SUBSTRATES | |||||||
| 1A2 | 2B6 | 2C8 | 2C9 | 2C19 | 2D6 | 2E1 | 3A4,5,7 |
|
clozapine cyclobenzaprine imipramine mexiletine naproxen riluzole tacrine2 theophylline2 |
bupropion1 cyclophosphamide efavirenz1 ifosfamide methadone |
paclitaxel torsemide amodiaquine2 cerivastatin repaglinide |
NSAIDs: diclofenac ibuprofen piroxicam Oral Hypoglycemics: tolbutamide glipizide Angiotensin II Blockers: losartan irbesartan Others: celecoxib fluvastatin naproxen phenytoin rosiglitazone sulfamethoxazole tamoxifen tolbutamide torsemide warfarin1 |
PPIs: lansoprazole omeprazole2 pantoprazole rabeprazole Anti-epileptics: diazepam phenytoin phenobarbitone Others: amitriptyline clomipramine clopidogrel cyclophosphamide progesterone |
Beta Blockers: S-metoprolol propafenone timolol Antidepressants: amitriptyline clomipramine desipramine imipramine paroxetine Antipsychotics: haloperidol risperidone thioridazine Others: aripiprazole codeine dextromethorphan1 duloxetine flecainide mexilletine ondansetron tamoxifen tramadol venlafaxine |
Anesthetics: enflurane halothane isoflurane methoxyflurane sevoflurane Others: acetaminophen→NAPQI aniline2 benzene chlorzoxazone1 ethanol N,N-dimethyl formamide theophylline→8-OH |
Macrolide antibiotics: clarithromycin erythromycin2 (not 3A5) NOT azithromycin telithromycin Anti-arrhythmics: quinidine→3-OH (not 3A5) Benzodiazepines: alprazolam diazepam→3OH midazolam1 triazolam2 Immune Modulators: cyclosporine tacrolimus (FK506) HIV Antivirals: indinavir ritonavir saquinavir Prokinetics: cisapride Antihistamines: astemizole chlorpheniramine Calcium Channel Blockers: amlodipine diltiazem felodipine nifedipine2 nisoldipine nitrendipine verapamil HMG CoA Reductase Inhibitors: atorvastatin lovastatin NOT pravastatin NOT rosuvastatin simvastatin Others: aripiprazole buspirone gleevec haloperidol methadone pimozide quinine sildenafil tamoxifen trazodone vincristine |
INHIBITORS | |||||||
|
| |||||||
| 1A2 | 2B6 | 2C8 | 2C9 | 2C19 | 2D6 | 2E1 | 3A4,5,7 |
cimetidinefluoroquinolones fluvoxamine1 ticlopidine |
thiotepa ticlopidine2 |
gemfibrozilmontelukast1 |
fluconazole2 amiodaroneisoniazid |
fluoxetine fluvoxamine ketoconazole lansoprazole omeprazole ticlopidine2 |
bupropion fluoxetine paroxetine quinidine1 duloxetine amiodarone cimetidinechlorpheniramine clomipramine doxepin haloperidol methadone mibefradil ritonavir |
disulfiram |
HIV Antivirals: indinavir nelfinavir ritonavir clarithromycin itraconazole ketoconazole nefazodone erythromycin grapefruit juice verapamil2 diltiazem cimetidineamiodarone NOT azithromycin fluvoxamine mibefradil troleandomycin |
INDUCERS | |||||||
| 1A2 | 2B6 | 2C8 | 2C9 | 2C19 | 2D6 | 2E1 | 3A4,5,7 |
| tobacco |
phenobarbital phenytoin rifampin |
rifampin secobarbital |
ethanol isoniazid |
carbamazepine phenobarbital2 phenytoin2 pioglitazone rifabutin rifampin1 St. John's wort troglitazone1 |
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GENETICS | |||||||
| 1A2 | 2B6 | 2C8 | 2C9 | 2C19 | 2D6 | 2E1 | 3A4,5,7 |
| Chr | Chr | Chr | Chr | Chr | Chr 22 | Chr | Chr |
| Haplotypes: *2=PM *3=PM |
Haplotypes: *2=PM (99% in Asians) *3=PM (87% in Whites) |
Haplotypes: *2=EM (similar to WT) *3=PM (truncates protein) *4=PM (non-functional) *5=PM (whole gene del.) *6=PM (truncates protein) *9=IM/EM (reduces func.) *10=IM (reduces func.) *17=IM (reduces func.) *29=IM (reduces func.) *41=IM (reduces func.) |
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| Metabolizer Phenotypes: PM = Poor IM = Intermediate EM = Extensive UM = Ultrarapid | |||||||

A Strong inhibitor is one that causes a > 5-fold increase in the plasma AUC values or more than 80% decrease in clearance.
A Moderate inhibitor is one that causes a > 2-fold increase in the plasma AUC values or 50-80% decrease in clearance.
A Weak inhibitor is one that causes a > 1.25-fold but < 2-fold increase in the plasma AUC values or 20-50% decrease in clearance.
All other inhibitors.