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

Table 2.

In vivo database for the interactions involving CYP2D6

Substrate Inhibitor AUC ratio Ki* (µm) [I]av/ Ki [I]av,u/ Ki [I]max/ Ki [I]in/ Ki Reference
Flecainide Amiodarone  1.37  43 (20)  0.11  0.0023  0.11   0.57 2.01
 Atenolol Amitriptyline  1.24  30 (12)  0.13  0.0095  0.19   0.7 2.02
Metoprolol Amitriptyline  1.44  30 (12)  0.13  0.0095  0.19   0.7 2.02
Propranolol Chlorpromazine  1.69   4.8  0.11  0.004  0.13   2.2 2.03
 Atenolol  Cimetidine  1.07  40  0.1  0.081  0.24   1.3 2.04
Metoprolol Cimetidine  1.61  40  0.1  0.081  0.24   1.3 2.04
 Propranolol  Cimetidine  1.91  40  0.1  0.081  0.24   1.3 2.04
Propranolol Cimetidine  1.94  40  0.1  0.081  0.24   1.3 2.05
Propranolol Cimetidine  1.47  40  0.12  0.097  0.28   2 2.06
Imipramine Citalopram  1.15  24 (14)  0.015  0.0045  0.019   0.34 2.07
(Desipramine) Citalopram  1.47  24 (14)  0.015  0.0045  0.019   0.34 2.07
Levomepromazine Citalopram  0.74  24 (14)  0.015  0.0045  0.019   0.34 2.07
Atenolol Diltiazem  1.07  150  0.0005  0.0001  0.001   0.03 2.08
Metoprolol Diltiazem  1.33  150  0.0005  0.0001  0.001   0.03 2.08
Propranolol Diltiazem  1.48  150  0.0005  0.0001  0.001   0.03 2.08
Propranolol Diltiazem  1.33  150  0.0016  0.0003  0.003   0.091 2.09
Propranolol Verapamil  1.42  16  0.0072  0.0007  0.013   1 2.09
Metoprolol Diphenhydramine  1.61  10  0.056  0.012  0.076   1.2 2.10
R(+)-carvedilol Fluoxetine  1.77   0.54 (0.58)  0.7  0.042  0.81   8.1 2.11
Desipramine Fluoxetine  4.80   0.54 (0.58)  0.7  0.042  0.81   8.1 2.12
Desipramine Sertraline  1.20  10 (24)  0.0071  0.0001  0.01   1 2.12
Desipramine Fluoxetine  7.43   0.54 (0.58)  2.1  0.13  2.4  24 2.13
Imipramine Fluoxetine  3.33   0.54 (0.58)  2.1  0.13  2.4  24 2.13
(Desipramine) Fluoxetine  5.31   0.54 (0.58)  2.1  0.13  2.4  24 2.13
 Propafenone Fluoxetine  1.50   0.54 (0.58)  0.7  0.042  0.81   8.1 2.14
Ritonavir Fluoxetine  1.19   0.54 (0.58)  2.1  0.13  2.3  13 2.15
Tolterodine Fluoxetine  4.84   0.54 (0.58)  0.7  0.042  0.81   8.1 2.16
Desipramine Fluvoxamine  1.14   5.8  0.055  0.013  0.09   3.4 2.17
Imipramine Fluvoxamine  3.63   5.8  0.055  0.013  0.09   3.4 2.17
Metoprolol Hydroxychloroquine  1.65  66  0.025  0.015  0.025   1.1 2.18
Imipramine Labetalol  1.53   7  0.012  0.0062  0.026   5.4 2.19
(Desipramine) Labetalol  2.27   7  0.012  0.0062  0.026   5.4 2.19
Metoprolol Mexiletine HCl  1.82  30  0.095  0.035  0.13   1.5 2.20
Metoprolol (R) Omeprazole 1.01 240  0.0003  0.0001  0.008   0.03 2.21
Metoprolol (S) Omeprazole  1.02 240  0.0003  0.0001   0.03  2.21
Propranolol Omeprazole  1.02  240  0.0002  0.0001  0.004   0.015 2.22
Desipramine Paroxetine  4.64   0.69  0.1  0.0051  0.16   5.6 2.23
Imipramine Paroxetine  1.74   0.69  0.15  0.0076  0.24   8.4 2.24
(Desipramine) Paroxetine  4.28   0.69  0.15  0.0076  0.24   8.4 2.24
Metoprolol (R) Paroxetine  7.93   0.69  0.1  0.0051  0.13   2.8 2.25
Metoprolol (S) Paroxetine  5.08   0.69  0.1  0.0051   2.8  2.25
Perphenazine Paroxetine  6.96   0.69  0.1  0.0051  0.16   5.6 2.26
Desipramine Paroxetine  5.21   0.69  0.1  0.0051  0.16   5.6 2.27
Desipramine Sertraline  1.37  10 (24)   0.0065  0.0001  0.0091   1 2.27
 Propranolol  Propafenone   2.13   0.55  19   0.95  30  93 2.28
 Desipramine  Quinidine sulphate  7.50  0.082  5.5  0.72 16 210 2.29
Imipramine Quinidine sulphate  1.54  0.082  5.5  0.72 16 210 2.29
Encainide Quinidine sulphate  3.18  0.082  5.5  0.72  7.6  56 2.30
Encainide Quinidine sulphate 11.40  0.082  5  0.64  7.5  66 2.31
Metoprolol Quinidine sulphate  3.24  0.082  2.8  0.36  7.9 100 2.32
Mexiletine Quinidine sulphate  1.32  0.082  5.5  0.72  7.6  56 2.33
Propafenone Quinidine sulphate  2.70  0.082  4.1  0.54  6.2  55 2.34
Desipramine Ritonavir  2.45  4.8  1.8  0.036  3.4  11 2.35
Desipramine Sertraline  1.74  10 (24)  0.02  0.0002  0.027   3 2.36
Desipramine Sertraline  1.54  10 (24)  0.02  0.0002  0.027   3 2.37
Imipramine Sertraline  1.68  10 (24)  0.02  0.0002  0.027   3 2.37
(Desipramine) Sertraline  2.29  10 (24)  0.02  0.0002  0.027   3 2.37
Metoprolol Verapamil  1.33  16  0.0072  0.0007  0.013   1 2.38

Numbers in parentheses represent the values for metabolites.

References for Table 2

2.01Funck-Brentano et al. Clin Pharmacol Ther 1994; 55:256–69. 2.02Kirch et al. Br J Clin Pharmacol 1984; 17: 65S–8S. 2.03Vestal et al. Clin Pharmacol Ther 1979; 25: 19–24. 2.04Kirch et al. Klin Wochenschr 1982; 60: 1401–7. 2.05Reimann et al. Br J Clin Pharmacol 1981; 12: 785–90. 2.06Donn et al. J Clin Pharmacol 1984; 24: 500–8. 2.07Gram et al. Ther Drug Monit 1993; 15:18–24. 2.08Tateishi et al. Eur J Clin Pharmacol 1989; 36: 67–70. 2.09Hunt et al. Clin Pharmacol Ther 1990; 47: 584–91. 2.10Hamelin et al. Clin Pharmacol. Ther 2000; 67: 466–77. 2.11Graff et al. J Clin Pharmacol 2001; 41: 97–106. 2.12Preskorn et al. J Clin Psychopharmacol 1994; 14: 90–8. 2.13Bergstrom et al. Clin Pharmacol Ther 1992; 51: 239–48. 2.14Cai et al. Clin Pharmacol Ther 1999; 66: 516–21. 2.15Ouellet et al. Antimicrob Agents Chemother 1998; 42:3107–12.2.16Brynne et al. Br J Clin Pharmacol 1999; 48: 553–563. 2.17Spina et al. Ther Drug Monit 1993; 15: 243–6. 2.18Somer et al. Br J Clin Pharmacol 2000; 49: 549–54. 2.19Hermann et al. J Clin Pharmacol 1992; 32: 176–83. 2.20Sakamoto et al. Jpn J Clin Pharmacol Ther 1995; 26: 159–60. 2.21Andersson et al. Eur. J Clin Pharmacol 1991; 40: 61–5. 2.22Henry et al. Eur J Clin Pharmacol 1987; 33: 369–73. 2.23Brosen et al. Eur J Clin Pharmacol 1993; 44: 349–55. 2.24Albers et al. Psychiatry Res 1996; 59: 189–96. 2.25Hemeryck et al. Clin Pharmacol Ther 2000; 67:283–91. 2.26Ozdemir et al. Clin Pharmacol Ther 1997; 62:334–47. 2.27Alderman et al. J. Clin Psychopharmacol 1997; 17:284–91. 2.28Kowey et al. J Clin Pharmacol 1989; 29: 512–7. 2.29Brosen, Gram. Eur J. Clin Pharmacol 1989; 37:   155–60. 2.30Funck-Brentano et al. J Pharmacol Exp Ther 1989; 249: 134–42. 2.31Turgeon et al. J Pharmacol Exp Ther 1990; 255:642–9. 2.32Johnson, Burlew. Drug Metab Dispos 1996; 24:350–5. 2.33Turgeon et al. J Pharmacol Exp Ther 1991; 259:789–98. 2.34Funck-Brentano et al. Br J Clin Pharmacol 1989; 27: 435–44. 2.35von Moltke et al. J Pharm Sci 1998; 87: 1184–9. 2.36Zussman et al. Br J Clin Pharmacol 1995; 39: 550–1. 2.37Kurtz et al. Clin Pharmacol Ther 1997; 62: 145–56. 2.38Keech et al. Am J Cardiol 1986; 58: 551–2.