nifedipine Diltiazem  3.11  65  0.0036  0.0008  0.007   0.21 3.23
Simvastatin Diltiazem  4.82  65  0.0032  0.0007  0.0081   0.28 3.24
Triazolam Diltiazem  3.38  54  0.0029  0.0006  0.0056   0.17 3.25
Triazolam Diltiazem  2.30  54  0.0029  0.0006  0.0056   0.17 3.26
Alprazolam Erythromycin  2.47 120  0.005  0.0008  0.018   0.28 3.27
Buspirone Erythromycin  5.90 110  0.0075  0.0012  0.027   0.41 3.28
Buspirone Itraconazole  19.20   0.91 (2.2)  0.26  0.0005  0.32   9.9 3.28
Cerivastatin Erythromycin  1.21 110  0.0075  0.0012  0.027   0.41 3.29
Cyclosporin Erythromycin  2.22  66  0.0079  0.0013  0.022   0.33 3.30
Cyclosporin Erythromycin  2.15  66  0.016  0.0025  0.044   0.66 3.31
Felodipine Erythromycin  2.49 110  0.005  0.0008  0.014   0.21 3.32
Midazolam Erythromycin  4.42 170  0.0046  0.0004  0.016   0.25 3.33
Quinidine Erythromycin  1.19 110  0.005  0.0008  0.014   0.21 3.34
Quinidine Itraconazole  2.58   0.91 (2.2)  0.13  0.0003  0.19   9.8 3.34
Simvastatin Erythromycin  6.20 110  0.0075  0.0012  0.023   0.41 3.35
Simvastatin Verapamil  4.60  16  0.0047  0.0005  0.0087   0.68 3.35
Triazolam Erythromycin  2.06 120  0.0042  0.0007  0.015   0.23 3.36
Quinidine Felodipine  1.07  11  0.0003  <0.0001  0.0005   0.15 3.37
Quinidine Nifedipine  1.15  17  0.0047  0.0002  0.022   0.21 3.37
Cyclosporin Fluconazole  1.84  40  0.54  0.48  0.69   1.55 3.38
Midazolam Fluconazole  3.60   6  3.6  1.6  4.6   10 3.39
Midazolam Itraconazole  6.64   0.92 (6.3)  0.18  0.0004  0.26   19 3.39
Rifabutin Fluconazole  1.82  12  1.8  1.6  2.3   5.2 3.40
Triazolam Fluconazole  1.63  1.8  2.9  2.6  3.8   8.5 3.41
 Triazolam Fluconazole  2.05  1.8  5.9  5.2  7.6   17 3.41
Triazolam Fluconazole  4.42  1.8  12  10  15   34 3.41
Triazolam Fluconazole  2.46  1.8  5.9  5.2  7.6   17 3.42
Triazolam Terbinafine  0.81  100  0.012  <0.0001  0.02   0.55 3.42
Alprazolam Fluoxetine  1.34  65 (10)  0.088  0.0053  0.1   0.27 3.43
Alprazolam Fluoxetine  1.26  65 (10)  0.059  0.0035  0.063   0.12 3.44
Triazolam Fluoxetine  1.02  26 (5.4)  0.14  0.0085  0.16   0.61 3.45
Alprazolam Fluvoxamine  1.96  9.2  0.035  0.0080  0.057   2.2 3.46
Buspirone Fluvoxamine  2.35  11  0.029  0.0066  0.048   1.8 3.47
Quinidine Fluvoxamine  1.41  11  0.029  0.0066  0.048   1.8 3.48
Triazolam Isradipine  0.80  17  0.0001  <0.0001  0.0003   0.043 3.49
Triazolam Mibefradil  8.97  2.5  0.25  0.001  0.39   2.8 3.49
Alprazolam Itraconazole  2.66   0.95 (2.2)  0.26  0.0005  0.37   19 3.50
Astemizole Itraconazole  2.77   0.91 (2.2)  0.52  0.001  0.63   20 3.51
Atorvastatin Itraconazole  3.64   0.91 (2.2)  0.26  0.0005  0.38   20 3.52
Buspirone Itraconazole  14.50   0.91 (2.2)  0.26  0.0005  0.38   20 3.53
Cerivastatin Itraconazole  1.15   0.91 (2.2)  0.26  0.0005  0.38   20  3.54
Felodipine Itraconazole  6.34   0.91 (2.2)  0.26  0.0005  0.38   20 3.55
Lovastatin Itraconazole  22.10   0.91 (2.2)  0.26  0.0005  0.38   20 3.56
Lovastatin Itraconazole  15.40   0.91 (2.2)  0.13  0.0003  0.19   9.8 3.57
Midazolam Itraconazole  7.97   0.92 (6.3)  0.18  0.0004  0.26   19 3.58
Midazolam Itraconazole  5.75   0.92 (6.3)  0.089  0.0002  0.13   9.7 3.59
Midazolarn Itraconazole  10.80   0.92 (6.3)  0.36  0.0007  0.52   39 3.60
Midazolam Ketoconazole  15.90   0.088  5  0.025  26  270 3.60
Quinidine Itraconazole  2.42   0.91 (2.2)  0.26  0.0005  0.38   20 3.61
Simvastatin Itraconazole  18.60   0.91 (2.2)  0.26  0.0005  0.38   20 3.62
Triazolam Itraconazole  27.10   0.16 (0.2)  2.2  0.0044  3.2  110 3.63
Triazolam Ketoconazole  22.40   0.022  41  0.41  210 2200 3.63
Alprazolam Ketoconazole  3.98   0.061  15  0.15  40   400  3.64
Triazolam Ketoconazole  13.70   0.022  41  0.41  110 1100 3.64
Cyclosporin Ketoconazole  5.15   0.36  2.5  0.025  6.7   67 3.65
Cyclosporin Ketoconazole  5.31   0.36  1.2  0.012  6.2   66 3.66
Midazolam Ketoconazole  16.00   0.088  10  0.051  28  280 3.67
Nisoldipine Ketoconazole  24.40   0.099  4.5  0.045  23  240 3.68
Tacrolimus Ketoconazole  2.88  8  0.056  0.0006  0.28   3 3.69
Triazolam Ketoconazole  9.16  0.022  31  0.31  110 1100 3.70
Alprazolam Nefazodone  1.41  1.2  0.98  0.0089  2   24 3.71
Triazolam Nefazodone  3.90  1.2  0.98  0.0089  2   24 3.72
Cyclosporin Nifedipine  0.88  10  0.008  0.0003  0.037   0.36 3.73
Cyclosporin Verapamil  1.45  24  0.0036  0.0004  0.0066   0.51 3.73
Quinidine Nifedipine  0.98  17  0.0071  0.0003  0.023   0.21 3.74
Nifedipine Quinidine sulphate  1.37 160  0.019  0.0025  0.029   0.26 3.74
Midazolam Ranitidine  1.66 170  0.0027  0.0012  0.011   0.17 3.75
Alprazolam Ritonavir  2.48   0.065  71  1.4  120  340 3.76
Midazolam Roxithromycin  1.47 110  0.061  0.0012  0.19   0.26 3.77
Midazolam Saquinavir  5.14  3.5  0.12  0.0012  0.15   32 3.78
Quinidine Verapamil  1.47  16  0.0047  0.0005  0.0087   0.68 3.79
Quinidine Verapamil  1.50  16  0.0071  0.0007  0.013   1 3.79

*Numbers in parentheses represent the values for metabolites.

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