Page 76 - Basic _ Clinical Pharmacology ( PDFDrive )

62 SECTION I Basic Principles

TABLE 4–2 Human liver P450s (CYPs), and some of the drugs metabolized (substrates), inducers, and
selective inhibitors. Note: Some P450 substrates can be potent competitive inhibitors and/or
mechanism-based inactivators.

CYP Substrates Inducers Inhibitors
1A2 Acetaminophen, alosetron, antipyrine, caffeine, clomip- Charcoal-broiled foods, Artemisinin, atazanavir, cimetidine,
ramine, clozapine, duloxetine, flutamide, frovatriptan, cruciferous vegetables, ciprofloxacin, enoxacin, ethinyl estradiol,
melatonin, mexiletine, mirtazapine, olanzapine, phenacetin, grilled meat, lansoprazole, fluvoxamine, furafylline, galangin,
ramelteon, rasagiline, ropinirole, tacrine, tamoxifen, theoph- omeprazole, primidone, mexiletene, tacrine, thiabendazole,
ylline, tizanidine, triamterene, warfarin, zolmitriptan rifampin, smoking zileuton
2A6 Coumarin, dexmedetomidine, tobacco nitrosamines, nicotine Efavirenz, rifampin, Clotrimazole, isoniazid, ketoconazole,
(to cotinine and 2′-hydroxynicotine) phenobarbital letrozole, menthofuran, methimazole,
methoxsalen, miconazole,
tranylcypromine
2B6 Artemisinin, bupropion, clopidogrel, cyclophosphamide, Carbamazepine, cyclophos- Amiodarone, amlodipine, clopidogrel,
efavirenz, ifosfamide, irinotecan, ketamine, S-mephobarbital, phamide, fosphenytoin, clotrimazole, desipramine, disulfiram,
S-mephenytoin (N-demethylation to nirvanol), methadone, nevirapine, phenobarbital, doxorubicin, ethinyl estradiol, fluoxetine,
nevirapine, promethazine, propofol, selegiline, sertraline, primidone, rifampin fluvoxamine, isoflurane, ketoconazole,
ticlopidine mestranol, methimazole, nefazodone,
nelfinavir, orphenadrine, paroxetine,
phencyclidine, sertraline, thiotepa,
ticlopidine
2C8 Amiodarone, cabazitaxel, carbamazepine, chloroquine, Rifampin, barbiturates Deferasirox, gemfibrozil, lapatinib,
diclofenac, ibuprofen, paclitaxel, all-trans-retinoic acid, montelukast, pioglitazone, quercetin,
repaglinide, rosiglitazone, treprostinil rosiglitazone, trimethoprim
2C9 Alosetron, bosentan, celecoxib, chlorpropamide, diclofenac, Aminoglutethimide, Amiodarone, clopidogrel, delavirdine,
dronabinol, flurbiprofen, fluvastatin, glimepiride, glipizide, barbiturates, bosentan, disulfiram, doxifluridine, efavirenz,
glyburide, hexobarbital, ibuprofen, indomethacin, irbesartan, carbamazepine, phenytoin, fluconazole, fluvoxamine, fluorouracil,
losartan, meloxicam, montelukast, naproxen, nateglinide, primidone, rifabutin, imatinib, leflunomide, metronidazole,
phenobarbital, phenytoin, piroxicam, rosiglitazone, rifampin, rifapentine, miconazole, phenytoin, sulfamethoxa-
rosuvastatin, sulfamethoxazole, sulfaphenazole, ticrynafen, St. John’s wort zole, sulfaphenazole, sulfinpyrazone,
tolbutamide, torsemide, trimethadione, valsartan, S-warfarin tienilic acid, valproic acid, voriconazole
2C18 Tolbutamide, phenytoin Phenobarbital
2C19 Aripiprazole, carisoprodol, citalopram, clomipramine, clopi- Aminoglutethimide, N3-Benzylnirvanol, N3-benzylpheno-
dogrel, clozapine, desipramine, diazepam, diphenhydramine, artemisinin, barbiturates, barbital, chloramphenicol, cimetidine,
doxepin, escitalopram, fluoxetine, imipramine, lansoprazole, carbamazepine, phenytoin, clopidogrel, delavirdine, efavirenz,
S-mephenytoin, methadone, moclobemide, naproxen, primidone, rifampin, esomeprazole, felbamate, fluconazole,
nelfinavir, nirvanol, olanzapine, omeprazole, pantoprazole, rifapentine, St. John’s wort fluoxetine, fluvoxamine, isoniazid,
phenobarbital, phenytoin, proguanil, propranolol, rabeprazole, moclobemide, modafinil, nootkatone,
sertraline, thalidomide, voriconazole, R-warfarin omeprazole, ticlopidine, voriconazole
2D6 Amitriptyline, atomoxetine, bufuralol, bupranolol, carvedilol, Unknown Bupropion, cinacalcet, chloroquine,
chlorpheniramine, chlorpromazine, clomipramine, clozapine, diphenhydramine, fluoxetine,
codeine, debrisoquine, desipramine, dextromethorphan, haloperidol, imatinib, paroxetine,
dihydrocodeine, encainide, flecainide, fluoxetine, fluvox- propafenone, propoxyphene, quinidine,
amine, guanoxan, haloperidol, hydrocodone, imipramine, terbinafine, thioridazine
maprotiline, 4–methoxy-amphetamine, metoclopramide,
metoprolol, mexiletine, nebivolol, nortriptyline, oxycodone,
palonosetron, paroxetine, perhexiline, perphenazine, phen-
formin, propafenone, propoxyphene, propranolol, risperi-
done, selegiline (deprenyl), sparteine, tamoxifen,
thioridazine, timolol, tolterodine, tricyclic antidepressants,
tramadol, trazodone, venlafaxine
2E1 Acetaminophen, chlorzoxazone, dacarbazine, enflurane, Ethanol, isoniazid Amitriptyline, chlorpromazine, cimetidine,
ethanol (a minor pathway), halothane, isoflurane, isoniazid, clomethiazole, clotrimazole, clozapine,
sevoflurane, theophylline, trimethadione disulfiram, diethylthiocarbamate,
diallyl sulfide, econazole, methimazole,
methoxsalen, 4-methylpyrazole,
miconazole, modafinil, ritonavir,
selegiline, sildenafil, sulconazole,
ticlopidine, tioconazole
(continued)