Table 1.
Inhibitors and inducers of hepatic cytochrome P450 (CYP450) enzymes and drug transporters involved in drug metabolism.
CYP450 Substrates | Inhibitor | Inducer | |||
---|---|---|---|---|---|
Psychotropic | Other | Psychotropic | Other | ||
1A2 | Caffeine Theophyline TCAs Ropinirole Duloxetine Mirtazapine Clozapine Haloperidol Olanzapine Asenapine Tacrine Zolmitriptan |
Fluvoxamine+++ Fluoxetine+ Paroxetine+ Sertraline+ |
Cimetidine+ Omeprazole Fluoroquinolones Ticlopidine |
Phenobarbital Secobarbital Carbamazepine Phenytoin |
Modafinil Tobacco Charcoal-grilled meat Rifampin |
2C9 | Warfarin Losartan NSAIDs Glipizide ARBs |
Valproic acid+ Fluoxetine++ |
Fluconazole+++ Miconazole++ Amiodarone++ |
Secobarbital Carbamazepine |
Rifampin |
2C19 | BZDs PPIs SSRIs (citalopram) Amitriptyline |
Fluvoxamine+++ Fluoxetine+ |
Ketoconazole Cimetidine Omeprazole Lansoprazole |
Carbamazepine Valproic acid Phenobarbital Phenytoin |
Rifampin |
2D6 | β-blockers Class 1C antiarrhythmics Codeine Amitriptyline Sertraline Haloperidol TCAs Risperidone Iloperidone Tramadol Venlafaxine Duloxetine Aripiprazole |
Bupropion+++ Fluoxetine+++ Paroxetine+++ Duloxetine++ Sertraline+ Citalopram+ Escitalopram+ Haloperidol+ Thioridazine+ |
Terbinafine++ Quinidine+++ Cimetidine+ Amiodarone+ Mibefradil+ Ritonavir+ |
None | None |
3A4 | Acetominophen BZDs Statins Macrolides Quinidine Indinavir, Ritonavir Amlodipine, Felodopine Diltiazem Atorvastatin Buspirone Sertraline Venlafaxine Mirtazapine Haloperidol Iloperidone Trazodone |
Fluvoxamine+++ Nefazodone+++ |
Clarithromycin+++ Erythromycin++ Troleandomycin++ Fluconazole+++ Ketoconazole+++ Itraconazole+++ Indinavir+++ Cimetidine+ Verapamil++ Diltiazem++ |
Carbamazepine+++ Phenytoin+++ Phenobarbital++ St. John’s Wort++ Morphine+ Nicotine+ Topiramate+ Felbamate+ |
Rifampin+++ Ritonavir++ Indinavir++ Efavirenz Pioglitazone Glucocorticoids |
UGT | FGAs SGAs TCAs NSAIDs Carvedilol Furosemide Morphine Tramadol Lorazepam Oxazepam |
Diclofenac+++ NSAIDs++ Probenecid++ Valproic acid+ |
Carbamazepine++ Phenytoin++ Phenobarbital++ Lamotrigine+ |
Rifampin+ Carbapenems+ |
|
OATP1A2 | Atenolol Ciprofloxacin Pravastatin |
Grapefruit juice Verapamil |
|||
OATP2B1 | Statins | Grapefruit juice Cyclosporine |
|||
OAT1 | Captopril Furosemide |
Indomethacin Olmesartan Probenecid |
|||
OAT3 | Furosemide Olmesartan Pravastatin |
Gemfibrozil Indomethacin |
|||
OCT2 | Amatadine Lamivudine Metformin Ranitidine |
Bisoprolol Carvedilol Ranitidine |
|||
MDR1 (P-gp) | Digoxin Fexofenadine Ritonavir TCAs Atypical antipsychotics SSRIs Topiramate Gabapentin Carbamazepine Lamotrigine |
Trifluperazine Fluphenazine Haloperidol Amitriptyline Flurazepam |
Clarithromycin Cyclosporine Itraconazole Verapamil |
Midazolam Phenobarbital Phenytoin Hypericum Morphine Nicotine |
Clotrimazole Nifedipine Troglitazone |
ARBs, angiotensin receptor blockers; BZD, benzodiazepine; PPI, proton pump inhibitors; SSRI, selective serotonin reuptake inhibitors; TCA, tricyclic antidepressant; FGA, first generation antipsychotics; SGA, second generation antipsychotics; NSAIDs, non-steroidal anti-inflammatory drugs
Relative inhibition: + = (negligible-low); ++ = (moderate); +++ = (high)