Table 2.
Inhibitory specificities of clinical index inhibitors and additional perpetrator drugs
| Index inhibitor | BDDCS class | Enzyme | Other relevant enzymes/transporters | Refs. |
|---|---|---|---|---|
| Cimetidine | 3 |
OCT2 CYP2C19 CYP3A |
MATE1 CYP1A2 CYP2C9 CYP2D6 |
[5] |
| Ciprofloxacin | 4 | CYP1A2 | CYP3A4 | [4] |
| Clarithromycin | 3 | CYP3A4 |
CYP2C19 P-gp |
[4] |
| Diltiazem | 1 | CYP3A4 |
CYP1A2 CYP2D6 P-gp |
[5] |
| Disulfiram | 2 | CYP2E1 |
CYP1A2 CYP2C9 CYP2D6 |
[5] |
| Enoxacin | 4 | CYP1A2 | [4] | |
| Erythromycin | 4 | CYP3A4 | P-gp | [4] |
| Famotidine | 3 | Unknown | ||
| Fluconazole | 3 |
CYP2C9 CYP2C19 |
CYP3A4 | [4] |
| Itraconazole | 2 | CYP3A4 |
CYP2J2 P-gp |
[4] |
| Ketoconazole | 2 | CYP3A4 |
CYP2C19 P-gp |
[4] |
| Lidocaine | 1 | CYP3A4 | CYP1A2 | [7] |
| Nalidixic acid | 2 | Unknown | ||
| Nelfinavir | 2 | CYP3A4 | CYP2D6 | [8] |
| Norfloxacin | 4 | CYP1A2 | [9] | |
| Ofloxacin | 3 | Unknown | ||
| Olanzapine | 2 | Unknown | ||
| Ondansetron | 1 | Unknown | ||
| Primaquine | 1 | Unknown | ||
| Quinidine | 1 | CYP2D6 | P-gp | [4] |
| Ranitidine | 3 |
OCT2 CYP3A |
CYP2C9 CYP2D6 |
[5] |
| Rifampin (single dose) | 2 | OATPs | CYP3A4 | [6, 11] |
| Rifampin (multiple dose) | 2 |
(Inducer) CYP3A CYP2C9 P-gp |
(Inducer) CYP1A CYP2B6 CYP2C8 CYP2C19 |
[6] |
| Ritonavir (single dose) | 2 | CYP3A4 | P-gp | [4] |
| Ritonavir (multiple dose) | 2 | CYP induction | [4] | |
| Sulfaphenazole | 1 | CYP2C9 | [8] | |
| Terbinafine | 2 | CYP2D6 | CYP1A2 | [4] |
| Verapamil | 1 | CYP3A4 | P-gp | [4] |
BDDCS Biopharmaceutics Drug Disposition Classification System, CYP cytochrome P450, MATE Multidrug and Toxic Extrusion, OCT organic cation transporter, P-gp P-glycoprotein, Refs references