Comparison of the order of in vitro inhibition potency and magnitude of in vivo DDI for 21 drugs
Drug | In Vitro Potency Rank Order | In Vivo Potency Rank Ordera | Rank-Order Correspondence? |
|---|---|---|---|
| Cimetidine | 2D6 > 3A > 2C9≈1A2 | 3A > 1A2≈2C9≈2D6 | No |
| Citalopram | 2D6 > 3A≈2C19 > 2C9 > 1A2 | 2D6 > 3A≈2C19≈2C9≈1A2 | Yes |
| Clarithromycin | 3A > 2C19≈1A2≈2C9 | 3A > 2C19 > 2C9≈1A2 | Yes |
| Diltiazem | 3A > 2C9≈2D6 > 1A2 | 3A > 2D6≈1A2≈2C9 | Yes |
| Disulfiram | 2C9≈1A2 > 3A≈2C19 > 2D6 | 1A2≈2D6≈2C19≈2C9≈3A | Yes |
| Erythromycin | 3A > 1A2≈2C9 | 3A > 1A2≈2C9 | Yes |
| Fluconazole | 2C19≈3A≈2C9 > 1A2 | 2C19 > 2C9∼3A > 1A2 | Yes |
| Fluoxetine | 2D6 > 3A > 1A2 | 2D6 > 1A2≈3A | Yes |
| Fluvoxamine | 1A2 > 2C19 > 2D6≈2C9 > 3A | 2C19 > 1A2 > 3A > 2C9≈2D6 | No |
| Ketoconazole | 3A > 2C9≈2C19 > 1A2≈2D6 | 3A > 2C9 > 2C19≈1A2≈2D6 | Yes |
| Metronidazole | 3A≈1A2≈2C9 | 2C9≈1A2≈3A | Yes |
| Nefazodone | 3A > 2C9 > 1A2 | 3A > 2C9≈1A2 | Yes |
| Paroxetine | 2D6 > 1A2 > 2C19≈3A > 2C9 | 2D6 > 1A2≈2C9≈2C19≈3A | Yes |
| Propranolol | 1A2 > 3A > 2C9 | 1A2 > 3A≈2C9 | Yes |
| Ranitidine | 3A≈2D6 > 2C9≈1A2 | 3A≈2D6 > 2C9≈1A2 | Yes |
| Risperidone | 2D6 > 2C19 > 1A2 | 2C19≈1A2≈2D6 | Yes |
| Roxithromycin | 3A > 2C19≈1A2≈2C9 | 3A≈2C19≈1A2≈2C9 | Yes |
| Sertraline | 2D6 > 3A≈1A2 > 2C9 | 2D6≈1A2≈2C9≈3A | Yes |
| Terbinafine | 2D6 > 1A2 > 3A≈2C9 | 2D6 > 1A2≈2C9≈3A | Yes |
| Ticlopidine | 2C19 > 1A2 > 3A | 2C19 > 1A2 > 3A | Yes |
| Troleandomycin | 3A > 2C19≈1A2 | 3A > 1A2 > 2C19 | No |
↵ a Boldface designates those in vivo DDI in which the increase in exposure to the probe substrate was >2-fold