Table 2.
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.