Table 2.
Examples of pharmacokinetic consequences of phenoconversion following drug-induced inhibition of CYP2D6
| Phenoconverting inhibitor | Substrate | Ratio of substrate AUC with and without inhibitor |
|---|---|---|
| Quinidine | Mexiletine | 1.32 |
| Imipramine | 1.54 | |
| Propafenone | 2.70 | |
| Propranolol | 1.98–3.00 | |
| Metoprolol | 3.24 | |
| Desipramine | 7.50 | |
| Encainide | 11.40 | |
| Dextromethorphan | 13–49 (depending on the dose of quinidine) | |
| Fluoxetine | Propafenone | 1.50 |
| (R)-Carvedilol | 1.77 | |
| Imipramine | 3.33 | |
| Desipramine | 4.80 | |
| Tolterodine | 4.84 | |
| Paroxetine | Tamsulosin | 1.64 |
| Imipramine | 1.74 | |
| Aripiprazole | 2.36 | |
| (R,S)-Metoprolol | 4.21–6.16 | |
| (S)-Metoprolol | 5.08 | |
| Desipramine | 4.64–5.21 | |
| Atomoxetine | 6.50 | |
| Perphenazine | 6.96 | |
| (R)-Metoprolol | 7.93 | |
| Terbinafine | Paroxetine | 2.50 |
| Desipramine | 4.94 | |
| Cinacalcet | Desipramine | 3.6 |
| Dextromethorphan | 11.5 |
Abbreviation is as follows: AUC, area under the plasma concentration vs. time curve. [Compiled from literature review.]